ATE177752T1 - Neue inhibitoren von faktor xa - Google Patents

Neue inhibitoren von faktor xa

Info

Publication number
ATE177752T1
ATE177752T1 AT94904466T AT94904466T ATE177752T1 AT E177752 T1 ATE177752 T1 AT E177752T1 AT 94904466 T AT94904466 T AT 94904466T AT 94904466 T AT94904466 T AT 94904466T AT E177752 T1 ATE177752 T1 AT E177752T1
Authority
AT
Austria
Prior art keywords
factor
novel compounds
disclosed
inhibitors
new inhibitors
Prior art date
Application number
AT94904466T
Other languages
English (en)
Inventor
Terence Kevin Brunck
Thomas Roy Webb
William Charles Ripka
Original Assignee
Corvas Int 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 Corvas Int Inc filed Critical Corvas Int Inc
Application granted granted Critical
Publication of ATE177752T1 publication Critical patent/ATE177752T1/de

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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AT94904466T 1992-12-15 1993-12-15 Neue inhibitoren von faktor xa ATE177752T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US99120492A 1992-12-15 1992-12-15

Publications (1)

Publication Number Publication Date
ATE177752T1 true ATE177752T1 (de) 1999-04-15

Family

ID=25536978

Family Applications (1)

Application Number Title Priority Date Filing Date
AT94904466T ATE177752T1 (de) 1992-12-15 1993-12-15 Neue inhibitoren von faktor xa

Country Status (7)

Country Link
US (2) US5883077A (de)
EP (1) EP0675899B1 (de)
JP (1) JPH08504769A (de)
AT (1) ATE177752T1 (de)
CA (1) CA2151044A1 (de)
DE (1) DE69324041D1 (de)
WO (1) WO1994013693A1 (de)

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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
ATE251141T1 (de) * 1995-03-10 2003-10-15 Berlex Lab Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
US5691364A (en) * 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
US5612363A (en) * 1995-06-02 1997-03-18 Berlex Laboratories, Inc. N,N-di(aryl) cyclic urea derivatives as anti-coagulants
US5612378A (en) * 1995-06-06 1997-03-18 3-Dimensional Pharmaceuticals, Inc. Bis-arylsulfonylaminobenzamide derivatives and the use thereof as factor Xa inhibitors
US5741819A (en) * 1995-06-07 1998-04-21 3-Dimensional Pharmaceuticals, Inc. Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
US6046169A (en) * 1995-06-07 2000-04-04 Cor Therapeutics, Inc. Inhibitors of factor XA
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US5849759A (en) * 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
US5994375A (en) * 1996-02-12 1999-11-30 Berlex Laboratories, Inc. Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
HU222199B1 (hu) * 1996-06-05 2003-05-28 Gyógyszerkutató Intézet Kft. Véralvadásgátló hatású peptid-aldehid-származékok és a vegyületeket tartalmazó gyógyszerkészítmények
US6245743B1 (en) 1996-06-05 2001-06-12 Cor Therapeutics, Inc. Inhibitors of factor Xa
US5693641A (en) * 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
US5753635A (en) * 1996-08-16 1998-05-19 Berlex Laboratories, Inc. Purine derivatives and their use as anti-coagulants
US6008234A (en) * 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
WO1998011094A1 (en) 1996-09-12 1998-03-19 Schering Aktiengesellschaft Benzamidine derivatives substituted by cyclic amino acid or cycl ic hydroxy acid derivatives and their use as anti-coagulants
US6004985A (en) * 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. 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
CA2285659A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0977772A1 (de) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. Selektive faktor xa-inhibitoren
CA2285705A1 (en) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
AU7603098A (en) * 1997-06-06 1998-12-21 Emory University Exosite assay for anticoagulants
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6011047A (en) * 1997-11-26 2000-01-04 Corvas International Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors
US6204384B1 (en) 1997-11-26 2001-03-20 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
US6686364B2 (en) 1997-12-08 2004-02-03 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
US6140351A (en) * 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
EP1040108B1 (de) 1997-12-19 2004-02-25 Schering Aktiengesellschaft Ortho-anthranilamide derivate als antikoagulantien
AP1224A (en) 1998-03-19 2003-11-14 Bristol Myers Squibb Co Biphasic controlled release delivery system for high solubility pharmaceuticals and method.
US6787612B1 (en) 1998-07-24 2004-09-07 Dendreon Corporation Resin derivatization method and uses thereof
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) * 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
US6545054B1 (en) 1999-02-11 2003-04-08 Millennium Pharmaceuticals, Inc. Alkenyl and alkynyl compounds as inhibitors of factor Xa
US6350761B1 (en) 1999-07-30 2002-02-26 Berlex Laboratories, Inc. Benzenamine derivatives as anti-coagulants
WO2001036351A2 (en) 1999-11-19 2001-05-25 Corvas International, Inc. Plasminogen activator inhibitor antagonists related applications
AU2001250783A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
US7157596B2 (en) 2000-09-08 2007-01-02 Dendreon Corporation Inhibitors of serine protease activity of matriptase or MTSP1
DE60122750T2 (de) 2000-09-11 2006-12-21 Genentech, Inc., South San Francisco Amidin-Inhibitoren von Serin-Proteasen
US7312235B2 (en) 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
US6777431B2 (en) 2001-07-13 2004-08-17 Corvas International, Inc. Non-convalent thrombin inhibitors
EP1451147A4 (de) * 2001-07-24 2007-06-06 Pharmacore Inc Aminosäurederivate
EP1569912B1 (de) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidinderivate als faktor vii-a hemmer
IES20030299A2 (en) * 2002-04-23 2003-10-29 R Stephen Porter Inhibition of platelet aggregation
US6872827B2 (en) 2002-04-26 2005-03-29 Chembridge Research Laboratories, Inc. Somatostatin analogue compounds
US7019019B2 (en) * 2002-12-23 2006-03-28 Dendreon Corporation Matriptase inhibitors and methods of use
CA2525713A1 (en) 2003-05-20 2004-12-29 Genentech, Inc. Benzofuran inhibitors of factor viia
AU2004249670A1 (en) 2003-05-20 2004-12-29 Genentech, Inc. Acylsulfamide inhibitors of factor VIIa
CN1886398A (zh) 2003-10-09 2006-12-27 米伦纽姆医药公司 作为Xa因子抑制剂的经硫醚取代的苯甲酰胺
NZ552187A (en) 2004-06-18 2010-08-27 Millennium Pharm Inc Thiophene-2-carboxamide derivatives
WO2006055951A2 (en) 2004-11-19 2006-05-26 Portola Pharmaceuticals, Inc. Tetrahydroisoquinolines as factor xa inhibitors
US7678913B2 (en) 2004-12-07 2010-03-16 Portola Pharmaceuticals, Inc. Ureas as factor Xa inhibitors
CN102336702B (zh) 2005-11-08 2015-02-11 米伦纽姆医药公司 Xa因子抑制剂n-(5-氯-2-吡啶基)-2-[[4-[(二甲氨基)亚氨基甲基]苯甲酰基]氨基]-5-甲氧基-苯甲酰胺的医药盐和多晶型
EP2077995B1 (de) 2006-11-02 2012-02-08 Millennium Pharmaceuticals, Inc. Verfahren zur synthetisierung pharmazeutischer salze aus einem faktor-xa-hemmer
CN103153288B (zh) 2010-07-09 2017-02-15 詹姆斯·特林卡·格林 用于包括瑞格列净的短半衰期药物的组合立即/延迟释放递送系统
CA2961739C (en) 2014-08-20 2024-04-30 Portola Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
CN108883160B (zh) 2016-02-24 2022-06-28 博尔托拉制药公司 因子xa解毒剂的冻干制剂

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US4847201A (en) * 1985-02-05 1989-07-11 Cetus Corporation DNA encoding for CSF-1 and accompanying recombinant systems
US4882145A (en) * 1986-12-09 1989-11-21 Scripps Clinic And Research Foundation T cell epitopes of the hepatitis B virus nucleocapsid protein
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
US5200510A (en) * 1987-06-16 1993-04-06 Zymogenetics, Inc. Method for purifying factor viii:c, von willebrand factor and complexes thereof
JPH075634B2 (ja) * 1987-10-30 1995-01-25 日東紡績株式会社 トリペプチド類及びこれを含有する抗プラスミン剤
US5141862A (en) * 1990-04-17 1992-08-25 Smithkline Beecham Corporation Method of purifying tpa or plasminogen activator using a tripeptide of the formula: -X-Y-argininal wherein X and Y are selected from the group consisting of pro,phe,trp and tyr
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
US5367072A (en) * 1990-12-14 1994-11-22 Corvas International, Inc. Reagents for automated synthesis of peptide analogs
US5283293A (en) * 1990-12-14 1994-02-01 Corvas, Inc. Reagents for automated synthesis of peptide analogs
WO1993008211A1 (en) * 1991-10-23 1993-04-29 The Procter & Gamble Company Tripeptide derivative anti-inflammatory agents
AU1339092A (en) * 1991-12-13 1993-07-19 Corvas International, Inc. Reagents for automated synthesis of peptide analogs
US5534498A (en) * 1992-01-30 1996-07-09 Corvas International, Inc. Trypsin inhibitors

Also Published As

Publication number Publication date
WO1994013693A1 (en) 1994-06-23
US5739112A (en) 1998-04-14
EP0675899B1 (de) 1999-03-17
CA2151044A1 (en) 1994-06-23
EP0675899A4 (de) 1996-01-24
US5883077A (en) 1999-03-16
DE69324041D1 (de) 1999-04-22
JPH08504769A (ja) 1996-05-21
EP0675899A1 (de) 1995-10-11

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Legal Events

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