Tyrosine kinase inhibitors and benzoylacrylamide derivatives
    1.
    发明公开
    Tyrosine kinase inhibitors and benzoylacrylamide derivatives 失效
    酪氨酸激酶抑制剂和苯甲酰丙烯酰胺衍生物。

    公开(公告)号:EP0608897A3

    公开(公告)日:1997-02-12

    申请号:EP94101287.4

    申请日:1994-01-28

    摘要: Benzoylacrylamide derivatives of the formula (I):

    wherein R 1 and R 2 each independently represent a hydrogen atom, C 1 ~ C 5 alkyl, C 3 ~ C8 cycloalkyl optionally intervened by -NR 8 - (R 8 represents phenyl or C 1 ~ C 5 alkyl which is unsubstituted or substituted with phenyl),

    (n is an integer of 0 to 3 and X and Y each independently represent a hydrogen atom, a halogen atom, C 1 ~ C 5 alkyl or C 1 ~ C 5 alkoxy), -(CH 2 )m-A (m is an integer of 0 to 3 and A represents an optionally substitued heterocycle), -COR 9 (R 9 represents C 1 ~ C 5 alkyl which is unsubstituted or substituted with phenyl, phenyl which is unsubstituted or substituted with C 1 ~ C 5 alkyl or a halogen atom, or C 1 ~ C 5 alkoxy which is unsubstituted or substituted with phenyl) -SO 2 R 10 (R 10 represents C 1 ~ C 5 alkyl which is unsubstituted or substituted with phenyl or a halogen atom, or phenyl which is unsubstituted or substituted with C 1 ~ C 5 alkyl), or -OR 11 (R 11 represents a hydrogen atom, or C 1 ~ C 5 alkyl which is unsubstituted or substituted with phenyl); or when R 1 and R 2 are taken together, they represent C 3 ~ C6 alkylene optionally intervened by -O- or -NR 12- (R 12 represents a hydrogen atom, phenyl or C 1 ~ C 5 alkyl); and R 3 , R 4 , R 5 , R 6 and R 7 each independently represent a hydrogen atom, a halogen atom, C 1 ~ C 5 alkyl which is unsubstituted or substituted with a halogen atom or -OR 13 (R 13 represents a hydrogen atom or C 1 ~ C 5 alkyl which is unsubstituted or substituted with a halogen atom or phenyl); or when their adjacent substituents are taken together, they represet C 1 ~ C 3 oxyalkylene having one or two oxygen atoms, and pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing at least one of these compounds, which is useful as a tyrosine kinase inhibitor and useful for suppressing the growth of cnacer cells.

    摘要翻译: 式(I)的苯甲酰基丙烯酰胺衍生物:其中R 1和R 2各自独立地表示氢原子,C 1 -C 5烷基,任选被-NR 8取代的C 3 -C 8环烷基, - (R 8表示未被取代或被苯基取代的苯基或C 1 -C 5烷基),CHEM(n为0〜3的整数,X和Y各自独立地表示氢原子,卤素原子 ,C 1 -C 6烷基或C 1 -C 5烷氧基), - (CH 2)mA(m为0至3的整数,A表示任选取代的杂环),-COR 9(R 9) 未取代或被苯基取代的C 1 -C 5烷基,未被取代或被C 1 -C 5烷基或卤素原子取代的苯基或未被取代或被苯基取代的C 1 -C 5烷氧基)-SO 2 R (R 1)表示未取代或被苯基或卤素原子取代的C 1 -C 5烷基,或未被取代的苯基 或被C 1 -C 5烷基取代)或-OR 1(R 1)表示氢原子或未被取代或被苯基取代的C 1 -C 5烷基); 或当R 1和R 2一起时,它们表示任选被-O-或-NR 1 - 2 - (R 1)2表示的氢原子的C 3 -C 6亚烷基 原子,苯基或C 1 -C 5烷基); R 3,R 4,R 5,R 6和R 7各自独立地表示氢原子,卤原子,未取代或被卤素取代的C 1 -C 5烷基 原子或-OR 1 3(R 1)3表示氢原子或未被取代或被卤素原子或苯基取代的C 1 -C 5烷基); 或者当它们相邻的取代基一起被取代时,它们代表具有一个或两个氧原子的C 1 -C 3氧化烯及其药学上可接受的盐,以及含有这些化合物中的至少一种的药物组合物,其可用作酪氨酸激酶抑制剂 并可用于抑制膀胱细胞的生长。

    RETINOID PRODRUG COMPOUND
    7.
    发明公开
    RETINOID PRODRUG COMPOUND 审中-公开
    类维生素A的前体药物CONNECTION

    公开(公告)号:EP2216322A1

    公开(公告)日:2010-08-11

    申请号:EP07830918.4

    申请日:2007-10-31

    摘要: A compound represented by the following general formula (I) :

    [R 1 to R 5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents -NH-CO-, -CO-NH-, -N(COR 6 )-CO-, -CO-N(COR 7 )- (R 6 and R 7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents -Y-CH(R 12 )-COOH, -CHO, -CH-CH-COOH, or -COOR 13 (Y represents a single bond, -CH 2 -, -CH(OH)-, -CO-, -CO-NH-, or -CO-NH-CH 2 -CO-NH-, R 12 represents hydrogen atom or a lower alkyl group, and R 13 represents hydrogen atom, -CH(R 14 )-COOH (R 14 represents hydrogen atom, a lower alkyl group, or hydroxy group), -[CH 2 CH 2 -O] n -CH 2 -CH 2 -OH, CH2-O-[CH 2 CH 2 O] m -CH 2 -OH, or -[CH(CH 3 )-CO-O] p -CH(CH 3 )-COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.