Patent ID: 6602898
Filing Date: 2003-08-05
Classification: A61K,A61P,C07D

Abstract:
A compound represented by formula (1), whereinwhen the Xâ€”Y bond is a single bond, X and Y are independently selected from the group consisting of: CW1W2 wherein W1 and W2 are independently selected from the group comprising one of a hydrogen atom, a halogen, a hydroxyl group, a lower alkyl group, a substituted lower alkyl group, a lower alkoxy group, a cycloalkyl group and a cycloalkenyl group, C&boxH;O, and C&boxH;NOW3 wherein W3 comprises a hydrogen atom or a lower alkyl group; when the Xâ€”Y bond is a double bond, X and Y independently comprise CW4 wherein W4 comprises any one of a hydrogen atom, a halogen, a hydroxyl group, a lower alkyl group, a substituted lower alkyl group, a lower alkoxy group and an acyloxy group; Z comprises any one of S, S&boxH;O and SO2; U comprises C; R1 to R4 are independently selected from the group consisting of a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a substituted cycloalkyl group, a lower alkenyl group, a substituted lower alkenyl group, a lower alkynyl group, a substituted lower alkynyl group, a halogen, a lower alkylcarbonyl group, a substituted lower alkylcarbonyl group, a trihalomethyl group, V1W5, a nitro group, an amino group, a substituted amino group, a cyano group, an acyl group, an acylamino group, a substituted acyl group, a substituted acylamino group, an aromatic ring, a substituted aromatic ring, a heterocycle and a substituted heterocycle wherein V1 comprises any one of S, S&boxH;O and SO2, W5 comprises any one of a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a lower alkylcarbonyl group and a substituted lower alkylcarbonyl group, an acyloxy group and a trihalomethyl group; R5 to R8 are independently selected from the group consisting of a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a lower alkenyl group, a substituted lower alkenyl group, a lower alkynyl group, a substituted lower alkynyl group, a halogen, a lower alkylcarbonyl group, a substituted lower alkylcarbonyl group, a trihalomethyl group, V2W7, a nitro group, an amino group, a substituted amino group, an acylamino group, an aromatic ring, a substituted aromatic ring, a heterocycle and a substituted heterocycle; wherein V2 comprises one of S, S&boxH;O and SO2, W7 comprises one of a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a lower alkylcarbonyl group, a substituted lower alkylcarbonyl group and a trihalomethyl group, wherein: when X is CHW0, CW0W0 or CW0 at least one of R5 to R8 is a hydroxyl group, provided that at least one of R5, R7 or R8 is a hydroxy group when the Xâ€”Y bond is CH(C2H5)CO and R6 is a hydroxyl group and when X is other than CHW0, CW0W0 or CW0 at least one of R5 to R8 is a hydroxyl group and, at the same time, at least one of the other R5 to R8 is a group of OR wherein W0 is any one selected from a lower alkyl group and a substituted lower alkyl group and R is any one selected from the group consisting of a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a lower alkylcarbonyl group and a substituted lower alkylsilyl group; and when Xâ€”Y comprises CH2CH2, CHBrCH2, CH2CO, CHBrCO, CH&boxH;CH, CH&boxH;COCOCH3 or CH&boxH;COCH3, at least one of R1 to R4 is an aromatic ring, a substituted aromatic ring, a heterocycle or a substituted heterocycle provided that when both R6 and R7 are hydroxyl groups, any one of R1 to R4 is not a phenyl group; or at least one of R1 to R4 comprises SW8 or S(O)W9 wherein W8 and W9 independently comprise a lower alkyl group or a substituted lower alkyl group; or R2 comprises either a lower alkyl group or a substituted lower alkyl group and, at the same time, R8 comprises a hydroxyl group; or at least one of R1 to R4 comprises a lower alkylcarbonyl group provided that the number of carbon atoms of the lower alkyl group is 3 or more, a cycloalkylcarbonyl group or a cycloalkenylcarbonyl group and, at the same time, R8 is a hydroxyl group; or at least one of R1 to R4 comprises a cyano group; or at least one of R1 to R4 comprises a halogen and, at the same time, Z is any one of S, S&boxH;O and SO2; or R5 and R6 comprise hydroxyl groups and, at the same time, Z is S; or at least one of R1 to R4 comprises â€”C(&boxH;NOR)CH3 wherein R comprises a hydrogen atom or a lower alkyl group, an optical isomer thereof, a conjugate thereof or a pharmaceutically acceptable salt thereof.