Patent ID: 6392063
Filing Date: 2002-05-21
Classification: A61K,A61P,C07D

Abstract:
A taxane having the formula: wherein:A1 is H or a group having the formula Zâ€”C(O)NHCH(C6H5)CH(OR)â€”C(O)â€”, A2 is H, or CH3C(O)â€” and A3 is H or OH; Z is phenyl, benzyloxy, (CH3)3COâ€” or CH(CH3)&boxH;C(CH3)â€”; each of R and R1 is H or an acyl group having the formula Y1Y2, provided that (a) when R1 is H, A1 is Zâ€”C(O)NHCH(C6H5)CH(OR)C(O)â€” and R is said acyl group, and (b) when R is H, R1 is said acyl group; Y1 comprises a carbonyl group having a hydrolysis-promoting group substituted at the a carbon; Y2 is â€”CH3; wherein the &agr; carbon on which the hydrolysis-promoting group is substituted has a configuration selected from the group consisting of an (R) configuration, an (S) configuration and a mixture of (R) and (S) configurations.