EP0946164A4 - Integrin antagonists - Google Patents

Integrin antagonists

Info

Publication number
EP0946164A4
EP0946164A4 EP97913775A EP97913775A EP0946164A4 EP 0946164 A4 EP0946164 A4 EP 0946164A4 EP 97913775 A EP97913775 A EP 97913775A EP 97913775 A EP97913775 A EP 97913775A EP 0946164 A4 EP0946164 A4 EP 0946164A4
Authority
EP
European Patent Office
Prior art keywords
integrin antagonists
integrin
antagonists
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP97913775A
Other languages
German (de)
French (fr)
Other versions
EP0946164A1 (en
Inventor
Mark E Duggan
George D Hartman
William F Hoffman
Nathan C Ihle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9626308.2A external-priority patent/GB9626308D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0946164A1 publication Critical patent/EP0946164A1/en
Publication of EP0946164A4 publication Critical patent/EP0946164A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic 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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/73Unsubstituted amino or imino radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic 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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12Nitrogen atoms not forming part of a nitro radical
    • C07D239/14Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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 C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic 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 C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
EP97913775A 1996-10-30 1997-10-27 Integrin antagonists Withdrawn EP0946164A4 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US2922396P 1996-10-30 1996-10-30
US29223P 1996-10-30
GBGB9626308.2A GB9626308D0 (en) 1996-12-18 1996-12-18 av›3 antagonists
GB9626308 1996-12-18
PCT/US1997/019349 WO1998018461A1 (en) 1996-10-30 1997-10-27 Integrin antagonists

Publications (2)

Publication Number Publication Date
EP0946164A1 EP0946164A1 (en) 1999-10-06
EP0946164A4 true EP0946164A4 (en) 2000-08-23

Family

ID=26310673

Family Applications (1)

Application Number Title Priority Date Filing Date
EP97913775A Withdrawn EP0946164A4 (en) 1996-10-30 1997-10-27 Integrin antagonists

Country Status (4)

Country Link
EP (1) EP0946164A4 (en)
JP (1) JP2001504456A (en)
AU (1) AU717283B2 (en)
WO (1) WO1998018461A1 (en)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6017926A (en) * 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
US6048861A (en) 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6066648A (en) * 1997-12-17 2000-05-23 Merck & Co., Inc. Integrin receptor antagonists
US6211191B1 (en) 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists
NZ509797A (en) * 1998-07-10 2003-11-28 Univ Sydney Prophylactic treatments of neovascularisation in macular degeneration using a steroid
AU747784B2 (en) * 1998-07-29 2002-05-23 Merck & Co., Inc. Integrin receptor antagonists
EP1105389A4 (en) * 1998-08-13 2001-10-17 Merck & Co Inc Integrin receptor antagonists
FR2786182B1 (en) * 1998-11-24 2001-01-12 Hoechst Marion Roussel Inc NOVEL ACYLGUANIDINES DERIVATIVES, PROCESS FOR THEIR PREPARATION, THEIR USE AS MEDICAMENTS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
US6677360B2 (en) 1998-12-16 2004-01-13 Bayer Aktiengesellschaft Biphenyl and biphenyl-analogous compounds as integrin antagonists
US6291503B1 (en) 1999-01-15 2001-09-18 Bayer Aktiengesellschaft β-phenylalanine derivatives as integrin antagonists
CZ20013678A3 (en) * 1999-04-13 2002-07-17 Basf Aktiengesellschaft Ligands of integrin receptor
DZ3263A1 (en) 1999-06-02 2000-12-07 Merck & Co Inc ALPHA V INTEGRIN RECEPTOR ANTAGONISTS
WO2000075129A1 (en) * 1999-06-07 2000-12-14 Shire Biochem Inc. Thiophene integrin inhibitors
EP1065208A1 (en) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Substituted purine derivatives as inhibitors of cell adhesion
EP1065207A1 (en) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Naphthyridine derivatives, processes for their preparation, their use, and pharmaceutical compositions comprising them
DE19939981A1 (en) * 1999-08-24 2001-03-01 Merck Patent Gmbh New inhibitors of the integrin alphavß3
US6514964B1 (en) 1999-09-27 2003-02-04 Amgen Inc. Fused cycloheptane and fused azacycloheptane compounds and their methods of use
EP1229910A4 (en) * 1999-10-04 2003-10-01 Merck & Co Inc Integrin receptor antagonists
DE10039998A1 (en) * 2000-08-11 2002-02-21 Basf Ag New substituted diareno-azepine derivatives as integrin ligands
WO2001027082A1 (en) * 1999-10-08 2001-04-19 Meiji Seika Kaisha, Ltd. 3-AMINOPIPERIDINE DERIVATIVES AS INTEGRIN αvβ3 ANTAGONISTS
US6849639B2 (en) 1999-12-14 2005-02-01 Amgen Inc. Integrin inhibitors and their methods of use
EP1252162B1 (en) * 2000-01-20 2012-07-25 Merck Sharp & Dohme Corp. Alpha v integrin receptor antagonists
US6545029B2 (en) 2000-06-12 2003-04-08 Bayer Aktiengesellschaft Phenylserine derivatives as integrin antagonists
ES2376161T3 (en) * 2001-01-29 2012-03-09 Janssen Pharmaceuticals, Inc. SUBSTITUTE INDOLES AND THEIR USE AS AN INTEGRINE ANTAGONISTS.
DK1371646T3 (en) 2001-03-19 2010-07-05 Dainippon Sumitomo Pharma Co Aryl-substituted alicyclic compound and medical composition comprising the same
RU2316337C2 (en) 2001-04-24 2008-02-10 Мерк Патент Гмбх Combined therapy by using antiangiogenic agents and tnf-alpha
GB0112834D0 (en) 2001-05-25 2001-07-18 Smithkline Beecham Plc Medicaments
US7115596B2 (en) 2002-12-20 2006-10-03 Pharmacia Corporation Thiazole compounds as integrin receptor antagonists derivatives
ES2521679T3 (en) 2006-01-18 2014-11-13 Merck Patent Gmbh Specific therapy using integrin ligands for cancer treatment
MX2009007597A (en) 2007-01-18 2009-07-22 Merck Patent Gmbh Specific therapy and medicament using integrin ligands for treating cancer.
EA201101651A1 (en) 2009-05-25 2012-08-30 Мерк Патент Гмбх CONTINUOUS INTRODUCTION OF INTEGRINE LIGANDS FOR CANCER TREATMENT
PL3929196T3 (en) 2013-09-24 2023-12-11 Fujifilm Corporation Pharmaceutical composition of a nitrogen-containing compound or salt thereof, or metal complex thereof
DK3054936T5 (en) 2013-10-10 2024-03-18 Eastern Virginia Medical School 4-((2-HYDROXY-3-METHOXYBENZYL)AMINO) BENZENESULFONAMIDE DERIVATIVES AS 12-LIPOXYGENASE INHIBITORS
CN106572997A (en) 2014-05-30 2017-04-19 辉瑞公司 Carbonitrile derivatives as selective androgen receptor modulators
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998025892A1 (en) * 1996-12-09 1998-06-18 Eli Lilly And Company Integrin antagonists
WO1998044797A1 (en) * 1997-04-07 1998-10-15 Merck & Co., Inc. A method of treating cancer

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5416099A (en) * 1991-10-29 1995-05-16 Merck & Co., Inc. Fibrinogen receptor antagonists
EP0760658B1 (en) * 1994-05-27 2002-11-13 Merck & Co. Inc. Compounds for inhibiting osteoclast-mediated bone resorption

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998025892A1 (en) * 1996-12-09 1998-06-18 Eli Lilly And Company Integrin antagonists
WO1998044797A1 (en) * 1997-04-07 1998-10-15 Merck & Co., Inc. A method of treating cancer

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
EGBERTSON M S ET AL: "Nonpeptide GPIIB/IIIA inhibitors. 10. centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,GB,OXFORD, vol. 6, no. 21, 5 November 1996 (1996-11-05), pages 2519 - 2524, XP004135906, ISSN: 0960-894X *
See also references of WO9818461A1 *

Also Published As

Publication number Publication date
JP2001504456A (en) 2001-04-03
WO1998018461A1 (en) 1998-05-07
EP0946164A1 (en) 1999-10-06
AU5088498A (en) 1998-05-22
AU717283B2 (en) 2000-03-23

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