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Benzylidene- and cinnamylidine-malononitrile derivatives for the inhibition of proliferative processes in mammalian cells

机译:亚苄基和肉桂苷-丙二腈衍生物可抑制哺乳动物细胞的增殖过程

摘要

57 There are provided pharmaceutical compositions containing as an active ingredient a compound of the general formula (I):wherein R1 and R2 are each independently CN, CONH2 or COOH or one of R1 ad R2 may be -CSNH2 or, when R1 is CN, R2 can also be the groupR3 is H, CH3 or OH,R4, Rs, R6, R7 are each independently H, OH, C1-5 alkyl, C1-5 alkoxy, NH2, CHO, halogen, N02 or COOH, or R4 and R5 together may represent a group -O-CH2-O-;provided that: (a) when R4 ad R7 are each OH, R3, R5 and R6 are each H and one of R1 and R2 is CN, then the other of R1 and R2 cannot be CONH2; and (b) when R3 and R7 are each H, R5 is OH and R4 and R6 are both H or both C1 -5 alkyl, then R1 is CN and R2 is CN or the groupor a pharmaceutically acceptable salt thereof.;There are also provided some novel compounds of formula (I) above.;The compositions and compounds according to the invention are efficient protein-tyrosine kinase inhibitors and are suitable for the inhibition of proliferative processes in mammalian cells.
机译:57.提供了包含通式(I)的化合物作为活性成分的药物组合物: <图像文件=“ IMGA0001.GIF” he =“ 56” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 104” /> 其中R 1 和R 2 分别独立地是CN,CONH 2 或COOH或R 1 和R之一 2 可以是-CSNH 2 ,或者,当R 1 是CN时,R 2 也可以是该组 <图像文件=“ IMGA0002.GIF” he =“ 26” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 57” /> R 3 是H,CH 3 或OH, R 4 ,Rs,R 6 ,R 7 分别独立为H,OH,C 1-5 烷基,C 1-5 烷氧基,NH 2 ,CHO,卤素,N0 2 或COOH或R 4 和R 5 一起可以代表-O-CH 2 -O-组; 前提是:(a)当R 4 广告R 7 分别为OH,R 3 ,R 5 和R 6 分别为H和R < Sub> 1 和R 2 是CN,那么R 1 和R 2 中的另一个不能是CONH 2 ; (b)当R 3 和R 7 分别为H时,R 5 为OH和R 4 R 6 都是H或都是C 1 -5 烷基,则R 1 是CN,R 2 是CN或组 <图像文件=“ IMGA0003.GIF” he =“ 22” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 59” /> ;还提供了一些上述式(I)的新型化合物。;根据本发明的组合物和化合物是有效的蛋白酪氨酸激酶抑制剂,并且适合于在哺乳动物细胞中抑制增殖过程。

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