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EP0971891A4 - Thrombin-inhibitoren - Google Patents

Thrombin-inhibitoren

Info

Publication number
EP0971891A4
EP0971891A4 EP98902807A EP98902807A EP0971891A4 EP 0971891 A4 EP0971891 A4 EP 0971891A4 EP 98902807 A EP98902807 A EP 98902807A EP 98902807 A EP98902807 A EP 98902807A EP 0971891 A4 EP0971891 A4 EP 0971891A4
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Withdrawn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
EP98902807A
Other languages
English (en)
French (fr)
Other versions
EP0971891A1 (de
Inventor
Philip E Sanderson
Terry A Lyle
Craig Coburn
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 GBGB9704209.7A external-priority patent/GB9704209D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0971891A1 publication Critical patent/EP0971891A1/de
Publication of EP0971891A4 publication Critical patent/EP0971891A4/de
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • 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
    • A61P9/10—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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP98902807A 1997-01-22 1998-01-16 Thrombin-inhibitoren Withdrawn EP0971891A4 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US3614997P 1997-01-22 1997-01-22
US36149P 1997-01-22
GBGB9704209.7A GB9704209D0 (en) 1997-02-28 1997-02-28 Thrombin inhibitors
GB9704209 1997-02-28
PCT/US1998/000875 WO1998031670A1 (en) 1997-01-22 1998-01-16 Thrombin inhibitors

Publications (2)

Publication Number Publication Date
EP0971891A1 EP0971891A1 (de) 2000-01-19
EP0971891A4 true EP0971891A4 (de) 2000-04-19

Family

ID=26311088

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98902807A Withdrawn EP0971891A4 (de) 1997-01-22 1998-01-16 Thrombin-inhibitoren

Country Status (5)

Country Link
EP (1) EP0971891A4 (de)
JP (1) JP2001508796A (de)
AU (1) AU722429B2 (de)
CA (1) CA2277929A1 (de)
WO (1) WO1998031670A1 (de)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU744739B2 (en) * 1998-02-17 2002-02-28 Nippon Kayaku Kabushiki Kaisha Novel acetamide derivative and use thereof
CA2343109A1 (en) * 1998-09-28 2000-04-06 Merck & Co., Inc. Thrombin inhibitors
FR2786482B1 (fr) * 1998-11-27 2002-08-09 Synthelabo Nouveaux derives de 2-pyridone, leur preparation et leur application en therapeutique
WO2000039102A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones 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
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils 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
JP2003501352A (ja) 1999-05-27 2003-01-14 ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド プロテアーゼ阻害剤としてのオキサザ複素環
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
WO2001038323A1 (en) 1999-11-23 2001-05-31 Merck & Co., Inc. Pyrazinone thrombin inhibitors
WO2001068605A1 (en) 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
US20020022604A1 (en) 2000-04-05 2002-02-21 South Michael S. Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
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
WO2001087842A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
CA2415932A1 (en) 2000-07-17 2002-01-24 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
KR20030022353A (ko) 2000-08-04 2003-03-15 3-디멘져널 파마슈티칼즈 인코오포레이티드 사이클릭 옥시구아니딘 프로테아제 저해제
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
US6624180B2 (en) 2000-11-20 2003-09-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines 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
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
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.
CA2462305A1 (en) 2001-10-03 2003-04-10 Michael S. South 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
DK1490064T3 (da) 2002-02-14 2010-01-04 Pharmacia Corp Substituerede pyridinoner som modulatorer af p38 MAP kinase

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996018644A1 (en) * 1994-12-13 1996-06-20 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
WO1997001338A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors
WO1997030708A1 (en) * 1996-02-22 1997-08-28 Merck & Co., Inc. Pyridinone thrombin inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69634122D1 (de) * 1995-04-27 2005-02-03 Mitsubishi Pharma Corp Heterocyclische amidverbindungen und deren medizinische verwendung

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996018644A1 (en) * 1994-12-13 1996-06-20 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
WO1997001338A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors
WO1997030708A1 (en) * 1996-02-22 1997-08-28 Merck & Co., Inc. Pyridinone thrombin inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO9831670A1 *

Also Published As

Publication number Publication date
AU5961398A (en) 1998-08-07
CA2277929A1 (en) 1998-07-23
WO1998031670A1 (en) 1998-07-23
EP0971891A1 (de) 2000-01-19
AU722429B2 (en) 2000-08-03
JP2001508796A (ja) 2001-07-03

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Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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Effective date: 19990823

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A4 Supplementary search report drawn up and despatched

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STAA Information on the status of an ep patent application or granted ep patent

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18D Application deemed to be withdrawn

Effective date: 20040803