MD970253A - Inhibitori biciclici micromoleculari ai trombinei - Google Patents

Inhibitori biciclici micromoleculari ai trombinei

Info

Publication number
MD970253A
MD970253A MD97-0253A MD970253A MD970253A MD 970253 A MD970253 A MD 970253A MD 970253 A MD970253 A MD 970253A MD 970253 A MD970253 A MD 970253A
Authority
MD
Moldova
Prior art keywords
thrombin
micromolecular
thrombosis
inhibitors
bicyclic inhibitors
Prior art date
Application number
MD97-0253A
Other languages
English (en)
Russian (ru)
Inventor
John Dimaio
M. Arshad Siddiqui
John W GILLARD
Yves St-Denis
Micheline Tarazi
Patrice Preville
Sophie Levesque
Benoit Bachand
Аннетт Мэриан ДОХЕРТИ
Jeremy Jogn EDMONDS
Original Assignee
Biochem Pharma Inc.
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
Priority claimed from GBGB9426038.7A external-priority patent/GB9426038D0/en
Priority claimed from GBGB9510267.9A external-priority patent/GB9510267D0/en
Priority claimed from GBGB9510265.3A external-priority patent/GB9510265D0/en
Priority claimed from GBGB9510266.1A external-priority patent/GB9510266D0/en
Application filed by Biochem Pharma Inc. filed Critical Biochem Pharma Inc.
Publication of MD970253A publication Critical patent/MD970253A/ro

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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
    • C07K5/04—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
    • C07K5/06139—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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides 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
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Invenţia se referă la compuşi chimici noi care pot fi utilizaţi ca inhibitori competitivi ai enzimei de trombină.Sunt revendicaţi compuşii cu formula (I)metodele de tratament şi profilaxie a dereglărilor trombotice, cum este tromboza venelor, embolia pulmonară şi tromboza arterială, ce provoacă fenomene ischemice acute, cum este infarctul miocardic sau infarctul cerebral.
MD97-0253A 1994-12-22 1995-12-21 Inhibitori biciclici micromoleculari ai trombinei MD970253A (ro)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GBGB9426038.7A GB9426038D0 (en) 1994-12-22 1994-12-22 Low molecular weight bicyclic thrombin inhibitors
GBGB9503136.5A GB9503136D0 (en) 1994-12-22 1995-02-17 Low molecular weight bicyclic thrombin inhibitors
GBGB9510267.9A GB9510267D0 (en) 1995-05-22 1995-05-22 Low molecular weight thiobicyclic thrombin inhibitors
GBGB9510265.3A GB9510265D0 (en) 1995-05-22 1995-05-22 Low molecular weight diaminobicyclic thrombin inhibitors
GBGB9510266.1A GB9510266D0 (en) 1995-05-22 1995-05-22 Low molecular weight bicyclic thrombin inhibitors
PCT/CA1995/000708 WO1996019483A1 (en) 1994-12-22 1995-12-21 Low molecular weight bicyclic thrombin inhibitors

Publications (1)

Publication Number Publication Date
MD970253A true MD970253A (ro) 1999-05-31

Family

ID=27517273

Family Applications (1)

Application Number Title Priority Date Filing Date
MD97-0253A MD970253A (ro) 1994-12-22 1995-12-21 Inhibitori biciclici micromoleculari ai trombinei

Country Status (22)

Country Link
EP (1) EP0802916A1 (ro)
JP (1) JPH11508535A (ro)
CN (1) CN1175259A (ro)
AP (1) AP9701004A0 (ro)
AU (2) AU4250596A (ro)
BG (1) BG101647A (ro)
CA (1) CA2208772A1 (ro)
CZ (1) CZ189997A3 (ro)
EE (1) EE9700113A (ro)
FI (1) FI972466L (ro)
HU (1) HUT77651A (ro)
IL (1) IL116503A0 (ro)
IS (1) IS4504A (ro)
LV (1) LV12019B (ro)
MD (1) MD970253A (ro)
MX (1) MX9704718A (ro)
NO (1) NO972892L (ro)
NZ (1) NZ297360A (ro)
OA (1) OA10493A (ro)
PL (1) PL320965A1 (ro)
SK (1) SK83897A3 (ro)
WO (1) WO1996019483A1 (ro)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6699869B1 (en) 1995-03-24 2004-03-02 Myriad Genetics Inc. β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
US6020331A (en) 1995-03-24 2000-02-01 Molecumetics, Ltd. β-sheet mimetics and use thereof as protease inhibitors
US6245764B1 (en) 1995-03-24 2001-06-12 Molecumetics Ltd. β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
IT1277405B1 (it) * 1995-08-01 1997-11-10 Menarini Farma Ind Derivati di lattami biciclici come inibitori della trombina
IL119466A (en) * 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
CA2246256A1 (en) * 1996-02-13 1997-08-21 Akzo Nobel Nv Serine protease inhibitors
IL120311A (en) * 1996-03-01 2001-10-31 Akzo Nobel Nv Serine protease inhibitors and pharmaceuticals containing them
IL120310A (en) * 1996-03-01 2002-02-10 Akzo Nobel Nv Serine protease inhibitors and pharmaceuticals containing them
WO1997048706A1 (en) * 1996-06-18 1997-12-24 Warner-Lambert Company Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors
US6117896A (en) * 1997-02-10 2000-09-12 Molecumetics Ltd. Methods for regulating transcription factors
EP1661566A3 (en) * 1996-08-05 2008-04-16 Myriad Genetics, Inc. Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors
EP0915700B1 (en) * 1996-08-05 2006-03-22 Myriad Genetics, Inc. Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors
WO1998009987A1 (en) * 1996-09-06 1998-03-12 Biochem Pharma, Inc. Lactam inhibitors of thrombin
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998028326A1 (en) * 1996-12-23 1998-07-02 Biochem Pharma Inc. Bicyclic thrombin inhibitors
CA2285705A1 (en) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
WO1998046626A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
CA2285659A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
JP2001517623A (ja) * 1997-09-23 2001-10-09 メルク エンド カムパニー インコーポレーテッド トロンビン阻害薬
AU748887B2 (en) * 1998-02-12 2002-06-13 Myriad Genetics, Inc. Beta-sheet mimetics and methods relating to the use thereof
US6323219B1 (en) 1998-04-02 2001-11-27 Ortho-Mcneil Pharmaceutical, Inc. Methods for treating immunomediated inflammatory disorders
US8093293B2 (en) 1998-07-06 2012-01-10 Johnson & Johnson Consumer Companies, Inc. Methods for treating skin conditions
US8106094B2 (en) 1998-07-06 2012-01-31 Johnson & Johnson Consumer Companies, Inc. Compositions and methods for treating skin conditions
WO2000039102A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
EA200100815A1 (ru) 1999-01-27 2002-08-29 Орто-Макнейл Фармасьютикал, Инк. Пептидильные гетероциклические кетоны, применимые в качестве ингибиторов триптазы
FR2795072B1 (fr) * 1999-06-15 2001-07-27 Adir Nouveaux derives bicycliques d'amino-pyrazinones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US7309688B2 (en) 2000-10-27 2007-12-18 Johnson & Johnson Consumer Companies Topical anti-cancer compositions and methods of use thereof
DE60124080T2 (de) * 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
US6586418B2 (en) 2000-06-29 2003-07-01 Bristol-Myers Squibb Company Thrombin or factor Xa inhibitors
US8431550B2 (en) 2000-10-27 2013-04-30 Johnson & Johnson Consumer Companies, Inc. Topical anti-cancer compositions and methods of use thereof
FR2818277B1 (fr) * 2000-12-14 2003-01-24 Servier Lab Nouveaux derives bicycliques d'amino-pyrazinones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US7192615B2 (en) 2001-02-28 2007-03-20 J&J Consumer Companies, Inc. Compositions containing legume products
CN1642550A (zh) 2002-02-14 2005-07-20 美瑞德生物工程公司 β－折叠模拟物和组合物及其有关方法
US7629318B2 (en) 2002-03-22 2009-12-08 Gpc Biotech Ag Immunosuppressant compounds, methods and uses related thereto
US9758473B2 (en) 2014-10-06 2017-09-12 Cortexyme, Inc. Inhibitors of lysine gingipain
JO3637B1 (ar) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc مركبات بيرازولو- وترايازولو- بيريميدين مضادة للفيروسات rsv
WO2017083433A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
EP4480541A3 (en) 2016-09-16 2025-04-30 Lighthouse Pharmaceuticals, Inc. Ketone inhibitors of lysine gingipain
TW201932470A (zh) 2017-11-29 2019-08-16 愛爾蘭商健生科學愛爾蘭無限公司 具有抗ｒｓｖ活性之吡唑并嘧啶
EP3746444B1 (en) 2018-01-31 2023-09-27 Janssen Sciences Ireland Unlimited Company Cycloalkyl substituted pyrazolopyrimidines having activity against rsv
CA3095277A1 (en) 2018-04-23 2019-10-31 Janssen Sciences Ireland Unlimited Company Heteroaromatic compounds having activity against rsv

Also Published As

Publication number Publication date
EE9700113A (et) 1997-12-15
FI972466A0 (fi) 1997-06-11
FI972466A7 (fi) 1997-08-19
JPH11508535A (ja) 1999-07-27
HUT77651A (hu) 1998-07-28
OA10493A (en) 2002-04-10
IS4504A (is) 1997-06-11
CA2208772A1 (en) 1996-06-27
MX9704718A (es) 1998-06-28
WO1996019483A1 (en) 1996-06-27
PL320965A1 (en) 1997-11-24
NO972892L (no) 1997-08-20
CN1175259A (zh) 1998-03-04
AU4250596A (en) 1996-07-10
NO972892D0 (no) 1997-06-20
IL116503A0 (en) 1996-03-31
FI972466L (fi) 1997-08-19
AU715378B2 (en) 2000-02-03
EP0802916A1 (en) 1997-10-29
CZ189997A3 (cs) 1998-09-16
LV12019B (en) 1998-07-20
SK83897A3 (en) 1998-05-06
NZ297360A (en) 2000-03-27
BG101647A (bg) 1998-03-31
AU4062895A (en) 1996-07-04
LV12019A (lv) 1998-04-20
AP9701004A0 (en) 1997-07-31

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