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
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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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    • 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

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  • 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)
RU98117949/04A 1996-03-01 1997-02-26 Ингибиторы протеазы серина RU2178419C2 (ru)

Applications Claiming Priority (2)

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

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)

* 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.
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

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
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.

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
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
ES2180933T3 (es) 2003-02-16
HUP9900390A3 (en) 2000-11-28
CN1212704A (zh) 1999-03-31

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