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ES2184763T3 - Inhibidores de trombina. - Google Patents

Inhibidores de trombina.

Info

Publication number
ES2184763T3
ES2184763T3 ES94915883T ES94915883T ES2184763T3 ES 2184763 T3 ES2184763 T3 ES 2184763T3 ES 94915883 T ES94915883 T ES 94915883T ES 94915883 T ES94915883 T ES 94915883T ES 2184763 T3 ES2184763 T3 ES 2184763T3
Authority
ES
Spain
Prior art keywords
thrombin inhibitors
thrombin
anticoagulants
trypsin
enzymes
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 - Lifetime
Application number
ES94915883T
Other languages
English (en)
Inventor
Daniel F Veber
S Dale Lewis
Jules A Shafer
Dong-Mei Feng
Ruth F Nutt
Stephen F Brady
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
Application granted granted Critical
Publication of ES2184763T3 publication Critical patent/ES2184763T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • C07K5/08—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
    • 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
    • C07K5/0202—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-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE PRESENTAN DERIVADOS DEL CICLOHEXILAMINO 4-SUSTITUIDO QUE SON INHIBIDORES DE LA ZONA CATALITICA DE LA TROMBINA Y QUE SON UTILES COMO ANTICOAGULANTES. ESTOS COMPUESTOS MUESTRAN SELECTIVIDAD PARA LA TROMBINA SOBRE OTRAS ENZIMAS SIMILARES A LA TRIPSINA Y TIENEN BIOCAPACIDAD ORAL. PRESENTAN LA FORMULA (A) O (B), POR EJEMPLO (C).
ES94915883T 1993-04-30 1994-04-25 Inhibidores de trombina. Expired - Lifetime ES2184763T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US5561193A 1993-04-30 1993-04-30

Publications (1)

Publication Number Publication Date
ES2184763T3 true ES2184763T3 (es) 2003-04-16

Family

ID=21999019

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94915883T Expired - Lifetime ES2184763T3 (es) 1993-04-30 1994-04-25 Inhibidores de trombina.

Country Status (8)

Country Link
EP (1) EP0699074B1 (es)
JP (1) JP3486412B2 (es)
AT (1) ATE227581T1 (es)
AU (1) AU670381B2 (es)
CA (1) CA2159834A1 (es)
DE (1) DE69431718T2 (es)
ES (1) ES2184763T3 (es)
WO (1) WO1994025051A1 (es)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5658885A (en) * 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
JPH11503161A (ja) * 1995-04-04 1999-03-23 メルク エンド カンパニー インコーポレーテッド トロンビン阻害剤
US6046169A (en) * 1995-06-07 2000-04-04 Cor Therapeutics, Inc. Inhibitors of factor XA
US6022861A (en) * 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6211154B1 (en) * 1995-06-07 2001-04-03 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
JP2008024720A (ja) * 1995-07-26 2008-02-07 Mitsubishi Chemicals Corp ペニシラミンアミド誘導体
AU725483B2 (en) * 1995-07-26 2000-10-12 Mitsubishi Chemical Corporation Penicillaminamide derivatives
US6069232A (en) * 1995-10-02 2000-05-30 Hoechst Marion Roussel, Inc. Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors
CZ291690B6 (cs) * 1996-02-13 2003-05-14 Akzo Nobel N. V. Inhibitory serinové proteázy a farmaceutický prostředek
TW442452B (en) 1996-03-01 2001-06-23 Akzo Nobel Nv Serine protease inhibitors having an alkynylamino side chain
TW523513B (en) * 1996-03-01 2003-03-11 Akzo Nobel Nv Serine protease inhibitors
US5739354A (en) * 1996-03-26 1998-04-14 Hoechst Marion Roussel, Inc. Process for the preparation of N-methyl-D-phenylalanyl-N- 1- 3- (aminoiminomethyl)amino!propyl!-3,3-difluoro-2-oxohexyl!-L-prolinamide
US6245743B1 (en) 1996-06-05 2001-06-12 Cor Therapeutics, Inc. Inhibitors of factor Xa
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
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
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa 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
AU6896298A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0977773A1 (en) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6133256A (en) * 1997-04-14 2000-10-17 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
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
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1082324A4 (en) * 1998-05-26 2002-01-02 Merck & Co Inc IMIDAZOPYRIDINE COMPOUNDS AS THROMBINE INHIBITORS
WO2000018762A1 (en) * 1998-09-28 2000-04-06 Merck & Co., Inc. Thrombin inhibitors
EP1124822A4 (en) 1998-10-30 2002-04-03 Merck & Co Inc THROMBIN INHIBITORS
JP2002528542A (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
US6239132B1 (en) 1999-04-23 2001-05-29 Merck & Co., Inc. Thrombin inhibitors
CA2374654A1 (en) 1999-06-04 2000-12-14 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
WO2001038323A1 (en) 1999-11-23 2001-05-31 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1267876A1 (en) 2000-03-23 2003-01-02 Merck & Co., Inc. Thrombin inhibitors
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
CN102725300B (zh) 2009-12-22 2015-03-11 赛福伦公司 蛋白酶体抑制剂及其制备、纯化、和应用的方法
JP2015083542A (ja) * 2012-02-08 2015-04-30 大日本住友製薬株式会社 ３位置換プロリン誘導体
MX392422B (es) 2016-06-21 2025-03-24 Orion Ophthalmology LLC Derivados de prolinamida heterociclica
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
BR112020019325A2 (pt) * 2018-03-28 2021-01-05 Blade Therapeutics, Inc. Método de tratamento de doença fibrótica

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1161431A (en) * 1979-05-11 1984-01-31 Lars G. Svendsen Tripeptide derivatives
HU178398B (en) * 1979-06-12 1982-04-28 Gyogyszerkutato Intezet Process for producing new agmatine derivatives of activity against haemagglutination
HU192646B (en) * 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
GB9024129D0 (en) * 1990-11-06 1990-12-19 Thrombosis Research Trust Inhibitors and substrates of thrombin

Also Published As

Publication number Publication date
EP0699074A1 (en) 1996-03-06
DE69431718D1 (de) 2002-12-19
DE69431718T2 (de) 2003-07-10
JP3486412B2 (ja) 2004-01-13
ATE227581T1 (de) 2002-11-15
EP0699074B1 (en) 2002-11-13
WO1994025051A1 (en) 1994-11-10
CA2159834A1 (en) 1994-11-10
JPH08509735A (ja) 1996-10-15
AU6773894A (en) 1994-11-21
EP0699074A4 (en) 1998-03-11
AU670381B2 (en) 1996-07-11

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