RU2178419C2 - Ингибиторы протеазы серина - Google Patents

Ингибиторы протеазы серина Download PDF

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Publication number
RU2178419C2
RU2178419C2 RU98117949/04A RU98117949A RU2178419C2 RU 2178419 C2 RU2178419 C2 RU 2178419C2 RU 98117949/04 A RU98117949/04 A RU 98117949/04A RU 98117949 A RU98117949 A RU 98117949A RU 2178419 C2 RU2178419 C2 RU 2178419C2
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RU
Russia
Prior art keywords
pro
lysininyl
boc
cha
cbz
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RU98117949/04A
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English (en)
Russian (ru)
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RU98117949A (ru
Inventor
Эгберт Петер Аданг Антон
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Акцо Нобель Н.В.
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Publication of RU98117949A publication Critical patent/RU98117949A/ru
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (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)
RU98117949/04A 1996-03-01 1997-02-26 Ингибиторы протеазы серина RU2178419C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP96200543 1996-03-01
EP96200543.5 1996-03-01

Publications (2)

Publication Number Publication Date
RU98117949A RU98117949A (ru) 2000-10-20
RU2178419C2 true RU2178419C2 (ru) 2002-01-20

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
RU98117949/04A RU2178419C2 (ru) 1996-03-01 1997-02-26 Ингибиторы протеазы серина

Country Status (25)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2509776C2 (ru) * 2008-10-15 2014-03-20 ДАНИСКО ЮЭс ИНК. МОДИФИЦИРОВАННЫЕ ВАРИАНТЫ ИНГИБИТОРОВ ПРОТЕАЗ Bowman Birk

Families Citing this family (20)

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Publication number Priority date Publication date Assignee Title
CA2246256A1 (en) * 1996-02-13 1997-08-21 Akzo Nobel Nv Serine protease inhibitors
US6214841B1 (en) 1997-05-15 2001-04-10 Eli Lilly And Company Antithrombotic compound
TR200003159T2 (tr) 1998-04-30 2001-09-21 Agouron Pharmaceuticals,Inc. Antipicornaviral bileşikler, hazırlanışları ve kullanımları
EP1105412A1 (en) * 1998-08-17 2001-06-13 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
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
JP2003506457A (ja) 1999-08-04 2003-02-18 アグロン・ファーマシュウティカルズ・インコーポレーテッド 抗ピコルナウィルス化合物及び組成物、その医薬的使用、並びにその合成のための物質
WO2001096297A2 (en) 2000-06-14 2001-12-20 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
SK742003A3 (en) 2000-07-21 2003-06-03 Schering Corp Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
US7012066B2 (en) 2000-07-21 2006-03-14 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation 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
ATE483708T1 (de) 2004-03-08 2010-10-15 Prosidion Ltd Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
ATE424821T1 (de) 2004-12-02 2009-03-15 Prosidion Ltd Pyrrolopyridin-2-karbonsäureamide
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
JP7179721B2 (ja) 2016-06-21 2022-11-29 オリオン・オフサルモロジー・エルエルシー 複素環式プロリンアミド誘導体
EP4178955A1 (en) 2020-07-11 2023-05-17 Pfizer Inc. Antiviral heteroaryl ketone derivatives
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994025051A1 (en) * 1993-04-30 1994-11-10 Merck & Co., Inc. Thrombin inhibitors
RU2024549C1 (ru) * 1989-02-23 1994-12-15 Ф.Хоффманн-Ля Рош Аг Производные глицина или их физиологически приемлемые соли, обладающие способностью тормозить связывание фибриногена у фибриногенного рецептора тромбоцитов
EP0672658A1 (en) * 1994-03-04 1995-09-20 Eli Lilly And Company Antithrombotic agents
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
RU2142469C1 (ru) * 1993-06-03 1999-12-10 Астра Актиеболаг Пептидные производные, их стереоизомеры или физиологически приемлемые соли, обладающие противотромбозной, противосвертывающей или противовоспалительной активностью, способ их получения, фармацевтическая композиция, способ подавления тромбина, способ подавления кининогеназ, применение соединений в качестве исходных в синтезе ингибитора тромбина

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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
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
CN1175259A (zh) 1994-12-22 1998-03-04 生化制药有限公司 低分子量双环凝血酶抑制剂

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2024549C1 (ru) * 1989-02-23 1994-12-15 Ф.Хоффманн-Ля Рош Аг Производные глицина или их физиологически приемлемые соли, обладающие способностью тормозить связывание фибриногена у фибриногенного рецептора тромбоцитов
WO1994025051A1 (en) * 1993-04-30 1994-11-10 Merck & Co., Inc. Thrombin inhibitors
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
RU2142469C1 (ru) * 1993-06-03 1999-12-10 Астра Актиеболаг Пептидные производные, их стереоизомеры или физиологически приемлемые соли, обладающие противотромбозной, противосвертывающей или противовоспалительной активностью, способ их получения, фармацевтическая композиция, способ подавления тромбина, способ подавления кининогеназ, применение соединений в качестве исходных в синтезе ингибитора тромбина
EP0672658A1 (en) * 1994-03-04 1995-09-20 Eli Lilly And Company Antithrombotic agents

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2509776C2 (ru) * 2008-10-15 2014-03-20 ДАНИСКО ЮЭс ИНК. МОДИФИЦИРОВАННЫЕ ВАРИАНТЫ ИНГИБИТОРОВ ПРОТЕАЗ Bowman Birk

Also Published As

Publication number Publication date
ES2180933T3 (es) 2003-02-16
EP0886647A1 (en) 1998-12-30
KR19990087415A (ko) 1999-12-27
ATE221080T1 (de) 2002-08-15
IL120310A (en) 2002-02-10
HUP9900390A2 (hu) 1999-06-28
EP0886647B1 (en) 2002-07-24
HUP9900390A3 (en) 2000-11-28
CN1212704A (zh) 1999-03-31
ZA971667B (en) 1997-09-10
AR006310A1 (es) 1999-08-25
DE69714222T2 (de) 2003-02-20
AU709330B2 (en) 1999-08-26
JP2000506837A (ja) 2000-06-06
PL328875A1 (en) 1999-03-01
IL120310A0 (en) 1997-06-10
NZ331484A (en) 2000-01-28
DE69714222D1 (de) 2002-08-29
NO983991L (no) 1998-10-30
NO983991D0 (no) 1998-08-31
TW442452B (en) 2001-06-23
HK1021541A1 (en) 2000-06-16
CA2246246A1 (en) 1997-09-04
US6410684B1 (en) 2002-06-25
PT886647E (pt) 2002-12-31
TR199801704T2 (xx) 1998-12-21
AU1877597A (en) 1997-09-16
CZ277898A3 (cs) 1999-06-16
DK0886647T3 (da) 2002-11-04
BR9707808A (pt) 1999-07-27
WO1997031937A1 (en) 1997-09-04

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