Merck Patent GmbH

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IPC Class
A61P 35/00 - Antineoplastic agents 149
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings 45
C07D 471/04 - Ortho-condensed systems 45
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum 42
C07D 487/04 - Ortho-condensed systems 37
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1.

HETEROBIFUNCTIONAL MOLECULES AS TEAD INHIBITORS

      
Document Number 03237030
Status Pending
Filing Date 2022-10-31
Open to Public Date 2023-05-11
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Heinrich, Timo
  • Gehrtz, Paul

Abstract

Compounds of the formula (I) Q1-Q2-Q3 (I) in which Q1, Q2 and Q3 have the meanings indicated in Claim 1, degrade target proteins, and can be employed, inter alia, for the treatment of diseases and conditions mediated by such target proteins.

IPC Classes  ?

  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61P 35/00 - Antineoplastic agents
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

2.

MATERIAL AND METHOD FOR PERFORMING A SEPARATION BASED ON BORON CLUSTERS

      
Document Number 03237571
Status Pending
Filing Date 2022-11-07
Open to Public Date 2023-05-11
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Skudas, Romas
  • Holzgreve, Annika
  • Schulte, Michael
  • Keppner, Fabian
  • Knuplez, Tanja
  • Hailmann, Michael
  • Finze, Maik
  • Ignatyev, Nikolai

Abstract

This invention relates to a new stationary phase carrying boron clusters. Target molecules can interact with this stationary phase depending on the cluster type and the substituents. The stationary phase is suitable for SPE and chromatographic separations.

IPC Classes  ?

  • B01J 20/289 - Phases chemically bonded to a substrate, e.g. to silica or to polymers bonded via a spacer
  • B01J 39/17 - Organic material containing also inorganic materials, e.g. inert material coated with an ion-exchange resin
  • B01J 39/19 - Macromolecular compounds obtained otherwise than by reactions only involving unsaturated carbon-to-carbon bonds
  • B01D 15/00 - Separating processes involving the treatment of liquids with solid sorbents; Apparatus therefor
  • B01D 15/26 - Selective adsorption, e.g. chromatography characterised by the separation mechanism
  • B01D 15/38 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving specific interaction not covered by one or more of groups , e.g. affinity, ligand exchange or chiral chromatography
  • B01J 20/32 - Impregnating or coating

3.

TRICYCLIC HETEROCYCLES

      
Document Number 03236433
Status Pending
Filing Date 2022-10-26
Open to Public Date 2023-05-04
Owner
  • MERCK PATENT GMBH (Germany)
  • CANCER RESEARCH TECHNOLOGY LTD. (United Kingdom)
Inventor
  • Heinrich, Timo
  • Schlesiger, Sarah
  • Gunera, Jakub
  • Petersson, Carl
  • Koetzner, Lisa
  • Carswell, Emma
  • Unzue Lopez, Andrea

Abstract

The present invention relates to tricyclic heterocycles. These heterocyclic compounds are useful as TEAD binders and/or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases, in particular cancer.

IPC Classes  ?

  • C07D 495/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61P 35/00 - Antineoplastic agents
  • C07D 513/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains four or more hetero rings

4.

INTEGRATED SOLUTION FOR PROCESS INTENSIFICATION USING INLINE CONSTANTLY PRESSURIZED TANK: "ICPT"

      
Document Number 03233651
Status Pending
Filing Date 2022-09-27
Open to Public Date 2023-04-06
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Balbuena, Baptiste
  • Delacroix, Sebastien
  • Hajjami, Nargisse El
  • Kaschutnig, Paul
  • Durr, Josselyn Haas
  • Tomic-Skrbic, Sladjana

Abstract

Methods and procedures for operating biologics or biopharmaceutical purification protocols where disparate process steps requiring significantly different process parameters (e.g., pressure and flow rate) as continuous processes without the use of surge tanks, holding tanks or similar.

IPC Classes  ?

5.

METHODS FOR MONITORING CHROMATOGRAPHY RESINS DURING CONTINUOUS CHROMATOGRAPHY OPERATION

      
Document Number 03232551
Status Pending
Filing Date 2022-09-27
Open to Public Date 2023-04-06
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Kervennic, Damien
  • Moissonnier, Philippe

Abstract

Methods for the monitoring of quality and efficiency of chromatography columns operated in continuous mode without disruption of column operation by monitoring buffer change followed by smoothing and derivation of the recorded values.

IPC Classes  ?

  • G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups
  • B01D 15/20 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the conditioning of the sorbent material
  • G01N 30/86 - Signal analysis

6.

METHOD OF MANUFACTURE FOR EDIBLE, POROUS CROSS-LINKED HOLLOW FIBERS AND MEMBRANES BY PH INDUCED PHASE SEPARATION AND USES THEREOF

      
Document Number 03228564
Status Pending
Filing Date 2022-08-19
Open to Public Date 2023-02-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Dicker, Kevin T.
  • Sylvia, Ryan
  • Schnitzler, Aletta
  • Patel, Jaivin
  • Cera, Luca

Abstract

A method of manufacture of crosslinked, edible, porous hollow fibers and sheet membranes suitable for the manufacture of clean meat products, the hollow fibers and sheet membranes made therefrom and methods of use thereof.

IPC Classes  ?

  • C12M 1/12 - Apparatus for enzymology or microbiology with sterilisation, filtration, or dialysis means
  • B01D 63/02 - Hollow fibre modules

7.

COMBINATION RADIOTHERAPY

      
Document Number 03227836
Status Pending
Filing Date 2022-08-17
Open to Public Date 2023-02-23
Owner
  • TELIX PHARMACEUTICALS (INNOVATIONS) PTY LTD (Australia)
  • MERCK PATENT GMBH (Germany)
Inventor
  • Wheatcroft, Michael Paul
  • Yan, Edwin Bingbing
  • Scott, Andrew Mark
  • Johnstone, Cameron
  • Zimmermann, Astrid
  • Zenke, Frank

Abstract

The present invention relates to methods for treating diseases and conditions characterised by aberrant cell growth, e.g., cancers, comprising administering a combination of a DNA repair inhibitor and a molecular targeted radioimmunotherapeutic agent.

IPC Classes  ?

  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 51/10 - Antibodies or immunoglobulins; Fragments thereof
  • A61P 35/00 - Antineoplastic agents
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
  • C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes

8.

PROTEINS THAT DECOUPLE T CELL-MEDIATED TUMOR CYTOTOXICITY FROM RELEASE OF PRO-INFLAMMATORY CYTOKINES

      
Document Number 03228654
Status Pending
Filing Date 2022-08-09
Open to Public Date 2023-02-16
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Rabinovich, Brian
  • Dawson, Jessica
  • Zhou, Xueyuan
  • Becker, Stefan
  • Nanfack, Yves Fomekong
  • Schroeter, Christian
  • Toleikis, Lars
  • Doerner, Achim
  • Hock, Bjorn

Abstract

This disclosure relates generally to proteins target tumor cell killing comprising: a polypeptide or complex of two or more polypeptides that specifically binds ROR1, and a polypeptide or complex of two or more polypeptides that specifically binds CD3. In some embodiments, the present application provides antibodies that specifically bind ROR1. In some embodiments the application also provides therapeutic methods for using such proteins in the treatment of a cancer.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • C07K 16/46 - Hybrid immunoglobulins
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

9.

METHOD FOR REDUCING ENDOTOXIN LEVELS IN NUCLEIC ACID PURIFICATION

      
Document Number 03227947
Status Pending
Filing Date 2022-08-03
Open to Public Date 2023-02-09
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Heinen-Kreuzig, Anja
  • Kiesewetter, Andre
  • Stein, Andreas
  • Gupta, Akshat

Abstract

The present invention relates to a method for reducing endotoxin levels or removing endotoxins from nucleic acids. For this a non-ionic detergent selected from the group of alkylglycosides and secondary alcohol alkoxylates or mixtures thereof is added prior or during anion exchange chromatographic purification of the nucleic acids using a membrane or monolith-based sorbent.

IPC Classes  ?

  • C12N 15/10 - Processes for the isolation, preparation or purification of DNA or RNA

10.

WATER SOLUBLE PRODRUG, CONJUGATES AND USES THEREOF

      
Document Number 03226393
Status Pending
Filing Date 2022-07-20
Open to Public Date 2023-02-02
Owner
  • RAMOT AT TEL-AVIV UNIVERSITY LTD. (Israel)
  • MERCK PATENT GMBH (Germany)
Inventor
  • Shabat, Doron
  • Satchi-Fainaro, Ronit
  • Sweeney-Lasch, Stanley
  • Deutsch, Carl
  • Berger, Nir

Abstract

This invention provides prodrug and conjugates thereof, uses, kits and pharmaceutical compositions thereof.

IPC Classes  ?

  • C07C 211/46 - Aniline
  • C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

11.

SRPK INHIBITORS

      
Document Number 03227367
Status Pending
Filing Date 2022-07-28
Open to Public Date 2023-02-02
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Leiendecker, Matthias
  • Heinrich, Timo

Abstract

Novel compounds of formula (I), wherein W1, W2, W3, W4, R1, R2, R3, R4, R5, R6 and m have the meaning according to the claims, are SRPK inhibitors, and can be used, inter alia, for the treatment of hyperproliferative disorders.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
  • A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 17/06 - Antipsoriatics
  • A61P 25/04 - Centrally acting analgesics, e.g. opioids
  • A61P 27/02 - Ophthalmic agents
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P 35/00 - Antineoplastic agents
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems

12.

NOVEL CRYSTALLINE FORMS OF [(1R)-2-(1-BENZOFURAN-3-YL)-1-{[(1S,2R,4R)-7- OXABICYCLO[2.2.1]HEPTAN-2-YL]FORMAMIDO}ETHYL]BORONIC ACID, ADDUCTS THEREOF, AND PROCESSES TO OBTAIN

      
Document Number 03227452
Status Pending
Filing Date 2022-07-28
Open to Public Date 2023-02-02
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Gruia, Delia-Maria
  • Klein, Markus
  • Lange, Michael

Abstract

The present invention relates to a solid form of [(1R)-2-(1-benzofuran-3-yl)-1- {[(1S,2R,4R)-7-oxabicyclo[2.2.1]heptan-2-yl]formamido}ethyl]boronic acid, hydrates, solvates, and/or adducts thereof useful as LMP7 inhibitors.

IPC Classes  ?

13.

ANTI-PROTAC ANTIBODIES AND COMPLEXES

      
Document Number 03225636
Status Pending
Filing Date 2022-07-01
Open to Public Date 2023-01-05
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Rieker, Marcel
  • Jaeger, Sebastian
  • Rasche, Nicolas
  • Koenning, Doreen
  • Schroeter, Christian
  • Schneider, Hendrik

Abstract

The present invention relates to mono or bi-specific antibodies, or antibody fragments or fusion proteins thereof, capable of binding to the VHL ligand degrading moiety (degron) of a proteolysis targeting chimera (PROTAC) and, optionally, to a target protein. The invention also relates to complexes (PAX) of such antibodies, or antibody fragments or fusion proteins thereof, and PROTACS, as well as methods for their production, and medical as well as non- medical uses each thereof.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
  • C07K 16/44 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere
  • G01N 33/53 - Immunoassay; Biospecific binding assay; Materials therefor
  • G01N 33/573 - Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes

14.

VHH-BASED NKP30 BINDERS

      
Document Number 03224912
Status Pending
Filing Date 2022-06-22
Open to Public Date 2022-12-29
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Zielonka, Stefan
  • Toleikis, Lars
  • Krah, Simon
  • Pekar, Lukas
  • Evers, Andreas

Abstract

The present disclosure relates to VHH-based NKp30 binders with favorable characteristics. Moreover, the present disclosure relates to pharmaceutical compositions comprising such a compound and the use of such compounds and such pharmaceutical compositions in medical treatment methods.

IPC Classes  ?

  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • A61P 35/00 - Antineoplastic agents

15.

PROTEINS THAT BIND CD80 AND/OR CD86, AND OX40L

      
Document Number 03218785
Status Pending
Filing Date 2022-06-07
Open to Public Date 2022-12-15
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Gross, Alec
  • Sun, Chia Chi
  • Chen, Gang
  • Nanfack, Yves Fomekong
  • An, Qi
  • Zakeri, Bijan
  • Ji, Qingyong

Abstract

This disclosure relates generally to proteins that inhibit T cell costimulatory signaling comprising: a polypeptide or complex of two or more polypeptides that specifically binds CD80 and/or CD86, and a polypeptide or complex of two or more polypeptides that specifically binds OX40L. In some embodiments, the present application provides antibodies that specifically bind OX40L. In some embodiments the application also provides therapeutic methods for using such proteins in the treatment of autoimmune diseases.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • C12N 15/09 - Recombinant DNA-technology
  • C12N 15/13 - Immunoglobulins
  • C12P 21/08 - Monoclonal antibodies

16.

COMPOUNDS FOR THE TREATMENT OF GLIOBLASTOMA

      
Document Number 03222061
Status Pending
Filing Date 2022-06-02
Open to Public Date 2022-12-08
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Gann, Claudia-Nanette
  • Celik, Ilhan
  • Majd, Nazanin
  • De Groot, John Frederick
  • Weller, Michael

Abstract

The present invention encompasses cMET inhibitors for use in the treatment of glioblastoma, including disseminated glioblastoma harboring MET amplification.

IPC Classes  ?

  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61N 5/10 - X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
  • A61P 35/00 - Antineoplastic agents

17.

EGFR TARGETING FC ANTIGEN BINDING FRAGMENT-DRUG CONJUGATES

      
Document Number 03221411
Status Pending
Filing Date 2022-05-23
Open to Public Date 2022-12-01
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Jaeger, Sebastian
  • Schroeter, Christian

Abstract

The invention relates to EGFR targeting Fc antigen binding fragment-drug conjugates (EGFR F cab-drug conjugates) and the use of the EGFR F cab-drug conjugates of the present invention for the treatment and/or prevention of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such EGFR Fcab-drug conjugates. Further, the invention relates to EGFR F cab-label conjugates and diagnostic compositions containing such EGFR Fcab-label conjugates.

IPC Classes  ?

  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • A61P 35/00 - Antineoplastic agents

18.

HER2 TARGETING FC ANTIGEN BINDING FRAGMENT-DRUG CONJUGATES

      
Document Number 03218697
Status Pending
Filing Date 2022-04-29
Open to Public Date 2022-11-10
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Jaeger, Sebastian
  • Schroeter, Christian

Abstract

The invention relates to HER2 targeting Fc antigen binding fragment-drug conjugates (HER2 Fcab-drug conjugates) and the use of the HER2 Fcab-drug conjugates of the present invention for the treatment and/or prevention of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such HER2 Fcab-drug conjugates. Further, the invention relates to HER2 Fcab-label conjugates and diagnostic compositions containing such HER2 Fcab-label conjugates.

IPC Classes  ?

  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • A61K 49/00 - Preparations for testing in vivo
  • A61P 35/00 - Antineoplastic agents
  • C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

19.

2,8-DIHYDROPYRAZOLO[3,4-B]INDOLE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER

      
Document Number 03218932
Status Pending
Filing Date 2021-11-02
Open to Public Date 2022-11-10
Owner
  • MERCK PATENT GMBH (Germany)
  • CANCER RESEARCH TECHNOLOGY LTD. (United Kingdom)
Inventor
  • Heinrich, Timo
  • Schlesiger, Sarah
  • Gunera, Jakub
  • Koetzner, Lisa
  • Carswell, Emma
  • Blum, Andreas

Abstract

The present invention relates to tricyclic heterocycles. These heterocyclic compounds are useful as TEAD binders and/or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases, in particular cancer.

IPC Classes  ?

  • C07D 471/14 - Ortho-condensed systems
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/4196 - 1,2,4-Triazoles
  • A61K 31/4245 - Oxadiazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
  • A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 35/00 - Antineoplastic agents
  • C07D 487/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

20.

METHODS FOR THE ADMINISTRATION OF ADAMTS BINDING IMMUNOGLOBULINS

      
Document Number 03216512
Status Pending
Filing Date 2022-04-29
Open to Public Date 2022-11-03
Owner
  • NOVARTIS AG (Switzerland)
  • MERCK PATENT GMBH (Germany)
Inventor
  • Flesch, Gerard
  • Guehring, Hans
  • Schieker, Matthias Klaus

Abstract

Disclosed herein are methods and dosage regimens for the treatment of osteoarthritis (e.g., knee osteoarthritis). The methods and dosage regimens comprise administration of an ADAMTS5 inhibiting polypeptide in a therapeutically effective amount.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
  • C07K 16/46 - Hybrid immunoglobulins

21.

METHOD FOR EVALUATION OF A THIN-LAYER CHROMATOGRAPHY PLATE

      
Document Number 03201795
Status Pending
Filing Date 2021-11-12
Open to Public Date 2022-05-19
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Oberle, Michaela
  • Schunda, Eric
  • Fischer, Robert

Abstract

A method for evaluation of a thin-layer chromatography plate (2) after performing a separation process that separates components of a sample on the thin-layer chromatography plate (2) comprises a digitization step, wherein at least two digital images (1, 5) are taken that differ with respect to the wavelength range of illumination of the thin-layer chromatography plate (2). The method further comprises a position identification step wherein the position of the thin-layer chromatography plate (2) is identified for each of the at least two digital images (1, 5). Furthermore, the method comprises an evaluation step wherein an image information of the at least two digital images (1, 5) is superimposed for at least all regions with at least one visible spot (9, 10) within at least one of the at least two digital images (1, 5), so that the superimposition (10) of image information from identical regions of at least two digital images (1, 5) can be used for evaluation of the thin-layer chromatography.

IPC Classes  ?

  • G01N 21/31 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry
  • G01N 30/95 - Detectors specially adapted therefor; Signal analysis

22.

COVER FOR A THIN-LAYER CHROMATOGRAPHY DEVELOPMENT CHAMBER

      
Document Number 03201798
Status Pending
Filing Date 2021-11-12
Open to Public Date 2022-05-19
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Oberle, Michaela
  • Schunda, Eric
  • Fischer, Robert

Abstract

A thin-layer chromatography development chamber (1) that can be used for developing thin-layer chromatography plates (21) by introducing a liquid solvent onto a sample arranged on the surface of a thin-layer chromatography plate (21), whereby the solvent and the thin-layer chromatography plate (21) can be inserted into the development chamber (1), comprises a housing (2) with an opening (3). The opening (3) of the development chamber (1) can be closed with a cover (4) that comprises a data input unit (10) for entering or collecting data related to a development process performed within the development chamber (1). The cover (4) further comprises a data communication unit (16) that enables a wireless data transmission of the data related to the development process to a thin- layer chromatography data storage device (24).

IPC Classes  ?

  • G01N 30/90 - Plate chromatography, e.g. thin layer or paper chromatography
  • G01N 30/94 - Development

23.

KINASE INHIBITOR COMBINATIONS FOR CANCER TREATMENT

      
Document Number 03201799
Status Pending
Filing Date 2021-11-15
Open to Public Date 2022-05-19
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Clark, Anderson
  • Machl, Andreas
  • Huck, Bayard
  • Wilker, Erik
  • Kaleta, Remigiusz

Abstract

The invention relates to combinations of 4-[(S)-2-Azetidin-1-yl-1-(4-chloro-3-trifluoromethyl-phenyl)-ethylamino]-quinazoline-8-carboxylic acid amide and/or its physiologically acceptable salts and solvates, and an inhibitor of MEK kinase, and as an optional third inhibitor, with an inhibitor of EGFR, and the use of such combinations for the treatment of cancer, and to combinations of 4-[(S)-2-Azetidin-1-yl-1-(4-chloro-3-trifluoromethyl-phenyl)-ethylamino]-quinazoline-8-carboxylic acid amide and/or its physiologically acceptable salts and solvates, and an inhibitor of EGFR.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
  • A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61P 35/00 - Antineoplastic agents

24.

PROTEINS FOR THE DETECTION OF SCHISTOSOMA INFECTION

      
Document Number 03196094
Status Pending
Filing Date 2021-10-27
Open to Public Date 2022-05-05
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Greco, Beatrice
  • Oeuvray, Claude
  • Loukas, Alex
  • Pearson, Mark
  • Sotillo-Gallego, Javier

Abstract

The invention pertains to the field of diagnostic tools for the detection of Schistosoma infection. The invention pertains to proteins derived from Schistosoma Haematobium antigens, useful alone or in combination for the detection of anti-Schistosoma antibodies in biological samples, and thus for the diagnosis of Schistosoma infection in humans.

IPC Classes  ?

  • G01N 33/569 - Immunoassay; Biospecific binding assay; Materials therefor for microorganisms, e.g. protozoa, bacteria, viruses

25.

ATR INHIBITORS FOR USE IN THE TREATMENT OF VIRAL INFECTIONS

      
Document Number 03199472
Status Pending
Filing Date 2021-10-22
Open to Public Date 2022-05-05
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Betz, Ulrich
  • Fuchss, Thomas

Abstract

The present invention encompasses ATR inhibitor for use in the treatment of coronavirus infections, including COVID-19, alone or in combination with one or more additional therapeutic agents.

IPC Classes  ?

  • A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
  • A61K 31/4706 - 4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
  • A61K 38/21 - Interferons
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 31/14 - Antivirals for RNA viruses

26.

LMP7-SELECTIVE INHIBITORS FOR THE TREATMENT OF BLOOD DISORDERS AND SOLID TUMORS

      
Document Number 03198048
Status Pending
Filing Date 2021-10-05
Open to Public Date 2022-04-14
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Esdar, Christina
  • Friese-Hamim, Manja
  • Sanderson, Michael
  • Walter-Bausch, Gina

Abstract

The present invention relates to use of a-amino boronic acid derivatives which are useful for selectively inhibiting the activity of immunoproteasome subunit LMP7 and for the treatment of medical conditions affected by immunoproteasome activity such as blood disorders and solid tumors which are defined by specific genetic alterations and/or inadequate responsiveness to other therapeutic treatments In particular, the compounds of the present invention are selective LMP7 inhibitors which may be useful alone, or in combination for the treatment of blood disorders, such as multiple myeloma, and certain solid tumors.

IPC Classes  ?

  • A61K 31/00 - Medicinal preparations containing organic active ingredients
  • A61K 31/69 - Boron compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia

27.

METHODS FOR TARGET RELEASE FROM INTEIN COMPLEXES

      
Document Number 03191699
Status Pending
Filing Date 2021-09-27
Open to Public Date 2022-03-31
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Rammo, Oliver
  • Kohl, Vanessa

Abstract

The present disclosure relates to methods of releasing a target molecule from intein complexes comprising an intein-C tagged target molecule and intein-N polypeptides, by contacting the intein complexes with nitrogen containing heteroaromatic derivatives, and/or by increasing residence time of intein complexes in a medium effective to remove the target molecule. Modulating the pH further facilitates target release.

IPC Classes  ?

  • C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
  • C12N 11/082 - Enzymes or microbial cells immobilised on or in an organic carrier the carrier being a synthetic polymer obtained by reactions only involving carbon-to-carbon unsaturated bonds
  • C07K 14/005 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from viruses
  • C07K 14/245 - Escherichia (G)
  • C07K 14/505 - Erythropoietin (EPO)
  • C07K 19/00 - Hybrid peptides
  • C12N 9/02 - Oxidoreductases (1.), e.g. luciferase
  • C12N 15/62 - DNA sequences coding for fusion proteins
  • C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
  • C12P 21/06 - Preparation of peptides or proteins produced by the hydrolysis of a peptide bond, e.g. hydrolysate products

28.

PHARMACEUTICAL PREPARATION

      
Document Number 03190226
Status Pending
Filing Date 2021-09-15
Open to Public Date 2022-03-24
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Ambruosi, Alessandra
  • Mannini, Riccardo
  • Riehl, Markus
  • Becker, Axel

Abstract

The present invention relates to a solid pharmaceutical preparation of of 8-(1,3-Dimethyl-1H-pyrazol-4-yl)-1-(Sa)-(3-fluoro-5-methoxy-pyridin-4-yl)-7-methoxy-3-methyl-1,3-dihydro-imidazo[4,5-c]quinolin-2-one, as well as a method of making same, as well as medical uses thereof.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - Agglomerates; Granulates; Microbeadlets

29.

MOLECULES WITH SOLUBILITY TAG AND RELATED METHODS

      
Document Number 03192679
Status Pending
Filing Date 2021-09-17
Open to Public Date 2022-03-24
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Deutsch, Carl
  • Kelly, Sven
  • Crassier, Helene
  • Korpus, Christoph
  • Von Hagen, Joerg
  • Richter-Sander, Ulrike

Abstract

The present disclosure relates to molecules with a solubility tag, wherein the solubility tag comprises a chito-oligosaccharide, and to methods for increasing the solubility of a molecule. Moreover, the present disclosure relates to antibody-drug conjugates with solubility tag, methods and compounds for preparing such antibody-drug conjugates, methods for increasing the solubility of antibody-drug conjugates, antibody-drug conjugates prepared by such methods, as well as the use of such antibody-drug conjugates in medical treatment.

IPC Classes  ?

  • A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
  • C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

30.

NOVEL TREATMENT REGIMEN FOR THE TREATMENT OF AUTOIMMUNE DISORDERS

      
Document Number 03194812
Status Pending
Filing Date 2021-09-10
Open to Public Date 2022-03-17
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Boschert, Ursula
  • Wiedemann, Urs

Abstract

The present invention relates to a novel treatment regimen for the treatment of autoimmune disorders. Said novel treatment regimen preferably provides for an efficacious treatment of autoimmune disorders with an advantageous safety profile and/or a high quality of life for the patient. Preferably, said novel treatment regimen provides for an advantageous benefit-risk ratio for patients endangered by the risk of infections.

IPC Classes  ?

  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61P 37/00 - Drugs for immunological or allergic disorders

31.

ANTI-CEACAM5 ANTIBODIES AND CONJUGATES AND USES THEREOF

      
Document Number 03190586
Status Pending
Filing Date 2021-08-13
Open to Public Date 2022-03-10
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Anderl, Jan
  • Raab-Westphal, Sabine
  • Hecht, Stefan
  • Deutsch, Carl
  • Shan, Min
  • Konning, Doreen
  • Sloot, Willem N.
  • Hart, Felix
  • Schroter, Christian
  • Toleikis, Lars
  • Berger, Nir

Abstract

The invention provides antibodies which bind human CEACAM5 protein, as well as isolated nucleic acids and host cells comprising a sequence encoding said antibodies. The invention also provides immunoconjugates comprising said antibodies linked to a growth-inhibitory agent, and pharmaceutical compositions comprising antibodies or immunoconjugates of the invention. The invention also provides use of the antibodies, immunoconjugates and pharmaceutical compositions of the invention for the treatment of cancer or for diagnostic purposes.

IPC Classes  ?

  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies

32.

NKP30 BINDERS

      
Document Number 03191859
Status Pending
Filing Date 2021-08-31
Open to Public Date 2022-03-10
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Zielonka, Stefan
  • Toleikis, Lars
  • Krah, Simon
  • Pekar, Lukas

Abstract

The present disclosure relates to B7-H6-based compounds with favorable characteristics. Moreover, the present disclosure relates to pharmaceutical compositions comprising such a compound and the use of such compounds and such pharmaceutical compositions in medical treatment methods. Moreover, the present disclosure relates to methods for preparing a compound with an increased affinity for NKp30.

IPC Classes  ?

  • A61K 38/17 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans
  • A61P 35/00 - Antineoplastic agents
  • C07K 14/71 - Receptors; Cell surface antigens; Cell surface determinants for growth regulators
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
  • C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes

33.

PROCESS SYSTEM FOR BIOREACTOR-BASED CLEAN MEAT PRODUCTION

      
Document Number 03190611
Status Pending
Filing Date 2021-08-19
Open to Public Date 2022-02-24
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Weissenbach, Jean-Louis
  • Sylvia, Ryan
  • Von Der Brelie, Almut
  • Brandl, Melanie
  • Fesenfeld, Michaela

Abstract

The present invention is for a closed environment process for the growth and differentiation of cells and the culturing of cells to confluency for the production of tissue. The tissue may be a clean meat product.

IPC Classes  ?

  • C12M 3/00 - Tissue, human, animal or plant cell, or virus culture apparatus
  • C12N 5/0735 - Embryonic stem cells; Embryonic germ cells
  • C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
  • A23L 13/00 - Meat products; Meat meal; Preparation or treatment thereof
  • C12M 1/00 - Apparatus for enzymology or microbiology
  • C12M 3/02 - Tissue, human, animal or plant cell, or virus culture apparatus with means providing suspensions

34.

CONSUMABLE TISSUE-LIKE STRUCTURE GENERATED WITH MUSCLE CELLS GROWN ON EDIBLE HOLLOW FIBERS

      
Document Number 03190453
Status Pending
Filing Date 2021-08-19
Open to Public Date 2022-02-24
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Weissenbach, Jean-Louis
  • Sylvia, Ryan
  • Von Der Brelie, Almut
  • Brandl, Melanie
  • Fesenfeld, Michaela

Abstract

The present invention is directed toward edible hollow fibers and cartridges and bioreactors comprising the hollow fibers of the present invention, as well as, methods of production of structured clean meat products produced with the hollow fibers, cartridges and bioreactors of the present invention and the structured clean meat products produced by said methods. The macroscopic structure of structured clean meat grown on edible hollow fibers will result in a unique final structure. This final structure will contain a finite amount of fibers per unit area; with meat on the outside of the fibers.

IPC Classes  ?

  • A23L 13/00 - Meat products; Meat meal; Preparation or treatment thereof
  • C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
  • C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor

35.

NOZZLE FOR FLUID DEPLOYMENT IN BIOREACTORS

      
Document Number 03190789
Status Pending
Filing Date 2021-08-04
Open to Public Date 2022-02-10
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Berti Perez, Stefano
  • Jourdainne, Laurent

Abstract

A nozzle system for fluid deployment for treating a biological fluid within a bioreactor, having a bioreactor having an internal volume; an adjustable nozzle deployed within the internal volume; a reservoir capable of containing an agent; and a tubing connecting the reservoir and the adjustable nozzle, wherein the adjustable nozzle is capable of being adjusted to distribute a processing agent in a plurality of distribution streams.

IPC Classes  ?

36.

TRICYCLIC HETEROCYCLES

      
Document Number 03185634
Status Pending
Filing Date 2021-07-20
Open to Public Date 2022-01-27
Owner
  • MERCK PATENT GMBH (Germany)
  • CANCER RESEARCH TECHNOLOGY LTD. (United Kingdom)
Inventor
  • Heinrich, Timo
  • Schlesiger, Sarah
  • Gunera, Jakub
  • Koetzner, Lisa
  • Carswell, Emma
  • Blum, Andreas

Abstract

The present invention relates to tricyclic heterocycles. These heterocyclic compounds are useful as TEAD binders and/or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases, in particular cancer.

IPC Classes  ?

  • A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
  • A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
  • A61P 35/00 - Antineoplastic agents
  • C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
  • C07D 487/04 - Ortho-condensed systems

37.

VISCOSITY REDUCING EXCIPIENTS AND COMBINATIONS THEREOF FOR HIGHLY CONCENTRATED PROTEIN FORMULATIONS

      
Document Number 03187322
Status Pending
Filing Date 2021-07-12
Open to Public Date 2022-01-20
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Rosenkranz, Tobias
  • Braun, Stefan

Abstract

The present invention relates to liquid compositions and formulations comprising a protein having a reduced viscosity and/or increased stability. Furthermore, the invention relates to methods for reducing the viscosity and/or increasing the stability of a protein solution.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/08 - Solutions
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
  • A61K 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
  • A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
  • C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes

38.

DEVICE AND PROCESS FOR CELL CULTURE MEDIA PREPARATION AND PERFORMING CELL CULTURE

      
Document Number 03183646
Status Pending
Filing Date 2021-07-05
Open to Public Date 2022-01-13
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Sieck, Jochen Bastian
  • Schultheiss, Christian

Abstract

The present invention relates to a device and processes for producing liquid media for cell cultures, whereby the liquid media are produced automatically by dissolving ingredients in water. The present invention also relates to a device for producing media used in cell cultures or a substance produced by cell cultures using a bioreactor process.

IPC Classes  ?

  • C12M 1/02 - Apparatus for enzymology or microbiology with heat exchange means
  • C12M 1/26 - Inoculator or sampler
  • C12M 1/32 - Inoculator or sampler multiple field or continuous type
  • C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
  • C12M 1/36 - Apparatus for enzymology or microbiology including condition or time responsive control, e.g. automatically controlled fermentors

39.

COMBINATION OF A METHIONINE AMINOPEPTIDASE 2 INHIBITOR AND VEGFR/VEGF INHIBITOR

      
Document Number 03186322
Status Pending
Filing Date 2021-07-06
Open to Public Date 2022-01-13
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Friese-Hamim, Manja
  • Rohdich, Felix
  • Gimmi, Claude
  • Schultes, Christoph
  • Bogatyrova, Olga

Abstract

The invention relates to combinations of (S)-3-Hydroxy-1-(1H-indol-5-yl)-2-oxo- pyrrolidine-3-carboxylic acid 3,5-difluoro-benzylamide and a VEGFR/VEGF inhibitor, or their physiologically acceptable salts, as well as to the use of such combinations for the prophylaxis or treatment of cancer.

IPC Classes  ?

  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
  • A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/47 - Quinolines; Isoquinolines
  • A61K 31/5025 - Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61P 35/02 - Antineoplastic agents specific for leukemia

40.

TLR7/8 ANTAGONISTS AND USES THEREOF

      
Document Number 03182616
Status Pending
Filing Date 2021-06-01
Open to Public Date 2021-12-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Okitsu, Lukas Shinji
  • Demartino, Julie
  • Spangenberg, Thomas

Abstract

The present invention relates to compounds of the invention and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.

IPC Classes  ?

  • A61K 31/4706 - 4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 37/00 - Drugs for immunological or allergic disorders

41.

COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS

      
Document Number 03184498
Status Pending
Filing Date 2021-06-15
Open to Public Date 2021-12-23
Owner MERCK PATENT GMBH (Germany)
Inventor Betz, Ulrich

Abstract

The present invention encompasses an ATM inhibitor for use in the treatment of coronavirus infections, including COVID-19, alone or in combination with one or more additional therapeutic agents.

IPC Classes  ?

  • A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 31/14 - Antivirals for RNA viruses

42.

COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS

      
Document Number 03183649
Status Pending
Filing Date 2021-06-15
Open to Public Date 2021-12-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Betz, Ulrich
  • Fuchss, Thomas

Abstract

The present invention encompasses ATR inhibitor for use in the treatment of virus infections, including SARS-CoV infections such as COVID-19, alone or in combination with one or more additional therapeutic agents.

IPC Classes  ?

  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 31/14 - Antivirals for RNA viruses

43.

BISPECIFIC ANTIBODY-DRUG CONJUGATES TARGETING EGFR AND MUC1 AND USES THEREOF

      
Document Number 03185458
Status Pending
Filing Date 2021-06-03
Open to Public Date 2021-12-09
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Yam, Alice
  • Knuehl, Christine
  • Toleikis, Lars
  • Amendt, Christiane
  • Doerner, Achim
  • Li, Xiaofan
  • Stafford, Ryan
  • Henningsen, Robert
  • Zhou, Sihong

Abstract

Provided are immunoconjugates comprising bispecific anti-MUC 1/EGFR antibodies conjugated to hemiasterlin-based moieties via cleavable linkers, and pharmaceutical compositions thereof. Provided also are methods of treating cancer using such immunoconjugates and pharmaceutical compositions.

IPC Classes  ?

  • A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
  • A61P 35/00 - Antineoplastic agents
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells

44.

TRICYCLIC HETEROCYCLES USEFUL AS TEAD BINDERS

      
Document Number 03180798
Status Pending
Filing Date 2021-05-05
Open to Public Date 2021-11-11
Owner
  • MERCK PATENT GMBH (Germany)
  • CANCER RESEARCH TECHNOLOGY LTD. (United Kingdom)
Inventor
  • Heinrich, Timo
  • Schlesiger, Sarah
  • Gunera, Jakub
  • Carswell, Emma
  • Koetzner, Lisa
  • Blum, Andreas

Abstract

The present invention relates to tricyclic heterocycles. These heterocyclic compounds are useful as TEAD binders and/or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases, in particular cancer.

IPC Classes  ?

  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61P 35/00 - Antineoplastic agents
  • C07D 471/14 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 498/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

45.

PHARMACEUTICAL PROCESS

      
Document Number 03181613
Status Pending
Filing Date 2021-04-29
Open to Public Date 2021-11-04
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Werner, Joerg
  • Schlaps, Dieter

Abstract

The present disclosure relates to a computer-implemented method for eliminating the barriers of classical information systems and discloses a homogeneous data management system with the objective to streamline and automatize data integration for enriching pharmaceutical regulatory semantic model associated with a regulatory status of a pharmaceutical product.

IPC Classes  ?

  • G06F 16/36 - Creation of semantic tools, e.g. ontology or thesauri

46.

CRYSTALLINE FORMS OF 4-[(7-CHLORO-2-METHOXYBENZO[B][1,5]NAPHTHYRIDIN-10-YL)AMINO]-2,6-BIS(PYRROLIDIN-1-YLMETHYL)PHENOL AND SALTS THEREOF

      
Document Number 03175552
Status Pending
Filing Date 2021-04-14
Open to Public Date 2021-10-21
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Becker, Axel
  • Gruia, Delia-Maria

Abstract

The present invention relates to novel crystalline of 4-[(7-chloro-2- methoxy benzo[b][ 1, 5]na phthy rid in-10-yl)amino]-2,6-bis(pyrrolid in-1 - ylmethyOphenol and salts thereof, as well as processes of manufacturing the same, and pharmaceutical formulations and uses thereof in the treatment of parasitic infections such as malaria.

IPC Classes  ?

  • A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 33/06 - Antimalarials
  • C07D 471/04 - Ortho-condensed systems

47.

REUSE OF INTEIN-BOUND RESINS FOR PROTEIN PURIFICATION

      
Document Number 03176751
Status Pending
Filing Date 2021-03-23
Open to Public Date 2021-09-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Rammo, Oliver
  • Skudas, Romas

Abstract

The present disclosure relates to methods of protein purification by attaching an intein-C fragment to a target protein, passing a sample containing the intein-C tagged protein over a chromatographic resin carrying an intein-N fragment so as to create an intein-N intein- C complex, releasing the target protein from the intein-C fragment, and regenerating the column under conditions that disrupt the intein-N intein-C complex while preserving column functionality for multiple reuses.

IPC Classes  ?

  • C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes

48.

CONDENSED PYRIDINE DERIVASTIVES SUBSTITUED BY AMIDE FUNCTIONS AS ACSS2 INHIBITORS

      
Document Number 03175736
Status Pending
Filing Date 2021-03-16
Open to Public Date 2021-09-23
Owner
  • MERCK PATENT GMBH (Germany)
  • RYVU THERAPEUTICS S.A. (Poland)
Inventor
  • Koetzner, Lisa
  • Fuchss, Thomas
  • Schindler, Christina
  • Kuhn, Daniel

Abstract

The present invention relates to substituted amide derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.

IPC Classes  ?

49.

TETRAZOLE DERIVATIVES

      
Document Number 03175738
Status Pending
Filing Date 2021-03-16
Open to Public Date 2021-09-23
Owner
  • MERCK PATENT GMBH (Germany)
  • RYVU THERAPUTICS S.A. (Poland)
Inventor
  • Fuchss, Thomas
  • Koetzner, Lisa
  • Schindler, Christina
  • Kuhn, Daniel

Abstract

The present invention relates to substituted tetrazole derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.

IPC Classes  ?

  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61P 35/00 - Antineoplastic agents
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

50.

MODULAR INCUBATION CHAMBER AND METHOD OF VIRUS INACTIVATION

      
Document Number 03169397
Status Pending
Filing Date 2021-02-03
Open to Public Date 2021-08-12
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Coton, Thomas
  • Muldoon, Joseph William
  • Ormond, James

Abstract

An incubation chamber that may be provided in modular form in order to provide flexibility in flow rate and/or residence time of a product stream is disclosed. Assemblies including such incubation chambers for purification of biomolecules are also disclosed, as are methods for biomolecule purification, and in particular, methods for virus inactivation in an incubation chamber or in a plurality of incubation chambers arranged in series.

IPC Classes  ?

51.

USE OF THE GDF-5 MUTANT FOR THE TREATMENT OF PAIN AND CARTILAGE DESTRUCTION

      
Document Number 03165095
Status Pending
Filing Date 2020-12-15
Open to Public Date 2021-06-24
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Kleinschmidt-Doerr, Kerstin
  • Gigout, Anne
  • Werkmann, Daniela

Abstract

The present invention is directed to the use of the GDF-5 mutant with an amino acid exchange R399E for the treatment of cartilage defects and pain and a pharmacological composition of said GDF-5 mutant.

IPC Classes  ?

  • A61K 38/18 - Growth factors; Growth regulators
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • C07K 14/475 - Growth factors; Growth regulators

52.

CONDENSED THIOPHENE DERIVATIVES AS HYPOXIA INDUCIBLE FACTOR (HIF) INHIBITORS

      
Document Number 03162574
Status Pending
Filing Date 2020-11-24
Open to Public Date 2021-06-03
Owner
  • MERCK PATENT GMBH (Germany)
  • RYVU THERAPEUTICS S.A. (Poland)
Inventor
  • Leiendecker, Matthias
  • Buchstaller, Hans-Peter
  • Fuchss, Thomas

Abstract

Compounds of the formula I in which R1, R2, R3, R4, R5, n and m have the meanings indicated in Claim 1, are inhibitors of HIF-2a, and can be employed for the treatment of diseases such as cancer.

IPC Classes  ?

  • C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
  • A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
  • A61P 35/00 - Antineoplastic agents

53.

ANTI-TIGIT ANTIBODIES AND USES THEREOF

      
Document Number 03151307
Status Pending
Filing Date 2020-11-05
Open to Public Date 2021-05-14
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Zhang, Dong
  • Kelton, Christie
  • Li, Liwei
  • Nannemann, David
  • Yeh, Johannes
  • Iffland, Christel
  • An, Qi
  • Zhao, Xinyan

Abstract

The present application relates to anti-TIGIT antibodies or antigen binding fragments thereof, nucleic acid encoding the same, therapeutic compositions thereof, and their use to enhance T-cell function to upregulate cell-mediated immune responses and for the treatment of T cell dysfunctional disorders, such as tumor immunity, for the treatment of infectious diseases and cancer.

IPC Classes  ?

  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • A61P 35/00 - Antineoplastic agents
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
  • C12N 15/13 - Immunoglobulins
  • C12P 21/08 - Monoclonal antibodies

54.

COMBINED INHIBITION OF PD-1, TGFB AND TIGIT FOR THE TREATMENT OF CANCER

      
Document Number 03155219
Status Pending
Filing Date 2020-11-05
Open to Public Date 2021-05-14
Owner
  • MERCK PATENT GMBH (Germany)
  • GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 4) LTD. (United Kingdom)
Inventor
  • Xu, Chunxiao
  • Jiang, Feng
  • Zhang, Dong

Abstract

The present invention relates to combination therapies useful for the treatment of cancer. In particular, the invention relates to the combined use of a PD-1 inhibitor, a TGF? inhibitor, and a TIGIT inhibitor to treat cancer.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 14/71 - Receptors; Cell surface antigens; Cell surface determinants for growth regulators
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

55.

MATERIAL AND METHOD FOR PERFORMING A SEPARATION BASED ON HALOGEN BONDING

      
Document Number 03158568
Status Pending
Filing Date 2020-10-21
Open to Public Date 2021-04-29
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Hoge, Berthold Theo
  • Waltersmann, Paul Lukas
  • Bader, Anne Julia

Abstract

This invention relates to a new stationary phase carrying functional groups comprising a halogen substituted aromatic ring. Target molecules can interact with this stationary phase by halogen bonding. The stationary phase is suitable for SPE or chromatographic separations.

IPC Classes  ?

  • B01J 20/26 - Synthetic macromolecular compounds
  • B01D 15/08 - Selective adsorption, e.g. chromatography
  • B01J 20/28 - Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties
  • B01J 20/288 - Polar phases
  • B01J 20/32 - Impregnating or coating
  • C07K 1/16 - Extraction; Separation; Purification by chromatography

56.

ELUTION OF MONOCLONAL ANTIBODIES IN PROTEIN A AFFINITY CHROMATOGRAPHY

      
Document Number 03156648
Status Pending
Filing Date 2020-10-01
Open to Public Date 2021-04-08
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Korpus, Christoph
  • Hafiz, Supriyadi

Abstract

The invention provides a method for eluting a monoclonal antibody from a Protein A affinity chromatography column to which the monoclonal antibody is bound comprising a) contacting the affinity chromatography column with an elution buffer comprising a poly (ethylene glycol) polymer; b) collecting one or more fractions containing the monoclonal antibody obtained from step (a) c) combining the fractions obtained from step (b) to form an elution product pool.

IPC Classes  ?

  • C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

57.

PURIFICATION OF PROTEINS AND VIRAL INACTIVATION

      
Document Number 03156649
Status Pending
Filing Date 2020-10-01
Open to Public Date 2021-04-08
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Korpus, Christoph
  • Hafiz, Supriyadi
  • Krog, Alexandra
  • Skudas, Romas

Abstract

The invention provides a method for purifying a target protein from a cell culture sample, wherein the cell culture sample comprises the target protein, viral compounds and other product and process related impurities, comprising an affinity chromatography step, a virus inactivation step and optionally other purification steps, wherein the affinity chromatography step comprises a) loading an affinity chromatography column with the cell culture sample thereby binding the target protein to the affinity chromatography column; b) eluting the target protein from the affinity chromatography column by contacting the affinity chromatography column with an elution buffer having a pH < 6 and comprising an excipient, wherein the excipient is selected from the group consisting of disaccharides, polyols and poly (ethylene glycol) polymers; c) collecting one or more fractions containing the target protein obtained from step (b); d) potentially combining the fractions obtained from step (c) to form an elution product pool, and wherein the virus inactivation step comprises e) incubating the elution product pool at a pH from 2.5 to 4.5.

IPC Classes  ?

  • C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
  • C12N 7/04 - Inactivation or attenuation; Producing viral sub-units
  • C12P 21/00 - Preparation of peptides or proteins

58.

CAMPHORSULFONIC ACID AND COMBINATIONS THEREOF WITH CATIONIC EXCIPIENTS AS VISCOSITY REDUCING AGENTS IN HIGH CONCENTRATED PROTEIN FORMULATIONS

      
Document Number 03154653
Status Pending
Filing Date 2020-09-16
Open to Public Date 2021-03-25
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Rosenkranz, Tobias
  • Guebeli, Raphael Johannes
  • Henzler, Tanja
  • Krog, Alexandra
  • Hildebrandt, Christian

Abstract

The present invention relates to compositions of highly concentrated protein formulations showing reduced viscosity, which is induced by the addition of at least camphorsulfonic acid. The contained proteins in the prepared formulations are stabilized against aggregation and denaturation and are thus sufficiently storage-stable until administration to the patient.

IPC Classes  ?

  • A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
  • A61K 9/08 - Solutions
  • A61K 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids

59.

COMBINATION OF A POXVIRUS ENCODING HPV POLYPEPTIDES AND IL-2 WITH AN ANTI-PD-L1 ANTIBODY

      
Document Number 03155090
Status Pending
Filing Date 2020-09-21
Open to Public Date 2021-03-25
Owner
  • TRANSGENE (France)
  • MERCK PATENT GMBH (Germany)
  • PFIZER INC. (USA)
Inventor
  • Bendjama, Kaidre
  • Brandely Talbot, Maud
  • Tavernaro, Annette

Abstract

The present invention relates to a combination of a) a poxvirus vector encoding at least human papillomavirus (HPV) E6 and E7 polypeptides and an immunostimulatory cytokine, and b) an anti-PD-L1 antibody or antigen-binding fragment thereof, for use in the treatment of an HPV-positive cancer, wherein a first administration of said poxvirus is performed 5 to 10 days before the first administration of said anti-PD-L1 antibody, and subsequent administrations of said poxvirus and anti-PD-L1 antibody are performed.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 39/285 - Vaccinia virus or variola virus
  • A61P 31/20 - Antivirals for DNA viruses
  • A61P 35/00 - Antineoplastic agents
  • C07K 14/025 - Papovaviridae, e.g. papillomavirus, polyomavirus, SV40, BK virus, JC virus
  • C07K 14/55 - IL-2
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • C12N 7/01 - Viruses, e.g. bacteriophages, modified by introduction of foreign genetic material
  • C12N 15/863 - Poxviral vectors, e.g. vaccinia virus

60.

OPTIMIZED ANALYTE DERIVATIZATION FOR SYNERGISTIC APPLICATION WITH CRYSTAL SPONGE METHOD

      
Document Number 03148335
Status Pending
Filing Date 2020-08-26
Open to Public Date 2021-03-04
Owner MERCK PATENT GMBH (Germany)
Inventor Hierse, Wolfgang

Abstract

The invention provides a sample preparation method (100) comprising: providing a sample (10) comprising an organic molecule (20), wherein the organic molecule (20) comprises a target group (21), wherein the target group (21) is a nucleophilic group and/or an acidic group; a derivatization stage (110) comprising: derivatizing the target group (21) of the organic molecule (20) with a moiety (31) comprising one or more of (i) a hydrocarbon comprising group and (ii) a 3rd period atom comprising group, wherein the 3rd period atom is selected from the group consisting of Si, P, and S, thereby providing a derivatized organic molecule (30); a separation stage (120) comprising: subjecting the sample (10) to a separation process to provide a fraction (35) comprising the derivatized organic molecule (30); and a preparation stage (130) comprising: introducing the derivatized organic molecule (30) into a porous single crystal (40), to provide a derivatized organic molecule doped porous single crystal (50).

IPC Classes  ?

  • G01N 23/20008 - Constructional details of analysers, e.g. characterised by X-ray source, detector or optical system; Accessories therefor; Preparing specimens therefor
  • G01N 33/68 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
  • G01N 23/207 - Diffractometry, e.g. using a probe in a central position and one or more displaceable detectors in circumferential positions

61.

METHOD FOR ADDITIVE MANUFACTURE OF A PRODUCT, MANUFACTURING DEVICE AND SOLID PHARMACEUTICAL DOSAGE FORM

      
Document Number 03150809
Status Pending
Filing Date 2020-08-07
Open to Public Date 2021-02-18
Owner MERCK PATENT GMBH (Germany)
Inventor Bogdahn, Malte

Abstract

A Method for additive manufacture of a product comprises a layer arrangement step, whereby a layer (11) of small particles (12) of a product material is arranged, and further comprises a solidification step whereby a laser beam (3) is directed at predefined spots (8, 9, 10) within the layer (11) of small particles (12) for heating and connecting the small particles (12) of the product material at said spots (8, 9, 10), resulting in at least one solidified area of product material within the layer (11) of small particles (12). The product is manufactured by repeatedly performing the layer arrangement step and the solidification step, whereby each solidified area of product material of the current layer (11) is connected with a previously solidified part of the product until the product is generated by interconnected solidified areas of connected product material. Within the solidification step the laser beam (3) is divided into at least two separate subbeams (4) that are directed at separate spots (8, 9, 10) for simultaneously connecting the small particles (12) of the product material at these separate spots (8, 9, 10). The at least two separate subbeams (4) are directed at separate spots (8, 9, 10) at a distance towards each other.

IPC Classes  ?

  • B29C 64/153 - Processes of additive manufacturing using only solid materials using layers of powder being selectively joined, e.g. by selective laser sintering or melting
  • B33Y 10/00 - Processes of additive manufacturing
  • B33Y 30/00 - ADDITIVE MANUFACTURING, i.e. MANUFACTURING OF THREE-DIMENSIONAL [3D] OBJECTS BY ADDITIVE DEPOSITION, ADDITIVE AGGLOMERATION OR ADDITIVE LAYERING, e.g. BY 3D PRINTING, STEREOLITHOGRAPHY OR SELECTIVE LASER SINTERING - Details thereof or accessories therefor
  • B33Y 80/00 - Products made by additive manufacturing
  • B29C 64/268 - Arrangements for irradiation using electron beams [EB]
  • B22F 10/28 - Powder bed fusion, e.g. selective laser melting [SLM] or electron beam melting [EBM]

62.

4-(IMIDAZO[1,2-A]PYRIDIN-3-YL)-PYRIMIDINE DERIVATIVES

      
Document Number 03148227
Status Pending
Filing Date 2020-07-22
Open to Public Date 2021-01-28
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Dorsch, Dieter
  • Blum, Andreas
  • Buchstaller, Hans-Peter

Abstract

Compounds of the formula (I) in which R1, R2, V, X, Y and Z have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
  • A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
  • A61P 35/00 - Antineoplastic agents
  • C07D 239/30 - Halogen atoms or nitro radicals
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

63.

PHARMACEUTICAL PREPARATION

      
Document Number 03146384
Status Pending
Filing Date 2020-07-08
Open to Public Date 2021-01-14
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Schoch, Corinna
  • Riehl, Markus
  • Hooff, Gero
  • Klemm, Markus
  • Schmidt, Carsten
  • Weigandt, Markus

Abstract

The present invention relates to a solid pharmaceutical preparation of 3-(1 -{3-[5-(1-Methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6- dihydro-pyridazin-3-yl)-benzonitrile, a method of making same, and medical uses thereof.

IPC Classes  ?

  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 9/20 - Pills, lozenges or tablets
  • A61P 35/00 - Antineoplastic agents

64.

PROCESS FOR MANUFACTURING (S)-3-HYDROXY-1-(1H-INDOL-5-YL)-2-OXO-PYRROLIDINE-3-CARBOXYLIC ACID 3,5-DIFLUORO-BENZYLAMIDE

      
Document Number 03145579
Status Pending
Filing Date 2020-06-30
Open to Public Date 2021-01-07
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Heinrich, Timo
  • Seenisamy, Jeyaprakashnarayanan

Abstract

A process for manufacturing (S)-3-hydroxy-1-(1H-indol-5-yl)-2-oxo- pyrrolidine-3-carboxylic acid 3,5-difluoro-benzylamide.

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

65.

ANTIBODY DRUG CONJUGATE PURIFICATION

      
Document Number 03145763
Status Pending
Filing Date 2020-07-01
Open to Public Date 2021-01-07
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Skudas, Romas
  • Holzgreve, Annika
  • Schulte, Michael
  • Peeck, Lars
  • Zorn, Dominic

Abstract

The present invention relates to an ion exchange separation material with amino-acid based endgroups. This material is especially suitable for the separation and purification of ADCs.

IPC Classes  ?

  • B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
  • B01J 20/26 - Synthetic macromolecular compounds
  • B01J 20/281 - Sorbents specially adapted for preparative, analytical or investigative chromatography
  • C07K 1/16 - Extraction; Separation; Purification by chromatography
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

66.

GLYCOFORM PURIFICATION

      
Document Number 03145765
Status Pending
Filing Date 2020-07-01
Open to Public Date 2021-01-07
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Skudas, Romas
  • Holzgreve, Annika
  • Strobel, Alisa

Abstract

The present invention relates to a method for the separation and purification of glycoforms with an ion exchange separation material with amino-acid based endgroups.

IPC Classes  ?

  • C07K 1/16 - Extraction; Separation; Purification by chromatography
  • B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
  • B01J 20/26 - Synthetic macromolecular compounds
  • B01J 20/281 - Sorbents specially adapted for preparative, analytical or investigative chromatography
  • C07K 14/005 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from viruses
  • C07K 14/165 - Coronaviridae, e.g. avian infectious bronchitis virus
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies

67.

COMBINATION THERAPIES USING CDK INHIBITORS

      
Document Number 03141531
Status Pending
Filing Date 2020-05-20
Open to Public Date 2020-12-03
Owner
  • PFIZER INC. (USA)
  • MERCK PATENT GMBH (Germany)
Inventor
  • Dann, Stephen George
  • Oderup, Cecilia Marianne
  • Salek-Ardakani, Shahram

Abstract

This invention relates to a method for treating cancer by administering a CDK4/6 or a CDK2/4/6 inhibitor in combination with a PD-1 axis binding antagonist, and optionally an OX40 agonist and/or a 4-1BB agonist to a subject in need thereof.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 35/00 - Medicinal preparations containing materials or reaction products thereof with undetermined constitution

68.

PYRIMIDINONE DERIVATIVES AS SHP2 ANTAGONISTS

      
Document Number 03127475
Status Pending
Filing Date 2020-04-08
Open to Public Date 2020-10-15
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Jorand-Lebrun, Catherine
  • Boivin, Roch
  • Johnson, Theresa
  • Wang, Yanping
  • Xiao, Yufang
  • Chen, Xiaoling
  • Linde, Nina
  • Musch, Doreen
  • Kumar, Deepak

Abstract

The invention relates to pyrimidinone derivatives of the general Formula (II), or a pharmaceutically acceptable salt thereof, the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61P 35/00 - Antineoplastic agents
  • C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 471/10 - Spiro-condensed systems
  • C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
  • C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

69.

IMIDAZOLONYLQUINOLINE COMPOUNDS AND THERAPEUTIC USES THEREOF

      
Document Number 03134874
Status Pending
Filing Date 2020-03-25
Open to Public Date 2020-10-01
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Fuchss, Thomas
  • Becker, Axel
  • Kubas, Holger
  • Graedler, Ulrich

Abstract

The present invention relates to atropisomers, solid forms, salt forms and deuterated derivatives of the ATM inhibitor 8-(1,3-Dimethyl-1H-pyrazol-4-yl)-1-(3-fluoro-5-methoxy- pyridin-4-yl)-7-methoxy-3-methyl-1,3-dihydroimidazo[4,5-c]quinolin-2-one as well as compositions thereof. The stable atropisomers do not interconvert and are represented by the following formulae: Compound1, Compound2

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 35/00 - Antineoplastic agents

70.

PROCESS FOR THE PREPARATION OF LIPIDATED PROTEINACEOUS STRUCTURES

      
Document Number 03133136
Status Pending
Filing Date 2020-03-10
Open to Public Date 2020-09-17
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Woell, Steffen
  • Schiller, Stefan
  • Geissler, Simon

Abstract

The present invention relates to a process for the preparation of a conjugate, comprising a biological molecule, an enzymatic tag, a hydrophilic spacer, a linker and a lipophilic moiety using enzymatic coupling. A component comprising an enzymatic tag (e.g. a pentaglycine moiety), a hydrophilic spacer, a linker and a lipophilic moiety (e.g. lipid) is coupled enzymatically via to the biological molecule in an aqueous medium and subsequently purified. A C- terminal motif (LPXTG) for enzymatic conjugation by transpeptidases, e.g. sortase A is preferably present. Intended for linking biomolecules to e.g. liposomes, exosomes or for surface modification. Example of the component to be linked: DMA-PEG-G5.

IPC Classes  ?

  • G01N 33/543 - Immunoassay; Biospecific binding assay; Materials therefor with an insoluble carrier for immobilising immunochemicals
  • G01N 33/532 - Production of labelled immunochemicals

71.

CARBOXAMIDE-PYRIMIDINE DERIVATIVES AS SHP2 ANTAGONISTS

      
Document Number 03127361
Status Pending
Filing Date 2020-03-09
Open to Public Date 2020-09-10
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Jorand-Lebrun, Catherine
  • Boivin, Roch
  • Mochalkin, Igor
  • Johnson, Theresa
  • Linde, Nina
  • Musch, Doreen
  • Kumar, Deepak

Abstract

The invention relates to carboxamide-pyrimidine derivatives of the general formula (I), or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • C07D 239/42 - One nitrogen atom
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 451/14 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

72.

METHODS AND SYSTEMS FOR TOKEN-BASED ANCHORING OF A PHYSICAL OBJECT IN A DISTRIBUTED LEDGER ENVIRONMENT

      
Document Number 03129906
Status Pending
Filing Date 2020-02-11
Open to Public Date 2020-08-20
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Endress, Thomas
  • Szabo, Daniel
  • Berkermann, Frederic
  • Melgarejo Diaz, Natali
  • Brazel, Carl Christian
  • Platzoeder, Michael

Abstract

The invention relates to a computer-implemented method, system and computer program for tokenization of a physical object.Themethod comprises generating or receiving object identification data based on an inspection of the physical object, the object identification data comprising at least one cryptographic hash value as a collision-resistant virtual rep- resentation of the physical object;and generating a non-certified token being assigned to the physical object and representing the object identification data.The invention further relates to a computer-implemented method, system and computer program of certifying a token including object identification data. Moreover, the invention relates to a computer- implemented method, system and computer program of tokenization of a process.

IPC Classes  ?

  • H04L 9/32 - Arrangements for secret or secure communications; Network security protocols including means for verifying the identity or authority of a user of the system

73.

INDAZOLYL-ISOXAZOLE DERIVATIVES FOR THE TREATMENT OF DISEASES SUCH AS CANCER

      
Document Number 03129601
Status Pending
Filing Date 2020-02-10
Open to Public Date 2020-08-20
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Dorsch, Dieter
  • Blum, Andreas

Abstract

Compounds of the formula (I) in which R1, R2, X, Y and Z have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

IPC Classes  ?

  • C07D 231/56 - Benzopyrazoles; Hydrogenated benzopyrazoles
  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61P 35/00 - Antineoplastic agents
  • C07C 49/86 - Ketones containing a keto group bound to a six-membered aromatic ring containing —CHO groups
  • C07C 309/30 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
  • C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 471/10 - Spiro-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
  • C07D 491/08 - Bridged systems
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

74.

TREATMENT OF PATIENTS AT RISK OF RAPID PROGRESSION OF OSTEOARTHRITIS

      
Document Number 03127729
Status Pending
Filing Date 2020-02-07
Open to Public Date 2020-08-13
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Ladel, Christoph H.
  • Guehring, Hans

Abstract

The invention pertains to active compounds, in particular FGF-18 compounds, for use in the treatment of patients affected with a cartilage disorder, preferably osteoarthritis (OA), in particular for the treatment of patients who are at risk of rapid progression of the disorder.

IPC Classes  ?

  • A61K 38/18 - Growth factors; Growth regulators
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

75.

METHOD FOR CONTROLLING A CONDITION OF A PLANT

      
Document Number 03127922
Status Pending
Filing Date 2020-01-27
Open to Public Date 2020-08-06
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Okura, Hiroshi
  • Yamanashi, Ryota
  • Dertinger, Stephan
  • Stockum, Werner
  • Schaberger, Michael
  • Siragusa, Nina
  • Suzuki, Ryuta
  • Azuma, Kazuhisa
  • Kunimoto, Takashi

Abstract

The present invention relates to a method for controlling a condition of a plant.

IPC Classes  ?

  • C09K 11/02 - Use of particular materials as binders, particle coatings or suspension media therefor
  • A01G 7/04 - Electric or magnetic treatment of plants for promoting growth
  • C09K 11/67 - Luminescent, e.g. electroluminescent, chemiluminescent, materials containing inorganic luminescent materials containing refractory metals
  • C09K 11/68 - Luminescent, e.g. electroluminescent, chemiluminescent, materials containing inorganic luminescent materials containing refractory metals containing chromium, molybdenum or tungsten
  • C09K 11/77 - Luminescent, e.g. electroluminescent, chemiluminescent, materials containing inorganic luminescent materials containing rare earth metals

76.

HETEROCYCLIC DERIVATIVES

      
Document Number 03127268
Status Pending
Filing Date 2020-01-20
Open to Public Date 2020-07-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Heinrich, Timo
  • Schlesiger, Sarah

Abstract

Compounds of the formula (I): Q1-Q2-Q3, in which Q1, Q2 and Q3 have the meanings indicated in Claim 1, degrade target proteins, and can be employed, inter alia, for the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injury and different forms of inflammation.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/405 - Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61P 3/00 - Drugs for disorders of the metabolism
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 17/00 - Drugs for dermatological disorders
  • A61P 27/00 - Drugs for disorders of the senses
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P 33/00 - Antiparasitic agents
  • A61P 35/00 - Antineoplastic agents
  • C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/10 - Spiro-condensed systems

77.

THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

      
Document Number 03127284
Status Pending
Filing Date 2020-01-21
Open to Public Date 2020-07-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Tanzer Krauel, Eva-Maria
  • Schiemann, Kai
  • Crespo, Alejandro

Abstract

The invention relates to thiazolopyridine derivatives which fall under the general formula I, (I) and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61P 35/00 - Antineoplastic agents
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

78.

SYSTEM FOR CONTROLLING A LIGHT-DEPENDENT CONDITION OF AN ORGANISM AND METHOD OF DETERMINING A CONFIGURATION OF THE SYSTEM

      
Document Number 03127460
Status Pending
Filing Date 2020-01-21
Open to Public Date 2020-07-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Szabo, Daniel
  • Dertinger, Stephan
  • Schaberger, Michael

Abstract

The invention relates to the field of controlling the growth of an organism, or a plurality of organisms, such as particularly one more plants. Specifically, the invention is directed to a modulating system for modulating light to which an organism is to be exposed.

IPC Classes  ?

  • A01G 7/04 - Electric or magnetic treatment of plants for promoting growth
  • F21V 14/04 - Controlling the distribution of the light emitted by adjustment of elements by movement of reflectors

79.

METHOD FOR MODULATING A CONDITION OF A BIOLOGICAL CELL

      
Document Number 03126953
Status Pending
Filing Date 2020-01-16
Open to Public Date 2020-07-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Stockum, Werner
  • Schaberger, Michael
  • Dertinger, Stephan
  • Siragusa, Nina
  • Okura, Hiroshi

Abstract

The present invention refers to a method for modulating a condition of a biological cell.

IPC Classes  ?

  • C09K 11/02 - Use of particular materials as binders, particle coatings or suspension media therefor

80.

METHODS AND SYSTEMS FOR PREPARING AND PERFORMING AN OBJECT AUTHENTICATION

      
Document Number 03124167
Status Pending
Filing Date 2019-12-17
Open to Public Date 2020-07-16
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Endress, Thomas
  • Szabo, Daniel
  • Berkermann, Frederic
  • Melgarejo Diaz, Natali

Abstract

The present invention relates to the field of tracing and anti-counterfeit protection of physical objects, such as products, for example pharmaceuticals or other health-related products, and particularly to preparing and performing a secure authentication of such objects. Specifically, the invention is directed to a method and a system for preparing a subsequent secured authentication of a physical object or group of physical objects by a recipient thereof, to a method and system for authenticating a physical object or group of physical objects, to a method and system of securely providing a time-variant combination scheme for authenticating a physical object or group of physical objects according to the above methods, and to related computer programs corresponding to said methods. The invention is based on the concept of increasing the security level by increasing the information entropy of the data on which the anti-counterfeit protection is based by means of random data communicated to authenticating entities in an algorithmically hidden way. In some embodiments, the security concept provided by the invention is further based on blockchain technology, physical unclonable functions, and/or time- and location-based information, e.g. geocoordinates, and/or supply chain information.

IPC Classes  ?

  • H04W 4/029 - Location-based management or tracking services
  • H04L 9/06 - Arrangements for secret or secure communications; Network security protocols the encryption apparatus using shift registers or memories for blockwise coding, e.g. D.E.S. systems
  • H04L 9/30 - Public key, i.e. encryption algorithm being computationally infeasible to invert and users' encryption keys not requiring secrecy
  • H04L 9/32 - Arrangements for secret or secure communications; Network security protocols including means for verifying the identity or authority of a user of the system

81.

DISUBSTITUTED ALKYNE DERIVATIVES

      
Document Number 03120053
Status Pending
Filing Date 2019-12-20
Open to Public Date 2020-06-25
Owner
  • MERCK PATENT GMBH (Germany)
  • RYVU THERAPEUTICS S.A. (Poland)
Inventor
  • Heinrich, Timo
  • Petersson, Carl
  • Krier, Mireille
  • Gondela, Andrzej
  • Galezowski, Michal Mikolaj
  • Fabritius, Charles-Henry Robert Yves
  • Nowak, Mateusz Oktawian
  • Krol, Marcin

Abstract

The present invention relates to disubstituted alkyne derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.

IPC Classes  ?

  • C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
  • A61K 31/18 - Sulfonamides
  • A61P 35/00 - Antineoplastic agents
  • C07C 311/13 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
  • C07C 311/14 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
  • C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
  • C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
  • C07C 311/51 - Y being a hydrogen or a carbon atom
  • C07C 317/12 - Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings
  • C07C 317/14 - Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
  • C07C 317/44 - Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
  • C07D 209/08 - Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
  • C07D 213/79 - Acids; Esters
  • C07D 215/36 - Sulfur atoms
  • C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
  • C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
  • C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
  • C07D 307/79 - Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
  • C07D 307/82 - Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
  • C07D 333/62 - Benzo [b] thiophenes; Hydrogenated benzo [b] thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 513/04 - Ortho-condensed systems

82.

4-HETEROARYLCARBONYL-N-(PHENYL OR HETEROARYL) PIPERIDINE-1-CARBOXAMIDES AS INHIBITORS OF TANKYRASES

      
Document Number 03121697
Status Pending
Filing Date 2019-11-29
Open to Public Date 2020-06-11
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Buchstaller, Hans-Peter
  • Rohdich, Felix

Abstract

Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injury and different forms of inflammation.

IPC Classes  ?

  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61P 35/00 - Antineoplastic agents
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

83.

METHODS OF ADMINISTERING ANTI-TIM-3 ANTIBODIES

      
Document Number 03117371
Status Pending
Filing Date 2019-11-01
Open to Public Date 2020-05-07
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Ruisi, Mary
  • Zaynagetdinov, Rinat
  • Zhang, Dong
  • Zhao, Xinyan
  • An, Qi
  • Nannemann, David
  • Sood, Vanita D.
  • Iffland, Christel

Abstract

The invention is based, in part, upon the discovery of a family of antibodies that specifically bind human T Cell Immunoglobulin and Mucin Domain-3 (TIM-3). More specifically, this invention relates to a method of treating cancer by administering an anti-TIM-3 antibody in combination with an anti-PD-Ll/ ???ß Trap fusion protein. When administered to a human cancer patient or an animal model, the antibodies inhibit or reduce tumor growth in the human patient or animal model.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
  • A61P 35/00 - Antineoplastic agents
  • C07K 14/71 - Receptors; Cell surface antigens; Cell surface determinants for growth regulators
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • C07K 19/00 - Hybrid peptides

84.

ANTI-TIM-3 ANTIBODIES

      
Document Number 03117429
Status Pending
Filing Date 2019-11-01
Open to Public Date 2020-05-07
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Zhang, Dong
  • Zhao, Xinyan
  • An, Qi
  • Nannemann, David
  • Zaynagetdinov, Rinat
  • Sood, Vanita
  • Iffland, Christel

Abstract

The invention is based, in part, upon the discovery of a family of antibodies that specifically bind human T Cell Immunoglobulin and Mucin Domain-3 (TIM-3). The antibodies contain TIM-3 binding sites based on the CDRs of the antibodies. The antibodies can be used as therapeutic agents as a monotherapy or in combination with another therapeutic agent. When used as therapeutic agents, the antibodies can be optimized, e.g., affinity-matured, to improve biochemical and/or biophysical properties and/or to reduce or eliminate immunogenicity, when administered to a human patient. The antibodies inhibit TIM-3 from binding to TIM-3 ligands, e.g., galectin-9, phosphatidylserine (PtdSer) and carcinoembryonic antigen-related cell adhesion molecule 1 (CEACAM1). The disclosed antibodies can be used to inhibit the proliferation of tumor cells in vitro or in vivo. When administered to a human cancer patient or an animal model, the antibodies inhibit or reduce tumor growth in the human patient or animal model.

IPC Classes  ?

  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61P 35/00 - Antineoplastic agents
  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
  • C12N 15/13 - Immunoglobulins
  • C12P 21/08 - Monoclonal antibodies

85.

5-AZAINDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

      
Document Number 03117510
Status Pending
Filing Date 2019-10-22
Open to Public Date 2020-04-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Blayo, Anne-Laure
  • Manteau, Baptiste
  • Dorange, Ismet
  • Mayer, Stanislas
  • Schann, Stephan
  • Catelain, Thomas

Abstract

The present invention relates to novel 5-azaindazole derivatives of formula (I), as described and defined herein, and pharmaceutically acceptable salts, solvates and prodrug thereof, as well as pharmaceutical compositions comprising such compounds. The 5-azaindazole derivatives according to the invention have been found to be highly effective dual A2A/A2B adenosine receptor antagonists, and can thus be used as therapeutic agents, particularly in the treatment or prevention of hyperproliferative or infectious diseases or disorders.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P 35/00 - Antineoplastic agents
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

86.

5-AZAINDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

      
Document Number 03117512
Status Pending
Filing Date 2019-10-22
Open to Public Date 2020-04-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Blayo, Anne-Laure
  • Manteau, Baptiste
  • Amalric, Camille
  • Mayer, Stanislas
  • Schann, Stephan
  • Fer, Mickael

Abstract

The present invention relates to novel 5-azaindazole derivatives of formula (I), as described and defined herein, and pharmaceutically acceptable salts, solvates and prodrug thereof, as well as pharmaceutical compositions comprising such compounds. The 5-azaindazole derivatives according to the invention have been found to be highly effective dual A2A/A2B adenosine receptor antagonists, and can thus be used as therapeutic agents, particularly in the treatment or prevention of hyperproliferative or infectious diseases or disorders.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
  • A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
  • A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P 35/00 - Antineoplastic agents

87.

COMBINATION THERAPY UTILIZING DNA ALKYLATING AGENTS AND ATR INHIBITORS

      
Document Number 03116234
Status Pending
Filing Date 2019-10-14
Open to Public Date 2020-04-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Deutsch, Carl
  • Piater, Birgit
  • Rasche, Nicolas
  • Dahmen, Heike
  • Zenke, Frank
  • Zimmermann, Astrid
  • Rieker, Marcel

Abstract

The present invention relates to synergistic combinations of DNA-alkylating ADCs and ATR inhibitors.

IPC Classes  ?

  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 35/00 - Antineoplastic agents

88.

ABITUZUMAB FOR THE TREATMENT OF COLORECTAL CANCER

      
Document Number 03116669
Status Pending
Filing Date 2019-10-18
Open to Public Date 2020-04-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Massimini, Giorgio
  • Celik, Ilhan
  • Straub, Josef
  • Bruns, Rolf

Abstract

The invention is directed to methods of treatment of colorectal cancer, said treatment comprising the administration of the anti-alpha-v integrin (receptor) antibody Abituzumab. Preferably, the invention relates to methods of treating colorectal cancer, Stage II-IV colorectal cancer, metastatic colorectal cancer, left-sided colorectal cancer and/or left-sided metastatic colorectal comprising the administration of said Abituzumab to patients in need thereof. The instant invention also relates the use of Abituzumab for the manufacture of a medicament for treating colorectal cancer, preferably colorectal cancer as defined herein, and/or use of Abituzumab for the manufacture of a medicament for treating colorectal cancer in combination with suitable targeted therapy concepts, such as growth factor or growth factor receptor targeting monoclonal antibodies, and/or chemotherapy.

IPC Classes  ?

  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/04 - Antineoplastic agents specific for metastasis

89.

COMBINATION OF A PD-1 ANTAGONIST, AN ATR INHIBITOR AND A PLATINATING AGENT FOR THE TREATMENT OF CANCER

      
Document Number 03114024
Status Pending
Filing Date 2019-09-26
Open to Public Date 2020-04-02
Owner
  • MERCK PATENT GMBH (Germany)
  • PFIZER INC. (USA)
Inventor
  • Alimzhanov, Marat
  • Soulard, Patricia
  • Zenke, Frank
  • Dahmen, Heike
  • Zimmermann, Astrid
  • Schroeder, Andreas
  • Tadjalli Mehr, Keyvan
  • Falk, Martin

Abstract

The present invention relates to combination therapies useful for the treatment of cancer. In particular, the invention relates to a therapeutic combination which comprises a PD-1 antagonist, an ATR inhibitor and a platinating agent.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61P 35/00 - Antineoplastic agents

90.

MARKERS USEFUL IN ENRICHMENT STRATEGIES FOR THE TREATMENT OF OSTEOARTHRITIS

      
Document Number 03111671
Status Pending
Filing Date 2019-09-09
Open to Public Date 2020-03-19
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Ladel, Christoph H.
  • Guehring, Hans
  • Bay-Jensen, Anne-Christine
  • Karsdal, Morten
  • Qvist, Per

Abstract

The present invention relates to pharmacogenetics, more specifically to strategies involving biomarkers associated with the clinical response to a compound before or during treatment of a cartilage disorder, such as osteoarthritis. The present invention more particularly relates to the combination of JSW measurements and level of specific proteins present in the blood, serum, synovial fluid or in the urine, which can be used in strategies such as patients' enrichment in clinical trials, patients' selection strategy before or during treatment or for adapting the treatment of a patient in the frame of treatments for cartilage disorder, such as osteoarthritis.

IPC Classes  ?

  • C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material

91.

PROCESS FOR THE PREPARATION OF A COATED SOLID PHARMACEUTICAL DOSAGE FORM

      
Document Number 03112618
Status Pending
Filing Date 2019-09-12
Open to Public Date 2020-03-19
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Bogdahn, Malte
  • Schiller, Stefan
  • Hanefeld, Andrea
  • Geissler, Simon

Abstract

The present invention is directed to a process for the preparation of a coated solid pharmaceutical dosage form using 3D printing technology.

IPC Classes  ?

  • A61K 9/28 - Dragees; Coated pills or tablets
  • B29C 64/165 - Processes of additive manufacturing using a combination of solid and fluid materials, e.g. a powder selectively bound by a liquid binder, catalyst, inhibitor or energy absorber

92.

5-MORPHOLIN-4-YL-PYRAZOLO[4,3-B]PYRIDINE DERIVATIVES

      
Document Number 03111878
Status Pending
Filing Date 2019-09-04
Open to Public Date 2020-03-12
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Burgdorf, Lars
  • Tsaklakidis, Christos

Abstract

Compounds of the formula Ia and Ib in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of ATR, and can be employed for the treatment of diseases such as cancer.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

93.

FUSED IMIDAZOPYRIDINES AS REVERSIBLE INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK)

      
Document Number 03108732
Status Pending
Filing Date 2019-08-26
Open to Public Date 2020-03-05
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Caldwell, Richard
  • Liu-Bujalski, Lesley
  • Potnick, Justin
  • Neagu, Constantin
  • Kulkarni, Shashank
  • Jones, Reinaldo
  • Qiu, Hui

Abstract

The present invention relates to fused imidazo pyridine compounds of formula (I), and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

94.

TREATMENT OF TRIPLE NEGATIVE BREAST CANCER WITH TARGETED TGF-B INHIBITION

      
Document Number 03110276
Status Pending
Filing Date 2019-08-22
Open to Public Date 2020-02-27
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Locke, George
  • Dussault, Isabelle

Abstract

The present disclosure relates generally to methods for treating a patient diagnosed with triple negative breast cancer (TNBC), involving identifying a patient likely to respond to treatment via targeted TGF-ß inhibition with an anti-TGFß agent, and treating the subject with the anti-TGFß agent.

IPC Classes  ?

  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
  • G01N 33/574 - Immunoassay; Biospecific binding assay; Materials therefor for cancer

95.

TLR7/8 ANTAGONISTS AND USES THEREOF

      
Document Number 03108099
Status Pending
Filing Date 2019-07-29
Open to Public Date 2020-02-06
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Sherer, Brian
  • Lan, Ruoxi
  • Brugger, Nadia
  • Chen, Xiaoling
  • Toure, Momar
  • Cleary, Esther
  • Deselm, Lizbeth Celeste
  • Wang, Yanping

Abstract

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.

IPC Classes  ?

  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 471/10 - Spiro-condensed systems
  • C07D 495/10 - Spiro-condensed systems

96.

BORONIC ACID DERIVATIVES

      
Document Number 03107377
Status Pending
Filing Date 2019-07-23
Open to Public Date 2020-01-30
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Klein, Markus
  • Schadt, Oliver
  • Haselmayer, Philipp

Abstract

The present invention relates to a-amino boronic acid derivatives. These compounds are useful for inhibiting the activity of immunoproteasome (LMP7) and for the treatment and/or prevention of medical conditions affected by immunoproteasome activity such as inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer.

IPC Classes  ?

97.

A SUBSTITUTED AMINO-PYRIMIDINE COMPOUND FOR USE IN A METHOD FOR TREATMENT AND PREVENTION OF MULTIPLE SCLEROSIS

      
Document Number 03106772
Status Pending
Filing Date 2019-07-19
Open to Public Date 2020-01-23
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Dyroff, Martin
  • Mitchell, David
  • Papasouliotis, Orestis

Abstract

The invention provides methods, compositions, and medical kits for treating and preventing multiple sclerosis using 1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one or a pharmaceutically acceptable salt thereof according to preferred dosing regimens.

IPC Classes  ?

  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

98.

CRYSTALLINE SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND AMINO ACID ETHYL ESTERS

      
Document Number 03105251
Status Pending
Filing Date 2019-07-02
Open to Public Date 2020-01-09
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Moser, Rudolf
  • Groehn, Viola
  • Boehni Stamm, Ruth
  • Blatter, Fritz
  • Szelagiewicz, Martin

Abstract

The present invention refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and an amino acid ethyl ester like L-phenylalanine ethyl ester or L-methionine ethylester, wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to amino acid ethyl ester is from 1:0.3 to 1:3.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.

IPC Classes  ?

  • C07D 475/04 - Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
  • A23L 33/175 - Amino acids
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings

99.

COMBINATION THERAPY WITH TARGETED TGF-B INHIBITION FOR TREATMENT OF ADVANCED NON-SMALL CELL LUNG CANCER

      
Document Number 03105360
Status Pending
Filing Date 2019-07-01
Open to Public Date 2020-01-09
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Dussault, Isabelle
  • Grenga, Italia
  • Vugmeyster, Yulia
  • Khandelwal, Akash
  • Christensen, Olaf

Abstract

This disclosure relates generally to methods for treating a subject diagnosed with advanced non-small-cell lung cancer (NSCLC), involving targeted TGF-ß inhibition with a bi-functional fusion protein, in combination with administration of systemic chemotherapeutic agents, wherein the combination of the bi-functional fusion protein of the present disclosure with systemic chemotherapeutic agents enhances anticancer efficacy over systemic chemotherapeutic agents alone.

IPC Classes  ?

  • A61K 31/282 - Platinum compounds
  • A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
  • A61K 38/17 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 14/495 - Transforming growth factor (TGF)
  • C07K 14/705 - Receptors; Cell surface antigens; Cell surface determinants
  • C07K 14/71 - Receptors; Cell surface antigens; Cell surface determinants for growth regulators
  • C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
  • C07K 16/46 - Hybrid immunoglobulins

100.

CRYSTALLINE SALT OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND L-ISOLEUCINE ETHYL ESTER

      
Document Number 03105531
Status Pending
Filing Date 2019-07-02
Open to Public Date 2020-01-09
Owner MERCK PATENT GMBH (Germany)
Inventor
  • Moser, Rudolf
  • Groehn, Viola
  • Boehni Stamm, Ruth
  • Blatter, Fritz
  • Szelagiewicz, Martin

Abstract

The present invention is directed to a crystalline salt of 5-methyl-(6S)-tetrahydrofolic acid and L-isoleucine ethyl ester wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to L-isoleucine ethyl ester is from 1:0.3 to 1:2.0 (in mol/mol) and/or hydrates and/or solvates thereof, as well as, a process of obtaining the same.

IPC Classes  ?

  • C07D 475/04 - Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
  • A23L 33/10 - Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L 33/175 - Amino acids
  • A61K 31/223 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-amino acids
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 3/02 - Nutrients, e.g. vitamins, minerals
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
  • C30B 7/08 - Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions by cooling of the solution
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