EP0969840A4 - Thrombin inhibitoren - Google Patents

Thrombin inhibitoren

Info

Publication number
EP0969840A4
EP0969840A4 EP98911875A EP98911875A EP0969840A4 EP 0969840 A4 EP0969840 A4 EP 0969840A4 EP 98911875 A EP98911875 A EP 98911875A EP 98911875 A EP98911875 A EP 98911875A EP 0969840 A4 EP0969840 A4 EP 0969840A4
Authority
EP
European Patent Office
Prior art keywords
thrombin inhibitors
thrombin
inhibitors
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.)
Withdrawn
Application number
EP98911875A
Other languages
English (en)
French (fr)
Other versions
EP0969840A1 (de
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
Merck and Co 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 claimed from GBGB9716872.8A external-priority patent/GB9716872D0/en
Priority claimed from GBGB9800214.0A external-priority patent/GB9800214D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0969840A1 publication Critical patent/EP0969840A1/de
Publication of EP0969840A4 publication Critical patent/EP0969840A4/de
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
EP98911875A 1997-03-24 1998-03-20 Thrombin inhibitoren Withdrawn EP0969840A4 (de)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US4154397P 1997-03-24 1997-03-24
US41543P 1997-03-24
US4756197P 1997-05-22 1997-05-22
US47561P 1997-05-22
GB9716872 1997-08-08
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 1998-01-06
PCT/US1998/005486 WO1998042342A1 (en) 1997-03-24 1998-03-20 Thrombin inhibitors

Publications (2)

Publication Number Publication Date
EP0969840A1 EP0969840A1 (de) 2000-01-12
EP0969840A4 true EP0969840A4 (de) 2001-02-28

Family

ID=27451688

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98911875A Withdrawn EP0969840A4 (de) 1997-03-24 1998-03-20 Thrombin inhibitoren

Country Status (5)

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

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1082324A4 (de) * 1998-05-26 2002-01-02 Merck & Co Inc Imidazopyridinverbindungen als thrombininhibitoren
FR2786482B1 (fr) * 1998-11-27 2002-08-09 Synthelabo Nouveaux derives de 2-pyridone, leur preparation et leur application en therapeutique
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation 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
IL146245A0 (en) * 1999-05-19 2002-07-25 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
EP1586565A1 (de) * 1999-05-19 2005-10-19 Pharmacia Corporation Substituierte polycyclische aryl und heteroarylpyrazinone zur selektiven Hemmung von der Blutgerinnungskaskade
CA2373509A1 (en) * 1999-05-19 2000-11-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
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.
JP2003514905A (ja) 1999-11-23 2003-04-22 メルク エンド カムパニー インコーポレーテッド ピラジノン系トロンビン阻害薬
WO2001068605A1 (en) 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
ATE289299T1 (de) 2000-04-05 2005-03-15 Pharmacia Corp Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess
EP1268428A2 (de) 2000-04-05 2003-01-02 Pharmacia Corporation Polyzyklische aryl und heteroaryl substituierte 4-pyridon-derivate verwendbar zur selektiven hemmung der blutgerinnungskaskade
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
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
EP1351686A2 (de) 2000-11-20 2003-10-15 Pharmacia Corporation Substituierte polycyclische aryl- und heteroarylpyridine für die selektive hemmung der koagulationskaskade
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
WO2003093242A2 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
MXPA04003163A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos heterociclicos de 6 elementos utiles para inhibicion selectiva de la casdada 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
DK2288615T3 (en) 2008-05-21 2017-09-04 Genesis Tech Ltd SELECTIVE CASPASE INHIBITORS AND APPLICATIONS THEREOF
US9045524B2 (en) 2009-05-21 2015-06-02 Novagenesis Foundation Selective caspase inhibitors and uses thereof
EP2697246B1 (de) 2011-04-15 2018-03-07 Genesis Technologies Limited Selektive cysteinproteasehemmer und verwendungen davon
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
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
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
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
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
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997001338A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors
WO1997040024A1 (en) * 1996-04-23 1997-10-30 Merck & Co., Inc. Pyrazinone thrombin inhibitors

Family Cites Families (2)

* 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
US5668289A (en) * 1996-06-24 1997-09-16 Merck & Co., Inc. Pyridinone thrombin inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997001338A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors
WO1997040024A1 (en) * 1996-04-23 1997-10-30 Merck & Co., Inc. Pyrazinone thrombin inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO9842342A1 *

Also Published As

Publication number Publication date
EP0969840A1 (de) 2000-01-12
WO1998042342A1 (en) 1998-10-01
AU6572798A (en) 1998-10-20
JP2001518932A (ja) 2001-10-16
CA2283704A1 (en) 1998-10-01
AU728006B2 (en) 2001-01-04

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