WO2000071515A3 - INHIBITEURS DU FACTEUR Xa - Google Patents

INHIBITEURS DU FACTEUR Xa Download PDF

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Publication number
WO2000071515A3
WO2000071515A3 PCT/US2000/014193 US0014193W WO0071515A3 WO 2000071515 A3 WO2000071515 A3 WO 2000071515A3 US 0014193 W US0014193 W US 0014193W WO 0071515 A3 WO0071515 A3 WO 0071515A3
Authority
WO
WIPO (PCT)
Prior art keywords
factor
inhibitors
compounds
vitro
vivo
Prior art date
Application number
PCT/US2000/014193
Other languages
English (en)
Other versions
WO2000071515A2 (fr
Inventor
Bing-Yan Zhu
Robert M Scarborough
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
Priority to US09/576,635 priority Critical patent/US6673817B1/en
Application filed by Cor Therapeutics Inc filed Critical Cor Therapeutics Inc
Priority to AU52836/00A priority patent/AU5283600A/en
Priority to CA002374788A priority patent/CA2374788A1/fr
Priority to EP00937698A priority patent/EP1185511A2/fr
Priority to JP2000619772A priority patent/JP2003500390A/ja
Publication of WO2000071515A2 publication Critical patent/WO2000071515A2/fr
Publication of WO2000071515A3 publication Critical patent/WO2000071515A3/fr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45Sulfonamides, 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
    • C07C311/46Y being a hydrogen or a carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

L'invention concerne des nouveaux composés, leurs sels et les compositions associées, actifs contre le facteur Xa mammalien. Ces composés sont utilisés in vitro ou in vivo pour prévenir ou traiter les troubles de la coagulation.
PCT/US2000/014193 1999-05-24 2000-05-24 INHIBITEURS DU FACTEUR Xa WO2000071515A2 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US09/576,635 US6673817B1 (en) 1999-05-24 2000-05-20 Inhibitors of factor Xa
AU52836/00A AU5283600A (en) 1999-05-24 2000-05-24 Inhibitors of factor xa
CA002374788A CA2374788A1 (fr) 1999-05-24 2000-05-24 Inhibiteurs du facteur xa
EP00937698A EP1185511A2 (fr) 1999-05-24 2000-05-24 INHIBITEURS DU FACTEUR Xa
JP2000619772A JP2003500390A (ja) 1999-05-24 2000-05-24 Xa因子阻害剤

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 (2)

Publication Number Publication Date
WO2000071515A2 WO2000071515A2 (fr) 2000-11-30
WO2000071515A3 true WO2000071515A3 (fr) 2001-01-25

Family

ID=22469944

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2000/014193 WO2000071515A2 (fr) 1999-05-24 2000-05-24 INHIBITEURS DU FACTEUR Xa
PCT/US2000/014209 WO2000071516A2 (fr) 1999-05-24 2000-05-24 INHIBITEURS DU FACTEUR Xa

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2000/014209 WO2000071516A2 (fr) 1999-05-24 2000-05-24 INHIBITEURS DU FACTEUR Xa

Country Status (5)

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

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999047503A1 (fr) 1998-03-19 1999-09-23 Ajinomoto Co., Inc. Derives d'aminoisoquinoleine
TWI288745B (en) 2000-04-05 2007-10-21 Daiichi Seiyaku Co Ethylenediamine derivatives
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
DE10139060A1 (de) 2001-08-08 2003-02-20 Merck Patent Gmbh Phenylderivate
BR0307606A (pt) 2002-03-13 2004-12-21 Janssen Pharmaceutica Nv Derivados de piperazinila, piperidinila e morfolinila como inibidores de histona desacetilase
AU2003212335B8 (en) 2002-03-13 2009-04-23 Janssen Pharmaceutica N.V. Aminocarbonyl-derivatives as novel inhibitors of histone deacetylase
NZ534831A (en) 2002-03-13 2007-01-26 Janssen Pharmaceutica Nv Carbonylamino-derivatives having histone deacetylase (HDAC) inhibiting enzymatic activity
PE20040167A1 (es) 2002-03-28 2004-05-26 Novartis Ag Amidas del acido sulfamico
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
MXPA05010444A (es) * 2003-04-03 2005-11-04 Merck Patent Gmbh Compuestos de carbonilo.
PL1651612T3 (pl) 2003-07-22 2012-09-28 Astex Therapeutics Ltd Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3)
DE102004014945A1 (de) * 2004-03-26 2005-10-13 Merck Patent Gmbh Prolinylderivate
WO2006010750A1 (fr) 2004-07-28 2006-02-02 Janssen Pharmaceutica N.V. Derives d'indolyl alkyl amine substitues utilises en tant que nouveaux inhibiteurs d'histone deacetylase
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AU2007206942B2 (en) 2006-01-19 2012-08-23 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
WO2018093716A1 (fr) * 2016-11-18 2018-05-24 Merck Sharp & Dohme Corp. Inhibiteurs de facteur xiia
CN111818915B (zh) 2018-01-31 2024-05-24 德西费拉制药有限责任公司 治疗胃肠道间质瘤的组合疗法
TW202122082A (zh) 2019-08-12 2021-06-16 美商迪賽孚爾製藥有限公司 治療胃腸道基質瘤方法
AU2020329956B2 (en) 2019-08-12 2023-11-16 Deciphera Pharmaceuticals, Llc. Ripretinib for treating gastrointestinal stromal tumors
JP2023509628A (ja) 2019-12-30 2023-03-09 デシフェラ・ファーマシューティカルズ,エルエルシー 1-(4-ブロモ-5-(1-エチル-7-(メチルアミノ)-2-オキソ-1,2-ジヒドロ-1,6-ナフチリジン-3-イル)-2-フルオロフェニル)-3-フェニル尿素の組成物
BR112022013109A2 (pt) 2019-12-30 2022-09-06 Deciphera Pharmaceuticals Llc Formulações de inibidor de quinase amorfo e métodos de uso das mesmas
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 (fr) * 1996-08-16 1998-02-19 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines et -isoxazolidines et leurs derives
WO1998028269A1 (fr) * 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company COMPOSES HETEROAROMATIQUES CONTENANT DE L'AZOTE, UTILISES EN TANT QU'INHIBITEURS DU FACTEUR Xa

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998006694A1 (fr) * 1996-08-16 1998-02-19 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines et -isoxazolidines et leurs derives
WO1998028269A1 (fr) * 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company COMPOSES HETEROAROMATIQUES CONTENANT DE L'AZOTE, UTILISES EN TANT QU'INHIBITEURS DU FACTEUR Xa

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
WO2000071516A3 (fr) 2001-01-18
JP2003500391A (ja) 2003-01-07
JP2003500390A (ja) 2003-01-07
WO2000071516B1 (fr) 2001-03-01
AU5284000A (en) 2000-12-12
AU5283600A (en) 2000-12-12
CA2371904A1 (fr) 2000-11-30
EP1185512A2 (fr) 2002-03-13
WO2000071516A2 (fr) 2000-11-30
WO2000071515A2 (fr) 2000-11-30
EP1185511A2 (fr) 2002-03-13
CA2374788A1 (fr) 2000-11-30

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