EP0971891A4 - Thrombin inhibitors - Google Patents

Thrombin inhibitors

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Withdrawn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
German (de)
French (fr)
Other versions
EP0971891A1 (en
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/en
Publication of EP0971891A4 publication Critical patent/EP0971891A4/en
Withdrawn legal-status Critical Current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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
EP98902807A 1997-01-22 1998-01-16 Thrombin inhibitors Withdrawn EP0971891A4 (en)

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 (en) 2000-01-19
EP0971891A4 true EP0971891A4 (en) 2000-04-19

Family

ID=26311088

Family Applications (1)

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EP98902807A Withdrawn EP0971891A4 (en) 1997-01-22 1998-01-16 Thrombin inhibitors

Country Status (5)

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

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999041277A1 (en) * 1998-02-17 1999-08-19 Nippon Kayaku Kabushiki Kaisha Novel acetamide derivative and use thereof
AU758237B2 (en) * 1998-09-28 2003-03-20 Merck & Co., Inc. Thrombin inhibitors
FR2786482B1 (en) * 1998-11-27 2002-08-09 Synthelabo NOVEL 2-PYRIDONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
CA2320730A1 (en) 1998-12-23 2000-07-06 Renhua Li Thrombin or factor xa inhibitors
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
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
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones 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
AU5046600A (en) * 1999-05-27 2000-12-18 3-Dimensional Pharmaceuticals, Inc. Oxazaheterocycles as protease inhibitors
UA58636C2 (en) * 1999-06-04 2003-08-15 Мерк Енд Ко., Інк. Pyrazinone thrombin inhibitors, pharmaceutical composition, method for treatment conditions caused by thrombus formation
EP1259506A1 (en) 1999-11-23 2002-11-27 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU2001243598A1 (en) 2000-03-13 2001-09-24 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
EP1268428A2 (en) 2000-04-05 2003-01-02 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
AU2001249870A1 (en) 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
AU2001253363A1 (en) 2000-04-17 2001-10-30 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
WO2001087842A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
KR20030015393A (en) 2000-07-17 2003-02-20 3-디멘져널 파마슈티칼즈 인코오포레이티드 Cyclic oxyguanidine pyrazinones as protease inhibitors
EP1307432A1 (en) * 2000-08-04 2003-05-07 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine protease inhibitors
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
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
MXPA03004458A (en) 2000-11-20 2005-01-25 Pharmacia Corp 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
EP1432687A2 (en) 2001-10-03 2004-06-30 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
US6969715B2 (en) 2001-10-03 2005-11-29 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
BR0307631A (en) 2002-02-14 2004-12-21 Pharmacia Corp Pyridinones substituted as p38 map kinase modulators

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
CN1131210C (en) * 1995-04-27 2003-12-17 三菱制药株式会社 Heterocyclic amide compounds and medicinal use of the same

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
AU722429B2 (en) 2000-08-03
AU5961398A (en) 1998-08-07
JP2001508796A (en) 2001-07-03
WO1998031670A1 (en) 1998-07-23
CA2277929A1 (en) 1998-07-23
EP0971891A1 (en) 2000-01-19

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Legal Events

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