CA2374820A1 - Inhibiteurs du facteur xa - Google Patents

Inhibiteurs du facteur xa Download PDF

Info

Publication number
CA2374820A1
CA2374820A1 CA002374820A CA2374820A CA2374820A1 CA 2374820 A1 CA2374820 A1 CA 2374820A1 CA 002374820 A CA002374820 A CA 002374820A CA 2374820 A CA2374820 A CA 2374820A CA 2374820 A1 CA2374820 A1 CA 2374820A1
Authority
CA
Canada
Prior art keywords
group
4alkyl
phenyl
member selected
ring
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.)
Abandoned
Application number
CA002374820A
Other languages
English (en)
Inventor
Yonghong Song
Lane Clizbe
Charles Marlowe
Robert M. Scarborough
Ting Su
Bing-Yan Zhu
James Kanter
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.)
Individual
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
Publication of CA2374820A1 publication Critical patent/CA2374820A1/fr
Abandoned legal-status Critical Current

Links

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
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/08—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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by 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
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • C07D307/68—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
    • C07D413/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés représentés par la formule générale A-Y-D-E-G-J-Z-L, dans laquelle A-Y-D-E-G-J-Z et L sont tels que définis dans l'invention. Ces composés sont actifs contre le facteur Xa mammalien. Ils sont utilisés <i>in vitro</i> et <i>in vivo</i> pour prévenir ou traiter les troubles de la coagulation.
CA002374820A 1999-05-24 2000-05-24 Inhibiteurs du facteur xa Abandoned CA2374820A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13581999P 1999-05-24 1999-05-24
US60/135,819 1999-05-24
PCT/US2000/014207 WO2000071512A1 (fr) 1999-05-24 2000-05-24 Inhibiteurs du facteur xa

Publications (1)

Publication Number Publication Date
CA2374820A1 true CA2374820A1 (fr) 2000-11-30

Family

ID=22469841

Family Applications (2)

Application Number Title Priority Date Filing Date
CA002374820A Abandoned CA2374820A1 (fr) 1999-05-24 2000-05-24 Inhibiteurs du facteur xa
CA002382751A Abandoned CA2382751A1 (fr) 1999-05-24 2000-05-24 Inhibiteurs du facteur xa

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA002382751A Abandoned CA2382751A1 (fr) 1999-05-24 2000-05-24 Inhibiteurs du facteur xa

Country Status (5)

Country Link
EP (2) EP1189879A1 (fr)
JP (2) JP2003500387A (fr)
AU (2) AU5158100A (fr)
CA (2) CA2374820A1 (fr)
WO (2) WO2000071509A1 (fr)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2324153A1 (fr) 1998-03-19 1999-09-23 Ajinomoto Co., Inc. Derives d'aminoisoquinoleine
DE10008329A1 (de) * 2000-02-23 2001-08-30 Merck Patent Gmbh Aminosulfonylbiphenylderivate
DE10014645A1 (de) 2000-03-24 2001-09-27 Merck Patent Gmbh Substituierte Biphenylderivate
DE10037146A1 (de) * 2000-07-29 2002-02-07 Merck Patent Gmbh Acetamidderivate
DE10046272A1 (de) * 2000-09-19 2002-03-28 Merck Patent Gmbh Aminoheterocyclen (Faktor Xa Inhibitoren 14)
DE10117823A1 (de) * 2001-04-10 2002-10-17 Merck Patent Gmbh Oxalsäurederivate
DE10124867A1 (de) * 2001-05-22 2002-11-28 Boehringer Ingelheim Pharma Substituierte Aryl- und Heteroarylderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7005437B2 (en) 2001-05-22 2006-02-28 Boehringer Ingelheim Pharma Kg Substituted aryl and heteroaryl derivatives, the preparation thereof and the use therof as pharmaceutical compositions
DE10139060A1 (de) 2001-08-08 2003-02-20 Merck Patent Gmbh Phenylderivate
AR037097A1 (es) 2001-10-05 2004-10-20 Novartis Ag Compuestos acilsulfonamidas, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento
GB0124933D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124939D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124941D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124934D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
WO2003042190A1 (fr) 2001-11-12 2003-05-22 Pfizer Products Inc. Derives de n-adamantylalkyle benzamide en tant qu'antagonistes du recepteur p2x7
PT1474395E (pt) 2002-02-12 2008-01-02 Smithkline Beecham Corp Derivados de nicotinamida úteis como inibidores de p38
DE10214832A1 (de) * 2002-04-04 2003-10-16 Merck Patent Gmbh Phenylderivate 4
CN100513398C (zh) 2002-12-03 2009-07-15 Axys药物公司 作为因子viia抑制剂的2-(2-羟基联苯-3-基)-1h-苯并咪唑-5-甲脒衍生物
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
US7071223B1 (en) 2002-12-31 2006-07-04 Pfizer, Inc. Benzamide inhibitors of the P2X7 receptor
GB0308186D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308201D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
ES2396565T3 (es) 2003-05-12 2013-02-22 Pah Usa 15 Llc Inhibidores benzamida del receptor P2X7
GB0318814D0 (en) 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
AU2005258911A1 (en) 2004-06-29 2006-01-12 Pfizer Products Inc. Method for preparing 5-`4-(2-hydroxy-propyl)-3,5-dioxo-4,5-dihydro-3H`1,2,4!triazin-2-YL!-benzamide derivatives by deprotecting the hydroxyl-protected precursers
WO2006101937A1 (fr) 2005-03-18 2006-09-28 Janssen Pharmaceutica N.V. Acylhydrazones en tant que modulateurs de kinase
WO2008059370A2 (fr) 2006-11-17 2008-05-22 Pfizer Japan Inc. Composés bicyclocarboxyamides substitués
CA2804593C (fr) 2010-07-09 2015-11-24 Pfizer Limited Derives de biphenyloxybenzensulphonamide utiles en tant qu'inhibiteurs du canal sodique
CN104693097A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 一类含双酰肼和烷氧萘基结构的化合物、制备方法及其用途
CN104710341A (zh) * 2015-02-13 2015-06-17 佛山市赛维斯医药科技有限公司 一类含双酰肼和萘基结构的化合物、制备方法及其用途
CN104693096A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 含双酰肼和萘基结构的化合物、制备方法及其用途
CN104693099A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 一种含双酰肼和萘基结构的化合物及其用途
CN104693102A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 一种双酰肼类化合物、其制备方法及其用途
CN104693093A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 双酰肼类FXa抑制剂、制备方法及其用途
CN104693101A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 一种双酰肼类衍生物、其制备方法及其用途
CN104693095A (zh) * 2015-02-13 2015-06-10 佛山市赛维斯医药科技有限公司 一类双酰肼类FXa抑制剂及其用途
CN108976150B (zh) * 2017-06-05 2022-11-18 重庆博腾制药科技股份有限公司 一种3-乙基-4-氟苯腈的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0960102A1 (fr) * 1996-07-08 1999-12-01 Du Pont Pharmaceuticals Company AMIDINOINDOLES, AMIDINOAZOLES ET LEURS ANALOGUES AGISSANT EN TANT QU'INHIBITEURS DU FACTEUR Xa ET DE LA THROMBINE
US5886191A (en) * 1997-08-18 1999-03-23 Dupont Pharmaceuticals Company Amidinoindoles, amidinoazoles, and analogs thereof

Also Published As

Publication number Publication date
JP2003500387A (ja) 2003-01-07
EP1189879A1 (fr) 2002-03-27
WO2000071512A1 (fr) 2000-11-30
AU5283700A (en) 2000-12-12
JP2003500384A (ja) 2003-01-07
WO2000071509A1 (fr) 2000-11-30
AU5158100A (en) 2000-12-12
CA2382751A1 (fr) 2000-11-30
EP1183234A1 (fr) 2002-03-06

Similar Documents

Publication Publication Date Title
CA2374820A1 (fr) Inhibiteurs du facteur xa
US6399627B1 (en) Inhibitors of factor Xa
US6632815B2 (en) Inhibitors of factor Xa
US6545055B1 (en) Inhibitors of factor Xa
CA2385592C (fr) Benzamides et inhibiteurs correspondants du facteur xa
US20030114448A1 (en) Inhibitors of factor Xa
US6534535B1 (en) Inhibitors of factor Xa
CA2374947A1 (fr) Inhibiteurs du facteur xa
JP2003509412A (ja) Ｘａ因子阻害剤
US6686368B1 (en) Inhibitors of factor Xa
CA2371904A1 (fr) Inhibiteurs du facteur xa
US20040082786A1 (en) Piperazine based inhibitors of factor xa
EP1235807A1 (fr) INHIBITEURS DU FACTEUR Xa A BASE D&#39;ACIDES $g(b)-AMINES, ASPARTIQUES ET DIAMINOPROPIONIQUES
WO2002026718A2 (fr) Inhibiteurs du facteur xa à base de pyrimidine-4-one bicyclique
US20040077690A1 (en) Quaternary amidino based inhibitors of factor xa
EP1322643A1 (fr) Amides piperazine-2-un comme inhibiteurs du facteur xa

Legal Events

Date Code Title Description
FZDE Dead