EP0820453A4 - Thrombin-inhibitoren - Google Patents

Thrombin-inhibitoren

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Withdrawn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
English (en)
French (fr)
Other versions
EP0820453A1 (de
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/de
Publication of EP0820453A4 publication Critical patent/EP0820453A4/de
Withdrawn legal-status Critical Current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)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP96911520A 1995-04-04 1996-04-01 Thrombin-inhibitoren Withdrawn EP0820453A4 (de)

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 (en) 1995-04-04 1996-04-01 Thrombin inhibitors

Publications (2)

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

Family

ID=23649178

Family Applications (1)

Application Number Title Priority Date Filing Date
EP96911520A Withdrawn EP0820453A4 (de) 1995-04-04 1996-04-01 Thrombin-inhibitoren

Country Status (5)

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

Families Citing this family (57)

* 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
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as 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
EP0977773A1 (de) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. Selektive faktor xa-inhibitoren
NZ500353A (en) 1997-04-14 2002-02-01 Cor Therapeutics Inc Cyclic diaza compounds that are selective inhibitors of factor 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
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
US6218382B1 (en) 1997-08-11 2001-04-17 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
AU742178B2 (en) * 1998-05-26 2001-12-20 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
CA2343109A1 (en) * 1998-09-28 2000-04-06 Merck & Co., Inc. Thrombin inhibitors
WO2000026210A1 (en) 1998-10-30 2000-05-11 Merck & Co., Inc. Thrombin inhibitors
JP2002528543A (ja) 1998-10-30 2002-09-03 メルク エンド カムパニー インコーポレーテッド トロンビン阻害剤
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
CA2355792A1 (en) 1999-01-13 2000-07-20 Astrazeneca Ab New amidinobenzylamine derivatives and their use 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
JP2003501389A (ja) 1999-06-04 2003-01-14 メルク エンド カムパニー インコーポレーテッド トロンビン阻害物質
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
WO2001038323A1 (en) 1999-11-23 2001-05-31 Merck & Co., Inc. Pyrazinone thrombin inhibitors
US20030199571A1 (en) * 1999-12-24 2003-10-23 Gordon Bruton (Hetero) Bicyclymethanesulfonylamino-substituted hydroxamic acid derivatives
WO2001070229A1 (en) 2000-03-23 2001-09-27 Merck & Co., Inc. Thrombin inhibitors
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
CA2431588A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
US7144899B2 (en) 2001-02-09 2006-12-05 Merck & Co., Inc. Thrombin inhibitors
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
UY29600A1 (es) * 2005-06-17 2007-01-31 Astrazeneca Ab Nuevos heterociclos como inhibidores de trombina, composiciones farmacéuticas que los contienen, procedimientos para su preparación y aplicaciones
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
UY31923A (es) * 2008-06-23 2010-01-29 Astrazeneca Ab Nuevos heterociclos para su uso como inhibidores de trombina
GB2494851A (en) * 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
WO2014081618A1 (en) * 2012-11-20 2014-05-30 Merck Sharp & Dohme Corp. Thrombin inhibitors
GB2517908A (en) * 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors

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 (en) * 1993-04-30 1994-11-10 Merck & Co., Inc. Thrombin inhibitors

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 (en) * 1993-04-30 1994-11-10 Merck & Co., Inc. Thrombin inhibitors

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

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Legal Events

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