CA2208772A1 - Inhibiteurs de la thrombine bicyclique a faible poids moleculaire - Google Patents

Inhibiteurs de la thrombine bicyclique a faible poids moleculaire

Info

Publication number
CA2208772A1
CA2208772A1 CA002208772A CA2208772A CA2208772A1 CA 2208772 A1 CA2208772 A1 CA 2208772A1 CA 002208772 A CA002208772 A CA 002208772A CA 2208772 A CA2208772 A CA 2208772A CA 2208772 A1 CA2208772 A1 CA 2208772A1
Authority
CA
Canada
Prior art keywords
alkyl
compound according
oxo
aryl
cycloalkyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002208772A
Other languages
English (en)
Inventor
Benoit Bachand
Micheline Tarazi
Sophie Levesque
M. Arshad Siddiqui
John W. Gillard
Patrice Preville
Yves St-Denis
John Dimaio
Annette Marian Doherty
Jeremy John Edmunds
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shire Canada Inc
Original Assignee
Individual
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 GBGB9510265.3A external-priority patent/GB9510265D0/en
Priority claimed from GBGB9510266.1A external-priority patent/GB9510266D0/en
Priority claimed from GBGB9510267.9A external-priority patent/GB9510267D0/en
Application filed by Individual filed Critical Individual
Publication of CA2208772A1 publication Critical patent/CA2208772A1/fr
Abandoned legal-status Critical Current

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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (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)
CA002208772A 1994-12-22 1995-12-21 Inhibiteurs de la thrombine bicyclique a faible poids moleculaire Abandoned CA2208772A1 (fr)

Applications Claiming Priority (10)

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
GB9510267.9 1995-05-22
GB9503136.5 1995-05-22
GB9510265.3 1995-05-22
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
GBGB9510267.9A GB9510267D0 (en) 1995-05-22 1995-05-22 Low molecular weight thiobicyclic thrombin inhibitors
GB9426038.7 1995-05-22
GB9510266.1 1995-05-22

Publications (1)

Publication Number Publication Date
CA2208772A1 true CA2208772A1 (fr) 1996-06-27

Family

ID=27517273

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002208772A Abandoned CA2208772A1 (fr) 1994-12-22 1995-12-21 Inhibiteurs de la thrombine bicyclique a faible poids moleculaire

Country Status (22)

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

Families Citing this family (46)

* 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 (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
EP1007544A1 (fr) * 1996-02-13 2000-06-14 Akzo Nobel N.V. Inhibiteurs de la serine protease
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
AU3232597A (en) * 1996-06-18 1998-01-07 Warner-Lambert Company Pyrrolo{1,2-a}pyrazine-1,4-dione serine protease inhibitors
WO1998005333A1 (fr) * 1996-08-05 1998-02-12 Molecumetics Ltd. Utilisation de mimetiques de feuillets beta comme inhibiteurs de protease et de kinase ou comme inhibiteurs de facteurs de transcription
US6117896A (en) * 1997-02-10 2000-09-12 Molecumetics Ltd. Methods for regulating transcription factors
EP1661566A3 (fr) * 1996-08-05 2008-04-16 Myriad Genetics, Inc. Utilisation de mimétiques de feuillets beta comme inhibiteurs de protéase et de kinase ou comme inhibiteurs de facteurs de transcription
WO1998009987A1 (fr) * 1996-09-06 1998-03-12 Biochem Pharma, Inc. Inhibiteurs lactame de la thrombine
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998028326A1 (fr) * 1996-12-23 1998-07-02 Biochem Pharma Inc. Inhibiteurs bicycliques de thrombine
AU741099B2 (en) * 1997-04-14 2001-11-22 Millennium Pharmaceuticals, 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
US6369063B1 (en) 1997-04-14 2002-04-09 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
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1999015169A1 (fr) * 1997-09-23 1999-04-01 Merck & Co., Inc. Inhibiteurs de thrombine
CA2319766A1 (fr) * 1998-02-12 1999-08-19 Molecumetics Ltd. Imitateurs de .beta. feuillets et procedes lies a leur utilisation
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
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
SK10742001A3 (sk) 1999-01-27 2002-08-06 Ortho-Mcneil Pharmaceutical, Inc. Peptidylové heterocyklické ketóny použiteľné ako inhibítory tryptázy
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
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
WO2003068237A1 (fr) 2002-02-14 2003-08-21 Myriad Genetics, Inc. Mimetiques de feuillet $g(b) ; compositions et methodes connexes
KR20040106291A (ko) 2002-03-22 2004-12-17 지피씨 바이오테크 아게 면역억제 화합물, 이의 제조 방법 및 용도
PE20171335A1 (es) 2014-10-06 2017-09-13 Cortexyme Inc Inhibidores de gingipaina de lisina
JO3637B1 (ar) 2015-04-28 2020-08-27 Janssen Sciences Ireland Uc مركبات بيرازولو- وترايازولو- بيريميدين مضادة للفيروسات rsv
JP6877424B2 (ja) 2015-11-09 2021-05-26 コーテクシーミー， インコーポレイテッド アルギニンジンジパインの阻害剤
BR112019004864A8 (pt) 2016-09-16 2023-03-07 Cortexyme Inc Inibidores cetona de lisina 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
EA202091835A1 (ru) 2018-01-31 2020-10-20 Янссен Сайенсиз Айрлэнд Анлимитед Компани Замещенные циклоалкилом пиразолопиримидины, обладающие активностью против rsv
ES2957316T3 (es) 2018-04-23 2024-01-17 Janssen Sciences Ireland Unlimited Co Compuestos heteroaromáticos que tienen actividad contra VSR

Also Published As

Publication number Publication date
WO1996019483A1 (fr) 1996-06-27
NZ297360A (en) 2000-03-27
PL320965A1 (en) 1997-11-24
CN1175259A (zh) 1998-03-04
AU4250596A (en) 1996-07-10
AP9701004A0 (en) 1997-07-31
NO972892D0 (no) 1997-06-20
IS4504A (is) 1997-06-11
SK83897A3 (en) 1998-05-06
BG101647A (en) 1998-03-31
CZ189997A3 (cs) 1998-09-16
AU715378B2 (en) 2000-02-03
AU4062895A (en) 1996-07-04
MD970253A (ro) 1999-05-31
MX9704718A (es) 1998-06-28
EE9700113A (et) 1997-12-15
OA10493A (en) 2002-04-10
LV12019B (en) 1998-07-20
HUT77651A (hu) 1998-07-28
NO972892L (no) 1997-08-20
FI972466A0 (fi) 1997-06-11
LV12019A (lv) 1998-04-20
EP0802916A1 (fr) 1997-10-29
FI972466A (fi) 1997-08-19
IL116503A0 (en) 1996-03-31
JPH11508535A (ja) 1999-07-27

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued