ES2180933T3 - Inhibidor de la serina-proteasa. - Google Patents

Inhibidor de la serina-proteasa.

Info

Publication number
ES2180933T3
ES2180933T3 ES97905099T ES97905099T ES2180933T3 ES 2180933 T3 ES2180933 T3 ES 2180933T3 ES 97905099 T ES97905099 T ES 97905099T ES 97905099 T ES97905099 T ES 97905099T ES 2180933 T3 ES2180933 T3 ES 2180933T3
Authority
ES
Spain
Prior art keywords
proteasa
serina
inhibitor
thrombin
prevention
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
ES97905099T
Other languages
English (en)
Inventor
Anton Egbert Peter Adang
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.)
Akzo Nobel NV
Original Assignee
Akzo Nobel NV
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 Akzo Nobel NV filed Critical Akzo Nobel NV
Application granted granted Critical
Publication of ES2180933T3 publication Critical patent/ES2180933T3/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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • C07K5/02—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
    • 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
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

LA INVENCION SE REFIERE A UN COMPUESTO DE FORMULA (I), DONDE A, B, X, Y Y R SON TAL Y COMO SE LOS DEFINE EN LA DESCRIPCION, O BIEN UN PRECURSOR FARMACEUTICO O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO. DICHOS COMPUESTOS PRESENTAN ACTIVIDAD ANTICOAGULANTE Y SE PUEDEN UTILIZAR PARA EL TRATAMIENTO O PREVENCION DE ENFERMEDADES RELACIONADAS CON LA TROMBINA.
ES97905099T 1996-03-01 1997-02-26 Inhibidor de la serina-proteasa. Expired - Lifetime ES2180933T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP96200543 1996-03-01

Publications (1)

Publication Number Publication Date
ES2180933T3 true ES2180933T3 (es) 2003-02-16

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
ES97905099T Expired - Lifetime ES2180933T3 (es) 1996-03-01 1997-02-26 Inhibidor de la serina-proteasa.

Country Status (25)

Country Link
US (1) US6410684B1 (es)
EP (1) EP0886647B1 (es)
JP (1) JP2000506837A (es)
KR (1) KR19990087415A (es)
CN (1) CN1212704A (es)
AR (1) AR006310A1 (es)
AT (1) ATE221080T1 (es)
AU (1) AU709330B2 (es)
BR (1) BR9707808A (es)
CA (1) CA2246246A1 (es)
CZ (1) CZ277898A3 (es)
DE (1) DE69714222T2 (es)
DK (1) DK0886647T3 (es)
ES (1) ES2180933T3 (es)
HU (1) HUP9900390A3 (es)
IL (1) IL120310A (es)
NO (1) NO983991L (es)
NZ (1) NZ331484A (es)
PL (1) PL328875A1 (es)
PT (1) PT886647E (es)
RU (1) RU2178419C2 (es)
TR (1) TR199801704T2 (es)
TW (1) TW442452B (es)
WO (1) WO1997031937A1 (es)
ZA (1) ZA971667B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ291690B6 (cs) * 1996-02-13 2003-05-14 Akzo Nobel N. V. Inhibitory serinové proteázy a farmaceutický prostředek
JP2001525823A (ja) 1997-05-15 2001-12-11 イーライ・リリー・アンド・カンパニー 抗血栓化合物
CA2326763A1 (en) 1998-04-30 1999-11-11 Theodore O. Johnson, Jr. Antipicornaviral compounds and compositions, their pharmaceutical uses, and methods for their synthesis
WO2000009542A1 (en) * 1998-08-17 2000-02-24 Cortech, Inc. SERINE PROTEASE INHIBITORS COMPRISING α-KETO HETEROCYCLES
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
US6849605B1 (en) 1999-03-05 2005-02-01 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
AU3511500A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
EP1206484B1 (en) * 1999-08-04 2004-10-06 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
US6632825B2 (en) 2000-06-14 2003-10-14 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
KR20030081297A (ko) 2000-07-21 2003-10-17 쉐링 코포레이션 Ｃ형 간염 바이러스의 ｎｓ3-세린 프로테아제억제제로서의 신규한 펩티드
DK1385870T3 (da) 2000-07-21 2010-07-05 Schering Corp Peptider som inhibitorer af NS3-serinprotease fra hepatitis C-virus
JP2004518688A (ja) 2001-01-30 2004-06-24 ブリストル−マイヤーズ　スクイブ　カンパニー ファクターＸａ阻害剤のスルホンアミドラクタムおよびその方法
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
DE602005023965D1 (de) 2004-03-08 2010-11-18 Prosidion Ltd Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
ATE424821T1 (de) 2004-12-02 2009-03-15 Prosidion Ltd Pyrrolopyridin-2-karbonsäureamide
BRPI0823193A2 (pt) * 2008-10-15 2019-09-24 Danisco Us Inc inibidores de protease de bowman birk variantes modificados
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
PL3472149T3 (pl) 2016-06-21 2024-02-12 Orion Ophthalmology LLC Heterocykliczne pochodne prolinamidu
JP2023533016A (ja) 2020-07-11 2023-08-01 ファイザー・インク 抗ウイルス性ヘテロアリールケトン誘導体
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4556655A (en) * 1984-09-24 1985-12-03 Schering Corporation Antihypertensive compounds having both diuretic and angiotensin converting enzyme inhibitory activity
CA2008116C (en) * 1989-02-23 2001-11-20 Thomas Weller Glycine derivatives
ZW11290A1 (en) * 1989-07-14 1990-10-31 Smithkline Beecham Corp Hemoregulatory peptides
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
CA2159834A1 (en) * 1993-04-30 1994-11-10 Daniel F. Veber Thrombin inhibitors
SE9301916D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them
ZA951618B (en) 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5561146A (en) 1994-06-10 1996-10-01 Bristol-Myers Squibb Company Modified guanidino and amidino thrombin inhibitors
WO1995035311A1 (en) * 1994-06-17 1995-12-28 Corvas International, Inc. 3-amino-2-oxo-1-piperidineacetic derivatives as enzyme inhibitors
JPH0820597A (ja) * 1994-07-07 1996-01-23 Meiji Seika Kaisha Ltd トロンビン阻害作用を有する複素環カルボニル化合物
WO1996019483A1 (en) * 1994-12-22 1996-06-27 Biochem Pharma Inc. Low molecular weight bicyclic thrombin inhibitors

Also Published As

Publication number Publication date
TW442452B (en) 2001-06-23
HK1021541A1 (en) 2000-06-16
WO1997031937A1 (en) 1997-09-04
HUP9900390A2 (hu) 1999-06-28
ATE221080T1 (de) 2002-08-15
RU2178419C2 (ru) 2002-01-20
PL328875A1 (en) 1999-03-01
NZ331484A (en) 2000-01-28
ZA971667B (en) 1997-09-10
IL120310A0 (en) 1997-06-10
DE69714222D1 (de) 2002-08-29
KR19990087415A (ko) 1999-12-27
NO983991D0 (no) 1998-08-31
HUP9900390A3 (en) 2000-11-28
PT886647E (pt) 2002-12-31
AU709330B2 (en) 1999-08-26
DK0886647T3 (da) 2002-11-04
CA2246246A1 (en) 1997-09-04
CZ277898A3 (cs) 1999-06-16
US6410684B1 (en) 2002-06-25
AU1877597A (en) 1997-09-16
TR199801704T2 (xx) 1998-12-21
IL120310A (en) 2002-02-10
AR006310A1 (es) 1999-08-25
DE69714222T2 (de) 2003-02-20
CN1212704A (zh) 1999-03-31
EP0886647A1 (en) 1998-12-30
JP2000506837A (ja) 2000-06-06
NO983991L (no) 1998-10-30
EP0886647B1 (en) 2002-07-24
BR9707808A (pt) 1999-07-27

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