IL120310A - מעכבי סרין פרוטאז ותכשירי רוקחות המכילים אותם - Google Patents

מעכבי סרין פרוטאז ותכשירי רוקחות המכילים אותם

Info

Publication number
IL120310A
IL120310A IL12031097A IL12031097A IL120310A IL 120310 A IL120310 A IL 120310A IL 12031097 A IL12031097 A IL 12031097A IL 12031097 A IL12031097 A IL 12031097A IL 120310 A IL120310 A IL 120310A
Authority
IL
Israel
Prior art keywords
alkyl
pro
chr2
boc
cha
Prior art date
Application number
IL12031097A
Other languages
English (en)
Other versions
IL120310A0 (en
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 IL120310A0 publication Critical patent/IL120310A0/xx
Publication of IL120310A publication Critical patent/IL120310A/he

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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)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (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)
IL12031097A 1996-03-01 1997-02-25 מעכבי סרין פרוטאז ותכשירי רוקחות המכילים אותם IL120310A (he)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
IL120310A0 IL120310A0 (en) 1997-06-10
IL120310A true IL120310A (he) 2002-02-10

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
IL12031097A IL120310A (he) 1996-03-01 1997-02-25 מעכבי סרין פרוטאז ותכשירי רוקחות המכילים אותם

Country Status (26)

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

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1007544A1 (en) * 1996-02-13 2000-06-14 Akzo Nobel N.V. Serine protease inhibitors
CA2289625A1 (en) 1997-05-15 1998-11-19 Charles Van Jackson Antithrombotic compound
CN1198838C (zh) 1998-04-30 2005-04-27 阿格罗尼制药公司 抗小rna病毒化合物及其制备方法和用途
AU9031598A (en) * 1998-08-17 2000-03-06 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
WO2000051624A2 (en) 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation 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
ES2230135T3 (es) * 1999-08-04 2005-05-01 Agouron Pharmaceuticals, Inc. Compuestos y composiciones anti-picornavirales; utilizaciones farmaceuticas y materiales utilizados para su sintesis.
PL365470A1 (en) 2000-06-14 2005-01-10 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
HUP0303358A3 (en) * 2000-07-21 2005-10-28 Schering Corp Novel peptides as ns3-serine protease inhibitors of hepatitis c virus and pharmaceutical compositions containing them
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
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
EP1725555B1 (en) 2004-03-08 2010-10-06 Prosidion Ltd. Pyrrolopyridine-2-carboxylic acid hydrazides as inhibitors of glycogen phosphorylase
WO2006059164A2 (en) 2004-12-02 2006-06-08 Prosidion Limited Pyrrolopyridine-2-carboxylic acid amides
MX2011003803A (es) * 2008-10-15 2011-07-04 Danisco Inc Inhibidores de proteasa 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
CN114685453A (zh) 2016-06-21 2022-07-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
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
JP3486412B2 (ja) * 1993-04-30 2004-01-13 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
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
JPH10503176A (ja) 1994-06-17 1998-03-24 コーバス インターナショナル, インコーポレイテッド 酵素インヒビターとしての3−アミノ−2−オキソ−1−ピペリジン酢酸誘導体
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
SK83897A3 (en) 1994-12-22 1998-05-06 Iaf Biochem Int Low molecular weight bicyclic thrombin inhibitors

Also Published As

Publication number Publication date
DE69714222T2 (de) 2003-02-20
CZ277898A3 (cs) 1999-06-16
DE69714222D1 (de) 2002-08-29
NO983991D0 (no) 1998-08-31
PT886647E (pt) 2002-12-31
BR9707808A (pt) 1999-07-27
EP0886647A1 (en) 1998-12-30
ATE221080T1 (de) 2002-08-15
CA2246246A1 (en) 1997-09-04
US6410684B1 (en) 2002-06-25
EP0886647B1 (en) 2002-07-24
HK1021541A1 (en) 2000-06-16
JP2000506837A (ja) 2000-06-06
AU1877597A (en) 1997-09-16
DK0886647T3 (da) 2002-11-04
CN1212704A (zh) 1999-03-31
AR006310A1 (es) 1999-08-25
TW442452B (en) 2001-06-23
TR199801704T2 (xx) 1998-12-21
PL328875A1 (en) 1999-03-01
ES2180933T3 (es) 2003-02-16
NO983991L (no) 1998-10-30
IL120310A0 (en) 1997-06-10
HUP9900390A2 (hu) 1999-06-28
ZA971667B (en) 1997-09-10
WO1997031937A1 (en) 1997-09-04
RU2178419C2 (ru) 2002-01-20
HUP9900390A3 (en) 2000-11-28
KR19990087415A (ko) 1999-12-27
AU709330B2 (en) 1999-08-26
NZ331484A (en) 2000-01-28

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Legal Events

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FF Patent granted
KB Patent renewed
RH1 Patent not in force