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AP9701004A0 - Low molecular weight bicyclic thrombin inhibitors. - Google Patents

Low molecular weight bicyclic thrombin inhibitors.

Info

Publication number
AP9701004A0
AP9701004A0 APAP/P/1997/001004A AP9701004A AP9701004A0 AP 9701004 A0 AP9701004 A0 AP 9701004A0 AP 9701004 A AP9701004 A AP 9701004A AP 9701004 A0 AP9701004 A0 AP 9701004A0
Authority
AP
ARIPO
Prior art keywords
compositions
molecular weight
low molecular
thrombin inhibitors
compounds
Prior art date
Application number
APAP/P/1997/001004A
Inventor
John Gillard
John Dimaio
Arshad M 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 AP9701004A0 publication Critical patent/AP9701004A0/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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin having formula (i), their preparation and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.
APAP/P/1997/001004A 1994-12-22 1995-12-21 Low molecular weight bicyclic thrombin inhibitors. AP9701004A0 (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
AP9701004A0 true AP9701004A0 (en) 1997-07-31

Family

ID=27517273

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1997/001004A AP9701004A0 (en) 1994-12-22 1995-12-21 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) FI972466L (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 (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6245764B1 (en) 1995-03-24 2001-06-12 Molecumetics Ltd. 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
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
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
CN1212706A (en) * 1996-02-13 1999-03-31 阿克佐诺贝尔公司 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
US6117896A (en) 1997-02-10 2000-09-12 Molecumetics Ltd. Methods for regulating transcription factors
ES2262184T3 (en) * 1996-08-05 2006-11-16 Myriad Genetics, Inc. USE OF BETA SHEET MIMETICS AS PROTEASE AND KINASA INHIBITORS OR 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
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
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
AU5526098A (en) * 1996-12-23 1998-07-17 Biochem Pharma Inc. Bicyclic thrombin inhibitors
CA2285659A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
NZ500353A (en) 1997-04-14 2002-02-01 Cor Therapeutics Inc Cyclic diaza compounds that are selective inhibitors of factor Xa
WO1998046628A1 (en) * 1997-04-14 1998-10-22 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
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
EP1017383A4 (en) * 1997-09-23 2001-11-28 Merck & Co Inc THROMBIN INHIBITORS
ATE230414T1 (en) * 1998-02-12 2003-01-15 Molecumetics Ltd BETA SHEET MIMETICS AND METHOD OF USE THEREOF
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
EP1140862A4 (en) 1998-12-23 2004-07-28 Bristol Myers Squibb Pharma Co THROMBIN OR FACTOR Xa INHIBITORS
US6469036B1 (en) 1999-01-27 2002-10-22 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
US7309688B2 (en) 2000-10-27 2007-12-18 Johnson & Johnson Consumer Companies Topical anti-cancer compositions and methods of use thereof
EP1265849B1 (en) * 2000-03-23 2006-10-25 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
CA2413241A1 (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
NZ535315A (en) 2002-03-22 2008-02-29 Gpc Biotech Ag Immunosuppressant compounds, methods and uses related thereto
CN111349053A (en) 2014-10-06 2020-06-30 库特克希米公司 Inhibitors of lysine porphyromonas gingivalis protease
JO3637B1 (en) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc Rsv antiviral pyrazolo- and triazolo-pyrimidine compounds
WO2017083433A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
CA3036862A1 (en) 2016-09-16 2018-03-22 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
MX2020008061A (en) 2018-01-31 2020-09-09 Janssen Sciences Ireland Unlimited Co Cycloalkyl substituted pyrazolopyrimidines having activity against rsv.
MX2020011200A (en) 2018-04-23 2020-11-13 Janssen Sciences Ireland Unlimited Co Heteroaromatic compounds having activity against rsv.

Also Published As

Publication number Publication date
LV12019A (en) 1998-04-20
FI972466A7 (en) 1997-08-19
CZ189997A3 (en) 1998-09-16
LV12019B (en) 1998-07-20
AU715378B2 (en) 2000-02-03
AU4250596A (en) 1996-07-10
BG101647A (en) 1998-03-31
OA10493A (en) 2002-04-10
SK83897A3 (en) 1998-05-06
IL116503A0 (en) 1996-03-31
MX9704718A (en) 1998-06-28
MD970253A (en) 1999-05-31
HUT77651A (en) 1998-07-28
EP0802916A1 (en) 1997-10-29
EE9700113A (en) 1997-12-15
FI972466A0 (en) 1997-06-11
CN1175259A (en) 1998-03-04
NO972892D0 (en) 1997-06-20
AU4062895A (en) 1996-07-04
PL320965A1 (en) 1997-11-24
NO972892L (en) 1997-08-20
WO1996019483A1 (en) 1996-06-27
JPH11508535A (en) 1999-07-27
IS4504A (en) 1997-06-11
FI972466L (en) 1997-08-19
NZ297360A (en) 2000-03-27
CA2208772A1 (en) 1996-06-27

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