Merck Serono SA

Switzerland

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        World 62
        United States 48
        Canada 16
Date
2020 2
Before 2019 124
IPC Class
A61P 37/00 - Drugs for immunological or allergic disorders 16
A61K 31/4245 - Oxadiazoles 11
A61K 38/21 - Interferons 10
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] 10
A61P 35/00 - Antineoplastic agents 10
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Status
Pending 2
Registered / In Force 124
Found results for  patents
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1.

Methods of treating pruritic disease with IL-31 monoclonal antibodies

      
Application Number 16834607
Grant Number 11542327
Status In Force
Filing Date 2020-03-30
First Publication Date 2020-08-20
Grant Date 2023-01-03
Owner
  • ZYMOGENETICS INC. (USA)
  • MERCK SERONO S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
  • C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells

2.

CLADRIBINE REGIMEN FOR TREATING MULTIPLE SCLEROSIS

      
Application Number 16782094
Status Pending
Filing Date 2020-02-05
First Publication Date 2020-05-21
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Brentzel, Jr., H. James
  • Lopez-Bresnahan, Maria
  • Ammoury, Nazih

Abstract

The present invention relates to the use of multiple doses of Cladribine combined with beta interferon for the treatment of multiple sclerosis in patients who are refractory to at least one conventional therapy.

IPC Classes  ?

  • A61K 31/00 - Medicinal preparations containing organic active ingredients
  • A61K 9/20 - Pills, lozenges or tablets
  • 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 38/21 - Interferons

3.

Membrane bound reporter molecules and their use in cell sorting

      
Application Number 15975848
Grant Number 11513120
Status In Force
Filing Date 2018-05-10
First Publication Date 2018-11-15
Grant Date 2022-11-29
Owner MERCK SERONO S.A (Switzerland)
Inventor
  • Helman, Daniel
  • Toister-Achituv, Mira
  • Bar-Shimon, Meirav
  • Smolarsky, Moshe

Abstract

The present invention relates to nucleic acid molecules comprising a nucleic acid sequence encoding a membrane-bound biotin mimetic peptide (BMP) or biotin acceptor peptide (BAP). The invention also relates to a method for selection of high producer cells secreting a protein of interest.

IPC Classes  ?

  • C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
  • G01N 33/569 - Immunoassay; Biospecific binding assay; Materials therefor for microorganisms, e.g. protozoa, bacteria, viruses
  • C12Q 1/6897 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids involving reporter genes operably linked to promoters
  • G01N 33/58 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
  • C12N 15/79 - Vectors or expression systems specially adapted for eukaryotic hosts

4.

Nucleic acid molecules encoding humanized IL-31 monoclonal antibodies

      
Application Number 15963497
Grant Number 10640559
Status In Force
Filing Date 2018-04-26
First Publication Date 2018-10-25
Grant Date 2020-05-05
Owner
  • ZymoGenetics, Inc. (USA)
  • Merck Serono S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • C12N 1/19 - Yeasts; Culture media therefor modified by introduction of foreign genetic material
  • C12N 1/21 - Bacteria; Culture media therefor modified by introduction of foreign genetic material
  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
  • C12N 15/13 - Immunoglobulins
  • C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
  • C12N 15/79 - Vectors or expression systems specially adapted for eukaryotic hosts
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies

5.

Cladribine regimen for treating multiple sclerosis

      
Application Number 15928123
Grant Number 10555913
Status In Force
Filing Date 2018-03-22
First Publication Date 2018-07-26
Grant Date 2020-02-11
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Brentzel, Jr., H. James
  • Lopez-Bresnahan, Maria
  • Ammoury, Nazih

Abstract

The present invention relates to the use of multiple doses of Cladribine combined with beta interferon for the treatment of multiple sclerosis in patients who are refractory to at least one conventional therapy.

IPC Classes  ?

  • A61K 31/00 - Medicinal preparations containing organic active ingredients
  • 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 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
  • A61K 9/20 - Pills, lozenges or tablets
  • 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 38/21 - Interferons

6.

Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

      
Application Number 15729046
Grant Number 10259795
Status In Force
Filing Date 2017-10-10
First Publication Date 2018-07-19
Grant Date 2019-04-16
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Page, Patrick Naxos
  • Schwarz, Matthias
  • Jorand-Lebrun, Catherine
  • Quattropani, Anna
  • Pomel, Vincent

Abstract

The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as pre-term labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

IPC Classes  ?

  • C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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

7.

Method of treating pruritus with IL-31 monoclonal antibody formulations

      
Application Number 15648252
Grant Number 09982044
Status In Force
Filing Date 2017-07-12
First Publication Date 2017-11-02
Grant Date 2018-05-29
Owner
  • ZYMOGENETICS INC. (USA)
  • MERCK SERONO S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies

8.

L-VALINATE OF HYDROXYPROPYLTHIAZOLIDINE CARBOXAMIDE DERIVATIVE AND SALT FORM, CRYSTAL POLYMORPH THEREOF

      
Document Number 03009576
Status Pending
Filing Date 2017-01-04
Open to Public Date 2017-07-13
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Naxos Page, Patrick
  • Schwarz, Matthias
  • Jorand-Lebrun, Catherine
  • Quattropani, Anna
  • Pomel, Vincent

Abstract

The invention provides the L-valinate ester of a hydroxypropylthiazolidine carboxamide derivative of formula (I), (2S)-3-([1,1'-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1- phenylpropyl]-1,3-thiazolidine-2- carboxamide, as well as salts and crystal polymorphs thereof. The compound inhibits the prostaglandin F receptor (PGF2alpha) and is useful in the treatment of disorders such as preterm labor at the early gestational stage or dysmennorrhea.

IPC Classes  ?

  • C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
  • A61K 31/426 - 1,3-Thiazoles
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 15/00 - Drugs for genital or sexual disorders; Contraceptives
  • A61P 15/06 - Antiabortive agents; Labour repressants

9.

L-VALINATE OF HYDROXYPROPYLTHIAZOLIDINE CARBOXAMIDE DERIVATIVE AND SALT FORM, CRYSTAL POLYMORPH THEREOF

      
Application Number EP2017050101
Publication Number 2017/118641
Status In Force
Filing Date 2017-01-04
Publication Date 2017-07-13
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Naxos Page, Patrick
  • Schwarz, Matthias
  • Jorand-Lebrun, Catherine
  • Quattropani, Anna
  • Pomel, Vincent

Abstract

The invention provides the L-valinate ester of a hydroxypropylthiazolidine carboxamide derivative of formula (I), (2S)-3-([1,1'-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1- phenylpropyl]-1,3-thiazolidine-2- carboxamide, as well as salts and crystal polymorphs thereof. The compound inhibits the prostaglandin F receptor (PGF2alpha) and is useful in the treatment of disorders such as preterm labor at the early gestational stage or dysmennorrhea.

IPC Classes  ?

  • C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
  • A61K 31/426 - 1,3-Thiazoles
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 15/00 - Drugs for genital or sexual disorders; Contraceptives
  • A61P 15/06 - Antiabortive agents; Labour repressants

10.

Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

      
Application Number 15231549
Grant Number 09834528
Status In Force
Filing Date 2016-08-08
First Publication Date 2017-07-06
Grant Date 2017-12-05
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Page, Patrick Naxos
  • Schwarz, Matthias
  • Jorand-Lebrun, Catherine
  • Quattropani, Anna
  • Pomel, Vincent

Abstract

The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorph s thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as pre-term labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

IPC Classes  ?

  • C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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

11.

IL-31 monoclonal antibody formulations

      
Application Number 15208990
Grant Number 09738715
Status In Force
Filing Date 2016-07-13
First Publication Date 2016-10-27
Grant Date 2017-08-22
Owner
  • ZYMOGENETICS INC. (USA)
  • MERCK SERONO S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons

12.

α-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

      
Application Number 14987586
Grant Number 09447055
Status In Force
Filing Date 2016-01-04
First Publication Date 2016-09-20
Grant Date 2016-09-20
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Page, Patrick Naxos
  • Schwarz, Matthias
  • Jorand-Lebrun, Catherine
  • Quattropani, Anna
  • Pomel, Vincent

Abstract

The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as pre-term labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

IPC Classes  ?

  • C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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

13.

Method of treating pruritus with IL-31 monoclonal antibodies

      
Application Number 14645769
Grant Number 09416184
Status In Force
Filing Date 2015-03-12
First Publication Date 2015-07-02
Grant Date 2016-08-16
Owner
  • ZymoGenetics, Inc. (USA)
  • Merck Serono S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies

14.

Puro-DHFR quadrifunctional marker and its use in protein production

      
Application Number 14481983
Grant Number 09175284
Status In Force
Filing Date 2014-09-10
First Publication Date 2015-01-22
Grant Date 2015-11-03
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Kobr, Michel
  • Dupraz, Philippe

Abstract

This invention relates to industrial production of proteins. More specifically, the invention relates to the res-DHFR surrogate marker, which corresponds to a fusion between DHFR and a protein conferring resistance to a toxic compound or conferring a metabolic advantage. The invention further relates to the use of res-DHFR for screening cells for high expression of a protein of interest. The invention is illustrated by the Puro-DHFR surrogate marker, which corresponds to a fusion between the puromycin N-acetyltransferase and dihydrofolate reductase (DHFR).

IPC Classes  ?

  • C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
  • C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
  • C12N 9/96 - Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
  • G01N 33/74 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones

15.

PEPTIDE

      
Application Number IB2014058233
Publication Number 2014/111840
Status In Force
Filing Date 2014-01-13
Publication Date 2014-07-24
Owner
  • APITOPE INTERNATIONAL NV (Belgium)
  • MERCK SERONO S.A. (Switzerland)
Inventor
  • Wraith, David
  • Streeter, Heather

Abstract

There is provided a peptide which is capable of binding to an MHC molecule in vitro and being presented to a T cell without antigen processing (i.e. an apitope) which peptide comprises a portion of the region 40-60 of myelin oligodendrocyte glycoprotein (MOG). In particular there is provided an apitope which is selected from the following myelin oligodendrocyte glycoprotein peptides: MOG 41-55, 43-57, 44-58 and 45-59. There is also provided the use of such a peptide in a pharmaceutical composition and a method to treat and/or prevent a disease using such a peptide.

IPC Classes  ?

  • C07K 14/705 - Receptors; Cell surface antigens; Cell surface determinants

16.

PEPTIDE

      
Application Number IB2014058234
Publication Number 2014/111841
Status In Force
Filing Date 2014-01-13
Publication Date 2014-07-24
Owner
  • APITOPE INTERNATIONAL NV (Belgium)
  • MERCK SERONO S.A. (Switzerland)
Inventor
  • Wraith, David
  • Streeter, Heather
  • Ordonez, Laurence

Abstract

There is provided a peptide which is capable of binding to an MHC molecule in vitro and being presented to a T cell without antigen processing (i.e. an apitope) which peptide comprises all or a portion of the following proteolipid protein (PLP) peptides: PLP 36-61: HE ALTGTEKLIET YF SKN YQD YEYLI (SEQ ID NO. 1) PLP 179-206: TWTTCQSIAFPSKTSASIGSLCADARMY (SEQ ID NO. 2) PLP 207-234: GVLPWNAFPGKVCGSNLLSICKTAEFQM (SEQ ID NO. 3). There is also provided the use of such a peptide in a pharmaceutical composition and a method to treat and/or prevent a disease using such a peptide.

IPC Classes  ?

  • C07K 14/47 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates from mammals

17.

Polynucleotides encoding IL-31 monoclonal antibodies

      
Application Number 14174870
Grant Number 09005921
Status In Force
Filing Date 2014-02-07
First Publication Date 2014-07-03
Grant Date 2015-04-14
Owner
  • ZymoGenetics, Inc. (USA)
  • Merck Serono S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
  • C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies

18.

3-arylamino pyridine derivatives

      
Application Number 13940065
Grant Number 08841459
Status In Force
Filing Date 2013-07-11
First Publication Date 2014-02-20
Grant Date 2014-09-23
Owner Merck Serono SA (Switzerland)
Inventor
  • Deppe, Holger
  • Schwarz, Matthias
  • Abel, Ulrich
  • Feurer, Achim
  • Grädler, Ulrich
  • Otte, Kerstin
  • Sekul, Renate
  • Thiemann, Meinolf
  • Goutopoulos, Andreas
  • Jiang, Xuliang

Abstract

The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

IPC Classes  ?

  • C07D 213/72 - Nitrogen atoms
  • C07D 213/46 - Oxygen atoms
  • A01N 43/58 - 1,2-Diazines; Hydrogenated 1,2-diazines
  • 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 213/79 - Acids; Esters
  • 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 295/13 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
  • C07D 213/81 - Amides; Imides
  • C07D 295/125 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
  • C07D 295/32 - Nitrogen atoms acylated with carboxylic or carbonic acids, or their nitrogen or sulfur analogues
  • C07D 213/89 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom

19.

Low fucose cell lines and uses thereof

      
Application Number 14003767
Grant Number 09574003
Status In Force
Filing Date 2012-03-05
First Publication Date 2014-01-02
Grant Date 2017-02-21
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Helman, Daniel
  • Barshimon, Meirav
  • Toister-Achituv, Mira

Abstract

A method of selecting cells having zero fucose level useful as host cells for expressing recombinant proteins is disclosed. The method comprises: (d) introducing genetic mutations into a population of CHO cells by contacting the cells with a methotrexate (MTX), (e) contacting the population of CHO cells comprising mutated cells with a non-toxic fucose binding agent for an amount of time that allows binding of the fucose binding agent to a fucose moiety on a cell membrane of the population of cells, wherein the amount of time does not allow killing of the cells; and (f) depleting from the population of cells comprising mutated cells, a subpopulation of cells which bind the fucose binding agent, thereby selecting cells useful as host cells for expressing recombinant proteins, the selected cells having zero fucose content. There are also disclosed cells and cell lines useful as host cells for expressing recombinant proteins.

IPC Classes  ?

  • 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
  • A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
  • 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 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
  • C12N 9/04 - Oxidoreductases (1.), e.g. luciferase acting on CHOH groups as donors, e.g. glucose oxidase, lactate dehydrogenase (1.1)
  • C12N 9/10 - Transferases (2.)
  • C12N 9/88 - Lyases (4.)
  • C12N 15/01 - Preparation of mutants without inserting foreign genetic material therein; Screening processes therefor
  • C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells

20.

Nucleic acid molecules encoding humanized antibody molecules specific for IL-31

      
Application Number 13908436
Grant Number 08685669
Status In Force
Filing Date 2013-06-03
First Publication Date 2013-11-07
Grant Date 2014-04-01
Owner
  • ZymoGenetics, Inc. (USA)
  • Merck Serono S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
  • C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression

21.

Indazolyl triazol derivatives

      
Application Number 13995803
Grant Number 09073892
Status In Force
Filing Date 2011-12-16
First Publication Date 2013-10-17
Grant Date 2015-07-07
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Jorand-Lebrun, Catherine
  • Crosignani, Stefano
  • Dorbais, Jerome
  • Grippi-Vallotton, Tania
  • Pretre, Adeline

Abstract

Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.

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
  • 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
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • 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
  • 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 31/551 - 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

22.

Puro-DHFR quadrifunctional marker and its use in protein production

      
Application Number 13742495
Grant Number 08841106
Status In Force
Filing Date 2013-01-16
First Publication Date 2013-07-04
Grant Date 2014-09-23
Owner Merck Serono SA (Switzerland)
Inventor
  • Kobr, Michel
  • Dupraz, Philippe

Abstract

This invention relates to industrial production of proteins. More specifically, the invention relates to the res-DHFR surrogate marker, which corresponds to a fusion between DHFR and a protein conferring resistance to a toxic compound or conferring a metabolic advantage. The invention further relates to the use of res-DHFR for screening cells for high expression of a protein of interest. The invention is illustrated by the Puro-DHFR surrogate marker, which corresponds to a fusion between the puromycin N-acetyltransferase and dihydrofolate reductase (DHFR).

IPC Classes  ?

  • C12N 9/00 - Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
  • C12N 15/00 - Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
  • G01N 33/74 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones
  • C12N 9/96 - Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates

23.

3-arylamino pyridine derivatives

      
Application Number 13472721
Grant Number 08524911
Status In Force
Filing Date 2012-05-16
First Publication Date 2012-11-22
Grant Date 2013-09-03
Owner Merck Serono SA (Switzerland)
Inventor
  • Abel, Ulrich
  • Deppe, Holger
  • Feurer, Achim
  • Grädler, Ulrich
  • Otte, Kerstin
  • Sekul, Renate
  • Thiemann, Meinolf
  • Goutopoulos, Andreas
  • Schwarz, Matthias
  • Jiang, Xuliang

Abstract

The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

IPC Classes  ?

24.

Tricyclic pyrazol amine derivatives

      
Application Number 13509291
Grant Number 09073940
Status In Force
Filing Date 2010-11-12
First Publication Date 2012-09-20
Grant Date 2015-07-07
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Gaillard, Pascale
  • Jeanclaude-Etter, Isabelle
  • Pomel, Vincent
  • Sebille, Eric
  • Jeyaprakashnarayanan, Seenisamy
  • Muzerelle, Mathilde

Abstract

This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.

IPC Classes  ?

25.

LOW FUCOSE CELL LINES AND USES THEREOF

      
Document Number 02829110
Status In Force
Filing Date 2012-03-05
Open to Public Date 2012-09-13
Grant Date 2019-01-15
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Helman, Daniel
  • Toister-Achituv, Mira
  • Bar-Shimon, Meirav

Abstract

A method of selecting cells having zero fucose level useful as host cells for expressing recombinant proteins is disclosed. The method comprises: (d) introducing genetic mutations into a population of CHO cells by contacting the cells with a methotrexate (MTX), (e) contacting the population of CHO cells comprising mutated cells with a non-toxic fucose binding agent for an amount of time that allows binding of the fucose binding agent to a fucose moiety on a cell membrane of the population of cells, wherein the amount of time does not allow killing of the cells; and (f) depleting from the population of cells comprising mutated cells, a subpopulation of cells which bind the fucose binding agent, thereby selecting cells useful as host cells for expressing recombinant proteins, the selected cells having zero fucose content. There are also disclosed cells and cell lines useful as host cells for expressing recombinant proteins.

IPC Classes  ?

  • C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
  • C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
  • C12N 15/01 - Preparation of mutants without inserting foreign genetic material therein; Screening processes therefor
  • C12N 15/13 - Immunoglobulins
  • C12N 15/60 - Lyases (4)
  • C12N 15/87 - Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
  • C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione

26.

LOW FUCOSE CELL LINES AND USES THEREOF

      
Application Number IL2012000109
Publication Number 2012/120500
Status In Force
Filing Date 2012-03-05
Publication Date 2012-09-13
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Helman, Daniel
  • Bar-Shimon, Meirav
  • Toister-Achituv, Mira

Abstract

A method of selecting cells having zero fucose level useful as host cells for expressing recombinant proteins is disclosed. The method comprises: (d) introducing genetic mutations into a population of CHO cells by contacting the cells with a methotrexate (MTX), (e) contacting the population of CHO cells comprising mutated cells with a non-toxic fucose binding agent for an amount of time that allows binding of the fucose binding agent to a fucose moiety on a cell membrane of the population of cells, wherein the amount of time does not allow killing of the cells; and (f) depleting from the population of cells comprising mutated cells, a subpopulation of cells which bind the fucose binding agent, thereby selecting cells useful as host cells for expressing recombinant proteins, the selected cells having zero fucose content. There are also disclosed cells and cell lines useful as host cells for expressing recombinant proteins.

IPC Classes  ?

  • C12N 15/10 - Processes for the isolation, preparation or purification of DNA or RNA
  • C12N 9/10 - Transferases (2.)
  • C12N 15/01 - Preparation of mutants without inserting foreign genetic material therein; Screening processes therefor

27.

MEMBRANE BOUND REPORTER MOLECULES AND THEIR USE IN CELL SORTING

      
Document Number 02821397
Status In Force
Filing Date 2011-12-19
Open to Public Date 2012-06-28
Grant Date 2019-01-08
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Helman, Daniel
  • Toister-Achituv, Mira
  • Bar-Shimon, Meirav
  • Smolarsky, Moshe

Abstract

The present invention relates to nucleic acid molecules comprising a nucleic acid sequence encoding a membrane-bound biotin mimetic peptide (BMP) or biotin acceptor peptide (BAP). The invention also relates to a method for selection of high producer cells secreting a protein of interest.

IPC Classes  ?

  • C12N 15/62 - DNA sequences coding for fusion proteins
  • C12N 15/10 - Processes for the isolation, preparation or purification of DNA or RNA
  • C12N 15/13 - Immunoglobulins
  • C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
  • C12N 15/65 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression using markers
  • C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
  • G01N 33/53 - Immunoassay; Biospecific binding assay; Materials therefor
  • C07K 14/61 - Growth hormone (GH) (Somatotropin)
  • C07K 14/705 - Receptors; Cell surface antigens; Cell surface determinants

28.

INDAZOLYL TRIAZOLE DERIVATIVES AS IRAK INHIBITORS

      
Application Number EP2011073015
Publication Number 2012/084704
Status In Force
Filing Date 2011-12-16
Publication Date 2012-06-28
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Jorand-Lebrun, Catherine
  • Crosignani, Stefano
  • Dorbais, Jerome
  • Grippi-Vallotton, Tania
  • Pretre, Adeline

Abstract

Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.

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
  • 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
  • A61K 31/4192 - 1,2,3-Triazoles

29.

MEMBRANE BOUND REPORTER MOLECULES AND THEIR USE IN CELL SORTING

      
Application Number IL2011000956
Publication Number 2012/085911
Status In Force
Filing Date 2011-12-19
Publication Date 2012-06-28
Owner MERCK SERONO S.A (Switzerland)
Inventor
  • Helman, Daniel
  • Toister-Achituv, Mira
  • Bar-Shimon, Meirav
  • Smolarsky, Moshe

Abstract

The present invention relates to nucleic acid molecules comprising a nucleic acid sequence encoding a membrane-bound biotin mimetic peptide (BMP) or biotin acceptor peptide (BAP). The invention also relates to a method for selection of high producer cells secreting a protein of interest.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
  • C12N 15/10 - Processes for the isolation, preparation or purification of DNA or RNA

30.

INDAZOLYL TRIAZOLE DERIVATIVES AS IRAK INHIBITORS

      
Document Number 02822166
Status In Force
Filing Date 2011-12-16
Open to Public Date 2012-06-28
Grant Date 2019-10-29
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Jorand-Lebrun, Catherine
  • Crosignani, Stefano
  • Dorbais, Jerome
  • Grippi-Vallotton, Tania
  • Pretre, Adeline

Abstract

Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.

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 31/4192 - 1,2,3-Triazoles
  • 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

31.

ANTIBODY WITH SPECIFICITY FOR GM-CSF (I)

      
Application Number EP2011070340
Publication Number 2012/066071
Status In Force
Filing Date 2011-11-17
Publication Date 2012-05-24
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Magnenat, Laurent
  • Leger, Olivier

Abstract

The present invention relates to antibodies with specificity for granulocyte- macrophage colony stimulating factor (GM-CSF). More particularly, the invention relates to humanized monoclonal antibodies that bind specifically to human GM-CSF with high affinity. The invention also relates to nucleic acids encoding the antibodies, vectors for expression of these nucleic acids, and host cells for producing said antibodies. Further, the invention relates to the use of said antibodies in the diagnosis or treatment of autoimmune or inflammatory diseases.

IPC Classes  ?

  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons

32.

ANTIBODY WITH SPECIFICITY FOR GM-CSF (II)

      
Application Number EP2011070375
Publication Number 2012/066089
Status In Force
Filing Date 2011-11-17
Publication Date 2012-05-24
Owner
  • MERCK SERONO SA (Switzerland)
  • CRC for Asthma & Airways (Australia)
Inventor
  • Magnenat, Laurent
  • Léger, Olivier
  • Mackay, Charles
  • Zahra, David Georges

Abstract

The present invention relates to antibodies with specificity for granulocyte-macrophage colony stimulating factor (GM-CSF). More particularly, the invention relates to humanized monoclonal antibodies that bind specifically to human GM-CSF with high affinity. The invention also relates to nucleic acids encoding the antibodies, vectors for expression of these nucleic acids, and host cells for producing said antibodies. Further, the invention relates to the use of said antibodies in the diagnosis or treatment of autoimmune or inflammatory diseases.

IPC Classes  ?

  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons

33.

GENOMIC MARKERS FOR PREDICTION OF LONG-TERM RESPONSE TO GROWTH HORMONE (GH) THERAPY

      
Application Number EP2011064951
Publication Number 2012/028633
Status In Force
Filing Date 2011-08-31
Publication Date 2012-03-08
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Croteau, Pascal
  • Raelson, John
  • Wojcik, Jérôme
  • Destenaves, Benoit
  • Olivier, Clément
  • Schnieper-Samec, Sonia

Abstract

The present invention relates to the use of genetic markers to identify the response to growth hormone treatment in Growth Hormone Deficiency (GHD) or Turner Syndrome (TS) patients as well as a method of treating GHD or TS patients and kits for genotyping.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

34.

COMBINATION TREATMENT OF MULTIPLE SCLEROSIS

      
Application Number EP2011064080
Publication Number 2012/022740
Status In Force
Filing Date 2011-08-16
Publication Date 2012-02-23
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Beelke, Manolo
  • Dauvillier, Jérôme
  • Guilleret, Isabelle
  • Monnet, Emmanuel

Abstract

The present invention is related to the use of Vitamin D in combination with Interferon-beta for the treatment of multiple sclerosis.

IPC Classes  ?

  • A61K 31/59 - Compounds containing 9,10-seco-cyclopenta[a]hydro- phenanthrene ring systems
  • A61K 31/592 - 9,10-Secoergostane derivatives, e.g. ergocalciferol, vitamin D2
  • A61K 31/593 - 9,10-Secocholestane derivatives, e.g. cholecalciferol, vitamin D3
  • A61K 38/21 - Interferons
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 37/00 - Drugs for immunological or allergic disorders

35.

Dihydroorotate dehydrogenase inhibitors

      
Application Number 13262640
Grant Number 09006454
Status In Force
Filing Date 2010-03-26
First Publication Date 2012-02-02
Grant Date 2015-04-14
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Thunuguntla, Siva Sanjeeva Rao
  • Subramanya, Hosahalli
  • Kunnam, Satish Reddy
  • Sanivaru Vijay, Sekhar Reddy
  • Bingi, Chakrapani
  • Kusanur, Raviraj
  • Schwarz, Matthias
  • Arlt, Michael

Abstract

b, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.

IPC Classes  ?

  • C07D 235/18 - Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
  • C07D 403/10 - 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 carbon chain containing aromatic rings
  • 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 401/10 - 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 aromatic rings
  • 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 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • 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 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
  • 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 409/10 - 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 carbon chain containing aromatic rings
  • C07D 413/10 - 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 linked by a carbon chain containing aromatic rings
  • C07D 417/10 - 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 carbon chain containing aromatic rings
  • C07D 471/04 - Ortho-condensed systems

36.

5-(BIPHENYL-4-YL)-3-PHENYL-1,2,4-OXADIAZOLYL DERIVATIVES AS LIGANDS ON THE SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTORS

      
Application Number EP2011061372
Publication Number 2012/004287
Status In Force
Filing Date 2011-07-06
Publication Date 2012-01-12
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Bombrun, Agnes
  • Quattropani, Anna
  • Gonzalez, Jerome
  • Dorbais, Jerome
  • Knight, Chris
  • Baker-Glenn, Charles

Abstract

The present invention provides compounds of Formula (I), as selective S1 P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases.

IPC Classes  ?

  • C07D 271/06 - 1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
  • A61K 31/4245 - Oxadiazoles
  • A61P 37/02 - Immunomodulators
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • 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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

37.

Pyrazine derivatives and use as PI3K inhibitors

      
Application Number 13222072
Grant Number 08877757
Status In Force
Filing Date 2011-08-31
First Publication Date 2011-12-22
Grant Date 2014-11-04
Owner Merck Serono SA (Switzerland)
Inventor
  • Gaillard, Pascale
  • Quattropani, Anna
  • Pomel, Vincent
  • Rueckle, Thomas
  • Klicic, Jasna
  • Church, Dennis

Abstract

The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

IPC Classes  ?

  • A01N 43/58 - 1,2-Diazines; Hydrogenated 1,2-diazines
  • A01N 43/60 - 1,4-Diazines; Hydrogenated 1,4-diazines
  • A61K 31/50 - Pyridazines; Hydrogenated pyridazines
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
  • 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 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 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 471/04 - Ortho-condensed systems
  • C07D 407/12 - 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 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 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 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 413/12 - 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 linked by a chain containing hetero atoms as chain links

38.

2-morpholino-pyrido[3,2-D]pyrimidines

      
Application Number 13147449
Grant Number 08609666
Status In Force
Filing Date 2010-02-04
First Publication Date 2011-12-01
Grant Date 2013-12-17
Owner Merck Serono SA (Switzerland)
Inventor
  • Montagne, Cyril
  • Bombrun, Agnés
  • Desforges-Bouscary, Gwenaelle
  • Quattropani, Anna
  • Gaillard, Pascale

Abstract

This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.

IPC Classes  ?

  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 471/04 - Ortho-condensed systems

39.

CLADRIBINE TREATMENT OF MULTIPLE SCLEROSIS IN PATIENT GROUPS DEFINED BY GENOTYPE

      
Application Number EP2011054388
Publication Number 2011/117267
Status In Force
Filing Date 2011-03-23
Publication Date 2011-09-29
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Wojcik, Jérôme
  • Monnet, Emmanuel

Abstract

The invention relates to a method for determining the capacity of a subject suffering from Relapsing-Remitting Multiple Sclerosis (RRMS) to respond to treatment with Cladribine, said method comprising determining the polymorphism genotype of the subject in at least one SNP located on chromosome X, particularly an SNP located in the Duchenne Muscular Dystrophy (DMD) gene, for example rs5971598. The invention also relates to Cladribine for use in treating Relapsing-Remitting Multiple Sclerosis (RRMS) in a subject, wherein the treatment is specifically adapted to the capacity of the subject to respond to Cladribine treatment, as predicted by genotype.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

40.

3-arylamino pyridine derivatives

      
Application Number 13112490
Grant Number 08198457
Status In Force
Filing Date 2011-05-20
First Publication Date 2011-09-15
Grant Date 2012-06-12
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Abel, Ulrich
  • Deppe, Holger
  • Feurer, Achim
  • Grädler, Ulrich
  • Otte, Kerstin
  • Sekul, Renate
  • Thiemann, Meinolf
  • Goutopoulos, Andreas
  • Schwarz, Matthias
  • Jiang, Xuliang

Abstract

The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

IPC Classes  ?

  • C07D 213/72 - Nitrogen atoms
  • C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • A01N 43/58 - 1,2-Diazines; Hydrogenated 1,2-diazines

41.

SAFINAMIDE IN THE TREATMENT OF DYSKINESIA

      
Application Number EP2011051836
Publication Number 2011/098456
Status In Force
Filing Date 2011-02-08
Publication Date 2011-08-18
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Von Raison, Florian
  • Weiner, David
  • Roach, Arthur
  • Cuenoud, Bernard
  • Bartoszyk, Gerd

Abstract

The present invention relates to the treatment and prophylaxis of dyskinesias, preferably dyskinesias associated with dopaminergic therapy.

IPC Classes  ?

  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)

42.

HUMANIZED ANTIBODIES AGAINST HUMAN IL-22RA

      
Application Number EP2010067332
Publication Number 2011/061119
Status In Force
Filing Date 2010-11-12
Publication Date 2011-05-26
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Beckmann, Roland
  • Johnson-Leger, Caroline

Abstract

The invention relates to humanized antibodies against human IL-22RA and to their use in the treatment of psoriasis and other immune-mediated diseases such as psoriatic arthritis and atopic dermatitis.

IPC Classes  ?

  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • A61P 17/06 - Antipsoriatics
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • 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

43.

TRICYCLIC PYRAZOL AMINE DERIVATIVES AS PI3K INHIBITORS

      
Document Number 02778174
Status In Force
Filing Date 2010-11-12
Open to Public Date 2011-05-19
Grant Date 2018-02-20
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Gaillard, Pascale
  • Jeanclaude-Etter, Isabelle
  • Pomel, Vincent
  • Sebille, Eric
  • Jeyaprakashnarayanan, Seenisamy
  • Muzerelle, Mathilde

Abstract

This specification relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers (see formula I*).

IPC Classes  ?

  • C07D 495/04 - Ortho-condensed systems
  • A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • C07D 495/14 - Ortho-condensed systems

44.

TRICYCLIC PYRAZOL AMINE DERIVATIVES

      
Application Number EP2010067412
Publication Number 2011/058149
Status In Force
Filing Date 2010-11-12
Publication Date 2011-05-19
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Gaillard, Pascale
  • Jeanclaude-Etter, Isabelle
  • Pomel, Vincent
  • Sebille, Eric
  • Jeyaprakashnarayanan, Seenisamy
  • Muzerelle, Mathilde

Abstract

This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.

IPC Classes  ?

  • C07D 495/04 - Ortho-condensed systems
  • C07D 495/14 - Ortho-condensed systems
  • A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61P 37/00 - Drugs for immunological or allergic disorders

45.

Thiazole derivatives and use thereof

      
Application Number 12952231
Grant Number 08399497
Status In Force
Filing Date 2010-11-23
First Publication Date 2011-04-14
Grant Date 2013-03-19
Owner Merck Serono SA (Switzerland)
Inventor
  • Quattropani, Anna
  • Covini, David
  • Pomel, Vincent
  • Dorbais, Jerome
  • Rueckle, Thomas

Abstract

The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
  • 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

46.

COMPOSITIONS AND METHODS FOR TREATING GROWTH HORMONE DEFICIENCY

      
Application Number EP2010062652
Publication Number 2011/026815
Status In Force
Filing Date 2010-08-30
Publication Date 2011-03-10
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Theocharis, Theo
  • Larroque, Sylvain
  • Bernard, Laurence

Abstract

The present invention relates to methods of predicting the level of response to treatment with growth hormone in an individual having Growth Hormone Deficiency (GHD) or Turner Syndrome (TS).

IPC Classes  ?

  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
  • G01N 33/74 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones
  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
  • A61K 38/27 - Growth hormone [GH] (Somatotropin)

47.

TETRAZOLE DERIVATIVES

      
Application Number EP2010060151
Publication Number 2011/006935
Status In Force
Filing Date 2010-07-14
Publication Date 2011-01-20
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Crosignani, Stefano
  • Cleva, Christophe
  • Quattropani, Anna
  • Desforges, Gwenaelle
  • Bombrun, Agnes

Abstract

The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.

IPC Classes  ?

  • C07D 257/04 - Five-membered rings
  • 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 413/12 - 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 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
  • A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
  • A61P 37/00 - Drugs for immunological or allergic disorders

48.

TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS

      
Application Number EP2010060154
Publication Number 2011/006936
Status In Force
Filing Date 2010-07-14
Publication Date 2011-01-20
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Crosignani, Stefano
  • Jorand-Lebrun, Catherine
  • Grippi-Vallotton, Tania

Abstract

The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g. toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light eruption (e.g. photo-irritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).

IPC Classes  ?

  • C07D 487/10 - Spiro-condensed systems
  • A61P 37/08 - Antiallergic agents
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil

49.

PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS

      
Application Number EP2010057893
Publication Number 2010/142628
Status In Force
Filing Date 2010-06-07
Publication Date 2010-12-16
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Quattropani, Anna
  • Baker-Glenn, Charles
  • Blackaby, Wesley
  • Knight, Chris

Abstract

The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases. Wherein R1, R2 and R3 are as defined in the description.

IPC Classes  ?

  • 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 471/04 - Ortho-condensed systems
  • A61K 31/4245 - Oxadiazoles
  • A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

50.

Triazole oxadiazoles derivatives

      
Application Number 12809816
Grant Number 08202856
Status In Force
Filing Date 2008-12-17
First Publication Date 2010-12-02
Grant Date 2012-06-19
Owner Merck Serono SA (Switzerland)
Inventor
  • Quattropani, Anna
  • Cleva, Christophe
  • Sebille, Eric
  • Schwarz, Matthias
  • Marin, Delphine
  • Bombrun, Agnes
  • Blackaby, Wesley
  • Baker-Glenn, Charles
  • Knight, Chris
  • Rouse, Craig

Abstract

The invention relates to compounds of formula I: b, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • 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 31/444 - 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/4245 - Oxadiazoles
  • 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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic 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 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 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
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • 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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
  • A61P 17/06 - Antipsoriatics
  • A61P 11/06 - Antiasthmatics

51.

Oxadiazole diaryl compounds

      
Application Number 12675254
Grant Number 08404676
Status In Force
Filing Date 2008-10-01
First Publication Date 2010-12-02
Grant Date 2013-03-26
Owner Merck Serono SA (Switzerland)
Inventor
  • Montagne, Cyril
  • Quattropani, Anna
  • Sauer, Wolfgang
  • Bombrun, Agnes

Abstract

The invention relates to compounds of formula (I): c and W, have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • 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 31/454 - 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
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/4245 - Oxadiazoles
  • 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 31/4545 - 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
  • C07D 401/10 - 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 aromatic rings
  • C07D 413/10 - 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 linked by a carbon chain containing aromatic rings
  • C07D 271/06 - 1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
  • 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
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
  • A61P 17/06 - Antipsoriatics
  • A61P 27/02 - Ophthalmic agents
  • A61P 11/06 - Antiasthmatics
  • 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 7/06 - Antianaemics
  • A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P 35/00 - Antineoplastic agents
  • A61P 43/00 - Drugs for specific purposes, not provided for in groups

52.

Method of treating peripheral vascular diseases using IL-18 inhibitors

      
Application Number 12791052
Grant Number 09566313
Status In Force
Filing Date 2010-06-01
First Publication Date 2010-11-18
Grant Date 2017-02-14
Owner
  • MERCK SERONO SA (Switzerland)
  • INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (France)
Inventor
  • Chvatchko, Yolande
  • Tedgui, Alain
  • Mallat, Ziad

Abstract

The invention relates to the use of an inhibitor of IL-18 in the preparation of a medicament for treatment and/or prevention of peripheral vascular diseases. The invention further relates to the use of an IL-18 inhibitor for prevention of limb amputation.

IPC Classes  ?

  • A61K 38/17 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans

53.

GENETIC SEVERITY MARKERS IN MULTIPLE SCLEROSIS

      
Application Number EP2010053871
Publication Number 2010/127906
Status In Force
Filing Date 2010-03-25
Publication Date 2010-11-11
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Abderrahim, Hadi
  • Wojcik, Jérôme
  • Esposito, Federica
  • Debailleul, Virginie

Abstract

The present invention relates to the use of SNPs in predicting susceptibility and/or severity of Multiple Sclerosis in an individual. The SNPs are located in the introns of the glycosylation enzymes MGAT5 and XYLTl, 3' of HIFlAN, within introns of MEGF11, FGF14, PDE9A and CDH13 and within desert regions of 4q34 and 17p13.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

54.

Tablet dispenser

      
Application Number 29356960
Grant Number D0625912
Status In Force
Filing Date 2010-03-04
First Publication Date 2010-10-26
Grant Date 2010-10-26
Owner Merck Serono SA (Switzerland)
Inventor
  • Sprada, John Peter
  • Prasser, Robert

55.

LH liquid formulations

      
Application Number 12681688
Grant Number 08664369
Status In Force
Filing Date 2008-10-29
First Publication Date 2010-10-14
Grant Date 2014-03-04
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Agostinetto, Rita
  • Samaritani, Fabrizio
  • Del Rio, Alessandra
  • Richard, Joel

Abstract

The invention relates to liquid pharmaceutical formulations of luteinizing hormone (LH) for single- or multi-dose administration.

IPC Classes  ?

  • C07K 14/59 - Follicle-stimulating hormone (FSH); Chorionic gonadotropins, e.g. HCG; Luteinising hormone (LH); Thyroid-stimulating hormone (TSH)
  • C07K 7/23 - Luteinising hormone-releasing hormone (LHRH); Related peptides
  • A61K 38/09 - Luteinising hormone-releasing hormone [LHRH]; Related peptides
  • A61K 38/24 - Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g. HCG; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]

56.

OXADIAZOLE DERIVATIVES

      
Application Number EP2010054100
Publication Number 2010/115751
Status In Force
Filing Date 2010-03-29
Publication Date 2010-10-14
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Quattropani, Anna
  • Montagne, Cyril
  • Sauer, Wolfgang
  • Crosignani, Stefano
  • Bombrun, Agnès

Abstract

The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

57.

DIHYDROOROTATE DEHYDROGENASE INHIBITORS

      
Application Number EP2010054034
Publication Number 2010/115736
Status In Force
Filing Date 2010-03-26
Publication Date 2010-10-14
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Thunuguntla, Siva Sanjeeva Rao
  • Subramanya, Hosahalli
  • Kunnam, Satish Reddy
  • Sanivaru Vijay, Sekhar Reddy
  • Bingi, Chakrapani
  • Kusanur, Raviraj
  • Schwarz, Matthias
  • Arlt, Michael

Abstract

The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.

IPC Classes  ?

  • 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 235/18 - Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
  • 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
  • C07D 401/10 - 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 aromatic 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 409/10 - 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 carbon chain containing aromatic rings
  • C07D 413/10 - 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 linked by a carbon chain containing aromatic rings
  • C07D 417/10 - 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 carbon chain containing aromatic rings
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/33 - Heterocyclic compounds
  • A61P 35/00 - Antineoplastic agents

58.

Arylamino N-heteraryl compounds as MEK inhibitors

      
Application Number 12815071
Grant Number 08802703
Status In Force
Filing Date 2010-06-14
First Publication Date 2010-10-07
Grant Date 2014-08-12
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Goutopoulos, Andreas
  • Askew, Jr., Benny C.
  • Diep, Nhut Kiet
  • Karra, Srinivasa R.
  • Schwarz, Matthias
  • Yu, Henry

Abstract

The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.

IPC Classes  ?

  • A61K 31/465 - Nicotine; Derivatives thereof
  • A61K 31/4412 - Non-condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
  • A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
  • C07D 213/81 - Amides; Imides
  • C07D 213/80 - Acids; Esters in position 3
  • C07D 213/82 - Amides; Imides in position 3
  • 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 213/84 - Nitriles
  • C07D 237/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
  • C07D 213/79 - Acids; Esters
  • A61P 35/00 - Antineoplastic agents
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

59.

OXADIAZOLE DERIVATIVES

      
Application Number EP2010054103
Publication Number 2010/112461
Status In Force
Filing Date 2010-03-29
Publication Date 2010-10-07
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Quattropani, Anna
  • Montagne, Cyril
  • Sauer, Wolfgang
  • Crosignani, Stefano
  • Bombrun, Agnes

Abstract

The invention relates to compounds of formula (I); wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

60.

Oxadiazole derivatives

      
Application Number 12675235
Grant Number 08202865
Status In Force
Filing Date 2008-10-01
First Publication Date 2010-09-23
Grant Date 2012-06-19
Owner Merck Serono SA (Switzerland)
Inventor
  • Quattropani, Anna
  • Montagne, Cyril
  • Sauer, Wolfgang
  • Crosignani, Stefano
  • Bombrun, Agnes
  • Muzerelle, Mathilde
  • Dorbais, Jermone
  • Marin, Delphine
  • Gonzalez, Jerome
  • Gerber, Patrick

Abstract

The invention relates to compounds of formula I: b, W, Q and S have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • 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
  • 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 31/4245 - Oxadiazoles
  • C07D 413/02 - 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
  • C07D 271/06 - 1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles

61.

BANK1 RELATED SNPS AND SLE AND/OR MS SUSCEPTIBILITY

      
Application Number EP2010052554
Publication Number 2010/100113
Status In Force
Filing Date 2010-03-01
Publication Date 2010-09-10
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Wojcik, Jérôme
  • Alarcón-Riquelme, Marta
  • Castillejo-López, Casimiro

Abstract

The invention relates to a method of genotyping and for predicting the susceptibility for SLE and/or MS by using SNPs related to BANK1 alone or in combination with at least one other SNP.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

62.

OXAZOLE PYRIDINE DERIVATIVES USEFUL AS S1P1 RECEPTOR AGONISTS

      
Application Number EP2010052613
Publication Number 2010/100142
Status In Force
Filing Date 2010-03-02
Publication Date 2010-09-10
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Quattropani, Anna
  • Gerber, Patrick
  • Dorbais, Jerome

Abstract

The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.

IPC Classes  ?

  • 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
  • A61K 31/4245 - Oxadiazoles
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

63.

FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE

      
Application Number EP2010052615
Publication Number 2010/100144
Status In Force
Filing Date 2010-03-02
Publication Date 2010-09-10
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Swinnen, Dominique
  • Jorand-Lebrun, Catherine
  • Grippi-Vallotton, Tania
  • Gerber, Patrick
  • Gonzalez, Jerome
  • Shaw, Jeffrey
  • Jeyaprakashnarayanan, Seenisamy

Abstract

The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.

IPC Classes  ?

  • C07D 277/82 - Nitrogen atoms
  • C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 419/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61K 31/415 - 1,2-Diazoles
  • A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

64.

Tablet dispenser

      
Application Number 29356957
Grant Number D0622499
Status In Force
Filing Date 2010-03-04
First Publication Date 2010-08-31
Grant Date 2010-08-31
Owner Merck Serono SA (Switzerland)
Inventor
  • Sprada, John Peter
  • Prasser, Robert

65.

GENETIC MARKERS FOR DIAGNOSING PRIMARY PROGRESSIVE FORMS OF MULTIPLE SCLEROSIS

      
Application Number EP2010050378
Publication Number 2010/094525
Status In Force
Filing Date 2010-01-14
Publication Date 2010-08-26
Owner Merck Serono S.A. (Switzerland)
Inventor
  • Abderrahim, Hadi
  • Wojcik, Jérôme
  • Esposito, Federica
  • Comi, Giancarlo
  • Martinelli Boneschi, Filippo

Abstract

The present invention relates to the use of SNPs in Multiple Sclerosis.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

66.

2-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES

      
Document Number 02751501
Status In Force
Filing Date 2010-02-04
Open to Public Date 2010-08-19
Grant Date 2018-01-16
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Montagne, Cyril
  • Bombrun, Agnes
  • Desforges-Bouscary, Gwenaelle
  • Quattropani, Anna
  • Gaillard, Pascale

Abstract

This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune deseases, inflammatory disorders, multiple sclerosis and other deseases like cancers.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

67.

6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis

      
Application Number 12671996
Grant Number 08399448
Status In Force
Filing Date 2008-07-29
First Publication Date 2010-08-19
Grant Date 2013-03-19
Owner Merck Serono SA (Switzerland)
Inventor
  • Bombrun, Agnes
  • Schwarz, Matthias
  • Crosignani, Stefano
  • Covini, David
  • Marin, Delphine

Abstract

The invention relates to compounds of formula (I): 2 have the meanings given in claim 1. The compounds are useful, for example, in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • A61K 31/33 - Heterocyclic compounds
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/535 - 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
  • C07D 239/24 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
  • 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 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 413/12 - 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 linked by a chain containing hetero atoms as chain links

68.

PHENOXY ACETIC ACID DERIVATIVES

      
Application Number EP2010051567
Publication Number 2010/092043
Status In Force
Filing Date 2010-02-09
Publication Date 2010-08-19
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Crosignani, Stefano
  • Jorand-Lebrun, Catherine
  • Cleva, Christophe
  • Pretre, Adeline

Abstract

The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.

IPC Classes  ?

  • C07C 59/70 - Ethers of hydroxy-acetic acid
  • A61P 7/06 - Antianaemics
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • 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
  • A61P 17/00 - Drugs for dermatological disorders
  • A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
  • C07D 213/30 - Oxygen atoms
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
  • C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
  • C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
  • C07D 277/24 - Radicals substituted by oxygen atoms
  • C07D 333/28 - Halogen atoms
  • 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 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

69.

2-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES

      
Application Number EP2010051373
Publication Number 2010/091996
Status In Force
Filing Date 2010-02-04
Publication Date 2010-08-19
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Montagne, Cyril
  • Bombrun, Agnès
  • Desforges-Bouscary, Gwenaelle
  • Quattropani, Anna
  • Gaillard, Pascale

Abstract

This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune deseases, inflammatory disorders, multiple sclerosis and other deseases like cancers.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

70.

Cladribine regimen for treating multiple sclerosis

      
Application Number 12766173
Grant Number 08377903
Status In Force
Filing Date 2010-04-23
First Publication Date 2010-08-12
Grant Date 2013-02-19
Owner MERCK SERONO SA (Switzerland)
Inventor
  • De Luca, Giampiero
  • Ythier, Arnaud
  • Munafo, Alain
  • Lopez-Bresnahan, Maria

Abstract

The present invention is related to the use of Cladribine for the preparation of a pharmaceutical formulation for the treatment of multiple sclerosis, especially relapsing-remitting multiple sclerosis or early secondary progressive multiple sclerosis, wherein the preparation is to be the orally administered and wherein re-treatments are possible.

IPC Classes  ?

  • A61K 31/52 - Purines, e.g. adenine
  • 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
  • A61K 38/21 - Interferons
  • A61K 9/00 - Medicinal preparations characterised by special physical form

71.

PURO-DHFR quadrifunctional marker and its use in protein production

      
Application Number 12601553
Grant Number 08357535
Status In Force
Filing Date 2008-06-06
First Publication Date 2010-07-01
Grant Date 2013-01-22
Owner Merck Serono SA (Switzerland)
Inventor
  • Kobr, Michel
  • Dupraz, Philippe

Abstract

This invention relates to industrial production of proteins. More specifically, the invention relates to the res-DHFR surrogate marker, which corresponds to a fusion between DHFR and a protein conferring resistance to a toxic compound or conferring a metabolic advantage. The invention further relates to the use of res-DHFR for screening cells for high expression of a protein of interest. The invention is illustrated by the Puro-DHFR surrogate marker, which corresponds to a fusion between the puromycin N-acetyltransferase and dihydrofolate reductase (DHFR).

IPC Classes  ?

  • C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
  • C12P 21/00 - Preparation of peptides or proteins

72.

OXADIAZOLE FUSED HETEROCYCLIC DERIVATIVES USEFUL FOR THE TREATMENT OF MULTIPLE SCLEROSIS

      
Application Number EP2009067171
Publication Number 2010/069949
Status In Force
Filing Date 2009-12-15
Publication Date 2010-06-24
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Muzerelle, Mathilde
  • Quattropani, Anna
  • Montagne, Cyril
  • Dorbais, Jérôme

Abstract

The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.

IPC Classes  ?

  • 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
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/435 - 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
  • A61K 31/4245 - Oxadiazoles
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • 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

73.

COMPOSITIONS AND METHODS FOR TREATING GROWTH HORMONE DEFICIENCY

      
Application Number EP2009065853
Publication Number 2010/060935
Status In Force
Filing Date 2009-11-25
Publication Date 2010-06-03
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Tuefferd, Marianne
  • Dauvillier, Jérôme
  • Delaye, Arnaud
  • Schnieper-Samec, Sonia

Abstract

The present invention relates to the use of genetic markers to identify the response to growth hormone treatment in Growth Hormone Deficiency (GHD) or Turner Syndrome (TS) patients as well as a method of treating GHD or TS patients and kits for genotyping.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

74.

MEDICATION DISPENSER

      
Application Number IB2009007006
Publication Number 2010/055377
Status In Force
Filing Date 2009-10-01
Publication Date 2010-05-20
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Ballard, Brian, Lee
  • Sprada, Peter, John

Abstract

A dispenser for the delivery of medication comprises: - a support (9, 10) supporting an array of blister(s) (11) each containing a medication dose, said support (9, 10) having an array of through hole(s) (19, 25) below said blister(s) (11) respectively, - an actuating member (13) located above said support (9, 10), said actuating member (13) being movable in translation relative to said support (9, 10), by at least one step, in a determined direction (d) parallel to said support (9, 10), and - means (29, 57) for converting each of said step(s) of translational motion of the actuating member (13) into a pressure exerted on corresponding one(s) of said blister(s) (11) towards the corresponding through hole(s) (19, 25) to expel the corresponding medication dose(s) through said corresponding through hole(s) (19, 25).

IPC Classes  ?

  • B65D 83/04 - Containers or packages with special means for dispensing contents for dispensing annular, disc-shaped, or spherical or like small articles, e.g. tablets or pills
  • A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets

75.

4 -MORPHOLINO-PYRIDO [3, 2 -D] PYRIMIDINES ACTIVE ON PI3K

      
Application Number EP2009062664
Publication Number 2010/037765
Status In Force
Filing Date 2009-09-30
Publication Date 2010-04-08
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Pomel, Vincent
  • Gaillard, Pascale
  • Desforges, Gwenaelle
  • Quattropani, Anna
  • Montagne, Cyril

Abstract

This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune deseases, inflammatory disorders, multiple sclerosis and other deseases like cancers.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61P 35/00 - Antineoplastic agents
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

76.

SOLID LIPID MICROCAPSULES CONTAINING hGH

      
Application Number EP2009005826
Publication Number 2010/017965
Status In Force
Filing Date 2009-08-11
Publication Date 2010-02-18
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Richard, Joel
  • Fais, Fabio
  • Baldascini, Helen Gabriela

Abstract

The invention relates to growth hormone (GH) formulations having sustained-release properties, in particular human growth hormone (hGH) and methods for their preparation. The growth hormone formulations can be manufactured without denaturing of the protein and can conveniently be administrated to the person in need thereof by using a conventional syringe via a needle having a small diameter.

IPC Classes  ?

  • A61K 9/50 - Microcapsules
  • A61P 5/06 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
  • A61K 38/27 - Growth hormone [GH] (Somatotropin)

77.

Cladribine regimen for treating multiple sclerosis

      
Application Number 12301083
Grant Number 09925151
Status In Force
Filing Date 2007-05-23
First Publication Date 2010-01-28
Grant Date 2018-03-27
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Brentzel, Jr., H. James
  • Lopez-Bresnahan, Maria
  • Ammoury, Nazih

Abstract

The present invention relates to the use of multiple doses of Cladribine combined with beta interferon for the treatment of multiple sclerosis in patients who are refractory to at least one conventional therapy.

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
  • 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 31/00 - Medicinal preparations containing organic active ingredients
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 38/21 - Interferons

78.

USE OF GENETIC MARKERS FOR IDENTIFYING THE RESPONSE TO INTERFERON TREATMENT IN MULTIPLE SCLEROSIS PATIENTS

      
Application Number EP2009059283
Publication Number 2010/010057
Status In Force
Filing Date 2009-07-20
Publication Date 2010-01-28
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Monnet, Emmanuel
  • Bouzekri, Nourdine

Abstract

The present invention relates to the use of genetic markers to identify the response to interferon-beta (IFN-beta) treatment in Multiple Sclerosis (MS) patients as well as a method for treating MS patients and kits for genotyping.

IPC Classes  ?

  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids

79.

FUSED BICYCLIC COMPOUNDS AND USE THEREOF AS PI3K INHIBITORS

      
Application Number EP2009055172
Publication Number 2009/133127
Status In Force
Filing Date 2009-04-29
Publication Date 2009-11-05
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Swinnen, Dominique
  • Jorand-Lebrun, Catherine
  • Grippi-Vallotton, Tania
  • Gerber, Patrick
  • Gonzalez, Jerome
  • Shaw, Jeffrey, P.

Abstract

The invention relates to compounds of formula (I), for the regulation of phosphoinositides 3-kinases activity and related diseases.

IPC Classes  ?

  • C07D 277/82 - Nitrogen atoms
  • C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
  • 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 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 487/04 - Ortho-condensed systems
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P 35/00 - Antineoplastic agents
  • A61P 37/00 - Drugs for immunological or allergic disorders

80.

SULFONAMIDES

      
Application Number EP2009054204
Publication Number 2009/124962
Status In Force
Filing Date 2009-04-08
Publication Date 2009-10-15
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Crosignani, Stefano
  • Cleva, Christophe
  • Tsaklakidis, Christos
  • Burgdorf, Lars

Abstract

The invention relates to compounds of formula (I) wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 1, for the treatment of CXCR3 related diseases.

IPC Classes  ?

  • C07C 311/19 - 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 hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
  • C07D 213/36 - Radicals substituted by singly-bound nitrogen atoms
  • A61K 31/18 - Sulfonamides
  • 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
  • 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
  • C07D 213/42 - Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
  • C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
  • C07D 213/82 - Amides; Imides in position 3
  • C07D 217/16 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
  • C07D 239/52 - Two oxygen atoms
  • C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 257/04 - Five-membered rings
  • C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
  • C07D 265/36 - 1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
  • C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

81.

CHILD-RESISTANT MEDICATION CONTAINER

      
Application Number IB2009005131
Publication Number 2009/125267
Status In Force
Filing Date 2009-03-31
Publication Date 2009-10-15
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Sprada, Peter, John
  • Prasser, Robert

Abstract

Child-resistant medication container comprising: a housing (1; 40) having an open end (5;18), - a support (7; 46) for supporting medication, said support being slidably mounted in the housing, - first locking means (31,32; 59, 60, 61, 62; 91, 92) for locking the support in the housing and for unlocking the support so that the support may be slid to the outside of the housing through the open end, said first locking means comprising a first locking member (31; 59; 91) coupled to the housing and a second locking member (32; 61).coupled to the support, said first and second locking members being engageable with each other, and at least one button (13; 50, 51; 83, 84) operable to act on the first locking means, said at least one button comprising a first button (13; 50; 83) operable to disengage the first (31; 59; 91) and second (32; 61) locking members, second locking means (23, 30; 65, 69; 86, 89) for maintaining engagement between the first (31; 59; 91) and second (32; 61) locking members, and a second button (14; 52; 80) operable to act on the second locking means to permit disengaging the first (31; 59; 91) and second (32; 61) locking members by operating the first button (13; 50; 83).

IPC Classes  ?

  • B65D 83/04 - Containers or packages with special means for dispensing contents for dispensing annular, disc-shaped, or spherical or like small articles, e.g. tablets or pills

82.

PTPH1 INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

      
Application Number EP2009053151
Publication Number 2009/118259
Status In Force
Filing Date 2009-03-17
Publication Date 2009-10-01
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Patrignani, Claudia
  • Muzio, Valeria
  • Magnone, Maria-Chiara
  • Zaratin, Paola
  • Greco, Béatrice

Abstract

The present invention relates to the use of PTPH1 inhibitors in the prevention or treatment of Alzheimer's Disease, or a symptom thereof. The present invention also relates to a method of identifying compounds useful in the prevention or treatment of Alzheimer's Disease, or a symptom thereof.

IPC Classes  ?

  • A61K 9/127 - Liposomes
  • A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 38/00 - Medicinal preparations containing peptides
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

83.

VARIATION OF RECOMBINANT EXPRESSION TITRES BY OPTIMISING BACTERIAL RIBOSOME BINDING SITES

      
Application Number EP2009053024
Publication Number 2009/112587
Status In Force
Filing Date 2009-03-13
Publication Date 2009-09-17
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Chevalet, Laurent
  • Maundrell, Kinsey

Abstract

The present invention provides a method for optimising the ribosome binding site of a promoter for the expression of a gene encoding a polypeptide of interest, placed under the control of said promoter. The invention also relates to a vector containing such optimised promoters, a prokaryotic host cell transformed by said vector, as well as a method for producing a recombinant protein of interest.

IPC Classes  ?

  • C12N 15/67 - General methods for enhancing the expression
  • C12N 15/70 - Vectors or expression systems specially adapted for E. coli

84.

Humanized antibody molecules specific for IL-31

      
Application Number 12329820
Grant Number 08470979
Status In Force
Filing Date 2008-12-08
First Publication Date 2009-08-20
Grant Date 2013-06-25
Owner
  • ZymoGenetics, Inc. (USA)
  • Merck Serono S/A (Switzerland)
Inventor
  • Bondensgaard, Kent
  • Beckmann, Roland

Abstract

The invention provides humanized mouse anti-human IL-31 antibodies and antibody fragments that are capable of binding IL-31 and thereby neutralizing, inhibiting, limiting, or reducing the proinflammatory or pro-pruritic effects of IL-31.

IPC Classes  ?

  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
  • C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons

85.

PEG-INTERFERON-BETA FORMULATIONS

      
Application Number EP2008067876
Publication Number 2009/080699
Status In Force
Filing Date 2008-12-18
Publication Date 2009-07-02
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Del Rio, Alessandra
  • Richard, Joel

Abstract

The invention relates to a liquid pharmaceutical composition comprising a pegylated IFN-β (PEG- IFN-β), an excipient, a surfactant and a buffer wherein said excipient is a polyol, wherein said surfactant is a non-ionic surfactant and wherein said buffer is a sodium acetate buffer.

IPC Classes  ?

  • A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
  • A61K 38/21 - Interferons

86.

TRIAZOLE OXADIAZOLES DERIVATIVES

      
Application Number EP2008067776
Publication Number 2009/080663
Status In Force
Filing Date 2008-12-17
Publication Date 2009-07-02
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Quattropani, Anna
  • Cleva, Christophe
  • Sebille, Eric
  • Schwarz, Matthias
  • Marin, Delphine
  • Bombrun, Agnès
  • Blackaby, Wesley
  • Baker-Glenn, Charles
  • Knight, Chris
  • Rouse, Craig

Abstract

The invention relates to compounds of formula (I), wherein R1, R2, Ra, Rb, X have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • 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
  • A61K 31/4245 - Oxadiazoles
  • A61P 37/00 - Drugs for immunological or allergic disorders

87.

SARP-1 FUSION PROTEINS AND USES THEREOF

      
Application Number EP2008067298
Publication Number 2009/074637
Status In Force
Filing Date 2008-12-11
Publication Date 2009-06-18
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Saborio, Gabriela
  • Karmirantzou, Maria

Abstract

The invention relates to a fusion protein comprising a mature SARP-1 polypeptide without the Netrindomain, the fusion protein further comprising an Fc region of an immunoglobulin, wherein the fusion protein lacks certain N-terminal amino acids of the mature SARP-1 polypeptide. The invention further relates to the use of said fusion protein fortreating cancer, a fibrotic disorder or a cardiovascular disorder.

IPC Classes  ?

  • C07K 14/47 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates from mammals

88.

ALLELE AND ISOTOPE-SPECIFIC INTERVENTION ON MHC CLASS II MOLECULES ASSOCIATED WITH AUTOIMMUNE DISEASES BY MEANS OF PEPTIDES

      
Application Number EP2008010230
Publication Number 2009/071276
Status In Force
Filing Date 2008-12-03
Publication Date 2009-06-11
Owner MERCK SERONO SA (Switzerland)
Inventor
  • Weissert, Robert
  • Wiesmueller, Karl-Heinz
  • De Graaf, Katrien, L.

Abstract

The present invention relates to a peptide for the treatment or prophylaxis of an autoimmune disease, a nucleic acid molecule coding for said peptide, a pharmaceutical composition comprising the peptide and/or the nucleic acid molecule, and to a method for the treatment and/or prophylaxis of an autoimmune disease.

IPC Classes  ?

  • C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids

89.

NOVEL BANK1 SPLICE VARIANT

      
Application Number EP2008065980
Publication Number 2009/068481
Status In Force
Filing Date 2008-11-21
Publication Date 2009-06-04
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Abderrahim, Hadi
  • Kozyrev, Sergei V.

Abstract

The present invention relates to a new splice variant of BANK1, the use of SNPs in BANK1 for diagnostics and the use of antagonists to modulate BANK1 and/or the BANK1 pathway.

IPC Classes  ?

  • C07K 14/47 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates from mammals
  • C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
  • C12N 15/52 - Genes encoding for enzymes or proenzymes

90.

LH LIQUID FORMULATIONS

      
Application Number EP2008064679
Publication Number 2009/056569
Status In Force
Filing Date 2008-10-29
Publication Date 2009-05-07
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Agostinetto, Rita
  • Samaritani, Fabrizio
  • Del Rio, Alessandra
  • Richard, Joel

Abstract

The invention relates to liquid pharmaceutical formulations of luteinizing hormone (LH) for single- or multi-dose administration.

IPC Classes  ?

  • A61K 9/08 - Solutions
  • A61K 38/24 - Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g. HCG; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]
  • A61P 5/06 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH

91.

METHOD FOR PURIFYING FC-FUSION PROTEINS

      
Application Number EP2008064208
Publication Number 2009/053358
Status In Force
Filing Date 2008-10-21
Publication Date 2009-04-30
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Delvaille, David
  • Ziegler, Thierry
  • Eon-Duval, Alex

Abstract

The invention relates to a method for the purification of Fc-fusion proteins via blue dye affinity chromatography, in particular for the reduction of the amount of free Fc-moieties in an Fc- fusion proteins preparation.

IPC Classes  ?

  • C07K 14/565 - IFN-beta
  • C07K 19/00 - Hybrid peptides
  • C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
  • C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes

92.

METHOD FOR PURIFYING AN FC-CONTAINING PROTEIN

      
Application Number EP2008064210
Publication Number 2009/053360
Status In Force
Filing Date 2008-10-21
Publication Date 2009-04-30
Owner MERCK SERONO S.A. (Switzerland)
Inventor Eon-Duval, Alex

Abstract

The invention relates to a method for the purification of an Fc-containing protein via blue dye affinity chromatography, in particular for the reduction of the amount of free Fc-moieties in an Fc-containing protein preparation.

IPC Classes  ?

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

93.

SINGLE IFN-BETA FUSED TO A MUTATED IGG FC FRAGMENT

      
Application Number EP2008064224
Publication Number 2009/053368
Status In Force
Filing Date 2008-10-21
Publication Date 2009-04-30
Owner
  • MERCK SERONO S.A. (Switzerland)
  • BOZZATO, Giuliano (Switzerland)
Inventor Bozzato, Gian Battista

Abstract

The invention relates to a protein comprising a single IFN-beta fused to a mutated IgG Fc domain containing two subunits, wherein the first subunit comprises a mutated IgG Fc arm not linked to a IFN-beta protein, and the second subunit comprises a mutated IgG Fc arm linked to a single IFN-beta protein, and wherein said mutated IgG Fc domain is an immunoglobulin gamma-1 Fc domain and wherein said Fc domain comprises at least five mutations.

IPC Classes  ?

94.

COMBINATIONS OF (1R, 2R, 3S, 4S) -N4- (3-AMINOCARBONYLBICYCLO [2. 2. 1] HEPT-5-ENE-2-YL) - 5-FLUORO-N2- [ ( 3 - METHYL-4- (4 -METHYLPIPERAZIN-1-YL] PHENYL-2, 4-PYRIMIDINEAMINE

      
Application Number EP2008063729
Publication Number 2009/050143
Status In Force
Filing Date 2008-10-13
Publication Date 2009-04-23
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Romanelli, Angela
  • Gianella-Borradori, Athos
  • Raymond, Eric
  • Serova, Maria
  • Faivre, Sandrine

Abstract

The invention relates to combinations of (1 R,2R,3S,4S)-N4-(3- aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[(3-nnethyl-4-(4- methylpiperazin-1 -yl)]phenyl-2,4-pyrimidinediamine and/or its physiologically acceptable salts and solvates, and other cancer therapeutics, and the use of such combinations for the treatment of cancer.

IPC Classes  ?

  • A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • 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

95.

3-arylamino pyridine derivatives

      
Application Number 11665651
Grant Number 07956191
Status In Force
Filing Date 2005-10-19
First Publication Date 2009-04-09
Grant Date 2011-06-07
Owner Merck Serono SA (Switzerland)
Inventor
  • Abel, Ulrich
  • Deppe, Holger
  • Feurer, Achim
  • Grädler, Ulrich
  • Otte, Kerstin
  • Sekul, Renate
  • Thiemann, Meinolf
  • Goutopoulos, Andreas
  • Schwarz, Matthias
  • Jiang, Xuliang

Abstract

The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

IPC Classes  ?

96.

OXADIAZOLE DERIVATIVES

      
Application Number EP2008063180
Publication Number 2009/043889
Status In Force
Filing Date 2008-10-01
Publication Date 2009-04-09
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Quattropani, Anna
  • Montagne, Cyril
  • Sauer, Wolfgang
  • Crosignani, Stefano
  • Bombrun, Agnes
  • Muzerelle, Mathilde
  • Dorbais, Jerome
  • Marin, Delphine
  • Gonzalez, Jérôme
  • Gerber, Patrick

Abstract

The invention relates to compounds of formula (I). The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • 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 413/10 - 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 linked by a carbon chain containing aromatic rings
  • A61K 31/4245 - Oxadiazoles
  • A61P 37/00 - Drugs for immunological or allergic disorders

97.

OXADIAZOLE DIARYL COMPOUNDS

      
Application Number EP2008063185
Publication Number 2009/043890
Status In Force
Filing Date 2008-10-01
Publication Date 2009-04-09
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Montagne, Cyril
  • Quattropani, Anna
  • Sauer, Wolfgang
  • Bombrun, Agnès

Abstract

The invention relates to compounds of formula (I): wherein R1, R2, Ra , Rb,Rc and W, have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

98.

Cladribine regimen for treating multiple sclerosis

      
Application Number 11722018
Grant Number 07713947
Status In Force
Filing Date 2005-12-20
First Publication Date 2009-03-26
Grant Date 2010-05-11
Owner Merck Serono S.A. (Switzerland)
Inventor
  • De Luca, Giampiero
  • Ythier, Arnaud
  • Munafo, Alain
  • Lopez-Bresnahan, Maria

Abstract

The present invention is related to the use of Cladribine for the preparation of a pharmaceutical formulation for the treatment of multiple sclerosis, especially relapsing-remitting multiple sclerosis or early secondary progressive multiple sclerosis, wherein the preparation is to be orally administered and wherein re-treatments are possible.

IPC Classes  ?

  • A61K 31/52 - Purines, e.g. adenine
  • 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
  • A61K 38/21 - Interferons
  • A61K 9/00 - Medicinal preparations characterised by special physical form

99.

TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS

      
Application Number EP2008060884
Publication Number 2009/027283
Status In Force
Filing Date 2008-08-20
Publication Date 2009-03-05
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Swinnen, Dominique
  • Jorand-Lebrun, Catherine
  • Grippi - Vallotton, Tania
  • Muzerelle, Mathilde
  • Royle, Amanda
  • Macritchie, Jacqueline
  • Hill, Richard
  • Shaw, Jeffrey P.

Abstract

The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatorydiseases, cardiovascular disceases and/or neurodegenerative diseases and a process for their preparation.

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]

100.

6-AMINO-PYRIMIDINE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH BIND TO THE SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR FOR THE TREATMENT OF MULTIPLE SCLEROSIS

      
Application Number EP2008059933
Publication Number 2009/019167
Status In Force
Filing Date 2008-07-29
Publication Date 2009-02-12
Owner MERCK SERONO S.A. (Switzerland)
Inventor
  • Bombrun, Agnes
  • Schwarz, Matthias
  • Crosignani, Stefano
  • Covini, David
  • Marin, Delphine

Abstract

The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

IPC Classes  ?

  • C07D 239/42 - One nitrogen atom
  • C07D 239/34 - One oxygen atom
  • A61K 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
  • A61P 29/02 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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