EP0820453A4 - Thrombin inhibitors - Google Patents

Thrombin inhibitors

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Withdrawn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)
French (fr)
Other versions
EP0820453A1 (en
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/en
Publication of EP0820453A4 publication Critical patent/EP0820453A4/en
Withdrawn legal-status Critical Current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
EP96911520A 1995-04-04 1996-04-01 Thrombin inhibitors Withdrawn EP0820453A4 (en)

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 (en) 1998-01-28
EP0820453A4 true EP0820453A4 (en) 2001-08-29

Family

ID=23649178

Family Applications (1)

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EP96911520A Withdrawn EP0820453A4 (en) 1995-04-04 1996-04-01 Thrombin inhibitors

Country Status (5)

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

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 (en) 1995-12-21 1999-04-28 Astrazeneca Ab THROMBIN INHIBITOR PRODROGES, A PHARMACEUTICAL FORMULATION THAT INCLUDES THEM, THE USE OF SUCH PRODROGES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND A PROCEDURE FOR ITS PREPARATION
SE9602263D0 (en) 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
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
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
WO1998046626A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
CA2285705A1 (en) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
AR013084A1 (en) 1997-06-19 2000-12-13 Astrazeneca Ab USEFUL AMIDINE DERIVATIVES AS THROMBIN INHIBITORS, PHARMACEUTICAL COMPOSITION, USE OF SUCH COMPOUNDS FOR THE PREPARATION OF MEDICINES AND THE PROCESS FOR THE PREPARATION OF THE MENTIONED COMPOUNDS
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 (en) 1997-12-05 1997-12-05 Astra Ab New compounds
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
WO1999061442A1 (en) * 1998-05-26 1999-12-02 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
EP1117660A4 (en) * 1998-09-28 2002-01-09 Merck & Co Inc Thrombin inhibitors
EP1124823A1 (en) 1998-10-30 2001-08-22 Merck & Co., Inc. Thrombin inhibitors
EP1124822A4 (en) 1998-10-30 2002-04-03 Merck & Co Inc Thrombin inhibitors
SE9804313D0 (en) 1998-12-14 1998-12-14 Astra Ab New compounds
CN1170842C (en) 1999-01-13 2004-10-13 阿斯特拉曾尼卡有限公司 New amidinobenzylamine derivatives and their use as thrombin inhibitors
AR023510A1 (en) 1999-04-21 2002-09-04 Astrazeneca Ab A TEAM OF PARTS, PHARMACEUTICAL FORMULATION AND USE OF A THROMBIN INHIBITOR.
US6239132B1 (en) 1999-04-23 2001-05-29 Merck & Co., Inc. Thrombin inhibitors
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
WO2000074682A1 (en) 1999-06-04 2000-12-14 Merck & Co., Inc. Thrombin inhibitors
JP2003514905A (en) 1999-11-23 2003-04-22 メルク エンド カムパニー インコーポレーテッド Pyrazinone thrombin inhibitors
AU2207001A (en) * 1999-12-24 2001-07-09 Smithkline Beecham Plc Novel compounds and process
AU2001245856A1 (en) 2000-03-23 2001-10-03 Merck & Co., Inc. Thrombin inhibitors
SE0001803D0 (en) 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
AR035216A1 (en) 2000-12-01 2004-05-05 Astrazeneca Ab MANDELIC ACID DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE DERIVATIVES, USE OF THESE DERIVATIVES FOR THE MANUFACTURE OF MEDICINES, TREATMENT METHODS, PROCESSES FOR THE PREPARATION OF THESE DERIVATIVES, AND INTERMEDIARY COMPOUNDS
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AU2002230836A1 (en) 2000-12-18 2002-07-01 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 (en) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
SE0201661D0 (en) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
CA2610428A1 (en) * 2005-06-17 2006-12-21 Astrazeneca Ab Thrombin inhibiting 2-oxo-1, 2, 5, 6-tetrahydropyridine derivatives
DE102006001574A1 (en) * 2006-01-12 2007-07-19 Bayer Healthcare Ag Acylaminoimidazole
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
CN102131802A (en) * 2008-06-23 2011-07-20 阿斯利康(瑞典)有限公司 New heterocyclic carboxamides for use as thrombin inhibitors
GB2494851A (en) * 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
EP2922535B1 (en) 2012-11-20 2021-11-10 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 (en) * 1985-11-13 1987-05-26 Suntory Ltd Novel pyrrolidine derivative having prolylendopeptidase inhibiting action its production and use thereof
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 (en) * 1985-11-13 1987-05-26 Suntory Ltd Novel pyrrolidine derivative having prolylendopeptidase inhibiting action its production and use thereof
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
EP0820453A1 (en) 1998-01-28
WO1996031504A1 (en) 1996-10-10
AU5438596A (en) 1996-10-23
AU698911B2 (en) 1998-11-12
JPH11503161A (en) 1999-03-23

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