WO1998028282A3 - OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS - Google Patents

OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS Download PDF

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Publication number
WO1998028282A3
WO1998028282A3 PCT/US1997/023470 US9723470W WO9828282A3 WO 1998028282 A3 WO1998028282 A3 WO 1998028282A3 US 9723470 W US9723470 W US 9723470W WO 9828282 A3 WO9828282 A3 WO 9828282A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
factor
oxygen
sulfur containing
membered heteroaromatics
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.)
Ceased
Application number
PCT/US1997/023470
Other languages
French (fr)
Other versions
WO1998028282A2 (en
Inventor
James Russell Pruitt
John Matthew Fevig
Mimi Lifen Quan
Donald Joseph Phillip Pinto
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.)
Bristol Myers Squibb Pharma Co
Original Assignee
DuPont Merck Pharmaceutical Co
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
Application filed by DuPont Merck Pharmaceutical Co filed Critical DuPont Merck Pharmaceutical Co
Priority to AT97954988T priority Critical patent/ATE236890T1/en
Priority to JP52896298A priority patent/JP2001506271A/en
Priority to DE69720773T priority patent/DE69720773T2/en
Priority to EP97954988A priority patent/EP0946528B1/en
Priority to AU66459/98A priority patent/AU6645998A/en
Priority to CA002276034A priority patent/CA2276034A1/en
Publication of WO1998028282A2 publication Critical patent/WO1998028282A2/en
Publication of WO1998028282A3 publication Critical patent/WO1998028282A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • C07D263/30—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
    • C07D263/34—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 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
    • 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
    • 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
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—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
    • C07D277/32—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 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D413/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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 C07D415/00
    • C07D417/02—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 C07D415/00 containing two hetero rings
    • C07D417/12—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 C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Catalysts (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Furan Compounds (AREA)

Abstract

The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula (I), or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
PCT/US1997/023470 1996-12-23 1997-12-18 OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS Ceased WO1998028282A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
AT97954988T ATE236890T1 (en) 1996-12-23 1997-12-18 OXYGEN OR SULFUR CONTAINING 5-MEMBED HETEROAROMATIC DERIVATIVES AS FACTOR XA INHIBITORS
JP52896298A JP2001506271A (en) 1996-12-23 1997-12-18 Heterocyclic aromatic compounds containing oxygen or sulfur as factor Xa inhibitors
DE69720773T DE69720773T2 (en) 1996-12-23 1997-12-18 OXYGEN OR SULFUR CONTAINING 5-PIECE HETEROAROMATIS DERIVATIVE AS FACTOR Xa HEMMER
EP97954988A EP0946528B1 (en) 1996-12-23 1997-12-18 OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
AU66459/98A AU6645998A (en) 1996-12-23 1997-12-18 Oxygen or sulfur containing heteroaromatics as factor xa inhibitors
CA002276034A CA2276034A1 (en) 1996-12-23 1997-12-18 Oxygen or sulfur containing 5-membered heteroaromatics as factor xa inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US77181496A 1996-12-23 1996-12-23
US08/771,814 1996-12-23
US87976397A 1997-06-20 1997-06-20
US08/879,763 1997-06-20

Publications (2)

Publication Number Publication Date
WO1998028282A2 WO1998028282A2 (en) 1998-07-02
WO1998028282A3 true WO1998028282A3 (en) 1998-09-17

Family

ID=27118522

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/023470 Ceased WO1998028282A2 (en) 1996-12-23 1997-12-18 OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS

Country Status (8)

Country Link
EP (1) EP0946528B1 (en)
JP (1) JP2001506271A (en)
AT (1) ATE236890T1 (en)
AU (1) AU6645998A (en)
CA (1) CA2276034A1 (en)
DE (1) DE69720773T2 (en)
ES (1) ES2196396T3 (en)
WO (1) WO1998028282A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7528143B2 (en) 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US9149527B2 (en) 2010-06-07 2015-10-06 Novomedix, Llc Furanyl compounds and the use thereof

Families Citing this family (76)

* Cited by examiner, † Cited by third party
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WO1998057934A1 (en) * 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company (AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS
WO2000038683A1 (en) * 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
CA2361428A1 (en) 1999-02-11 2000-08-17 Cor Therapeutics, Inc. Inhibitors of factor xa
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
PL215901B1 (en) * 1999-04-15 2014-02-28 Bristol Myers Squibb Co Cyclic protein tyrosine kinase inhibitors
EP1185509A2 (en) * 1999-05-24 2002-03-13 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
JP2004507439A (en) 1999-07-16 2004-03-11 ブリストル−マイヤーズ　スクイブ　ファーマ　カンパニー Nitrogen-containing heterobicyclic compounds as factor Xa inhibitors
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
DE60040676D1 (en) * 1999-09-17 2008-12-11 Millennium Pharm Inc BENZAMIDES AND SIMILAR INHIBITORS OF FACTOR Xa
JP2003509412A (en) * 1999-09-17 2003-03-11 シーオーアール セラピューティクス インコーポレイテッド Factor Xa inhibitor
DE10008329A1 (en) * 2000-02-23 2001-08-30 Merck Patent Gmbh New aminosulfonyl-biphenyl derivatives are Factor Xa and Factor VIIa inhibitors useful e.g. for treating thrombosis, myocardial infarction, arteriosclerosis, inflammation or angina pectoris
AU2001250783A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
DE10027025A1 (en) * 2000-05-31 2001-12-06 Merck Patent Gmbh Clycinamides
EP1296982B1 (en) 2000-06-23 2007-09-19 Bristol-Myers Squibb Pharma Company 1-(heteroaryl-phenyl)-condensed pyrazol derivatives as factor xa inhibitors
AU2001268711A1 (en) 2000-06-23 2002-01-08 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
CA2429426A1 (en) 2000-11-17 2002-05-23 Takeda Chemical Industries, Ltd. Isoxazole derivatives
MXPA03009378A (en) 2001-04-13 2004-01-29 Vertex Pharma Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases.
TWI331526B (en) 2001-09-21 2010-10-11 Bristol Myers Squibb Pharma Co Lactam-containing compounds and derivatives thereof as factor xa inhibitors
CA2461202C (en) 2001-09-21 2011-07-12 Donald Pinto Lactam-containing compounds and derivatives thereof as factor xa inhibitors
WO2003093242A2 (en) * 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
AU2002350217A1 (en) * 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
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US7312214B2 (en) 2002-05-10 2007-12-25 Bristol-Myers Squibb Company 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
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US6933308B2 (en) 2002-12-20 2005-08-23 Bristol-Myers Squibb Company Aminoalkyl thiazole derivatives as KCNQ modulators
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US7122557B2 (en) 2003-03-18 2006-10-17 Bristol-Myers Squibb Company Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
CN1826121B (en) * 2003-07-23 2013-05-29 幸讬制药公司 Application of Phenyl and Pyridyl Derivatives in Preparation of Drugs for Regulating Calcium Ion Release and Activating Calcium Channels
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Citations (5)

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WO1996038426A1 (en) * 1995-05-31 1996-12-05 The Du Pont Merck Pharmaceutical Company Novel isoxazoline and isoxazole fibrinogen receptor antagonists
US5668159A (en) * 1996-05-08 1997-09-16 The Dupont Merck Pharmaceutical Company 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists

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Patent Citations (5)

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Publication number Priority date Publication date Assignee Title
EP0513387A1 (en) * 1990-11-30 1992-11-19 Otsuka Pharmaceutical Co., Ltd. Active oxygen inhibitor
US5317103A (en) * 1991-01-15 1994-05-31 Merck Sharp & Dohme Limited Indole-substituted five-membered heteroaromatic compounds as 5-HT1 agonists
WO1995018111A1 (en) * 1993-12-28 1995-07-06 The Du Pont Merck Pharmaceutical Company Compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
WO1996038426A1 (en) * 1995-05-31 1996-12-05 The Du Pont Merck Pharmaceutical Company Novel isoxazoline and isoxazole fibrinogen receptor antagonists
US5668159A (en) * 1996-05-08 1997-09-16 The Dupont Merck Pharmaceutical Company 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7528143B2 (en) 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US9149527B2 (en) 2010-06-07 2015-10-06 Novomedix, Llc Furanyl compounds and the use thereof

Also Published As

Publication number Publication date
ATE236890T1 (en) 2003-04-15
AU6645998A (en) 1998-07-17
EP0946528A2 (en) 1999-10-06
WO1998028282A2 (en) 1998-07-02
EP0946528B1 (en) 2003-04-09
DE69720773D1 (en) 2003-05-15
JP2001506271A (en) 2001-05-15
DE69720773T2 (en) 2004-01-29
ES2196396T3 (en) 2003-12-16
CA2276034A1 (en) 1998-07-02

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