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.
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
2.
COVER FOR A THIN-LAYER CHROMATOGRAPHY DEVELOPMENT CHAMBER
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).
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.
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
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.
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.
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
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.
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.
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
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.
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.
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
10.
NOVEL TREATMENT REGIMEN FOR THE TREATMENT OF AUTOIMMUNE DISORDERS
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.
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
11.
ANTI-CEACAM5 ANTIBODIES AND CONJUGATES AND USES THEREOF
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.
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
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.
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
13.
CONSUMABLE TISSUE-LIKE STRUCTURE GENERATED WITH MUSCLE CELLS GROWN ON EDIBLE HOLLOW FIBERS
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.
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.
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.
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.
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
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
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.
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
18.
DEVICE AND PROCESS FOR CELL CULTURE MEDIA PREPARATION AND PERFORMING CELL CULTURE
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.
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.
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 31/5025 - 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
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
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.
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
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.
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.
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
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.
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
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
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.
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.
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
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.
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.
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.
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
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
30.
MODULAR INCUBATION CHAMBER AND METHOD OF VIRUS INACTIVATION
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.
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.
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.
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
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.
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
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.
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
35.
MATERIAL AND METHOD FOR PERFORMING A SEPARATION BASED ON HALOGEN BONDING
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.
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
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.
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.
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.
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
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.
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
40.
OPTIMIZED ANALYTE DERIVATIZATION FOR SYNERGISTIC APPLICATION WITH CRYSTAL SPONGE METHOD
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).
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.
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 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]
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.
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
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 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
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.
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
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.
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
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.
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
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.
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.
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
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 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
49.
IMIDAZOLONYLQUINOLINE COMPOUNDS AND THERAPEUTIC USES THEREOF
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
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
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.
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.
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
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
52.
METHODS AND SYSTEMS FOR TOKEN-BASED ANCHORING OF A PHYSICAL OBJECT IN A DISTRIBUTED LEDGER ENVIRONMENT
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.
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
53.
INDAZOLYL-ISOXAZOLE DERIVATIVES FOR THE TREATMENT OF DISEASES SUCH AS CANCER
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.
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 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
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.
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.
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 31/405 - 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
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
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.
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
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
58.
SYSTEM FOR CONTROLLING A LIGHT-DEPENDENT CONDITION OF AN ORGANISM AND METHOD OF DETERMINING A CONFIGURATION OF THE SYSTEM
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.
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.
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
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.
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 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 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
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.
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
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
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.
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
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.
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
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.
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
66.
5-AZAINDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS
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.
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
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
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.
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
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.
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.
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
71.
PROCESS FOR THE PREPARATION OF A COATED SOLID PHARMACEUTICAL DOSAGE FORM
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
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.
The present invention relates to fused imidazo pyridine compounds of formula (I), and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
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
74.
TREATMENT OF TRIPLE NEGATIVE BREAST CANCER WITH TARGETED TGF-B INHIBITION
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.
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
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
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
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.
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.
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
78.
CRYSTALLINE SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND AMINO ACID ETHYL ESTERS
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.
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
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
79.
COMBINATION THERAPY WITH TARGETED TGF-B INHIBITION FOR TREATMENT OF ADVANCED NON-SMALL CELL LUNG CANCER
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.
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
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.
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
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
81.
CRYSTALLINE SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND L-LEUCINE ETHYL ESTER
The present inventionrefers to a crystalline salt comprising5-methyl-(6S)-tetrahydrofolic acid L-leucine ethyl ester wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid and L-leucine 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.
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
A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
82.
CRYSTALLINE SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND L-VALINE ETHYL ESTER
The present invention refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and L-valine ethyl ester wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid and L-valine 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.
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
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 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
83.
DOSING REGIMENS FOR TARGETED TGF-B INHIBITION FOR USE IN TREATING BILIARY TRACT CANCER
This disclosure relates to dosage regimens for targeted TGF-ß inhibition with a bi-functional fusion protein for use in a method of treating biliary tract cancer or inhibiting biliary tract tumor growth in treatment naive patients, or patients with locally advanced or metastatic BTC who have failed or are intolerant to first-line systemic chemotherapy.
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 9/00 - Medicinal preparations characterised by special physical form
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
NOVEL CRYSTALLINE FORMS OF 1-(4-{[6-AMINO-5-(4-PHENOXY-PHENYL)-PYRIMIDIN-4-YLAMINO]-METHYL}-4-FLUORO-PIPERIDIN-1-YL)-PROPENONE, SALT FORMS THEREOF, AND PROCESSES TO OBTAIN
The present invention relates to a solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone (compound 1), or pharmaceutically acceptable salts thereof, useful as BTK inhibitors.
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
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH (USA)
Inventor
Russell, Stephen J.
Bexon, Alice
Peng, Kah-Whye
Diaz, Rosa Marie
Abstract
The present application is directed to therapeutic regimens and methods of treating cancer, with the regimens and methods comprising administering to the subject a programmed death-ligand 1 (PD-L1) inhibitor and a recombinant vesicular stomatitis virus that has been engineered to expresses interferon beta (VSV-IFNß-NIS).
A01N 63/00 - Biocides, pest repellants or attractants, or plant growth regulators containing microorganisms, viruses, microbial fungi, animals or substances produced by, or obtained from, microorganisms, viruses, microbial fungi or animals, e.g. enzymes or fermen
This disclosure relates generally to dosage regimens for targeted TGF-ß inhibition with a bi-functional fusion protein for use in a method of treating a treatment naive patient diagnosed with stage III non-small cell lung cancer (NSCLC), and/or mitigating a pathological condition associated with chemotherapy and radiotherapy (cCRT).
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
Compounds of the formula (I) in which R1, R2, R3, R4 and n have the meanings indicated in Claim 1, are inhibitors of HIF-2a, and can be employed for the treatment of diseases such as cancer.
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
C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
88.
DOSING REGIMENS FOR TARGETED TGF-B INHIBITION FOR USE IN TREATING CANCER IN TREATMENT NAIVE SUBJECTS
This disclosure relates to dosage regimens for targeted TGF-ß inhibition with a bi-functional fusion protein for use in a method of treating cancer or inhibiting tumor growth in treatment naive patients.
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 9/00 - Medicinal preparations characterised by special physical form
The present invention relates to the field of tracing and anti-counterfeit protection of objects, e.g. products,and particularly to an automatic recognition and authentication of such objects.Specifically, the invention relates to a system and a method of receiving object data representing one or more discriminating characteristics of a physical object or group of physical objects. The method comprises: processing the object data by means of a machine-learning-based object recognition process to obtain discriminating data representing one or more collision resistant virtual representations of the physical object or group of physical objects; comparing at least one of the discriminating data and an original hash value derived therefrom by application of a pre-determined cryptographic hash function thereto with corresponding reference data stored in one or more data repositories with restricted access; and, if said comparison with the reference data results in a match, outputting digitally signed identification data comprising said hash value. Potential applications of the invention comprise particularly object authenticity checks for track & trace and anti- counterfeiting purposes, for example without limitation in the fields of automotive/aerospace spare parts, 3D-printed objects,pharmaceutical products or other health-related products, such health-care products, lab disposables, and clinical test disposables.
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
90.
COMBINED INHIBITION OF PD-1/PD-L1, TGF.BETA. AND DNA-PK FOR THE TREATMENT OF CANCER
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 axis binding antagonist, a TGFß inhibitor and a DNA-PK inhibitor, optionally together with one or more additional chemotherapeutic agents or radiotherapy. The therapeutic combination is particularly intended for use in treating a subject having a cancer that tests positive for PD-L1 expression.
The present invention provides compounds of Formula (I'), or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g. cancer).
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
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
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 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 413/04 - 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
92.
ADDITIVES FOR PROTEIN FORMULATIONS TO IMPROVE THERMAL STABILITY
The present invention relates to excipients for special protein formulations, which are suitable to improve the thermal stability against denaturation and deactivation. In particular, the present invention relates to additives for thermostabilizing of vaccine formulations.
The present invention relates to a method for stabilizing protein or peptide comprising formulations, which includes the step of adding selected meglumine salts to protein solutions, especially to solutions of pharmaceutical active proteins. But the present invention also relates to the stabilized composition comprising proteins or peptides and selected meglumine salts. Another objective of the present invention is to provide pharmaceutical compositions comprising antibody molecules stabilized by selected meglumine salts and methods for producing corresponding stabilized pharmaceutical compositions, and kit comprising these compositions.
The present invention relates to compositions of highly concentrated protein formulations showing reduced viscosity. The contained proteins in the prepared formulations are stabilized against aggregation and denaturation and are thus sufficiently storage-stable until administration to the patient.
The present invention relates to a combination comprising as a first active ingredient 6-fluoro-2-(4-morpholin-4-ylmethyl-phenyl)-quinoline-4-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide or a prodrug or pharmaceutically acceptable salt thereof and as a second active ingredient pyronaridine or a prodrug or pharmaceutically acceptable salt thereof. The present invention also relates to a combination of three antimalarial active ingredients, namely of 6-fluoro-2-(4-morpholin-4-ylmethyl-phenyl)-quinoline-4-carboxylic acid (2- pyrrolidin-1-yl-ethyl)-amide or a prodrug or salt thereof, pyronaridine or pharmaceutically acceptable salt thereof,and artemisinin or derivatives thereof. The invention further relates to pharmaceutical compositions comprising such a combination and use thereof in the treatment and/or prevention of malaria.
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/366 - Lactones having six-membered rings, e.g. delta-lactones
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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]
The present invention relates to compounds that can be used to induce immunogenic cell death (ICD). In some instances, two or more compounds are combined to induce ICD. The invention also relates to the combination of ICD-inducing compounds with an agent stimulating the immune system, such as an immune checkpoint inhibitor, in particular, to 5 treat cancer or inhibit tumor growth.
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
The present invention relates to an improved process for the preparation of metformin hydrochloride, an important drug in the first line treatment of Type II Diabetes.
C07C 277/08 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
99.
QUINOLINE COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF
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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
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
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
patents
