Benzoylethylene derivative

Details Benzoylethylene derivative Benzoylethylene derivative

C - Chemistry, Metallurgy

07

C

C07C 255/40 (2006.01) A61K 31/135 (2006.01) A61K 31/16 (2006.01) A61K 31/215 (2006.01) A61K 31/275 (2006.01) A61K 31/33 (2006.01) C07C 59/90 (2006.01) C07C 69/738 (2006.01) C07C 225/16 (2006.01) C07C 225/20 (2006.01) C07C 229/44 (2006.01) C07C 235/78 (2006.01) C07C 255/41 (2006.01) C07C 255/42 (2006.01) C07C 255/43 (2006.01) C07C 255/56 (2006.01) C07C 317/28 (2006.01) C07C 323/29 (2006.01) C07C 323/62 (2006.01) C07D 211/14 (2006.01) C07D 295/084 (2006.01) C07D 295/104 (2006.01) C07D 295/125 (2006.01) C07D 2

Patent

CA 2178914

A benzoylethylene derivative represented by general formula (I) and a salt thereof wherein R1 to R5 represent each hydrogen, -OR9 (R9 being hydrogen, C1- C5 alkyl, etc.), etc.; R6 represents hydrogen, C1-C5 alkyl, etc.; R7 represents hydrogen, cyano, C1-C5 alkyl, -SOqR15 (q being 0, 1 or 2, and R15 being thienyl, phenyl, etc.), etc.; and R8 represents cyano, -CR22R23X (R22 and R23 being each hydrogen, C1-C5 alkyl, etc., and X being -NR24R25 (wherein R24 and R25 represent each C1-C5 alkyl, or R24 and R25 are combined together to represent alkylene, etc.)), etc. The derivative has potent activities of tyrosine kinase inhibition and cancer cell growth inhibition and is useful as a carcinostatic agent.

Dérivé du benzoyléthylène, et ses sels, de formule générale (1) dans laquelle R?1¿ à R?5¿ représentent chacun hydrogène, -OR?9¿ (R?9¿ représentant hydrogène, C¿1?-C¿5? alkyle, etc.) etc.; R?6¿ représente hydrogène, C¿1?-C¿5? alkyle; R?7¿ représente hydrogène, cyano, C¿1?-C¿5? alkyle, -SO¿q?R?15¿ (q valant 0, 1, ou 2 et R?15¿ équivalant à thyényle, phényle etc.), etc.; R?8¿ représente, cyano, -CR?22¿R?23¿ (R?22¿ et R?23¿ représentant chacun hydrogène, C¿1?-C¿5? alkyle etc., et X représentant -NR?24¿R?25¿ (R?24¿ et R?25¿ équivalant chacun à C¿1?-C¿5? alkyle, ou R?24¿ et R?25¿ étant combinés ensemble pour représenter alkylène, etc.)), etc. Ce dérivé présente des activités puissantes d'inhibition de la tyrosine kinase et de la croissance des cellules cancéreuses, et s'avère utile comme agent cancérostatique.

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