HUP9900390A2 - Szerin-proteáz-inhibitorok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Szerin-proteáz-inhibitorok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP9900390A2
HUP9900390A2 HU9900390A HUP9900390A HUP9900390A2 HU P9900390 A2 HUP9900390 A2 HU P9900390A2 HU 9900390 A HU9900390 A HU 9900390A HU P9900390 A HUP9900390 A HU P9900390A HU P9900390 A2 HUP9900390 A2 HU P9900390A2
Authority
HU
Hungary
Prior art keywords
amino acid
side chain
hydrophobic side
pharmaceutical compositions
compositions containing
Prior art date
Application number
HU9900390A
Other languages
English (en)
Inventor
Anton Egbert Peter Adang
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 HUP9900390A2 publication Critical patent/HUP9900390A2/hu
Publication of HUP9900390A3 publication Critical patent/HUP9900390A3/hu

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A találmány (I) általánős képletű vegyületekre vőnatkőzik, ahől aszűbsztitűensek főbb jelentései a következők: A jelentésehidrőgénatőm, adőtt esetben szűbsztitűált D,L-a-hidrőxi-acetil-csőpőrtvagy egy N-védőcsőpőrt; B jelentése egy kötés, -NH-CH[(CH2)pC(O)OH]-C(O)- képletű aminősav vagy annak észterszármazéka -, ahől p jelentése0, 1, 2 vagy 3- vagy egy L- vagy D-aminősav hidrőfób őldallánccal,amely hidrőfób őldallánc 1-12 szénatőmős alkilcsőpőrtőt jelent; Xjelentése hidrőfób őldalláncú L-aminősav, szerin, treőnin vagy egygyűrűs aminősav; Y jelentése H, -CHF2, -CF3 vagy -CO-NH-(1-6szénatőmős alkilén)-C6H5 csőpőrt. A találmány szerinti vegyületekantikőagűláns hatékőnyságúak, és trőmbinnal összefüggő betegségekkezelésére vagy megelőzésére használhatók fel. ŕ
HU9900390A 1996-03-01 1997-02-26 Serine protease inhibitors, and pharmaceutical compositions containing them HUP9900390A3 (en)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
HUP9900390A2 true HUP9900390A2 (hu) 1999-06-28
HUP9900390A3 HUP9900390A3 (en) 2000-11-28

Family

ID=8223736

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9900390A HUP9900390A3 (en) 1996-03-01 1997-02-26 Serine protease inhibitors, and pharmaceutical compositions containing them

Country Status (26)

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

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997030073A1 (en) * 1996-02-13 1997-08-21 Akzo Nobel N.V. Serine protease inhibitors
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
HUP0400624A2 (hu) 1998-04-30 2004-06-28 Agouron Pharmaceuticals, Inc. Picornavírus-ellenes vegyületek, előállításuk és alkalmazásuk
EP1105412A1 (en) * 1998-08-17 2001-06-13 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
US6489308B1 (en) 1999-03-05 2002-12-03 Trustees Of University Of Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of nitric-oxide-induced clinical conditions
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
CA2380647A1 (en) 1999-08-04 2001-02-15 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
JP2004503533A (ja) 2000-06-14 2004-02-05 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 抗ピコルナウイ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
PL206255B1 (pl) 2000-07-21 2010-07-30 Dendreon Corporationdendreon Corporation Inhibitor proteazy wirusa zapalenia wątroby C, zawierająca go kompozycja farmaceutyczna i zastosowanie inhibitora do wytwarzania leku do leczenia chorób związanych z HCV oraz zastosowanie do wytwarzania kompozycji do stosowania w kombinowanej terapii
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
BR0112666A (pt) 2000-07-21 2003-06-10 Schering Corp Peptìdeos como inibidores de ns3-serina protease de vìrus da hepatite c
WO2002060894A2 (en) 2001-01-30 2002-08-08 Bristol-Myers Squibb Company Sulfonamide lactam inhibitors of factor xa
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
EP1819332B1 (en) 2004-12-02 2009-03-11 Prosidion Limited Pyrrolopyridine-2-carboxylic acid amides
CA2740197A1 (en) * 2008-10-15 2010-04-22 Danisco Us Inc. Modified variant bowman birk protease inhibitors
CN109476637B (zh) 2016-06-21 2022-02-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
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
ATE227581T1 (de) * 1993-04-30 2002-11-15 Merck & Co Inc Thrombin-inhibitoren
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
NZ331484A (en) 2000-01-28
TW442452B (en) 2001-06-23
CA2246246A1 (en) 1997-09-04
KR19990087415A (ko) 1999-12-27
HUP9900390A3 (en) 2000-11-28
PL328875A1 (en) 1999-03-01
JP2000506837A (ja) 2000-06-06
EP0886647B1 (en) 2002-07-24
RU2178419C2 (ru) 2002-01-20
US6410684B1 (en) 2002-06-25
CN1212704A (zh) 1999-03-31
PT886647E (pt) 2002-12-31
WO1997031937A1 (en) 1997-09-04
DE69714222D1 (de) 2002-08-29
BR9707808A (pt) 1999-07-27
ATE221080T1 (de) 2002-08-15
ES2180933T3 (es) 2003-02-16
DK0886647T3 (da) 2002-11-04
ZA971667B (en) 1997-09-10
AU1877597A (en) 1997-09-16
IL120310A (en) 2002-02-10
AR006310A1 (es) 1999-08-25
AU709330B2 (en) 1999-08-26
NO983991D0 (no) 1998-08-31
IL120310A0 (en) 1997-06-10
TR199801704T2 (xx) 1998-12-21
NO983991L (no) 1998-10-30
CZ277898A3 (cs) 1999-06-16
HK1021541A1 (en) 2000-06-16
EP0886647A1 (en) 1998-12-30
DE69714222T2 (de) 2003-02-20

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