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NO983991L - Serin-protease-inhibitorer - Google Patents

Serin-protease-inhibitorer

Info

Publication number
NO983991L
NO983991L NO983991A NO983991A NO983991L NO 983991 L NO983991 L NO 983991L NO 983991 A NO983991 A NO 983991A NO 983991 A NO983991 A NO 983991A NO 983991 L NO983991 L NO 983991L
Authority
NO
Norway
Prior art keywords
protease inhibitors
serine protease
thrombin
prodrug
prevention
Prior art date
Application number
NO983991A
Other languages
English (en)
Other versions
NO983991D0 (no
Inventor
Anton Egbert Peter Adang
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
Publication of NO983991D0 publication Critical patent/NO983991D0/no
Publication of NO983991L publication Critical patent/NO983991L/no

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)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (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

Oppfinnelsen vedrører en forbindelse med formel (I), hvor A, B, X, Y og r er som definert i beskrivelsen, eller et promedikament derav eller et famasøytisk akseptabelt salt derav. Forbindelsene ifølge oppfinnelsen har antikoagulerende aktivitet og kan anvendes i behandling eller forbyggelse av trombinrelaterte sykdommer.
NO983991A 1996-03-01 1998-08-31 Serin-protease-inhibitorer NO983991L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP96200543 1996-03-01
PCT/EP1997/000938 WO1997031937A1 (en) 1996-03-01 1997-02-26 Serine protease inhibitors

Publications (2)

Publication Number Publication Date
NO983991D0 NO983991D0 (no) 1998-08-31
NO983991L true NO983991L (no) 1998-10-30

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
NO983991A NO983991L (no) 1996-03-01 1998-08-31 Serin-protease-inhibitorer

Country Status (26)

Country Link
US (1) US6410684B1 (no)
EP (1) EP0886647B1 (no)
JP (1) JP2000506837A (no)
KR (1) KR19990087415A (no)
CN (1) CN1212704A (no)
AR (1) AR006310A1 (no)
AT (1) ATE221080T1 (no)
AU (1) AU709330B2 (no)
BR (1) BR9707808A (no)
CA (1) CA2246246A1 (no)
CZ (1) CZ277898A3 (no)
DE (1) DE69714222T2 (no)
DK (1) DK0886647T3 (no)
ES (1) ES2180933T3 (no)
HK (1) HK1021541A1 (no)
HU (1) HUP9900390A3 (no)
IL (1) IL120310A (no)
NO (1) NO983991L (no)
NZ (1) NZ331484A (no)
PL (1) PL328875A1 (no)
PT (1) PT886647E (no)
RU (1) RU2178419C2 (no)
TR (1) TR199801704T2 (no)
TW (1) TW442452B (no)
WO (1) WO1997031937A1 (no)
ZA (1) ZA971667B (no)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU719216B2 (en) * 1996-02-13 2000-05-04 Akzo Nobel N.V. Serine protease inhibitors
US6214841B1 (en) 1997-05-15 2001-04-10 Eli Lilly And Company Antithrombotic compound
SI20428A (sl) 1998-04-30 2001-06-30 Agouron Pharmaceuticals, Inc. Antipicornavirusne spojine, njihova priprava in uporaba
WO2000009542A1 (en) * 1998-08-17 2000-02-24 Cortech, Inc. SERINE PROTEASE INHIBITORS COMPRISING α-KETO HETEROCYCLES
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
US7704958B1 (en) 1999-03-05 2010-04-27 Bio Holding, Inc. Methods and compositions for inhibiting apoptosis using serine protease inhibitors
US6489308B1 (en) 1999-03-05 2002-12-03 Trustees Of University Of Technology Corporation 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
CN1525957A (zh) 2000-06-14 2004-09-01 ������ҩ�����޹�˾ 抗细小核糖核酸病毒的化合物与组合物,它们的药物用途,以及用于其合成的物质
SK288064B6 (sk) 2000-07-21 2013-04-03 Merck Sharp & Dohme Corp. Peptide compounds, pharmaceutical compositions comprising them and their use
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
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
ATE483708T1 (de) 2004-03-08 2010-10-15 Prosidion Ltd Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
EP1819332B1 (en) 2004-12-02 2009-03-11 Prosidion Limited Pyrrolopyridine-2-carboxylic acid amides
EP2344531B1 (en) * 2008-10-15 2014-12-10 Danisco US Inc. Modified variant bowman birk protease inhibitors
KR20230153504A (ko) 2016-06-21 2023-11-06 오리온 옵탈몰로지 엘엘씨 헤테로시클릭 프롤린아미드 유도체
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds

Family Cites Families (10)

* 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
ZW11290A1 (en) * 1989-07-14 1990-10-31 Smithkline Beecham Corp Hemoregulatory peptides
ES2184763T3 (es) 1993-04-30 2003-04-16 Merck & Co Inc Inhibidores de trombina.
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
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
JPH11508535A (ja) 1994-12-22 1999-07-27 バイオケム ファーマ インコーポレイテッド 低分子量２環式トロンビン阻害剤

Also Published As

Publication number Publication date
TW442452B (en) 2001-06-23
DE69714222T2 (de) 2003-02-20
ES2180933T3 (es) 2003-02-16
HK1021541A1 (en) 2000-06-16
WO1997031937A1 (en) 1997-09-04
ATE221080T1 (de) 2002-08-15
BR9707808A (pt) 1999-07-27
AU709330B2 (en) 1999-08-26
PL328875A1 (en) 1999-03-01
NO983991D0 (no) 1998-08-31
TR199801704T2 (xx) 1998-12-21
EP0886647A1 (en) 1998-12-30
DK0886647T3 (da) 2002-11-04
IL120310A (en) 2002-02-10
HUP9900390A2 (hu) 1999-06-28
HUP9900390A3 (en) 2000-11-28
CA2246246A1 (en) 1997-09-04
CN1212704A (zh) 1999-03-31
EP0886647B1 (en) 2002-07-24
ZA971667B (en) 1997-09-10
AU1877597A (en) 1997-09-16
PT886647E (pt) 2002-12-31
KR19990087415A (ko) 1999-12-27
IL120310A0 (en) 1997-06-10
CZ277898A3 (cs) 1999-06-16
AR006310A1 (es) 1999-08-25
DE69714222D1 (de) 2002-08-29
RU2178419C2 (ru) 2002-01-20
JP2000506837A (ja) 2000-06-06
US6410684B1 (en) 2002-06-25
NZ331484A (en) 2000-01-28

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