AU728006B2 - Thrombin inhibitors - Google Patents

Thrombin inhibitors Download PDF

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Publication number
AU728006B2
AU728006B2 AU65727/98A AU6572798A AU728006B2 AU 728006 B2 AU728006 B2 AU 728006B2 AU 65727/98 A AU65727/98 A AU 65727/98A AU 6572798 A AU6572798 A AU 6572798A AU 728006 B2 AU728006 B2 AU 728006B2
Authority
AU
Australia
Prior art keywords
compound
blood
methyl
mammal
cycloalkyl
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.)
Ceased
Application number
AU65727/98A
Other languages
English (en)
Other versions
AU6572798A (en
Inventor
Bruce D Dorsey
Richard C. A. Isaacs
Adel M. Naylor-Olsen
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 AU6572798A publication Critical patent/AU6572798A/en
Application granted granted Critical
Publication of AU728006B2 publication Critical patent/AU728006B2/en
Anticipated expiration legal-status Critical
Ceased 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (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)
AU65727/98A 1997-03-24 1998-03-20 Thrombin inhibitors Ceased AU728006B2 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US4154397P 1997-03-24 1997-03-24
US60/041543 1997-03-24
US4756197P 1997-05-22 1997-05-22
US60/047561 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
AU6572798A AU6572798A (en) 1998-10-20
AU728006B2 true AU728006B2 (en) 2001-01-04

Family

ID=27451688

Family Applications (1)

Application Number Title Priority Date Filing Date
AU65727/98A Ceased AU728006B2 (en) 1997-03-24 1998-03-20 Thrombin inhibitors

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
AU742178B2 (en) * 1998-05-26 2001-12-20 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
FR2786482B1 (fr) * 1998-11-27 2002-08-09 Synthelabo Nouveaux derives de 2-pyridone, leur preparation et leur application en therapeutique
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones 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
IL146244A0 (en) * 1999-05-19 2002-07-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyridones 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
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
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
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
CZ20014115A3 (cs) * 1999-05-19 2002-05-15 Pharmacia Corporation Substituované polycyklické aryl a heteroaryl pyrazinony vhodné pro selektivní inhibici koagulační kaskády
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
ATE344249T1 (de) 1999-07-19 2006-11-15 Merck Frosst Canada Ltd Pyrazinone, diese verbindungen enthaltende zusammenstellungen
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
CA2405306A1 (en) 2000-04-05 2001-10-18 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
CA2405684A1 (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
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
MXPA03004458A (es) 2000-11-20 2005-01-25 Pharmacia Corp Arilpiridinas y heteroarilpiridinas sustituidas utiles para inhibicion selectiva de la cascada de coagulacion.
EP1438292A1 (de) 2001-10-03 2004-07-21 Pharmacia Corporation 6-gliedrige heterocyclische verbindungen, die sich zur selektiven inhibierung der koagulationskaskade eignen
AU2002367752A1 (en) 2001-10-03 2003-11-17 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
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
WO2006111633A2 (fr) 2005-04-18 2006-10-26 Sc Dicophar Utilisation de la lecithine comme medicament dans le traitement du psoriasis
US8791235B2 (en) 2008-05-21 2014-07-29 Novagenesis Foundation Selective caspase inhibitors and uses thereof
WO2010133000A1 (en) 2009-05-21 2010-11-25 New World Laboratories Inc. Selective caspase inhibitors and uses thereof
DK2697246T3 (en) 2011-04-15 2018-05-28 Genesis Tech Limited SELECTIVE CYSTEIN PROTEASE INHIBITORS AND USES THEREOF
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
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
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
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
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

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
CA2224437A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors
AU714985B2 (en) * 1996-04-23 2000-01-13 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
AU6572798A (en) 1998-10-20
JP2001518932A (ja) 2001-10-16
EP0969840A1 (de) 2000-01-12
EP0969840A4 (de) 2001-02-28
CA2283704A1 (en) 1998-10-01
WO1998042342A1 (en) 1998-10-01

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Legal Events

Date Code Title Description
MK14 Patent ceased section 143(a) (annual fees not paid) or expired