发明名称 Oxindoles which are inhibitors of CDK-1 and their application in therapeutics
摘要 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.
申请公布号 US2004110770(A1) 申请公布日期 2004.06.10
申请号 US20030644411 申请日期 2003.08.20
申请人 AVENTIS PHARMA SA 发明人 RIOU JEAN-FRANCOIS;MARATRAT MICHEL;GRONDARD LUCILE;THOMPSON FABIENNE;PETITGENET ODILE;MAILLIET PATRICK;LAVAYRE JACQUES
分类号 A61P35/00;A61P43/00;C07D401/06;C07D401/14;C07D409/14;(IPC1-7):A61K31/506;A61K31/443;A61K31/417;A61K31/404;C0743/02 主分类号 A61P35/00
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