WO1996019491A1 - Peptides de cetoarginine heterocycliques utilises comme inhibiteurs de thrombine - Google Patents

Peptides de cetoarginine heterocycliques utilises comme inhibiteurs de thrombine Download PDF

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Publication number
WO1996019491A1
WO1996019491A1 PCT/CA1995/000711 CA9500711W WO9619491A1 WO 1996019491 A1 WO1996019491 A1 WO 1996019491A1 CA 9500711 W CA9500711 W CA 9500711W WO 9619491 A1 WO9619491 A1 WO 9619491A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
aryl
group
compound according
substituted
Prior art date
Application number
PCT/CA1995/000711
Other languages
English (en)
Inventor
John Gillard
John Dimaio
M. Arshad Siddiqui
Patrice Preville
Dominique Lafleur
Annette Marian Doherty
Jeremy John Edmonds
Original Assignee
Biochem Pharma 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 GBGB9426038.7A external-priority patent/GB9426038D0/en
Priority claimed from GBGB9504403.8A external-priority patent/GB9504403D0/en
Priority claimed from GBGB9504404.6A external-priority patent/GB9504404D0/en
Application filed by Biochem Pharma Inc. filed Critical Biochem Pharma Inc.
Priority to EP95940926A priority Critical patent/EP0799240A1/fr
Priority to JP8519385A priority patent/JPH10513151A/ja
Priority to AU42508/96A priority patent/AU4250896A/en
Publication of WO1996019491A1 publication Critical patent/WO1996019491A1/fr

Links

Classifications

    • 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
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Abstract

Cette invention se rapporte à de nouveaux inhibiteurs utiles de l'enzyme thrombine de la formule (I) et plus particulièrement à un composé utilisé dans leur préparation, et à des compositions pharmaceutiques. L'invention se rapporte également à l'utilisation de ces composés et compositions in vitro comme anticoagulants et in vivo comme agents s'appliquant au traitement et à la prophylaxie de troubles thrombotiques, tels que la thrombose veineuse, l'embolie pulmonaire et la thrombose artérielle donnant lieu à des accidents ischémiques aigus, tels que l'infarctus du myocarde ou l'infarctus cérébral. De plus, ces composés et compositions sont thérapeutiquement utiles dans la prévention et le traitement de la coagulopathie associée aux interventions de pontage coronarien ainsi qu'à des incidents relatifs à la resténose après une angioplastie transluminale.
PCT/CA1995/000711 1994-12-22 1995-12-21 Peptides de cetoarginine heterocycliques utilises comme inhibiteurs de thrombine WO1996019491A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP95940926A EP0799240A1 (fr) 1994-12-22 1995-12-21 Peptides de cetoarginine heterocycliques utilises comme inhibiteurs de thrombine
JP8519385A JPH10513151A (ja) 1994-12-22 1995-12-21 トロンビン阻害剤としての複素環式ケトアルギニンペプチド
AU42508/96A AU4250896A (en) 1994-12-22 1995-12-21 Heterocyclic keto arginine peptides as thrombin inhibitors

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
GB9426038.7 1994-12-22
GBGB9426038.7A GB9426038D0 (en) 1994-12-22 1994-12-22 Low molecular weight bicyclic thrombin inhibitors
GBGB9503136.5A GB9503136D0 (en) 1994-12-22 1995-02-17 Low molecular weight bicyclic thrombin inhibitors
GB9503136.5 1995-02-17
GB9504403.8 1995-03-06
GB9504404.6 1995-03-06
GBGB9504403.8A GB9504403D0 (en) 1995-03-06 1995-03-06 Heterocyclic keto arginine peptides as thrombin inhibitors
GBGB9504404.6A GB9504404D0 (en) 1995-03-06 1995-03-06 Heterocyclic keto arginine peptides as thrombin inhibitors

Publications (1)

Publication Number Publication Date
WO1996019491A1 true WO1996019491A1 (fr) 1996-06-27

Family

ID=27451243

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA1995/000711 WO1996019491A1 (fr) 1994-12-22 1995-12-21 Peptides de cetoarginine heterocycliques utilises comme inhibiteurs de thrombine

Country Status (6)

Country Link
EP (1) EP0799240A1 (fr)
JP (1) JPH10513151A (fr)
AU (2) AU4250896A (fr)
CA (1) CA2208773A1 (fr)
IL (1) IL116502A0 (fr)
WO (1) WO1996019491A1 (fr)

Cited By (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996040744A1 (fr) * 1995-06-07 1996-12-19 Cor Therapeutics, Inc. INHIBITEURS CETOHETEROCYCLIQUES DU FACTEUR Xa
WO1998007308A2 (fr) * 1996-08-23 1998-02-26 Akzo Nobel N.V. Inhibiteurs de la thrombine
WO1998009987A1 (fr) * 1996-09-06 1998-03-12 Biochem Pharma, Inc. Inhibiteurs lactame de la thrombine
WO1998016524A1 (fr) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. DERIVES HETEROCYCLIQUES UTILISES COMME INHIBITEURS DE FACTEUR Xa
WO1998016547A1 (fr) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1998016525A1 (fr) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1998028326A1 (fr) * 1996-12-23 1998-07-02 Biochem Pharma Inc. Inhibiteurs bicycliques de thrombine
WO1998046627A1 (fr) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1998046626A1 (fr) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1998046628A1 (fr) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1999007731A1 (fr) * 1997-08-11 1999-02-18 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1999007732A1 (fr) * 1997-08-11 1999-02-18 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6063794A (en) * 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6323219B1 (en) 1998-04-02 2001-11-27 Ortho-Mcneil Pharmaceutical, Inc. Methods for treating immunomediated inflammatory disorders
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6469036B1 (en) 1999-01-27 2002-10-22 Ortho-Mcneil Pharmaceutical, Inc. Peptidyl heterocyclic ketones useful as tryptase inhibitors
AU753842B2 (en) * 1997-08-11 2002-10-31 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US7897144B2 (en) 2001-02-28 2011-03-01 Johnson & Johnson Comsumer Companies, Inc. Compositions containing legume products
US8093293B2 (en) 1998-07-06 2012-01-10 Johnson & Johnson Consumer Companies, Inc. Methods for treating skin conditions
US8106094B2 (en) 1998-07-06 2012-01-31 Johnson & Johnson Consumer Companies, Inc. Compositions and methods for treating skin conditions
US8263630B2 (en) 2008-02-12 2012-09-11 Bristol-Myers Squibb Company 1,2,3-triazoles as 11-beta hydroxysteroid dehydrogenase type I inhibitors
US8431550B2 (en) 2000-10-27 2013-04-30 Johnson & Johnson Consumer Companies, Inc. Topical anti-cancer compositions and methods of use thereof
US9173887B2 (en) 2010-12-22 2015-11-03 Abbvie Inc. Hepatitis C inhibitors and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4191753A (en) * 1978-11-06 1980-03-04 University Of Miami Anti-hypertensive peptide analogs
EP0462884A1 (fr) * 1990-06-18 1991-12-27 Adir Et Compagnie Dérivés de TRH, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4191753A (en) * 1978-11-06 1980-03-04 University Of Miami Anti-hypertensive peptide analogs
EP0462884A1 (fr) * 1990-06-18 1991-12-27 Adir Et Compagnie Dérivés de TRH, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent

Cited By (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996040744A1 (fr) * 1995-06-07 1996-12-19 Cor Therapeutics, Inc. INHIBITEURS CETOHETEROCYCLIQUES DU FACTEUR Xa
US6197748B1 (en) 1995-06-07 2001-03-06 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
WO1998007308A2 (fr) * 1996-08-23 1998-02-26 Akzo Nobel N.V. Inhibiteurs de la thrombine
WO1998007308A3 (fr) * 1996-08-23 2000-08-24 Akzo Nobel Nv Inhibiteurs de la thrombine
WO1998009987A1 (fr) * 1996-09-06 1998-03-12 Biochem Pharma, Inc. Inhibiteurs lactame de la thrombine
WO1998016524A1 (fr) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. DERIVES HETEROCYCLIQUES UTILISES COMME INHIBITEURS DE FACTEUR Xa
US6525076B1 (en) 1996-10-11 2003-02-25 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998016525A1 (fr) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998016547A1 (fr) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6063794A (en) * 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
WO1998028326A1 (fr) * 1996-12-23 1998-07-02 Biochem Pharma Inc. Inhibiteurs bicycliques de thrombine
WO1998046628A1 (fr) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
WO1998046627A1 (fr) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6204268B1 (en) 1997-04-14 2001-03-20 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6369063B1 (en) 1997-04-14 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998046626A1 (fr) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
WO1999007732A1 (fr) * 1997-08-11 1999-02-18 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1999007731A1 (fr) * 1997-08-11 1999-02-18 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
AU753842B2 (en) * 1997-08-11 2002-10-31 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US6323219B1 (en) 1998-04-02 2001-11-27 Ortho-Mcneil Pharmaceutical, Inc. Methods for treating immunomediated inflammatory disorders
US8093293B2 (en) 1998-07-06 2012-01-10 Johnson & Johnson Consumer Companies, Inc. Methods for treating skin conditions
US8106094B2 (en) 1998-07-06 2012-01-31 Johnson & Johnson Consumer Companies, Inc. Compositions and methods for treating skin conditions
US7132418B2 (en) 1999-01-27 2006-11-07 Ortho-Mcneil Pharmaceutical, Inc. Peptidyl heterocyclic ketones useful as tryptase inhibitors
US6469036B1 (en) 1999-01-27 2002-10-22 Ortho-Mcneil Pharmaceutical, Inc. Peptidyl heterocyclic ketones useful as tryptase inhibitors
US8431550B2 (en) 2000-10-27 2013-04-30 Johnson & Johnson Consumer Companies, Inc. Topical anti-cancer compositions and methods of use thereof
US7897144B2 (en) 2001-02-28 2011-03-01 Johnson & Johnson Comsumer Companies, Inc. Compositions containing legume products
US8263630B2 (en) 2008-02-12 2012-09-11 Bristol-Myers Squibb Company 1,2,3-triazoles as 11-beta hydroxysteroid dehydrogenase type I inhibitors
US9173887B2 (en) 2010-12-22 2015-11-03 Abbvie Inc. Hepatitis C inhibitors and uses thereof
US9453007B2 (en) 2010-12-22 2016-09-27 Abbvie Inc. Hepatitis C inhibitors and uses thereof
US9567355B2 (en) 2010-12-22 2017-02-14 Abbvie Inc. Hepatitis C inhibitors and uses thereof

Also Published As

Publication number Publication date
CA2208773A1 (fr) 1996-06-27
AU4062795A (en) 1996-06-27
EP0799240A1 (fr) 1997-10-08
JPH10513151A (ja) 1998-12-15
MX9704594A (es) 1998-07-31
IL116502A0 (en) 1996-03-31
AU4250896A (en) 1996-07-10
AU699679B2 (en) 1998-12-10

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