Benzoylacetylene derivatives

Details Benzoylacetylene derivatives Benzoylacetylene derivatives

C - Chemistry, Metallurgy

07

C

C07C 225/00 (2006.01) A61K 31/00 (2006.01) C07C 17/26 (2006.01) C07C 43/23 (2006.01) C07C 45/00 (2006.01) C07C 45/29 (2006.01) C07C 45/67 (2006.01) C07C 49/794 (2006.01) C07C 49/796 (2006.01) C07C 49/807 (2006.01) C07C 49/813 (2006.01) C07C 49/835 (2006.01) C07C 49/84 (2006.01) C07C 69/007 (2006.01) C07C 69/017 (2006.01) C07C 69/738 (2006.01) C07C 205/45 (2006.01) C07C 225/16 (2006.01) C07C 225/20 (2006.01) C07C 235/16 (2006.01) C07C 235/78 (2006.01) C07C 271/18 (2006.01) C07C 275/28 (2006.01) C07C 275/38 (

Patent

CA 2128991

Abstract of the disclosure A compound of the following formula (I) Image ??? (I) wherein R1~ R5 are independently hydrogen; -OR7 wherein R7 is hydrogen, C1~ C5 alkyl optionally substituted by halogen or phenyl, or -COR8 wherein R8 is phenyl or C1~ C5 alkyl optionally substituted by phenyl; halogen; C1~ C5 alkyl optionally substituted by halogen; -NR9R10 wherein R9 and R10 are independently hydrogen, phenyl, C1~ C5 alkyl optionally substituted by phenyl, benzoyl, or acetyl; -SOpR11 wherein p is 0, 1 or 2, R11 is C1~ C5 alkyl or phenyl; cyano; or nitro; or when adjacent substituents are taken together, they may represent C1~ C3 oxyalkylene having one or two oxygen atoms, R6 is hydrogen; C1~ C5 alkyl; Image -128- wherein Y1, Y2 and Y3 are independently hydrogen, pyridyl, C1~ C5 alkyl, phenyl or halogen; Image wherein Z1, Z2 and Z3 ore independently hydrogen, C1~ C5 alkyl or halogen; C3~ C12 trialkylsilyl; -COR12 wherein R12 is C1~ C5 alkyl, phenyl, C1~ C5 alkoxy optionally substituted by phenyl, or -NR13R14 wherein R13 and R14 are independently hydrogen, C1~ C5 alkyl optionally substituted by phenyl, or phenyl optionally substituted by halogen; or -CR15R16X wherein R15 and R16 are independently hydrogen, phenyl, C1~ C5 alkyl optionally substituted by phenyl, or C3~ C8 cycloalkyl, or when taken together to be C3~ C7 alkylene optionally substituted by C1~ C5 alkyl, X is -OR17 wherein R17 is hydrogen, C1~ C5 alkyl optionally substituted by phenyl, or -COR18 wherein R18 is phenyl or C1~ C5 alkyl optionally substituted by phenyl, -COR19 wherein R19 is hydroxyl, phenyl optionally substituted by C1~ C5 alkyl, C1~ C5 alkyl optionally substituted by phenyl, C1~ C5 alkoxy optionally substituted by phenyl, or -NR20R21 wherein R20 and R21 are independently hydrogen, C1~ C5 alkyl or phenyl optionally substituted by halogen, -SOpR22 wherein p is 0, 1 or 2, R22 is -129- C1~ C5 alkyl or phenyl, or -NR23R24 wherein R23 and R24 are independently hydrogen, phenyl optionally substituted by halogen or C1~ C5 alkyl, or C1~ C5 alkyl optionally substituted by hydroxyl, phenyl, C1~ C5 alkylamino, C2~ C8 dialkylamino or indolyl, C3~ C8 cycloalkyl, pyridyl, -SO2R27 wherein R27 is phenyl optionally substituted by C1 ~ C3 alkoxy, or -COR25 wherein R25 is C1~ C5 alkyl, phenyl, or C1~ C5 alkoxy optionally substituted by pyridyl, N-methylpyridyl, N-oxopyridyl or phenyl optionally substituted by carboxyl or sodium carboxylate, or when R23 and R24 are taken together, they are C3~ C6 alkylene optionally containing therein -O-, Image or -NR26- wherein R26 is hydrogen, phenyl or C1~ C5 alkyl, or C3~ C6 alkylene optionally substituted by C1~ C5 alkyl with a proviso that when R6 is hydrogen, R2 and R3 are not methoxy, or its salt, 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 cancer cells. -130-

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