| 摘要 |
The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (-OPO3H2), C1- 4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that a t least 2 of R1, R2 and R3 are C1-4alkoxy; A is -CO-, -C(O)O-, -CON(R8)- (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is -O-, -CO-, N(R9)CO-, -CON(R9)-, -N(R9)C(O)O-, -N(R9)CON(R10)-, -N(R9)SO2-, -SO2N(R9)- o r a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl,aminoC1-3alkyl and hydroxyC1-3alkyl ); b is O or an integer from 1 to 4 inclusive, (provided that when bis O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N-(C1-4alkyl)amino, N,N-di(C1-3alkyl)amino, o r of the formula-Y1(CH2)0R11 or -NHCH(R12)COOH;[wherein Y1 is a direct single bond, -O-, -C(O)-, -N(R13)C(O)- or -C(O)N(R13)- (wherein R13 is hydrogen, C1 - 4alkyl,C1-3alkoxyC2-3alkyl, aminoC2-3alkyl or hydroxyC2-3alkyl); e is O or a n integer from 1 to 4 inclusive. |
