CA2122571A1 - Adhesion receptor antagonists - Google Patents

Adhesion receptor antagonists

Info

Publication number
CA2122571A1
CA2122571A1 CA002122571A CA2122571A CA2122571A1 CA 2122571 A1 CA2122571 A1 CA 2122571A1 CA 002122571 A CA002122571 A CA 002122571A CA 2122571 A CA2122571 A CA 2122571A CA 2122571 A1 CA2122571 A1 CA 2122571A1
Authority
CA
Canada
Prior art keywords
receptor antagonists
adhesion receptor
fibrinogen
formula
mations
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.)
Granted
Application number
CA002122571A
Other languages
French (fr)
Other versions
CA2122571C (en
Inventor
Peter Raddatz
Joachim Gante
Horst Juraszyk
Hanns Wurziger
Helmut Prucher
Sabine Bernotat-Danielowski
Guido Melzer
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 Patent GmbH
Original Assignee
Merck Patent GmbH
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 DE4405633A external-priority patent/DE4405633A1/en
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA2122571A1 publication Critical patent/CA2122571A1/en
Application granted granted Critical
Publication of CA2122571C publication Critical patent/CA2122571C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/06—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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Abstract

Novel compounds of the formula I
(see formula I) in which R1, X and Y have the meanings given in Patent Claim 1, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thromboses, stroke, cardiac infarction, inflam-mations, arteriosclerosis, osteoporosis and tumours.
CA002122571A 1993-05-01 1994-04-29 Adhesion receptor antagonists Expired - Fee Related CA2122571C (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE4314378 1993-05-01
DEP4314378.4 1993-05-01
DE4405633A DE4405633A1 (en) 1993-05-01 1994-02-22 Adhesion receptor antagonists
DEP4405633.8 1994-02-22

Publications (2)

Publication Number Publication Date
CA2122571A1 true CA2122571A1 (en) 1994-11-02
CA2122571C CA2122571C (en) 2005-04-12

Family

ID=25925455

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002122571A Expired - Fee Related CA2122571C (en) 1993-05-01 1994-04-29 Adhesion receptor antagonists

Country Status (16)

Country Link
US (1) US5532255A (en)
EP (1) EP0623615B1 (en)
JP (1) JP3570744B2 (en)
CN (1) CN1052231C (en)
AT (1) ATE181735T1 (en)
AU (1) AU675698B2 (en)
CA (1) CA2122571C (en)
CZ (1) CZ285761B6 (en)
DK (1) DK0623615T3 (en)
ES (1) ES2134870T3 (en)
GR (1) GR3031271T3 (en)
HU (1) HU224549B1 (en)
NO (1) NO301419B1 (en)
PL (1) PL178131B1 (en)
RU (1) RU2145961C1 (en)
SK (1) SK281469B6 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5627197A (en) * 1995-02-15 1997-05-06 Merck Patent Gesellschaft Mit Beschrankter Haftung Adhesion receptor antagonists
WO2000029407A1 (en) * 1998-11-18 2000-05-25 Du Pont Pharmaceuticals Company Isoxazoline fibrinogen receptor antagonists

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DE4332384A1 (en) * 1993-09-23 1995-03-30 Merck Patent Gmbh Adhesion receptor antagonists III
DE4429461A1 (en) * 1994-08-19 1996-02-22 Merck Patent Gmbh Adhesion receptor antagonists
DE19516483A1 (en) * 1995-05-05 1996-11-07 Merck Patent Gmbh Adhesion receptor antagonists
DE19524765A1 (en) * 1995-07-07 1997-01-09 Boehringer Mannheim Gmbh New oxazolidinone derivatives, processes for their preparation and medicaments containing these compounds
TR199801961T2 (en) * 1996-03-30 1999-01-18 Boehringer Mannheim Gmbh New oxalidine derivatives, processes for their production, and pharmaceuticals containing these compounds.
US5925635A (en) * 1996-04-17 1999-07-20 Dupont Pharmaceuticals Company N-(amidinophenyl) cyclourea analogs as factor XA inhibitors
US5877166A (en) * 1996-04-29 1999-03-02 Sri International Enantiomerically pure 2-aminopurine phosphonate nucleotide analogs as antiviral agents
DE19755268A1 (en) * 1997-12-12 1999-06-17 Merck Patent Gmbh Benzamidine derivatives
ID30299A (en) 1998-06-05 2001-11-22 Astrazeneca Ab OKSAZOLIDINON DERIVES, THE PROCESS OF MAKING IT AND THE PHARMACY COMPOSITION THAT CONTAINS IT
BR9912638A (en) * 1998-08-07 2001-05-02 Smithkline Beecham Corp Vitronectin receptor antagonists
DE19835950A1 (en) * 1998-08-08 2000-02-10 Merck Patent Gmbh Piperazinone derivatives
WO2000029406A2 (en) 1998-11-18 2000-05-25 Du Pont Pharmaceuticals Company Novel isoxazoline fibrinogen receptor antagonists
PL350291A1 (en) 1998-12-23 2002-12-02 Searle & Co Method of using a cyclooxygenase-2 inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
GB9928568D0 (en) 1999-12-03 2000-02-02 Zeneca Ltd Chemical compounds
DE19958153A1 (en) * 1999-12-03 2001-06-07 Yamanouchi Pharma Co Ltd Oxazolidinone derivatives
DE19962924A1 (en) 1999-12-24 2001-07-05 Bayer Ag Substituted oxazolidinones and their use
GB0009803D0 (en) * 2000-04-25 2000-06-07 Astrazeneca Ab Chemical compounds
DE10129725A1 (en) 2001-06-20 2003-01-02 Bayer Ag Combination therapy of substituted oxazolidinones
DE10152460A1 (en) * 2001-10-24 2003-05-08 Bayer Ag stents
RU2314831C2 (en) 2002-01-22 2008-01-20 Фармация Энд Апджон Компани Infection-proof medical devices
US7141588B2 (en) * 2002-02-25 2006-11-28 Pfizer, Inc. N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
DE10300111A1 (en) 2003-01-07 2004-07-15 Bayer Healthcare Ag Process for the preparation of 5-chloro-N - ({(5S) -2-oxo-3- [4- (3-oxo-4-morpholinyl) phenyl] -1,3-oxazolidin-5-yl} methyl ) -2-thiophenecarboxamide
DE10322469A1 (en) * 2003-05-19 2004-12-16 Bayer Healthcare Ag Heterocyclic compounds
JP4664634B2 (en) * 2003-09-05 2011-04-06 富山化学工業株式会社 Novel benzamidine derivatives or salts thereof
DE10355461A1 (en) 2003-11-27 2005-06-23 Bayer Healthcare Ag Solid, high bioavailabilty oral formulations of N-substituted 5-chloro-2-thiophene-carboxamide derivative in hydrophilized form, useful for combating thrombo-embolic diseases
US7842815B2 (en) * 2004-06-17 2010-11-30 Infinity Pharmaceuticals, Inc. Compounds and methods for inhibiting the interaction of BCL proteins with binding partners
JP2008512097A (en) * 2004-09-07 2008-04-24 アーケミックス コーポレイション Aptamer medicinal chemistry
US7566701B2 (en) * 2004-09-07 2009-07-28 Archemix Corp. Aptamers to von Willebrand Factor and their use as thrombotic disease therapeutics
EP1789096A4 (en) 2004-09-07 2009-07-08 Archemix Corp Aptamers to von willebrand factor and their use as thrombotic disease therapeutics
DE102004062475A1 (en) * 2004-12-24 2006-07-06 Bayer Healthcare Ag Solid, orally administrable, modified release pharmaceutical dosage forms
EP1685841A1 (en) 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention and treatment of thromboembolic disorders
DE102005045518A1 (en) 2005-09-23 2007-03-29 Bayer Healthcare Ag New 5-thienylaminocarbonylmethyl-oxazolidin-2-one derivatives, useful for treating and preventing thromboembolic disease, are selective inhibitors of coagulation factor Xa
US8188270B2 (en) 2005-10-04 2012-05-29 Bayer Schering Pharma Aktiengesellschaft Polymorphous form of 5-chloro-N-({(5S)-2-oxo-3[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide
DE102005047561A1 (en) 2005-10-04 2007-04-05 Bayer Healthcare Ag Drug delivery system, useful to treat and/or prevent e.g. thromboembolic disease, comprises 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxo-4-morpholinyl)-phenyl)-1,3-oxazolidine-5-yl)-methyl)-2-thiophene carboxamide with fast release active substance
DE102005047558A1 (en) * 2005-10-04 2008-02-07 Bayer Healthcare Ag Combination therapy of substituted oxazolidinones for the prophylaxis and treatment of cerebral circulatory disorders
DE102005048824A1 (en) * 2005-10-10 2007-04-12 Bayer Healthcare Ag Treatment and prophylaxis of microangiopathies
DE102006051625A1 (en) * 2006-11-02 2008-05-08 Bayer Materialscience Ag Combination therapy of substituted oxazolidinones
DE102007018662A1 (en) * 2007-04-20 2008-10-23 Bayer Healthcare Ag Oxazolidinone for the treatment and prophylaxis of pulmonary hypertension
WO2008150495A2 (en) * 2007-06-01 2008-12-11 Archemix Corp. Vwf aptamer formulations and methods for use
DE102007028318A1 (en) 2007-06-20 2008-12-24 Bayer Healthcare Ag Oxazolidinone for the treatment and prophylaxis of sepsis
NZ586002A (en) * 2007-12-11 2012-06-29 Bayer Schering Pharma Ag Oxazolidinones for the treatment and/or prophylaxis of heart failure
EP2138178A1 (en) 2008-06-28 2009-12-30 Bayer Schering Pharma Aktiengesellschaft Oxazolidninones for the treatment fo chronic obstructive pulmonary disease (COPD) and/or asthma
EP2140866A1 (en) 2008-07-04 2010-01-06 Bayer Schering Pharma Aktiengesellschaft Oxazolidinones for the treatment of inflammatory conditions of the gastrointestinal tract
TWI759267B (en) 2015-07-02 2022-04-01 美商地平線罕見醫學製藥有限責任公司 Ado-resistant cysteamine analogs and uses thereof
CN110573499B (en) 2017-02-28 2023-04-21 莫菲克医疗股份有限公司 Inhibitors of αvβ6 integrin
CA3054792A1 (en) 2017-02-28 2018-09-07 Morphic Therapeutic, Inc. Inhibitors of .alpha.v.beta.6 integrin
PE20211640A1 (en) 2018-08-29 2021-08-24 Morphic Therapeutic Inc INHIBITION OF INTEGRIN xvß6
WO2023172726A1 (en) * 2022-03-10 2023-09-14 Baruch S. Blumberg Institute Novel diazepines that target yellow fever virus non-structural 4b (ns4b) protein and their method of use

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5627197A (en) * 1995-02-15 1997-05-06 Merck Patent Gesellschaft Mit Beschrankter Haftung Adhesion receptor antagonists
WO2000029407A1 (en) * 1998-11-18 2000-05-25 Du Pont Pharmaceuticals Company Isoxazoline fibrinogen receptor antagonists

Also Published As

Publication number Publication date
AU6064394A (en) 1994-11-03
HU9401274D0 (en) 1994-08-29
EP0623615B1 (en) 1999-06-30
NO941592D0 (en) 1994-04-29
JP3570744B2 (en) 2004-09-29
RU2145961C1 (en) 2000-02-27
CN1097421A (en) 1995-01-18
US5532255A (en) 1996-07-02
EP0623615A1 (en) 1994-11-09
CZ285761B6 (en) 1999-11-17
SK281469B6 (en) 2001-04-09
ATE181735T1 (en) 1999-07-15
HUT70541A (en) 1995-10-30
PL178131B1 (en) 2000-03-31
CA2122571C (en) 2005-04-12
JPH072847A (en) 1995-01-06
GR3031271T3 (en) 1999-12-31
DK0623615T3 (en) 1999-12-13
SK48494A3 (en) 1995-02-08
HU224549B1 (en) 2005-10-28
AU675698B2 (en) 1997-02-13
NO941592L (en) 1994-11-02
CZ101994A3 (en) 1994-11-16
ES2134870T3 (en) 1999-10-16
CN1052231C (en) 2000-05-10
NO301419B1 (en) 1997-10-27

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Legal Events

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EEER Examination request
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