CDK-1 INHIBITOR OXINDOLES AND THE APPLICATION THEREOF IN THERAPEUTICS

The present invention relates to a compound of formula (I): wherein R5 is selected from the group consisting of 3-pyridyl, 5-pyrimidinyl, -CONH-(C1-C4 alkyl), -NHCO-(C1-C4 alkyl), halogen, -SO2NH2, -NO2, -CF3 or thien-2-ylcarbonyl and -CO2R where R can be hydrogen or C1-C4 alkyl; and Ar is selected...

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Bibliographic Details
Main Authors MARATRAT, MICHEL, GRONDARD, LUCILE, LAVAYRE, JACQUES, MAILLIET, PATRICK, THOMPSON, FABIENNE, RIOU, JEAN-FRANCOIS, PETITGENET, ODILE
Format Patent
LanguageEnglish
French
German
Published 31.08.2005
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention relates to a compound of formula (I): wherein R5 is selected from the group consisting of 3-pyridyl, 5-pyrimidinyl, -CONH-(C1-C4 alkyl), -NHCO-(C1-C4 alkyl), halogen, -SO2NH2, -NO2, -CF3 or thien-2-ylcarbonyl and -CO2R where R can be hydrogen or C1-C4 alkyl; and Ar is selected from the group consisting of 5-imidazolyl, 2-pyrrolyl optionally substituted by a C1-C4 alkyl radical, 2-furyl or 2-thiazolyl, in the E or Z geometrical isomeric form or a mixture of the two geometrical isomeric forms. The invention is also directed to a method of treating primary and secondary tumours in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound of formula I. The invention is also directed to a method of using a compound of formula I to treat cancer, inhibit the proliferation of a cell and induce cell apoptosis, comprising contacting a cell with an effective amount of the compound of formula I., The invention is also directed to a method of preparing the compound of formula I.
Bibliography:Application Number: EP20020704891