CA2283704A1 - Inhibiteurs de thrombine - Google Patents

Inhibiteurs de thrombine Download PDF

Info

Publication number
CA2283704A1
CA2283704A1 CA002283704A CA2283704A CA2283704A1 CA 2283704 A1 CA2283704 A1 CA 2283704A1 CA 002283704 A CA002283704 A CA 002283704A CA 2283704 A CA2283704 A CA 2283704A CA 2283704 A1 CA2283704 A1 CA 2283704A1
Authority
CA
Canada
Prior art keywords
methyl
cycloalkyl
alkyl
nmr
mmol
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
CA002283704A
Other languages
English (en)
Inventor
Richard C. A. Isaacs
Adel M. Naylor-Olsen
Bruce D. Dorsey
Christina L. Newton
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 GBGB9716872.8A external-priority patent/GB9716872D0/en
Priority claimed from GBGB9800214.0A external-priority patent/GB9800214D0/en
Application filed by Individual filed Critical Individual
Publication of CA2283704A1 publication Critical patent/CA2283704A1/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
    • 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
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

L'invention concerne un composé inhibant la thrombine humaine et ayant la structure (I) ou (II) ou (III), ainsi que des sels pharmaceutiquement acceptables dudit composé (IV), caractérisé en ce que des composés tels que sont utiles pour inhiber la formation d'agrégats de plaquettes dans le sang d'un mammifère.
CA002283704A 1997-03-24 1998-03-20 Inhibiteurs de thrombine Abandoned CA2283704A1 (fr)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US4154397P 1997-03-24 1997-03-24
US60/041,543 1997-03-24
US4756197P 1997-05-22 1997-05-22
US60/047,561 1997-05-22
GBGB9716872.8A GB9716872D0 (en) 1997-08-08 1997-08-08 Thrombin Inhibitors
GBGB9800214.0A GB9800214D0 (en) 1998-01-06 1998-01-06 Throbin inibitors
GB9800214.0 1998-01-06
GB9716872.8 1998-01-06
PCT/US1998/005486 WO1998042342A1 (fr) 1997-03-24 1998-03-20 Inhibiteurs de thrombine

Publications (1)

Publication Number Publication Date
CA2283704A1 true CA2283704A1 (fr) 1998-10-01

Family

ID=27451688

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002283704A Abandoned CA2283704A1 (fr) 1997-03-24 1998-03-20 Inhibiteurs de thrombine

Country Status (5)

Country Link
EP (1) EP0969840A4 (fr)
JP (1) JP2001518932A (fr)
AU (1) AU728006B2 (fr)
CA (1) CA2283704A1 (fr)
WO (1) WO1998042342A1 (fr)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002516326A (ja) * 1998-05-26 2002-06-04 メルク エンド カムパニー インコーポレーテッド イミダゾピリジン系トロンビン阻害薬
FR2786482B1 (fr) * 1998-11-27 2002-08-09 Synthelabo Nouveaux derives de 2-pyridone, leur preparation et leur application en therapeutique
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
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils 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
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
NZ514876A (en) * 1999-05-19 2005-03-24 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyrazinones 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
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
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
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
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
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
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
US6969715B2 (en) 2001-10-03 2005-11-29 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
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.
SI21097A (sl) 2001-12-04 2003-06-30 Univerza V Ljubljani Inhibitorji trombina
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CA2606255C (fr) 2005-04-18 2013-10-08 Sc Dicophar Utilisation de la lecithine comme medicament dans le traitement du psoriasis
AU2009250295B2 (en) 2008-05-21 2014-05-01 Genesis Technologies Limited Selective caspase inhibitors and uses thereof
WO2010133000A1 (fr) 2009-05-21 2010-11-25 New World Laboratories Inc. Inhibiteurs sélectifs des caspases et leurs utilisations
CA2833082C (fr) 2011-04-15 2019-12-31 New World Laboratories, Inc. Inhibiteurs selectifs de cysteine protease et leurs utilisations
CN103265537B (zh) * 2013-05-14 2015-05-27 浙江医药高等专科学校 抗肿瘤化合物、其制备方法和用途
CN103396400B (zh) * 2013-07-16 2014-12-17 浙江医药高等专科学校 含吡唑酰胺类化合物、其制备方法和用途
CN103382198B (zh) * 2013-07-16 2014-11-19 浙江医药高等专科学校 吡唑酰胺类化合物、其制备方法和用途
CN103387568B (zh) * 2013-07-16 2014-11-05 浙江医药高等专科学校 一类化合物、其制备方法和用途
CN103387569B (zh) * 2013-07-16 2014-09-24 浙江医药高等专科学校 一类抗肿瘤化合物、其制备方法和用途
CN103382202B (zh) * 2013-07-16 2014-11-26 浙江医药高等专科学校 含呋喃取代的化合物、其制备方法和用途
CN103420993B (zh) * 2013-07-16 2014-12-17 浙江医药高等专科学校 含噻吩取代的化合物、其制备方法和用途

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUT70045A (en) * 1993-06-17 1995-09-28 Takeda Chemical Industries Ltd 2-piperazinone derivatives parmaceutical compositions containing them and process for producing them
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
NZ331993A (en) * 1996-04-23 2000-04-28 Merck & Co Inc Pyrazinone thrombin inhibitors
US5668289A (en) * 1996-06-24 1997-09-16 Merck & Co., Inc. Pyridinone thrombin inhibitors

Also Published As

Publication number Publication date
EP0969840A4 (fr) 2001-02-28
EP0969840A1 (fr) 2000-01-12
AU6572798A (en) 1998-10-20
WO1998042342A1 (fr) 1998-10-01
JP2001518932A (ja) 2001-10-16
AU728006B2 (en) 2001-01-04

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Legal Events

Date Code Title Description
FZDE Dead