申请人:Boehringer Ingelheim Pharma KG
公开号:US06762180B1
公开(公告)日:2004-07-13
Indolinones of the formula
having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are:
(a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,
(b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and
(c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
公式为的吲哚酮对受体酪氨酸激酶和细胞周期蛋白/CDK复合物,以及内皮细胞和各种肿瘤细胞的增殖具有抑制作用。示例包括:
(a) 3-Z-[1-(4-(哌啶-1-基甲基)-苯胺基)-1-苯基亚甲基]-6-乙氧羰基-2-吲哚酮,
(b) 3-Z-(1-(4-(哌啶-1-基甲基)-苯胺基)-1-苯基亚甲基)-6-氨基甲酰基-2-吲哚酮,以及
(c) 3-Z-[1-(4-(哌啶-1-基甲基)-苯胺基)-1-苯基亚甲基]-6-甲氧羰基-2-吲哚酮。