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:
An N-acyl-N-phenyltetrahydrophthalamic acid derivative represented by general formula (I), a process for producing the same, and a herbicide containing the same as the active ingredient: wherein X and Y represent each independently hydrogen or halogen; R1 represents hydrogen, halogen, lower alkoxy, lower alkenyloxy, lower alkynyloxy, lower alkoxyalkoxy or lower alkoxycarbonylalkoxy; R2 represents lower alkyl, halogenated lower alkyl, or (un)substituted phenyl; and R3 represents lower alkoxy, lower alkenyloxy, lower alkynyloxy, lower alkoxyalkoxy, benzyloxy, or lower alkoxycarbonylalkoxy. The herbicide is widely applicable to upland fields, paddy fields, orchards, pastures, turfs, forests, non-crop lands and so forth, and is highly safe to crops, thus proving very useful.
摘要:
An N-acyl-N-phenylmaleamic acid derivative represented by general formula (I), a process for producing the same, and a herbicide containing the same as the active ingredient, which is very useful as a herbicide because it can be widely applied to upland field, lowland, orchard, pasture, turf, forest and non-crop land, and is highly safe for crop. In formula (I), X and Y represent each independently hydrogen or halogen; R represents hydrogen, halogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxyalkyl or lower alkoxycarbonylalkyl; R represents lower alkyl, halogenated lower alkyl or (un)substituted phenyl; R represents hydrogen or lower alkyl; and R represents hydroxy, lower alkoxy, lower alkenyloxy, lower alkynyloxy, lower alkoxy-alkoxy, benzyloxy or lower alkoxycarbonylalkoxy.
摘要:
This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumour growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.
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.
摘要:
An N-aryloxyacyl-N-phenyltetrahydrophthalamic acid derivative represented by general formula (I), a process for producing the same, and a herbicide containing the same as the active ingredient, which is very useful as a herbicide because it can be widely applied to upland field, lowland, orchard, pasture, turf, forest and non-crop land, and is highly safe for crop. In formula (I), X and Y represent each independently hydrogen or halogen; R¹ represents hydrogen, halogen, lower alkyl, lower alkoxy, lower alkenyloxy, lower alkynyloxy, lower alkoxyalkoxy or lower alkoxycarbonylalkoxy; R² represents hydrogen or lower alkyl; R³ represents hydroxy, lower alkoxy, lower alkenyloxy, lower alkynyloxy, lower alkoxy-alkoxy, benzyloxy or lower alkoxycarbonylalkoxy; and m represents an integer of 0 to 5.