DE69507062D1 - Verbindungen zur Hemmung der Thrombin - Google Patents

Verbindungen zur Hemmung der Thrombin

Info

Publication number
DE69507062D1
DE69507062D1 DE69507062T DE69507062T DE69507062D1 DE 69507062 D1 DE69507062 D1 DE 69507062D1 DE 69507062 T DE69507062 T DE 69507062T DE 69507062 T DE69507062 T DE 69507062T DE 69507062 D1 DE69507062 D1 DE 69507062D1
Authority
DE
Germany
Prior art keywords
compounds
inhibit thrombin
inhibitors
thrombin
chem
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.)
Expired - Fee Related
Application number
DE69507062T
Other languages
English (en)
Other versions
DE69507062T2 (de
Inventor
Aaron Leigh Schacht
Gerald Floyd Smith
Michael Robert Wiley
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of DE69507062D1 publication Critical patent/DE69507062D1/de
Publication of DE69507062T2 publication Critical patent/DE69507062T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides 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
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
DE69507062T 1994-03-04 1995-03-03 Verbindungen zur Hemmung der Thrombin Expired - Fee Related DE69507062T2 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/206,351 US5885967A (en) 1994-03-04 1994-03-04 Antithrombotic agents

Publications (2)

Publication Number Publication Date
DE69507062D1 true DE69507062D1 (de) 1999-02-18
DE69507062T2 DE69507062T2 (de) 1999-06-10

Family

ID=22765975

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69507062T Expired - Fee Related DE69507062T2 (de) 1994-03-04 1995-03-03 Verbindungen zur Hemmung der Thrombin

Country Status (10)

Country Link
US (3) US5885967A (de)
EP (1) EP0672659B1 (de)
JP (1) JPH07258287A (de)
AT (1) ATE175404T1 (de)
CA (1) CA2143536A1 (de)
DE (1) DE69507062T2 (de)
DK (1) DK0672659T3 (de)
ES (1) ES2126211T3 (de)
GR (1) GR3029389T3 (de)
SI (1) SI0672659T1 (de)

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US6342504B1 (en) 1994-12-13 2002-01-29 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US6011158A (en) * 1994-12-13 2000-01-04 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US6025472A (en) * 1994-12-21 2000-02-15 Corvas International, Inc. N-substituted glycine derivatives as enzyme inhibitors
US5696231A (en) * 1994-12-21 1997-12-09 Corvas International, Inc. N-substituted glycine derivatives as enzyme inhibitors
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
JP3095787B2 (ja) * 1996-10-31 2000-10-10 ロシュ ダイアグノスティックス ゲーエムベーハー ＩＸａ因子の触媒活性の測定方法
WO1999026920A1 (en) * 1997-11-26 1999-06-03 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (ii)
US6204384B1 (en) 1997-11-26 2001-03-20 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
UA75093C2 (en) * 2000-10-06 2006-03-15 Dimensional Pharm Inc Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors
BR0215098A (pt) * 2001-11-26 2004-12-14 Genentech Inc Composição útil para remoção de coágulos de sangue, método para a remoção de coágulos de sangue, catéter e embalagens de múltiplos compartimentos
CU23203A1 (es) 2002-12-27 2007-05-18 Ct Ingenieria Genetica Biotech Formulaciones que contienen agentes de accion trombolitica para su administracion por via rectal
US7267971B2 (en) * 2003-03-25 2007-09-11 Council Of Scientific And Industrial Research Process for preparation of thermostable enzyme
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
EP1725555B1 (de) 2004-03-08 2010-10-06 Prosidion Ltd. Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
WO2006059164A2 (en) 2004-12-02 2006-06-08 Prosidion Limited Pyrrolopyridine-2-carboxylic acid amides
US7914705B2 (en) * 2005-01-10 2011-03-29 Robert Eliot Sisson Flowable electrical conductive liquid
WO2006101937A1 (en) 2005-03-18 2006-09-28 Janssen Pharmaceutica N.V. Acylhydrazones as kinase modulators
US20070086958A1 (en) * 2005-10-14 2007-04-19 Medafor, Incorporated Formation of medically useful gels comprising microporous particles and methods of use
US20070087061A1 (en) * 2005-10-14 2007-04-19 Medafor, Incorporated Method and composition for creating and/or activating a platelet-rich gel by contact with a porous particulate material, for use in wound care, tissue adhesion, or as a matrix for delivery of therapeutic components
EP2086571A2 (de) 2006-11-07 2009-08-12 Genentech, Inc. Anwendungen einer gewebe-plasminogen-aktivator-variante
US7850997B2 (en) * 2007-03-21 2010-12-14 Tim Romero Dietary compositions and methods of enhancing lean body mass and exercise performance

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HU177098B (en) * 1979-01-04 1981-07-28 Gyogyszerkutato Intezet Process for producing new peptidyl-n-carboxy-l-arginin-a
HU178398B (en) * 1979-06-12 1982-04-28 Gyogyszerkutato Intezet Process for producing new agmatine derivatives of activity against haemagglutination
HU184368B (en) * 1981-01-13 1984-08-28 Gyogyszerkutato Intezet Process for preparing d-phenyl-alanyl-l-propyl-l-arginine-ald ehyde-shulphate
HU192646B (en) * 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
DE3827415A1 (de) * 1988-08-12 1990-02-15 Behringwerke Ag Peptidderivate, verfahren zu ihrer herstellung und ihre verwendung
US5204323B1 (en) * 1988-10-06 1995-07-18 Ciba Geigy Corp Hirudin antidotal compositions and methods
EP0369391A3 (de) * 1988-11-15 1991-09-25 Boehringer Ingelheim Pharmaceuticals Inc. N-substituierte Amide
GB8910550D0 (en) * 1989-05-08 1989-06-21 Ici America Inc Substituted amides
GB8910547D0 (en) * 1989-05-08 1989-06-21 Ici America Inc Substituted ketones
CA2021660A1 (en) * 1989-07-26 1991-01-27 Philippe Bey Peptidase inhibitors
US5053392A (en) * 1989-12-01 1991-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Novel arginine, glycine, aspartic acid derivatives as platelet-aggregation inhibitors
JPH0813834B2 (ja) * 1990-08-01 1996-02-14 日東紡績株式会社 トリペプチド誘導体及びそれを有効成分とする蛋白分解酵素阻害剤
US5430023A (en) * 1990-09-28 1995-07-04 Eli Lilly And Company Tripeptide antithrombotic agents
IL99527A (en) * 1990-09-28 1997-08-14 Lilly Co Eli Tripeptide antithrombotic agents
EP0503203A1 (de) * 1991-03-15 1992-09-16 Merrell Dow Pharmaceuticals Inc. Neue Thrombin-Inhibitoren
CA2075154A1 (en) * 1991-08-06 1993-02-07 Neelakantan Balasubramanian Peptide aldehydes as antithrombotic agents
ZA926185B (en) * 1991-08-22 1993-03-01 Merrell Dow Pharma Novel orally-active elastase inhibitors.
SE9102462D0 (sv) * 1991-08-28 1991-08-28 Astra Ab New isosteric peptides
WO1993008211A1 (en) * 1991-10-23 1993-04-29 The Procter & Gamble Company Tripeptide derivative anti-inflammatory agents
US5416093A (en) * 1991-11-12 1995-05-16 Eli Lilly And Company Antithrombotic agents
US5252566A (en) * 1991-11-12 1993-10-12 Eli Lilly And Company Antithrombotic agents
US5250660A (en) * 1991-11-12 1993-10-05 Eli Lilly And Company Peptide purification process
CZ333492A3 (en) * 1991-11-12 1993-09-15 Lilly Co Eli Dipeptide of l-azetidine-2-carboxylic acids and l-argininaldehyde, process of its preparation and pharmaceutical preparation in which said dipeptide is comprised
SE9103612D0 (sv) * 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
EP0627929B1 (de) * 1992-02-14 1998-09-30 Corvas International, Inc. Inhibitoren der thrombose
AU675981B2 (en) * 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
SE9301911D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptide derivatives
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
EP0648780A1 (de) * 1993-08-26 1995-04-19 Bristol-Myers Squibb Company Heterozyklische Thrombinhemmer
IL111176A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
EP0722449A1 (de) * 1993-10-07 1996-07-24 The Du Pont Merck Pharmaceutical Company Boropeptid thrombin-inhibitoren, welche einen substituierten pyrrolidinring enthalten
IL111175A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
US5439888A (en) * 1994-03-04 1995-08-08 Eli Lilly And Company Antithrombotic agents
US5436229A (en) * 1994-03-04 1995-07-25 Eli Lilly And Company Bisulfite adducts of arginine aldehydes
US5484772A (en) * 1994-03-04 1996-01-16 Eli Lilly And Company Antithrombotic agents
US5488037A (en) * 1994-03-04 1996-01-30 Eli Lilly And Company Antithrombotic agents
FR2718451B1 (fr) * 1994-04-12 1996-05-10 Synthelabo Dérivés de peptides boroniques, leur préparation et leur application en thérapeutique.
FR2721611B1 (fr) * 1994-06-22 1996-09-27 Adir Nouveaux dérivés peptidiques de l'acide boronique, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent .

Also Published As

Publication number Publication date
US5885967A (en) 1999-03-23
EP0672659B1 (de) 1999-01-07
US6090787A (en) 2000-07-18
DE69507062T2 (de) 1999-06-10
GR3029389T3 (en) 1999-05-28
JPH07258287A (ja) 1995-10-09
US6124277A (en) 2000-09-26
CA2143536A1 (en) 1995-09-05
EP0672659A1 (de) 1995-09-20
SI0672659T1 (en) 1999-04-30
DK0672659T3 (da) 1999-05-17
ES2126211T3 (es) 1999-03-16
ATE175404T1 (de) 1999-01-15

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee