WO1999050255A3 - Disubstituted pyrazolines and triazolines as factor xa inhibitors - Google Patents

Disubstituted pyrazolines and triazolines as factor xa inhibitors Download PDF

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Publication number
WO1999050255A3
WO1999050255A3 PCT/US1999/006310 US9906310W WO9950255A3 WO 1999050255 A3 WO1999050255 A3 WO 1999050255A3 US 9906310 W US9906310 W US 9906310W WO 9950255 A3 WO9950255 A3 WO 9950255A3
Authority
WO
WIPO (PCT)
Prior art keywords
triazolines
inhibitors
factor
disubstituted pyrazolines
pyrazolines
Prior art date
Application number
PCT/US1999/006310
Other languages
French (fr)
Other versions
WO1999050255A2 (en
Inventor
Donald J P Pinto
Original Assignee
Du Pont Pharm 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 Du Pont Pharm Co filed Critical Du Pont Pharm Co
Priority to DE69920888T priority Critical patent/DE69920888T2/en
Priority to EP99912828A priority patent/EP1064270B1/en
Priority to AT99912828T priority patent/ATE278673T1/en
Priority to JP2000541159A priority patent/JP2002509924A/en
Priority to CA002321538A priority patent/CA2321538A1/en
Priority to AU31109/99A priority patent/AU3110999A/en
Publication of WO1999050255A2 publication Critical patent/WO1999050255A2/en
Publication of WO1999050255A3 publication Critical patent/WO1999050255A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Abstract

The present application describes disubstituted pyrazolines and triazolines of formulae (I) and (II), or pharmaceutically acceptable salt forms thereof, wherein one of M?1 and M2¿ may be N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.
PCT/US1999/006310 1998-03-27 1999-03-23 Disubstituted pyrazolines and triazolines as factor xa inhibitors WO1999050255A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
DE69920888T DE69920888T2 (en) 1998-03-27 1999-03-23 DISUBSTITUTED PYRAZOLINES AND TRIAZOLINES AS FACTOR XA INHIBITORS
EP99912828A EP1064270B1 (en) 1998-03-27 1999-03-23 Disubstituted pyrazolines and triazolines as factor xa inhibitors
AT99912828T ATE278673T1 (en) 1998-03-27 1999-03-23 DISUBSTITUTED PYRAZOLINES AND TRIAZOLINES AS FACTOR XA INHIBITORS
JP2000541159A JP2002509924A (en) 1998-03-27 1999-03-23 Disubstituted pyrazolines and triazolines as factor Xa inhibitors
CA002321538A CA2321538A1 (en) 1998-03-27 1999-03-23 Disubstituted pyrazolines and triazolines as factor xa inhibitors
AU31109/99A AU3110999A (en) 1998-03-27 1999-03-23 Disubstituted pyrazolines and triazolines as factor xa inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7972598P 1998-03-27 1998-03-27
US60/079,725 1998-03-27

Publications (2)

Publication Number Publication Date
WO1999050255A2 WO1999050255A2 (en) 1999-10-07
WO1999050255A3 true WO1999050255A3 (en) 1999-11-18

Family

ID=22152402

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/006310 WO1999050255A2 (en) 1998-03-27 1999-03-23 Disubstituted pyrazolines and triazolines as factor xa inhibitors

Country Status (9)

Country Link
US (3) US6191159B1 (en)
EP (1) EP1064270B1 (en)
JP (1) JP2002509924A (en)
AT (1) ATE278673T1 (en)
AU (1) AU3110999A (en)
CA (1) CA2321538A1 (en)
DE (1) DE69920888T2 (en)
ES (1) ES2230841T3 (en)
WO (1) WO1999050255A2 (en)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3110999A (en) * 1998-03-27 1999-10-18 Du Pont Pharmaceuticals Company Disubstituted pyrazolines and triazolines as factor xa inhibitors
US6858616B2 (en) 1998-12-23 2005-02-22 Bristol-Myers Squibb Pharma Company Nitrogen containing heterobicycles as factor Xa inhibitors
DK1140941T3 (en) 1998-12-23 2005-02-14 Bristol Myers Squibb Pharma Co Nitrogen-containing heterobicyclic compounds as factor Xa inhibitors
AU4307800A (en) * 1999-04-30 2000-11-17 Merab Lomia New indication for use of antiepileptic agents and medicines
US6329527B1 (en) 1999-10-21 2001-12-11 Bristol-Myers Squibb Pharma Company Synthesis of 1,3,5-trisubstituted pyrazoles
ATE373655T1 (en) * 2000-06-23 2007-10-15 Bristol Myers Squibb Pharma Co 1-(HETEROARYL-PHENYL)-CONDENSED PYRAZOLE DERIVATIVES AS FACTOR XA INHIBITORS
US6670362B2 (en) 2000-09-20 2003-12-30 Pfizer Inc. Pyridazine endothelin antagonists
US6982251B2 (en) * 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
US20060287254A1 (en) * 2001-01-26 2006-12-21 Schering Corporation Use of substituted azetidinone compounds for the treatment of sitosterolemia
RS51449B (en) * 2001-01-26 2011-04-30 Schering Corporation Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
US7053080B2 (en) * 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
PL204653B1 (en) 2001-09-21 2010-01-29 Bristol Myers Squibb Co Derivative of pyrazolo [3,4-c] pyridine, the use thereof and pharmaceutical composition
DE60216300T2 (en) * 2001-09-21 2007-06-28 Schering Corp. TREATMENT OF XANTHOM BY AZETIDINONE DERIVATIVES AS AN INHIBITOR OF STEROL ABSORPTION
TWI331526B (en) * 2001-09-21 2010-10-11 Bristol Myers Squibb Pharma Co Lactam-containing compounds and derivatives thereof as factor xa inhibitors
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
TW200302225A (en) 2001-12-04 2003-08-01 Bristol Myers Squibb Co Substituted amino methyl factor Xa inhibitors
EP1505966A4 (en) 2002-05-10 2006-08-30 Bristol Myers Squibb Co 1,1-disubstituted cycloalkyl derivatives as factor xa inhibitors
US20050256130A1 (en) * 2002-06-12 2005-11-17 Chemocentryx, Inc. Substituted piperazines
US7589199B2 (en) 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
CA2488202C (en) * 2002-06-12 2011-03-08 Chemocentryx, Inc. 1-aryl-4-substituted piperazine derivatives for use as ccr1 antagonists for the treatment of inflammation and immune disorders
US7842693B2 (en) * 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
AU2003302238A1 (en) 2002-12-03 2004-06-23 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
US7459442B2 (en) * 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
CN1756755A (en) * 2003-03-07 2006-04-05 先灵公司 Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
JP5137228B2 (en) * 2003-03-07 2013-02-06 メルク・シャープ・アンド・ドーム・コーポレーション Substituted azetidinone compounds, substituted azetidinone formulations and their use for the treatment of hypercholesterolemia
DE602004018617D1 (en) * 2003-03-07 2009-02-05 Schering Corp SUBSTITUTED AZETIDINONE DERIVATIVES, THEIR PHARMACEUTICAL FORMULATIONS AND THEIR USE FOR THE TREATMENT OF HYPERCHOLESTEROLMIA
US7122557B2 (en) 2003-03-18 2006-10-17 Bristol-Myers Squibb Company Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
US7235662B2 (en) * 2003-06-11 2007-06-26 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
US7435831B2 (en) * 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
EP1720545B1 (en) * 2004-03-03 2014-10-29 ChemoCentryx, Inc. Bicyclic and bridged nitrogen heterocycles
TWI349666B (en) 2004-03-12 2011-10-01 Lundbeck & Co As H Substituted morpholine and thiomorpholine derivatives
NZ571441A (en) * 2006-03-24 2010-08-27 Eisai R&D Man Co Ltd Triazolone derivative
CN101405275B (en) * 2006-03-24 2011-11-09 卫材R&D管理有限公司 Triazolone derivative
EP2202231A4 (en) 2007-09-21 2011-09-28 Eisai R&D Man Co Ltd 2,3-dihydroiminoisoindole derivative
RU2557908C1 (en) * 2014-07-04 2015-07-27 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Кубанский государственный аграрный университет" Method of incubation of chicken eggs
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof

Citations (10)

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Publication number Priority date Publication date Assignee Title
WO1995014682A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Isoxazoline compounds useful as fibrinogen receptor antagonists
WO1995014683A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Novel isoxazoline and isoxazole fibrinogen receptor antagonists
US5424334A (en) * 1991-12-19 1995-06-13 G. D. Searle & Co. Peptide mimetic compounds useful as platelet aggregation inhibitors
US5463071A (en) * 1991-07-27 1995-10-31 Dr. Karl Thomae Gmbh 5-membered heterocyclic compounds, processes for preparing them and pharmaceutical compositions containing these compounds
WO1997023212A1 (en) * 1995-12-21 1997-07-03 The Du Pont Merck Pharmaceutical Company ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS
WO1997030971A1 (en) * 1996-02-22 1997-08-28 The Du Pont Merck Pharmaceutical Company M-AMIDINO PHENYL ANALOGS AS FACTOR Xa INHIBITORS
WO1998028269A1 (en) * 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
WO1998057937A2 (en) * 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company Inhibitors of factor xa with a neutral p1 specificity group
WO1998057951A1 (en) * 1997-06-19 1998-12-23 Du Pont Pharmaceuticals Company NOVEL GUANIDINE MIMICS AS FACTOR Xa INHIBITORS
WO1998057934A1 (en) * 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company (AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS

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US5550147A (en) 1992-02-05 1996-08-27 Fujisawa Pharmaceutical Co., Ltd. Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
US5849736A (en) 1993-11-24 1998-12-15 The Dupont Merck Pharmaceutical Company Isoxazoline and isoxazole fibrinogen receptor antagonists
US5563158A (en) 1993-12-28 1996-10-08 The Dupont Merck Pharmaceutical Company Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
US5616601A (en) 1994-07-28 1997-04-01 Gd Searle & Co 1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation
WO1997047299A1 (en) * 1996-06-12 1997-12-18 3-Dimensional Pharmaceuticals, Inc. Amidino and guanidino heterocyclic protease inhibitors
AU3110999A (en) * 1998-03-27 1999-10-18 Du Pont Pharmaceuticals Company Disubstituted pyrazolines and triazolines as factor xa inhibitors

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5463071A (en) * 1991-07-27 1995-10-31 Dr. Karl Thomae Gmbh 5-membered heterocyclic compounds, processes for preparing them and pharmaceutical compositions containing these compounds
US5424334A (en) * 1991-12-19 1995-06-13 G. D. Searle & Co. Peptide mimetic compounds useful as platelet aggregation inhibitors
WO1995014682A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Isoxazoline compounds useful as fibrinogen receptor antagonists
WO1995014683A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Novel isoxazoline and isoxazole fibrinogen receptor antagonists
WO1997023212A1 (en) * 1995-12-21 1997-07-03 The Du Pont Merck Pharmaceutical Company ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS
WO1997030971A1 (en) * 1996-02-22 1997-08-28 The Du Pont Merck Pharmaceutical Company M-AMIDINO PHENYL ANALOGS AS FACTOR Xa INHIBITORS
WO1998028269A1 (en) * 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
WO1998057937A2 (en) * 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company Inhibitors of factor xa with a neutral p1 specificity group
WO1998057951A1 (en) * 1997-06-19 1998-12-23 Du Pont Pharmaceuticals Company NOVEL GUANIDINE MIMICS AS FACTOR Xa INHIBITORS
WO1998057934A1 (en) * 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company (AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS

Also Published As

Publication number Publication date
US6630468B2 (en) 2003-10-07
ATE278673T1 (en) 2004-10-15
EP1064270B1 (en) 2004-10-06
CA2321538A1 (en) 1999-10-07
EP1064270A2 (en) 2001-01-03
WO1999050255A2 (en) 1999-10-07
AU3110999A (en) 1999-10-18
US6191159B1 (en) 2001-02-20
DE69920888T2 (en) 2006-02-02
US20030105105A1 (en) 2003-06-05
JP2002509924A (en) 2002-04-02
US6436985B2 (en) 2002-08-20
DE69920888D1 (en) 2004-11-11
US20010000179A1 (en) 2001-04-05
ES2230841T3 (en) 2005-05-01

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