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WO1998054093A1 - Nouveaux inhibiteurs d'angiogenese - Google Patents

Nouveaux inhibiteurs d'angiogenese Download PDF

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Publication number
WO1998054093A1
WO1998054093A1 PCT/US1998/010590 US9810590W WO9854093A1 WO 1998054093 A1 WO1998054093 A1 WO 1998054093A1 US 9810590 W US9810590 W US 9810590W WO 9854093 A1 WO9854093 A1 WO 9854093A1
Authority
WO
WIPO (PCT)
Prior art keywords
pyrimidine
pyrazolo
pyridyl
compound
alkyl
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.)
Ceased
Application number
PCT/US1998/010590
Other languages
English (en)
Inventor
Mark T. Bilodeau
Randall W. Hungate
Richard L. Kendall
Ruth Rutledge
Kenneth A. Thomas, Jr.
Robert Rubino
Mark E. Fraley
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.)
Merck and Co Inc
Original Assignee
Merck and Co 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 GBGB9800681.0A external-priority patent/GB9800681D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Priority to EP98923719A priority Critical patent/EP0984692A4/fr
Priority to JP50079099A priority patent/JP2002501532A/ja
Priority to CA002291709A priority patent/CA2291709A1/fr
Priority to AU75944/98A priority patent/AU734009B2/en
Priority to US09/424,132 priority patent/US6380203B1/en
Publication of WO1998054093A1 publication Critical patent/WO1998054093A1/fr
Anticipated expiration legal-status Critical
Ceased 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Definitions

  • R 4 is H, Cj.io a] ky ⁇ , C 3 - 6 cycloalkyl, C 5 . 10 aryl, C 5 . 10 heteroaryl, C 3 . 10 heterocyclyl, C ⁇ - 6 alkoxyNR 7 R 8 , N0 2 , OH, -NH 2 or C 5 . 10 heteroaryl, said alkyl, aryl, heteroaryl and heterocyclyl being optionally substituted with from one to three members selected from R a ; and all other variables are as described above.
  • VEGF receptor kinase activity is measured by inco ⁇ oration of radio-labeled phosphate into polyglutamic acid, tyrosine, 4: 1 (pEY) substrate.
  • the phosphorylated pEY product is trapped onto a filter membrane and the incoporation of radio- labeled phosphate quantified by scintillation counting.
  • KDR (Terman, B.I. et al. Oncogene (1991) vol. 6, pp. 1677-1683.) and Flt-1 (Shibuya, M. et al. Oncogene (1990) vol. 5, pp. 519- 524) were cloned as glutathione S-transferase (GST) gene fusion proteins. This was accomplished by cloning the cytoplasmic domain of the KDR kinase as an in frame fusion at the carboxy terminus of the GST gene.
  • GST glutathione S-transferase

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La présente invention concerne des composés qui inhibent des enzymes de type tyrosine kinase, des compositions qui contiennent ces composés inhibant la tyrosine kinase, et des procédés d'utilisation des inhibiteurs de tyrosine kinase permettant de traiter des états/maladies dépendant de la tyrosine kinase tels que l'angiogénèse, le cancer, l'athérosclérose, la rétinopathie diabétique ou des maladies auto-immunes chez les mammifères.
PCT/US1998/010590 1997-05-30 1998-05-26 Nouveaux inhibiteurs d'angiogenese Ceased WO1998054093A1 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
EP98923719A EP0984692A4 (fr) 1997-05-30 1998-05-26 Nouveaux inhibiteurs d'angiogenese
JP50079099A JP2002501532A (ja) 1997-05-30 1998-05-26 新規血管形成阻害薬
CA002291709A CA2291709A1 (fr) 1997-05-30 1998-05-26 Nouveaux inhibiteurs d'angiogenese
AU75944/98A AU734009B2 (en) 1997-05-30 1998-05-26 Novel angiogenesis inhibitors
US09/424,132 US6380203B1 (en) 1998-01-14 1998-05-26 Angiogenesis inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US4807697P 1997-05-30 1997-05-30
US60/048,076 1997-05-30
GBGB9800681.0A GB9800681D0 (en) 1998-01-14 1998-01-14 Novel angiogenesis inhibitors
GB9800681.0 1998-01-14

Publications (1)

Publication Number Publication Date
WO1998054093A1 true WO1998054093A1 (fr) 1998-12-03

Family

ID=26312935

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/010590 Ceased WO1998054093A1 (fr) 1997-05-30 1998-05-26 Nouveaux inhibiteurs d'angiogenese

Country Status (5)

Country Link
EP (1) EP0984692A4 (fr)
JP (1) JP2002501532A (fr)
AU (1) AU734009B2 (fr)
CA (1) CA2291709A1 (fr)
WO (1) WO1998054093A1 (fr)

Cited By (162)

* Cited by examiner, † Cited by third party
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EP1109555A4 (fr) * 1998-08-31 2001-11-21 Merck & Co Inc Nouveaux inhibiteurs d'angiogenese
EP1161433A4 (fr) * 1999-03-11 2002-05-08 Merck & Co Inc Inhibiteurs de tyrosine kinase
EP1147107A4 (fr) * 1999-01-20 2002-05-22 Merck & Co Inc Inhibiteurs d'angiogenese
WO2002040485A1 (fr) * 2000-11-17 2002-05-23 Ishihara Sangyo Kaisha, Ltd. Medicaments preventifs ou therapeutiques contre le diabete, contenant des composes a heterocycle fusionne ou leurs sels
WO2003051886A1 (fr) * 2001-12-17 2003-06-26 Smithkline Beecham Corporation Derives de pyrazolopyridazine
US6593326B1 (en) 1998-12-24 2003-07-15 Astrazeneca Ab 2,4-diamino pyrimidine compounds having anti-cell proliferative activity
US6632820B1 (en) 1998-08-29 2003-10-14 Astrazeneca Ab Pyrimidine compounds
US6649759B2 (en) 2000-03-30 2003-11-18 Pfizer Inc. Neuropeptide Y antagonists
US6649608B2 (en) 2000-03-01 2003-11-18 Astrazeneca Ab 2,4-di(hetero-)arylamino (oxy)-5-substituted pyrimidines as antineoplastic agents
US6670368B1 (en) 1999-04-06 2003-12-30 Astrazeneca Ab Pyrimidine compounds with pharmaceutical activity
US6710052B2 (en) 2000-03-01 2004-03-23 Astrazeneca Pyrimidine compounds
US6716831B1 (en) 1999-03-06 2004-04-06 Astrazeneca Ab 2,4-diamino-pyrimidine deprivatives having anti-cell proliferative activity
WO2004087707A1 (fr) * 2003-03-31 2004-10-14 Vernalis (Cambridge) Limited Composes pyrazolopyrimidines et leur utilisation en medecine
US6833456B2 (en) 2002-03-01 2004-12-21 Agouron Pharmaceuticals, Inc. Indolyl-urea derivatives of thienopyridines useful as antiangiogenic agents, and methods for their use
US6838464B2 (en) 2000-03-01 2005-01-04 Astrazeneca Ab 2,4-Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineaoplastic agents
US6844341B2 (en) 2001-02-17 2005-01-18 Astrazeneca Ab Pyrimidine derivatives for inhibition of cell proliferation
US6855719B1 (en) 1999-08-21 2005-02-15 Astrazeneca Ab Imidazo[1,2-A]pyridine and pyrazolo[2,3-A]pyridine derivatives
US6869962B2 (en) 2002-06-14 2005-03-22 Agouron Pharmaceuticals, Inc. Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
US6887874B2 (en) 2000-08-09 2005-05-03 Astrazeneca Ab Cinnoline compounds
US6906065B2 (en) 2000-03-28 2005-06-14 Astrazeneca Ab 4-Amino-5-cyano-2-anilino-pyrimidine derivatives and their use as inhibitors of cell-cycle kinases
US6908920B2 (en) 2000-07-11 2005-06-21 Astrazeneca Ab Pyrimidine derivatives
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US6939872B2 (en) 2001-05-30 2005-09-06 Astrazeneca Ab 2-anilino-pyrimidine derivatives as cyclin dependent kinase inhibitors
US6969714B2 (en) 2000-09-05 2005-11-29 Astrazeneca Ab Imidazolo-5-YL-2-anilino-pyrimidines as agents for the inhibition of the cell proliferation
US6995171B2 (en) 2001-06-21 2006-02-07 Agouron Pharmaceuticals, Inc. Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents
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