EP0969840A4 - Thrombin inhibitors - Google Patents

Thrombin inhibitors

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Withdrawn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
German (de)
French (fr)
Other versions
EP0969840A1 (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
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/en
Publication of EP0969840A4 publication Critical patent/EP0969840A4/en
Withdrawn legal-status Critical Current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

Landscapes

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EP98911875A 1997-03-24 1998-03-20 Thrombin inhibitors Withdrawn EP0969840A4 (en)

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
GBGB9716872.8A GB9716872D0 (en) 1997-08-08 1997-08-08 Thrombin Inhibitors
GB9716872 1997-08-08
GB9800214 1998-01-06
GBGB9800214.0A GB9800214D0 (en) 1998-01-06 1998-01-06 Throbin inibitors
PCT/US1998/005486 WO1998042342A1 (en) 1997-03-24 1998-03-20 Thrombin inhibitors

Publications (2)

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

Family

ID=27451688

Family Applications (1)

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EP98911875A Withdrawn EP0969840A4 (en) 1997-03-24 1998-03-20 Thrombin inhibitors

Country Status (5)

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

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU742178B2 (en) * 1998-05-26 2001-12-20 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
FR2786482B1 (en) * 1998-11-27 2002-08-09 Synthelabo NOVEL 2-PYRIDONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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 (en) * 1999-05-19 2005-10-19 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
CN1351595A (en) * 1999-05-19 2002-05-29 法玛西雅公司 Substituted polycyclic aryl and heteroacryl pyrazinones 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
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils 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
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
MXPA01011805A (en) * 1999-05-19 2003-09-04 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade.
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
AU773317B2 (en) 1999-07-19 2004-05-20 Merck Canada Inc. Pyrazinones, compositions containing such compounds
EP1259506A1 (en) * 1999-11-23 2002-11-27 Merck & Co., Inc. Pyrazinone thrombin inhibitors
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes 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
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
WO2001079155A2 (en) 2000-04-17 2001-10-25 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
WO2002042272A2 (en) 2000-11-20 2002-05-30 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines 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
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
WO2003093242A2 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
MXPA04003163A (en) 2001-10-03 2004-07-08 Pharmacia Corp 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade.
SI21097A (en) 2001-12-04 2003-06-30 Univerza V Ljubljani Thrombine inhibitors
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
US7759325B2 (en) 2005-04-18 2010-07-20 Sc Dicophar Use of lecithin as a medication for the treatment of psoriasis
AU2009250295B2 (en) 2008-05-21 2014-05-01 Genesis Technologies Limited Selective caspase inhibitors and uses thereof
US9045524B2 (en) 2009-05-21 2015-06-02 Novagenesis Foundation Selective caspase inhibitors and uses thereof
CA2833082C (en) 2011-04-15 2019-12-31 New World Laboratories, Inc. Selective cysteine protease inhibitors and uses thereof
CN103265537B (en) * 2013-05-14 2015-05-27 浙江医药高等专科学校 Antitumor compounds, preparation method and application thereof
CN103396400B (en) * 2013-07-16 2014-12-17 浙江医药高等专科学校 Pyrazole amide compounds, and preparation method and application thereof
CN103387569B (en) * 2013-07-16 2014-09-24 浙江医药高等专科学校 Antineoplastic compounds, preparation method thereof and applications thereof
CN103387568B (en) * 2013-07-16 2014-11-05 浙江医药高等专科学校 Compounds, preparation method thereof and applications thereof
CN103382198B (en) * 2013-07-16 2014-11-19 浙江医药高等专科学校 Pyrazole amide compound, and preparation method thereof and application
CN103382202B (en) * 2013-07-16 2014-11-26 浙江医药高等专科学校 Compound containing furan substitute and preparation method and use thereof
CN103420993B (en) * 2013-07-16 2014-12-17 浙江医药高等专科学校 Thiophene substituent group-containing compound as well as preparation method and application thereof

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
AU728006B2 (en) 2001-01-04
CA2283704A1 (en) 1998-10-01
EP0969840A1 (en) 2000-01-12
AU6572798A (en) 1998-10-20
WO1998042342A1 (en) 1998-10-01
JP2001518932A (en) 2001-10-16

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Legal Events

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Effective date: 20041001