NO972892L - Bicyclic Low Molecular Weight Thrombin Inhibitors - Google Patents

Bicyclic Low Molecular Weight Thrombin Inhibitors

Info

Publication number
NO972892L
NO972892L NO972892A NO972892A NO972892L NO 972892 L NO972892 L NO 972892L NO 972892 A NO972892 A NO 972892A NO 972892 A NO972892 A NO 972892A NO 972892 L NO972892 L NO 972892L
Authority
NO
Norway
Prior art keywords
bicyclic
molecular weight
low molecular
thrombin inhibitors
weight thrombin
Prior art date
Application number
NO972892A
Other languages
Norwegian (no)
Other versions
NO972892D0 (en
Inventor
John Gillard
John Dimaio
M Arshad Siddiqui
Patrice Preville
Yves St-Denis
Micheline Tarazi
Sophie Levesque
Benoit Bachand
Jeremy John Edmunds
Annette Marian Doherty
Original Assignee
Iaf Biochem Int
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 Iaf Biochem Int filed Critical Iaf Biochem Int
Publication of NO972892D0 publication Critical patent/NO972892D0/en
Publication of NO972892L publication Critical patent/NO972892L/en

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)

Abstract

Foreliggende oppfinnelse angår heterocykliske, kompetitive inhibitorer av enzymet trombin, fremstilling av (dem og farmasøytiske preparater derav. Oppfinnelsen angår også anvendelse av slike forbindelser og preparater in vitro som antikoaguleringsmidler og in vivo som midler for befiandling og profylakse av trombotiske lidelser så som venøs trombose, lungeemboli og arterien trombose som er et resultat av akutte ischemi, så som myokardialt infarkt eller cerebralt infarkt. Disse forbindelsene og preparatene er videre terapeutisk nyttige for forhindring og behandling av koagulopatier knyttet til hjerte-bypass-operasjoner så vel som restenose etter transluminal angioplasti.This invention also relates to the use of such compounds and preparations in vitro as anticoagulants and in vivo as agents for the prophylaxis and prophylaxis of thrombotic disorders such as venous thrombosis. pulmonary embolism and artery thrombosis resulting from acute ischemia such as myocardial infarction or cerebral infarction.These compounds and preparations are therapeutically useful for the prevention and treatment of coagulopathies associated with cardiac bypass surgery as well as restenosis after transluminal angioplasty.

NO972892A 1994-12-22 1997-06-20 Bicyclic Low Molecular Weight Thrombin Inhibitors NO972892L (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 (2)

Publication Number Publication Date
NO972892D0 NO972892D0 (en) 1997-06-20
NO972892L true NO972892L (en) 1997-08-20

Family

ID=27517273

Family Applications (1)

Application Number Title Priority Date Filing Date
NO972892A NO972892L (en) 1994-12-22 1997-06-20 Bicyclic Low Molecular Weight 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
US6020331A (en) 1995-03-24 2000-02-01 Molecumetics, Ltd. β-sheet mimetics and use thereof as protease inhibitors
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
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
CA2246256A1 (en) * 1996-02-13 1997-08-21 Akzo Nobel Nv Serine protease inhibitors
TW442452B (en) 1996-03-01 2001-06-23 Akzo Nobel Nv Serine protease inhibitors having an alkynylamino side chain
IL120311A (en) * 1996-03-01 2001-10-31 Akzo Nobel Nv Serine protease inhibitors and pharmaceutical compositions containing them
AU3232597A (en) * 1996-06-18 1998-01-07 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
WO1998005333A1 (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
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
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
AU5526098A (en) * 1996-12-23 1998-07-17 Biochem Pharma Inc. Bicyclic thrombin inhibitors
JP2002514214A (en) 1997-04-14 2002-05-14 シーオーアール セラピューティクス インコーポレイテッド Selective factor Xa inhibitor
CA2285685A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
NZ500351A (en) * 1997-04-14 2001-10-26 Cor Therapeutics Inc Cyclic diaza compounds as 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
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
JP2001517623A (en) * 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 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
US8106094B2 (en) 1998-07-06 2012-01-31 Johnson & Johnson Consumer Companies, Inc. Compositions and methods for treating skin conditions
US8093293B2 (en) 1998-07-06 2012-01-10 Johnson & Johnson Consumer Companies, Inc. Methods for treating skin conditions
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
CA2361479A1 (en) 1999-01-27 2000-08-03 Ortho-Mcneil Pharmaceutical, Inc. Peptidyl heterocyclic ketones useful as tryptase 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
DE60124080T2 (en) * 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco COMPOUNDS AND METHOD FOR THE TREATMENT OF ALZHEIMER'S DISEASE
WO2002002519A2 (en) * 2000-06-29 2002-01-10 Bristol-Myers Squibb Pharma 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
JP2005526722A (en) 2002-02-14 2005-09-08 ミリアド・ジェネティックス・インコーポレイテッド β-sheet mimetics and related compositions and methods
WO2003082197A2 (en) 2002-03-22 2003-10-09 Gpc Biotech Ag Immunosuppressant compounds, methods and uses related thereto
ES2819218T3 (en) 2014-10-06 2021-04-15 Cortexyme Inc Gingipain lysine inhibitors
JO3637B1 (en) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc Rsv antiviral pyrazolo- and triazolo-pyrimidine compounds
EP3374352A4 (en) 2015-11-09 2019-10-02 Cortexyme, Inc. Inhibitors of arginine gingipain
EP3512846A4 (en) 2016-09-16 2020-06-10 Cortexyme, Inc. 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
KR20200116099A (en) 2018-01-31 2020-10-08 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 Cycloalkyl-substituted pyrazolopyrimidines with activity against RSV
EP3784667B1 (en) 2018-04-23 2023-08-16 Janssen Sciences Ireland Unlimited Company Heteroaromatic compounds having activity against rsv

Also Published As

Publication number Publication date
MX9704718A (en) 1998-06-28
PL320965A1 (en) 1997-11-24
FI972466A0 (en) 1997-06-11
JPH11508535A (en) 1999-07-27
MD970253A (en) 1999-05-31
CA2208772A1 (en) 1996-06-27
HUT77651A (en) 1998-07-28
EE9700113A (en) 1997-12-15
WO1996019483A1 (en) 1996-06-27
NZ297360A (en) 2000-03-27
AU4062895A (en) 1996-07-04
AP9701004A0 (en) 1997-07-31
AU4250596A (en) 1996-07-10
LV12019A (en) 1998-04-20
CZ189997A3 (en) 1998-09-16
FI972466A (en) 1997-08-19
LV12019B (en) 1998-07-20
IS4504A (en) 1997-06-11
EP0802916A1 (en) 1997-10-29
AU715378B2 (en) 2000-02-03
SK83897A3 (en) 1998-05-06
BG101647A (en) 1998-03-31
OA10493A (en) 2002-04-10
IL116503A0 (en) 1996-03-31
NO972892D0 (en) 1997-06-20
CN1175259A (en) 1998-03-04

Similar Documents

Publication Publication Date Title
NO972892L (en) Bicyclic Low Molecular Weight Thrombin Inhibitors
WO1995018830A3 (en) Inhibitors of human plasmin derived from the kunitz domains
TW372232B (en) Phenylalanine derivatives
NO177785C (en) Analogous Methods for Preparing Therapeutically Active Alkoxy-4 (1H) -pyridone Derivatives
IS2822B (en) Inhibits human phosphatidyl-inositol 3-kinase delta
BG103233A (en) Heterocyclic thioesters and ketones
NO20021281D0 (en) Wash off investment composition
BR9811099A (en) Urokinase inhibitors
EP1126836A4 (en) Benzamide potassium channel inhibitors
WO2004058185A3 (en) Antiangiogenesis by inhibiting protein kinase ck2 activity
de Feyter et al. Percutaneous transluminal coronary angioplasty for unstable angina
WO2000071515A3 (en) INHIBITORS OF FACTOR Xa
NO308897B1 (en) Benzothiazine dioxides as endothelin antagonists, processes for their preparation, pharmaceutical compositions comprising the compounds, and use of the compounds
EP0930067A3 (en) MMP inhibitors for the treatment of ocular angiogenesis
NO177312C (en) Process for the preparation of delayed effect hirudin derivatives
BR0008310A (en) Alpha-Alanine derivatives
AU4124089A (en) Use of ACE-inhibitor for suppressing the formation of neointima and the reduction of the vascular lumen by vascular wall thickening after vascular damage
TW369541B (en) Thrombin inhibitors
DK478585A (en) 4-ALCOXY-PYRIDO (2,3-D) PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND USE
BR0012391A (en) Diacylhydrazine derivatives
FI943850A (en) 3-alkyloxy, aryloxy or arylalkyloxybenzo (b) thiophene-2-carboxamides as inhibitors of cell adhesion
NO20002408L (en) 5-HT1F antagonists
WO1999002565A3 (en) Agent for the treatment and/or prophylaxis of microcirculation disorders
MX9704594A (en) Heterocyclic keto arginine peptides as thrombin inhibitors.
AUPP345098A0 (en) Novel anti-fibrinolytic agents