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)
Spanish (es)
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

    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Crystallography & Structural Chemistry (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)
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 (2)
EP (1) EP0886647B1 (2)
JP (1) JP2000506837A (2)
KR (1) KR19990087415A (2)
CN (1) CN1212704A (2)
AR (1) AR006310A1 (2)
AT (1) ATE221080T1 (2)
AU (1) AU709330B2 (2)
BR (1) BR9707808A (2)
CA (1) CA2246246A1 (2)
CZ (1) CZ277898A3 (2)
DE (1) DE69714222T2 (2)
DK (1) DK0886647T3 (2)
ES (1) ES2180933T3 (2)
HU (1) HUP9900390A3 (2)
IL (1) IL120310A (2)
NO (1) NO983991L (2)
NZ (1) NZ331484A (2)
PL (1) PL328875A1 (2)
PT (1) PT886647E (2)
RU (1) RU2178419C2 (2)
TR (1) TR199801704T2 (2)
TW (1) TW442452B (2)
WO (1) WO1997031937A1 (2)
ZA (1) ZA971667B (2)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2191193C2 (ru) * 1996-02-13 2002-10-20 Акцо Нобель Н.В. Ингибиторы серинпротеазы
US6214841B1 (en) 1997-05-15 2001-04-10 Eli Lilly And Company Antithrombotic compound
DK1073672T3 (da) 1998-04-30 2003-12-08 Agouron Pharma Antipicornavirale forbindelser, deres fremstilling og anvendelse
AU9031598A (en) * 1998-08-17 2000-03-06 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
WO2000051623A2 (en) 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
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
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
AU779321B2 (en) * 1999-08-04 2005-01-20 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
WO2001096297A2 (en) 2000-06-14 2001-12-20 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
CN1498224A (zh) 2000-07-21 2004-05-19 ���鹫˾ 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
SK742003A3 (en) * 2000-07-21 2003-06-03 Schering Corp Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
HUP0304058A2 (hu) 2001-01-30 2004-04-28 Bristol-Myers Squibb Company Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
JP2007527904A (ja) 2004-03-08 2007-10-04 プロシディオン・リミテッド グリコーゲンホスホリラーゼ阻害剤としてのピロロピリジン−2−カルボン酸ヒドラジド化合物
ES2324173T3 (es) 2004-12-02 2009-07-31 Prosidion Limited Amidas del acido pirrolopiridin-2-carboxilico.
BRPI0823193A2 (pt) * 2008-10-15 2019-09-24 Danisco Us Inc inibidores de protease de bowman birk variantes modificados
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
HUE064412T2 (hu) 2016-06-21 2024-03-28 Orion Ophthalmology LLC Heterociklusos prolinamid-származékok
CA3189027A1 (en) 2020-07-11 2022-01-20 Pfizer Inc. Antiviral heteroaryl ketone derivatives
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
DE69431718T2 (de) 1993-04-30 2003-07-10 Merck & Co., Inc. Thrombin-inhibitoren
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
ZA951618B (en) 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
ZA951617B (en) 1994-03-04 1997-02-27 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
AP9701004A0 (en) 1994-12-22 1997-07-31 Iaf Biochem Int Low molecular weight bicyclic thrombin inhibitors.

Also Published As

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

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