Tyrosine kinase inhibitors and benzoylacrylamide derivatives

Details Tyrosine kinase inhibitors and benzoylacrylamide derivatives Tyrosine kinase inhibitors and benzoylacrylamide derivatives

C - Chemistry, Metallurgy

07

C

C07C 235/78 (2006.01) A61K 31/165 (2006.01) A61K 31/33 (2006.01) B21F 19/00 (2006.01) C07C 235/88 (2006.01) C07D 207/337 (2006.01) C07D 209/20 (2006.01) C07D 211/58 (2006.01) C07D 213/75 (2006.01) C07D 295/185 (2006.01) C07D 307/54 (2006.01) C07D 317/60 (2006.01) C07D 333/24 (2006.01) C22F 1/00 (2006.01) H01B 12/10 (2006.01) H01B 13/00 (2006.01)

Patent

CA 2114333

ABSTRACT OF THE DISCLOSURE Benzoylacrylamide derivatives of the formula (I): Image (I) wherein R1 and R2 each independently represent a hydrogen atom, C1 ~ C5 alkyl, C3 ~ C8 cycloalkyl optionally intervened by -NR8- (R8 represents phenyl or C1 ~ C5 alkyl which is unsubstituted or substituted with phenyl), Image (n is an integer of 0 to 3 and X and Y each independently represent a hydrogen atom, a halogen atom, C1 ~ C5 alkyl or C1 ~ C5 alkoxy), -(CH2)m-A (m is an integer of 0 to 3 and A represents an optionally substitued heterocycle), -COR9 (R9 represents C1 ~ C5 alkyl which is unsubstituted or substituted with phenyl, phenyl which is unsubstituted or substituted with C1 ~ C5 alkyl or a halogen atom, or C1 ~ C5 alkoxy which is unsubstituted or substituted with phenyl) -SO2R10 (R10 represents C1 ~ C5 alkyl which is unsubstituted or substituted with phenyl or a halogen atom, or phenyl which is unsubstituted or substituted with C1 ~ C5 alkyl), or -OR11 (R11 represents a hydrogen atom, or C1 ~ C5 alkyl which is - 56 - unsubstituted or substituted with phenyl); or when R1 and R2 are taken together, they represent C3 ~ C6 alkylene optionally intervened by -O- or -NR12- (R12 represents a hydrogen atom, phenyl or C1 ~ C5 alkyl); and R3, R4, R5, R5 and R7 each independently represent a hydrogen atom, a halogen atom, C1 ~ C5 alkyl which is unsubstituted or substituted with a halogen atom or -OR13 (R13 represents a hydrogen atom or C1 ~ C5 alkyl which is unsubstituted or substituted with a halogen atom or phenyl); or when their adjacent substituents are taken together, they represent C1 ~ C3 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. - 57 -

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