TR199801704T2 - Serin proteaz inhibit�rleri. - Google Patents

Serin proteaz inhibit�rleri.

Info

Publication number
TR199801704T2
TR199801704T2 TR1998/01704T TR9801704T TR199801704T2 TR 199801704 T2 TR199801704 T2 TR 199801704T2 TR 1998/01704 T TR1998/01704 T TR 1998/01704T TR 9801704 T TR9801704 T TR 9801704T TR 199801704 T2 TR199801704 T2 TR 199801704T2
Authority
TR
Turkey
Prior art keywords
protease inhibitors
serine protease
compounds
prodrugs
formula
Prior art date
Application number
TR1998/01704T
Other languages
English (en)
Turkish (tr)
Inventor
Egbert Peter Adang Anton
Original Assignee
Akzo Nobel N.V.
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 N.V. filed Critical Akzo Nobel N.V.
Publication of TR199801704T2 publication Critical patent/TR199801704T2/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides 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
    • C07K5/0222Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • C07K5/06113Asp- or Asn-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
TR1998/01704T 1996-03-01 1997-02-26 Serin proteaz inhibit�rleri. TR199801704T2 (xx)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
TR199801704T2 true TR199801704T2 (xx) 1998-12-21

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
TR1998/01704T TR199801704T2 (xx) 1996-03-01 1997-02-26 Serin proteaz inhibit�rleri.

Country Status (25)

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

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
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
ES2180933T3 (es) 2003-02-16

Similar Documents

Publication Publication Date Title
TR199801704T2 (xx) Serin proteaz inhibit�rleri.
TR199801151T2 (xx) Trombin inhibit�r� �n ila�lar.
TR199801705T2 (xx) Serin proteaz inhibit�rleri.
DE60022508D1 (de) Inhibitoren von serin proteasen
TR199801569T2 (xx) Serin proteaz inhibit�rleri.
TR200103493T2 (tr) Metaloproteaz önleyicileri
TR200101120T2 (tr) Serin proteaz inhibitörü
EA200100675A1 (ru) Ингибиторы протеазы
DE60023266D1 (de) Serinprotease-inhibitoren
EA199700186A1 (ru) Новые дипептидные амидины, используемые в качестве ингибиторов тромбина
DK0558603T3 (da) Retrovirale proteaseinhibitorer
SE9602263D0 (sv) New amino acid derivatives
ATE260112T1 (de) Amidino proteaseinhibitoren
IS5511A (is) Ný efnasambönd
IS5966A (is) Nýjar amídínóafleiður og notkun þeirra sem þrombínhemlar
SE0001803D0 (sv) New compounds i
NO20030675L (no) Nye amidinoderivater og deres anvendelse som trombininhibitorer
MY132033A (en) New mandelic acid derivatives and their use as thrombin inhibitors
DK0666755T3 (da) Inhibering af HIV-infektion
BR0211847A (pt) Composto ou um derivado farmaceuticamente aceitável do mesmo, formulação farmacêutica, uso do composto ou do derivado, métodos para tratar uma condição onde a inibição de trombina é requerida, e para tratar uma condição onde a terapia anticoagulante é indicada, e, processo para a preparação de um composto
BG105985A (en) Prodrugs of thrombin inhibitors
PT937075E (pt) Novas imidazo- e oxazolo-piridinas como inibidores da fosfodiesterese
GEP20032923B (en) Sulphonamide Derivatives as Prodrugs of Aspartyl Protease Inhibitors, Pharmaceutical compositions containing the Same and Methods for Treatment