EP0820453A4 - Inhibiteurs de thrombine - Google Patents

Inhibiteurs de thrombine

Info

Publication number
EP0820453A4
EP0820453A4 EP96911520A EP96911520A EP0820453A4 EP 0820453 A4 EP0820453 A4 EP 0820453A4 EP 96911520 A EP96911520 A EP 96911520A EP 96911520 A EP96911520 A EP 96911520A EP 0820453 A4 EP0820453 A4 EP 0820453A4
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Withdrawn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
EP96911520A
Other languages
German (de)
English (en)
Other versions
EP0820453A1 (fr
Inventor
Dong-Mei Feng
Mark G Bock
Roger M Freidinger
Joseph P Vacca
Bruce D Dorsey
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
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0820453A1 publication Critical patent/EP0820453A1/fr
Publication of EP0820453A4 publication Critical patent/EP0820453A4/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • 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
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
EP96911520A 1995-04-04 1996-04-01 Inhibiteurs de thrombine Withdrawn EP0820453A4 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41624495A 1995-04-04 1995-04-04
US416244 1995-04-04
PCT/US1996/004460 WO1996031504A1 (fr) 1995-04-04 1996-04-01 Inhibiteurs de thrombine

Publications (2)

Publication Number Publication Date
EP0820453A1 EP0820453A1 (fr) 1998-01-28
EP0820453A4 true EP0820453A4 (fr) 2001-08-29

Family

ID=23649178

Family Applications (1)

Application Number Title Priority Date Filing Date
EP96911520A Withdrawn EP0820453A4 (fr) 1995-04-04 1996-04-01 Inhibiteurs de thrombine

Country Status (5)

Country Link
EP (1) EP0820453A4 (fr)
JP (1) JPH11503161A (fr)
AU (1) AU698911B2 (fr)
CA (1) CA2216859A1 (fr)
WO (1) WO1996031504A1 (fr)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
AR005245A1 (es) 1995-12-21 1999-04-28 Astrazeneca Ab Prodrogas de inhibidores de trombina, una formulación farmaceutica que las comprende, el uso de dichas prodrogas para la manufactura de un medicamento y un procedimiento para su preparacion
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
US5872138A (en) * 1996-09-13 1999-02-16 Merck & Co., Inc. Thrombin inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
US5869487A (en) * 1996-10-24 1999-02-09 Merck & Co., Inc. Pyrido 3,4-B!pyrazines for use as thrombin inhibitors
US6017934A (en) * 1997-01-22 2000-01-25 Merck & Co., Inc. Thrombin inhibitors
US5792779A (en) * 1997-02-19 1998-08-11 Merck & Co., Inc. Pyridinone thrombin inhibitors
US5932606A (en) * 1997-03-24 1999-08-03 Merck & Co., Inc. Pyrazinone, pyridinone, piperidine and pyrrolidine thrombin inhibitors
US6369063B1 (en) 1997-04-14 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
EP0977772A1 (fr) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. INHIBITEURS SELECTIFS DU FACTEUR Xa
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
AR013084A1 (es) 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6011038A (en) * 1997-09-05 2000-01-04 Merck & Co., Inc. Pyrazinone thrombin inhibitors
US6087373A (en) * 1997-09-23 2000-07-11 Merck & Co., Inc. Thrombin inhibitors
US6133297A (en) * 1997-09-30 2000-10-17 Merck & Co., Inc. Thrombin inhibitors
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1082324A4 (fr) * 1998-05-26 2002-01-02 Merck & Co Inc Composes d'imidazopyridine inhibiteurs de la thrombine
CA2343109A1 (fr) * 1998-09-28 2000-04-06 Merck & Co., Inc. Inhibiteurs de la thrombine
AU747776B2 (en) 1998-10-30 2002-05-23 Merck & Co., Inc. Thrombin inhibitors
WO2000026210A1 (fr) 1998-10-30 2000-05-11 Merck & Co., Inc. Inhibiteurs de la thrombine
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
NZ512714A (en) 1999-01-13 2003-10-31 Astrazeneca Ab Amidinobenzylamine derivatives useful as thrombin inhibitors
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
US6239132B1 (en) 1999-04-23 2001-05-29 Merck & Co., Inc. Thrombin inhibitors
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
CA2374654A1 (fr) 1999-06-04 2000-12-14 Merck & Co., Inc. Inhibiteurs de la thrombine
EP1259506A1 (fr) 1999-11-23 2002-11-27 Merck & Co., Inc. Inhibiteurs de thrombine a base de pyrazinone
AU2207001A (en) * 1999-12-24 2001-07-09 Smithkline Beecham Plc Novel compounds and process
EP1267876A1 (fr) 2000-03-23 2003-01-02 Merck & Co., Inc. Inhibiteurs de thrombine
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
JP2004516286A (ja) 2000-12-18 2004-06-03 メルク エンド カムパニー インコーポレーテッド ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
CA2436176A1 (fr) 2001-02-09 2002-08-22 Merck & Co., Inc. Inhibiteurs de thrombine
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
BRPI0612045A2 (pt) * 2005-06-17 2018-07-24 Astrazeneca Ab composto, formulação farmacêutica, uso de um composto, método de tratamento de uma condição, e, processo para preparação de um composto
DE102006001574A1 (de) * 2006-01-12 2007-07-19 Bayer Healthcare Ag Acylaminoimidazole
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
CA2727925A1 (fr) * 2008-06-23 2009-12-30 Astrazeneca Ab Nouveaux carboxamides heterocycliques utilises comme inhibiteurs de thrombine
GB2494851A (en) * 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
EP2922535B1 (fr) 2012-11-20 2021-11-10 Merck Sharp & Dohme Corp. Inhibiteurs de thrombine
GB2517908A (en) * 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
WO2021032933A1 (fr) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Inhibiteurs d'enzymes

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62114957A (ja) * 1985-11-13 1987-05-26 Suntory Ltd プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジン誘導体およびその製法並びに用途
WO1994025051A1 (fr) * 1993-04-30 1994-11-10 Merck & Co., Inc. Inhibiteurs de thrombine

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62114957A (ja) * 1985-11-13 1987-05-26 Suntory Ltd プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジン誘導体およびその製法並びに用途
WO1994025051A1 (fr) * 1993-04-30 1994-11-10 Merck & Co., Inc. Inhibiteurs de thrombine

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
KIKUMOTO R ET AL: "SELECTIVE INHIBITION OF THROMBIN BY (2R,4R)-4-METHYL-1-U(38METHYL-1,2,3,4-TETRAHYDRO-8-QUINOLINYL) SULFONYL-L-ARGINYL)-2-PIPERIDINECARBOX YLIC ACID", BIOCHEMISTRY,US,AMERICAN CHEMICAL SOCIETY. EASTON, PA, vol. 23, no. 1, 3 January 1984 (1984-01-03), pages 85 - 90, XP002049060, ISSN: 0006-2960 *
PATENT ABSTRACTS OF JAPAN vol. 011, no. 332 (C - 455) 29 October 1987 (1987-10-29) *
See also references of WO9631504A1 *

Also Published As

Publication number Publication date
EP0820453A1 (fr) 1998-01-28
WO1996031504A1 (fr) 1996-10-10
AU698911B2 (en) 1998-11-12
CA2216859A1 (fr) 1996-10-10
JPH11503161A (ja) 1999-03-23
AU5438596A (en) 1996-10-23

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Legal Events

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

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