CA2301520A1 - Inhibiteurs de thrombine a base de pyrazinone - Google Patents

Inhibiteurs de thrombine a base de pyrazinone Download PDF

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Publication number
CA2301520A1
CA2301520A1 CA002301520A CA2301520A CA2301520A1 CA 2301520 A1 CA2301520 A1 CA 2301520A1 CA 002301520 A CA002301520 A CA 002301520A CA 2301520 A CA2301520 A CA 2301520A CA 2301520 A1 CA2301520 A1 CA 2301520A1
Authority
CA
Canada
Prior art keywords
alkyl
halogen
cycloalkyl
unsubstituted
hydroxy
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
CA002301520A
Other languages
English (en)
Inventor
Philip E. Sanderson
Terry A. Lyle
Bruce D. Dorsey
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.)
Merck and Co Inc
Original Assignee
Individual
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 claimed from GBGB9801005.1A external-priority patent/GB9801005D0/en
Application filed by Individual filed Critical Individual
Publication of CA2301520A1 publication Critical patent/CA2301520A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

L'invention concerne des composés aptes à inhiber la thrombine et les occlusions thrombotiques associées, lesquels composés ont la structure (a), par exemple, la structure (17-1).
CA002301520A 1997-09-05 1998-09-03 Inhibiteurs de thrombine a base de pyrazinone Abandoned CA2301520A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US5805897P 1997-09-05 1997-09-05
US60/058,058 1997-09-05
GBGB9801005.1A GB9801005D0 (en) 1998-01-16 1998-01-16 Pyrazinone thrombin inhibitors
GB9801005.1 1998-01-16
PCT/US1998/018417 WO1999011267A1 (fr) 1997-09-05 1998-09-03 Inhibiteurs de thrombine a base de pyrazinone

Publications (1)

Publication Number Publication Date
CA2301520A1 true CA2301520A1 (fr) 1999-03-11

Family

ID=26312966

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002301520A Abandoned CA2301520A1 (fr) 1997-09-05 1998-09-03 Inhibiteurs de thrombine a base de pyrazinone

Country Status (4)

Country Link
EP (1) EP1017393A4 (fr)
JP (1) JP2001514227A (fr)
CA (1) CA2301520A1 (fr)
WO (1) WO1999011267A1 (fr)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9710809D0 (en) 1997-05-23 1997-07-23 Medical Res Council Nucleic acid binding proteins
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1589029B1 (fr) * 1998-06-11 2010-03-17 Ortho-McNeil Pharmaceuticals, Inc. Inhibiteurs de protéase à base de pyrazine
PT997474E (pt) 1998-08-14 2004-01-30 Pfizer Agentes antitromboticos
CA2348734A1 (fr) 1998-10-30 2000-05-11 Merck & Co., Inc. Inhibiteurs de la thrombine
CA2348530A1 (fr) 1998-10-30 2000-05-11 Merck & Co., Inc. Inhibiteurs de la thrombine
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
NZ514876A (en) * 1999-05-19 2005-03-24 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
WO2000069826A1 (fr) * 1999-05-19 2000-11-23 Pharmacia Corporation Pyridones aryle et heteroaryle polycycliques substituees utilisees pour l'inhibition selective de la cascade de coagulation
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
EP1586565A1 (fr) * 1999-05-19 2005-10-19 Pharmacia Corporation Pyrazinones d'hétéroaryle et d'aryle polycyclique substituées utiles à l'inhibition selective de la coagulation en cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
UA58636C2 (uk) * 1999-06-04 2003-08-15 Мерк Енд Ко., Інк. Піразинонові інгібітори тромбіну, фармацевтична композиція, спосіб інгібування утворення тромбів у крові, спосіб лікування станів, пов'язаних із тромбоутворенням
ES2274795T3 (es) 1999-07-19 2007-06-01 Merck Frosst Canada Ltd. Pirazinonas, composiciones que contienen tales compuestos.
WO2001038323A1 (fr) 1999-11-23 2001-05-31 Merck & Co., Inc. Inhibiteurs de thrombine a base de pyrazinone
US6852761B2 (en) 2000-03-13 2005-02-08 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
WO2001070229A1 (fr) 2000-03-23 2001-09-27 Merck & Co., Inc. Inhibiteurs de thrombine
US6693121B2 (en) 2000-04-05 2004-02-17 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
JP2004505014A (ja) 2000-04-05 2004-02-19 ファルマシア・コーポレーション 凝血カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換された４−ピロン類
WO2001079195A2 (fr) * 2000-04-14 2001-10-25 Corvas International, Inc. Nouveaux inhibiteurs de thrombine de type non covalent
US6506754B1 (en) * 2000-04-14 2003-01-14 Corvas International, Inc. Non-covalent thrombin inhibitors
JP2004501077A (ja) 2000-04-17 2004-01-15 ファルマシア・コーポレーション 凝固カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換１，４−キノン
WO2001092234A1 (fr) * 2000-06-01 2001-12-06 Merck & Co., Inc. Inhibiteurs de thrombine a base de pyrazinone
MXPA03000512A (es) * 2000-07-17 2003-10-06 Dimensional Pharm Inc Oxiguanidina-pirazinonas ciclicas como inhibidores de proteasas.
AU2001278997A1 (en) * 2000-07-28 2002-02-13 Merck And Co., Inc. Thrombin inhibitors
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
CA2430037A1 (fr) 2000-11-20 2002-05-30 Michael S. South Aryl-et-heteroaryl-pyridines polycycliques substituees utiles dans l'inhibition selective de la cascade de la coagulation
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
CA2430842A1 (fr) * 2000-12-06 2002-06-13 Merck & Co., Inc. Procede de preparation d'un inhibiteur de thrombines
JP2004520399A (ja) * 2001-02-09 2004-07-08 メルク　エンド　カムパニー　インコーポレーテッド トロンビン阻害剤
MXPA04003170A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos policiclicos, sustituidos, provisto de 5 miembros, utiles para la inhibicion selectiva de la cascada de coagulacion.
US6969715B2 (en) 2001-10-03 2005-11-29 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH11508558A (ja) * 1995-06-27 1999-07-27 メルク エンド カンパニー インコーポレーテッド ピリジノン トロンビン阻害剤
US5668289A (en) * 1996-06-24 1997-09-16 Merck & Co., Inc. Pyridinone thrombin inhibitors

Also Published As

Publication number Publication date
JP2001514227A (ja) 2001-09-11
EP1017393A1 (fr) 2000-07-12
EP1017393A4 (fr) 2002-01-23
WO1999011267A1 (fr) 1999-03-11

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Legal Events

Date Code Title Description
FZDE Dead