OA10493A - Low molecular weight bicyclic thrombin inhibitors - Google Patents

Low molecular weight bicyclic thrombin inhibitors Download PDF

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Publication number
OA10493A
OA10493A OA70029A OA70029A OA10493A OA 10493 A OA10493 A OA 10493A OA 70029 A OA70029 A OA 70029A OA 70029 A OA70029 A OA 70029A OA 10493 A OA10493 A OA 10493A
Authority
OA
OAPI
Prior art keywords
alkyl
compound according
oxo
cycloalkyl
group
Prior art date
Application number
OA70029A
Other languages
English (en)
Inventor
John Dimaio
Arshad M Siddiqui
John W Gillard
Yves St-Denis
Micheline Tarazi
Patrice Preville
Sophie Levesque
Benoit Bachand
Annette Marian Doherty
Jeremy John Edmunds
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 OA10493A publication Critical patent/OA10493A/en

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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)
OA70029A 1994-12-22 1997-06-18 Low molecular weight bicyclic thrombin inhibitors OA10493A (en)

Applications Claiming Priority (5)

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

Publications (1)

Publication Number Publication Date
OA10493A true OA10493A (en) 2002-04-10

Family

ID=27517273

Family Applications (1)

Application Number Title Priority Date Filing Date
OA70029A OA10493A (en) 1994-12-22 1997-06-18 Low molecular weight bicyclic thrombin inhibitors

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) FI972466A (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 (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 (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
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 pharmaceuticals 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 (es) * 1998-02-12 2003-10-16 Molecumetics Ltd Mimeticos de lamina beta y metodos relacionados con el uso de los mismos.
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 Xa FACTOR 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
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 (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
WO2003082197A2 (en) 2002-03-22 2003-10-09 Gpc Biotech Ag Immunosuppressant compounds, methods and uses related thereto
BR112017006920A8 (pt) 2014-10-06 2023-03-07 Quince Therapeutics Inc Inibidores de lisina gingipaína
JO3637B1 (ar) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc مركبات بيرازولو- وترايازولو- بيريميدين مضادة للفيروسات rsv
CA3004095A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
TWI787202B (zh) 2016-09-16 2022-12-21 美商昆斯治療公司 離胺酸牙齦蛋白酶（gingipain）之酮抑制劑
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
EA202091835A1 (ru) 2018-01-31 2020-10-20 Янссен Сайенсиз Айрлэнд Анлимитед Компани Замещенные циклоалкилом пиразолопиримидины, обладающие активностью против 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 (no) 1997-08-20
AU4062895A (en) 1996-07-04
CN1175259A (zh) 1998-03-04
CA2208772A1 (en) 1996-06-27
WO1996019483A1 (en) 1996-06-27
MD970253A (ro) 1999-05-31
AP9701004A0 (en) 1997-07-31
AU715378B2 (en) 2000-02-03
EE9700113A (et) 1997-12-15
BG101647A (en) 1998-03-31
HUT77651A (hu) 1998-07-28
IS4504A (is) 1997-06-11
SK83897A3 (en) 1998-05-06
MX9704718A (es) 1998-06-28
PL320965A1 (en) 1997-11-24
LV12019B (en) 1998-07-20
AU4250596A (en) 1996-07-10
FI972466A (fi) 1997-08-19
EP0802916A1 (en) 1997-10-29
FI972466A0 (fi) 1997-06-11
NZ297360A (en) 2000-03-27
JPH11508535A (ja) 1999-07-27
NO972892D0 (no) 1997-06-20
LV12019A (lv) 1998-04-20
CZ189997A3 (cs) 1998-09-16

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