Oxindoler som CDK-1-inhibitorer og deres anvendelse i terapi

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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Bibliographische Detailangaben
Hauptverfasser: MARATRAT, MICHEL, GRONDARD, LUCILE, LAVAYRE, JACQUES, MAILLIET, PATRICK, THOMPSON, FABIENNE, RIOU, JEAN-FRANCOIS, PETITGENET, ODILE
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Sprache:dan
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Zusammenfassung: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.