WO2000071516A3 - INHIBITORS OF FACTOR Xa - Google Patents

INHIBITORS OF FACTOR Xa Download PDF

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Publication number
WO2000071516A3
WO2000071516A3 PCT/US2000/014209 US0014209W WO0071516A3 WO 2000071516 A3 WO2000071516 A3 WO 2000071516A3 US 0014209 W US0014209 W US 0014209W WO 0071516 A3 WO0071516 A3 WO 0071516A3
Authority
WO
WIPO (PCT)
Prior art keywords
factor
inhibitors
compounds
formula
vitro
Prior art date
Application number
PCT/US2000/014209
Other languages
French (fr)
Other versions
WO2000071516A2 (en
WO2000071516B1 (en
Inventor
Bing-Yan Zhu
Robert M Scarborough
Lingyan Wang
Original Assignee
Cor Therapeutics 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
Application filed by Cor Therapeutics Inc filed Critical Cor Therapeutics Inc
Priority to CA002371904A priority Critical patent/CA2371904A1/en
Priority to EP00937704A priority patent/EP1185512A2/en
Priority to JP2000619773A priority patent/JP2003500391A/en
Priority to AU52840/00A priority patent/AU5284000A/en
Publication of WO2000071516A2 publication Critical patent/WO2000071516A2/en
Publication of WO2000071516A3 publication Critical patent/WO2000071516A3/en
Publication of WO2000071516B1 publication Critical patent/WO2000071516B1/en

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    • 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
    • C07D401/04—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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—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 no 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/04—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

Abstract

Compounds, e.g. described in claim 5, formula (I) and formula (II), where A-B is (1), their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
PCT/US2000/014209 1999-05-24 2000-05-24 INHIBITORS OF FACTOR Xa WO2000071516A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CA002371904A CA2371904A1 (en) 1999-05-24 2000-05-24 Inhibitors of factor xa
EP00937704A EP1185512A2 (en) 1999-05-24 2000-05-24 INHIBITORS OF FACTOR Xa
JP2000619773A JP2003500391A (en) 1999-05-24 2000-05-24 Factor Xa inhibitor
AU52840/00A AU5284000A (en) 1999-05-24 2000-05-24 Inhibitors of factor xa

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13583899P 1999-05-24 1999-05-24
US60/135,838 1999-05-24

Publications (3)

Publication Number Publication Date
WO2000071516A2 WO2000071516A2 (en) 2000-11-30
WO2000071516A3 true WO2000071516A3 (en) 2001-01-18
WO2000071516B1 WO2000071516B1 (en) 2001-03-01

Family

ID=22469944

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2000/014193 WO2000071515A2 (en) 1999-05-24 2000-05-24 INHIBITORS OF FACTOR Xa
PCT/US2000/014209 WO2000071516A2 (en) 1999-05-24 2000-05-24 INHIBITORS OF FACTOR Xa

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/US2000/014193 WO2000071515A2 (en) 1999-05-24 2000-05-24 INHIBITORS OF FACTOR Xa

Country Status (5)

Country Link
EP (2) EP1185512A2 (en)
JP (2) JP2003500390A (en)
AU (2) AU5284000A (en)
CA (2) CA2374788A1 (en)
WO (2) WO2000071515A2 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1302292A (en) 1998-03-19 2001-07-04 味之素株式会社 Aminoisoquinoline derivatives
TWI290136B (en) 2000-04-05 2007-11-21 Daiichi Seiyaku Co Ethylenediamine derivatives
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
DE10139060A1 (en) 2001-08-08 2003-02-20 Merck Patent Gmbh New bicyclic benzene derivatives useful as factor Xa and VIIa inhibitors, e.g. for treating thrombosis, myocardial infarct, arteriosclerosis, inflammation, stroke, angina, restenosis and tumors
CA2476067C (en) 2002-03-13 2011-09-20 Janssen Pharmaceutica N.V. Carbonylamino-derivatives as novel inhibitors of histone deacetylase
PL212089B1 (en) 2002-03-13 2012-08-31 Janssen Pharmaceutica Nv New inhibitors of histone deacetylase
WO2003076438A1 (en) 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase
AR039156A1 (en) 2002-03-28 2005-02-09 Novartis Ag AMIDAS OF SULFAMIC PIPERIDINYLAMINE ACID OR SULFAMIC PIPERAZINIL AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT IN DISEASES MEDIATED BY THE ACTION OF STEROID SULFATASE
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
KR20050118708A (en) 2003-04-03 2005-12-19 메르크 파텐트 게엠베하 Pyrrolidino-1,2-dicarboxy-1-(phenylamide)-2-(4-(3-oxo-morpholino-4-yl)-phenylamide) derivatives and related compounds for use as inhibitors of coagulation factor xa in the treatment of thrombo-embolic diseases
PL1651612T3 (en) 2003-07-22 2012-09-28 Astex Therapeutics Ltd 3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
DE102004014945A1 (en) * 2004-03-26 2005-10-13 Merck Patent Gmbh Prolinylderivate
WO2006010750A1 (en) 2004-07-28 2006-02-02 Janssen Pharmaceutica N.V. Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (en) 2005-01-21 2007-06-27 Astex Therapeutics Ltd PIPERIDIN ADDITION SALTS 4-IL-ACID AMID 4- (2,6-DICLORO-BENZOILAMINO) 1H-PIRAZOL-3-CARBOXILICO.
EP1979326B1 (en) 2006-01-19 2012-10-03 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
US11014920B2 (en) 2016-11-18 2021-05-25 Merck Sharp & Dohme Corp. Factor XIIa inhibitors
TW202122082A (en) 2019-08-12 2021-06-16 美商迪賽孚爾製藥有限公司 Methods of treating gastrointestinal stromal tumors
MX2022001863A (en) 2019-08-12 2022-05-30 Deciphera Pharmaceuticals Llc Ripretinib for treating gastrointestinal stromal tumors.
LT4084778T (en) 2019-12-30 2024-01-25 Deciphera Pharmaceuticals, Llc Amorphous kinase inhibitor formulations and methods of use thereof
IL293864A (en) 2019-12-30 2022-08-01 Deciphera Pharmaceuticals Llc Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998006694A1 (en) * 1996-08-16 1998-02-19 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
WO1998028269A1 (en) * 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998006694A1 (en) * 1996-08-16 1998-02-19 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
WO1998028269A1 (en) * 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WALLIS R B: "INHIBITORS OF COAGULATION FACTOR XA: FROM MACROMOLECULAR BEGINNINGS TO SMALL MOLECULES", CURRENT OPINION IN THERAPEUTIC PATENTS,, 1 August 1993 (1993-08-01), pages 1173 - 1179, XP000653726, ISSN: 0962-2594 *

Also Published As

Publication number Publication date
WO2000071516A2 (en) 2000-11-30
JP2003500391A (en) 2003-01-07
AU5284000A (en) 2000-12-12
EP1185512A2 (en) 2002-03-13
AU5283600A (en) 2000-12-12
EP1185511A2 (en) 2002-03-13
WO2000071516B1 (en) 2001-03-01
JP2003500390A (en) 2003-01-07
WO2000071515A2 (en) 2000-11-30
CA2374788A1 (en) 2000-11-30
CA2371904A1 (en) 2000-11-30
WO2000071515A3 (en) 2001-01-25

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