BG101647A - Low molecular weight bicyclic thrombin inhibitors - Google Patents

Low molecular weight bicyclic thrombin inhibitors

Info

Publication number
BG101647A
BG101647A BG101647A BG10164797A BG101647A BG 101647 A BG101647 A BG 101647A BG 101647 A BG101647 A BG 101647A BG 10164797 A BG10164797 A BG 10164797A BG 101647 A BG101647 A BG 101647A
Authority
BG
Bulgaria
Prior art keywords
molecular weight
low molecular
treatment
thrombin inhibitors
relates
Prior art date
Application number
BG101647A
Other languages
Bulgarian (bg)
Inventor
John Dimaio
Arshad Siddiqui
John Gillard
Yves St-Denis
Micheline Tarazi
Patrice Preville
Sophie Levesque
Benoit Bachand
Jeremy Edmonds
Annette Doherty
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 BG101647A publication Critical patent/BG101647A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P9/08Vasodilators for multiple indications
    • 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
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • 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
    • C07K5/04Peptides 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
    • C07K5/06139Dipeptides 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides 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
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)

Abstract

The invention relates to competitive heterocyclic inhibitorsof the enzyme thrombin with the formulauntil their preparation and to the pharmaceutical compositionscontaining them. The invention also relates to the application ofthese compounds and compositions in vitro as anticoagulants and invivo as agents for the treatment and prophylaxy of thrombosediseases such as venous thrombosis, lung artery embolism andarterial thromosis occuring in acute ischemic cases, such asinfarction of the myocardium or cerebral infarction. The compoundsand the compositions containing them are useful for the preventionand treatment of coagulapathies related to coronary bypassoperations as well as in other cases appearing as a result oftransluminal angioplasty.57 claims
BG101647A 1994-12-22 1997-06-20 Low molecular weight bicyclic thrombin inhibitors BG101647A (en)

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
BG101647A true BG101647A (en) 1998-03-31

Family

ID=27517273

Family Applications (1)

Application Number Title Priority Date Filing Date
BG101647A BG101647A (en) 1994-12-22 1997-06-20 Low molecular weight bicyclic thrombin inhibitors

Country Status (22)

Country Link
EP (1) EP0802916A1 (en)
JP (1) JPH11508535A (en)
CN (1) CN1175259A (en)
AP (1) AP9701004A0 (en)
AU (2) AU4250596A (en)
BG (1) BG101647A (en)
CA (1) CA2208772A1 (en)
CZ (1) CZ189997A3 (en)
EE (1) EE9700113A (en)
FI (1) FI972466A (en)
HU (1) HUT77651A (en)
IL (1) IL116503A0 (en)
IS (1) IS4504A (en)
LV (1) LV12019B (en)
MD (1) MD970253A (en)
MX (1) MX9704718A (en)
NO (1) NO972892L (en)
NZ (1) NZ297360A (en)
OA (1) OA10493A (en)
PL (1) PL320965A1 (en)
SK (1) SK83897A3 (en)
WO (1) WO1996019483A1 (en)

Families Citing this family (46)

* 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 (en) * 1995-08-01 1997-11-10 Menarini Farma Ind BICYCLIC LACTAM DERIVATIVES AS THROMBIN INHIBITORS
IL119466A (en) 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
US6034067A (en) * 1996-02-13 2000-03-07 Akzo Nobel, N.V. Serine protease inhibitors
IL120310A (en) * 1996-03-01 2002-02-10 Akzo Nobel Nv Serine protease inhibitors and pharmaceutical compositions containing them
TW523513B (en) * 1996-03-01 2003-03-11 Akzo Nobel Nv Serine protease inhibitors
US6124291A (en) * 1996-06-18 2000-09-26 Warner-Lambert Company Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors
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
CA2262900A1 (en) * 1996-08-05 1998-02-12 Molecumetics Ltd. Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors
US6117896A (en) 1997-02-10 2000-09-12 Molecumetics Ltd. Methods for regulating transcription factors
AU4172397A (en) * 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin
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
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
WO1998028326A1 (en) * 1996-12-23 1998-07-02 Biochem Pharma Inc. Bicyclic thrombin inhibitors
EP0975659A1 (en) * 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
AU6896298A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
NZ500352A (en) 1997-04-14 2001-10-26 Cor Therapeutics Inc Cyclic diaza 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
AU740447B2 (en) * 1997-09-23 2001-11-01 Merck & Co., Inc. Thrombin inhibitors
ES2192764T3 (en) * 1998-02-12 2003-10-16 Molecumetics Ltd MIMETICS OF LAMINA BETA AND METHODS RELATED TO THE USE OF THE SAME.
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
EP1140862A4 (en) 1998-12-23 2004-07-28 Bristol Myers Squibb Pharma Co THROMBIN OR FACTOR Xa INHIBITORS
EA200100815A1 (en) 1999-01-27 2002-08-29 Орто-Макнейл Фармасьютикал, Инк. PEPTIDILE HETEROCYCLIC KETONES USED AS TRIPTASE INHIBITORS
FR2795072B1 (en) * 1999-06-15 2001-07-27 Adir NOVEL BICYCLIC DERIVATIVES OF AMINO-PYRAZINONES, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
CA2401749A1 (en) * 2000-03-23 2001-09-27 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
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 (en) * 2000-12-14 2003-01-24 Servier Lab NOVEL BICYCLIC DERIVATIVES OF AMINO-PYRAZINONES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
US7192615B2 (en) 2001-02-28 2007-03-20 J&J Consumer Companies, Inc. Compositions containing legume products
CN1642550A (en) 2002-02-14 2005-07-20 美瑞德生物工程公司 Beta-sheet mimetics and composition and methods relating thereto
WO2003082197A2 (en) 2002-03-22 2003-10-09 Gpc Biotech Ag Immunosuppressant compounds, methods and uses related thereto
BR112017006920A8 (en) 2014-10-06 2023-03-07 Quince Therapeutics Inc GINGIPAINE LYSINE INHIBITORS
JO3637B1 (en) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc Rsv antiviral pyrazolo- and triazolo-pyrimidine compounds
CA3004095A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
TWI787202B (en) 2016-09-16 2022-12-21 美商昆斯治療公司 Ketone inhibitors of lysine gingipain
TW201932470A (en) 2017-11-29 2019-08-16 愛爾蘭商健生科學愛爾蘭無限公司 Pyrazolopyrimidines having activity against RSV
EA202091835A1 (en) 2018-01-31 2020-10-20 Янссен Сайенсиз Айрлэнд Анлимитед Компани CYCLOALKYL SUBSTITUTED PYRAZOLOPYRIMIDINES WITH AN ACTIVITY AGAINST RSV
AU2019260109B2 (en) 2018-04-23 2023-07-13 Janssen Sciences Ireland Unlimited Company Heteroaromatic compounds having activity against RSV

Also Published As

Publication number Publication date
IL116503A0 (en) 1996-03-31
NO972892L (en) 1997-08-20
AU4062895A (en) 1996-07-04
CN1175259A (en) 1998-03-04
CA2208772A1 (en) 1996-06-27
WO1996019483A1 (en) 1996-06-27
MD970253A (en) 1999-05-31
AP9701004A0 (en) 1997-07-31
AU715378B2 (en) 2000-02-03
EE9700113A (en) 1997-12-15
HUT77651A (en) 1998-07-28
IS4504A (en) 1997-06-11
SK83897A3 (en) 1998-05-06
MX9704718A (en) 1998-06-28
PL320965A1 (en) 1997-11-24
LV12019B (en) 1998-07-20
AU4250596A (en) 1996-07-10
FI972466A (en) 1997-08-19
EP0802916A1 (en) 1997-10-29
FI972466A0 (en) 1997-06-11
NZ297360A (en) 2000-03-27
JPH11508535A (en) 1999-07-27
NO972892D0 (en) 1997-06-20
LV12019A (en) 1998-04-20
OA10493A (en) 2002-04-10
CZ189997A3 (en) 1998-09-16

Similar Documents

Publication Publication Date Title
BG101647A (en) Low molecular weight bicyclic thrombin inhibitors
NL970045I2 (en) Desulfatohirudines, process for their preparation and pharmaceutical agents.
BG102071A (en) Minor molecule inhibitors of rotamase enzymic activity
NO177785C (en) Analogous Methods for Preparing Therapeutically Active Alkoxy-4 (1H) -pyridone Derivatives
DE68919361D1 (en) THERAPEUTIC COMPOSITIONS FOR THE TREATMENT OF MYOCARD INFARTS.
AP9100310A0 (en) Tnf inhibitors
PT1023267E (en) PYRIDYL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM
CA2208673A1 (en) Composition for inhibiting intimal hyperplasia using pdgf antagonists and heparin
ES2086436T3 (en) NEW PIPERIDYL ETHERS AND THIOETERES INHIBITORS OF CHOLESTEROL BIOSYNTHESIS.
DK302288A (en) Tissue Plasma Minogen Activator with Modified Circumstances
ES2088128T3 (en) ACAT INHIBITOR AMINOSULFONILUREAS.
TW369541B (en) Thrombin inhibitors
MX9304070A (en) PIPERIDYLAMIDES, PIPERIDYL SULPHONAMIDES AND NOVEL PIPERIDYLSULFOXAMIDES AS INHIBITORS OF CHOLESTEROL BIOSYNTHESIS.
EP0339878A3 (en) Propanamine derivatives
EP0208785A4 (en) Fibrinophilic urokinase complex and process for its preparation.
AUPP345098A0 (en) Novel anti-fibrinolytic agents
UA37211C2 (en) Derivatives OF 1,4-dihydropyridine in the form of racemate or enantiomers, 2-chloro-3-cyanobenzaldehyde as intermediary product for the preparation thereof and pharmaceutical composition having antagonist activity towards calcium cations
GR3023211T3 (en) Use of staphylokinase for the preparation of a pharmaceutical composition for treating arterial thrombosis
MX9704594A (en) Heterocyclic keto arginine peptides as thrombin inhibitors.
CA2024309A1 (en) Pharmaceutical compositions comprising modified and unmodified plasminogen activators and uses thereof
ATE69609T1 (en) CARDIOTONIC IMIDAZOLYLPHENYLPYRROL-2-ONE.
FR2633168B1 (en) STRUCTURAL ELEMENT, PARTICULARLY FOR FURNITURE OF THE TABLE, OFFICE OR THE LIKE TYPE
HU904162D0 (en) Medical compositions for the releasing of coronary convulsion by potentionating nitratic effect and for the releasing of fibrin
IT1206319B (en) DEVICE FOR SLIDING AND ANCHORING OF DRAWERS, BASKETS, BODIES REMOVABLE IN GENERAL, FROM FURNITURE AND OTHER.
IT8719950A0 (en) MODULAR STRUCTURE FOR THE CREATION OF FURNITURE, SHELVES, TABLES, TROLLEYS AND SIMILAR.