Patent ID: 6482850
Filing Date: 2002-11-19
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)C(O)â€”; Z is phenyl, benzyloxy, t-butoxy or CH(CH3)=C(CH3)â€”; A2 is H or CH3C(O)â€”; A3 is H or OH; R and R1 are independently H or an acyl group having an &agr; carbon atom substituted with a hydrolysis-promoting group; wherein the &agr; carbon atom of said acyl group has an (R) configuration, an (S) configuration or a mixture of (R) and (S) configurations; wherein the hydrolysis-promoting group is an atom or group of atoms more electronegative than hydrogen, provided that when the hydrolysis-promoting group comprises an oxygen or sulfur atom directly attached to the &agr; carbon atom of said acyl group, the hydrolysis-promoting group does not comprise a â€”C(O)Oâ€” radical; with the proviso that (a) when R1 is H, A1 is Zâ€”C(O)NHCH(C6H5)CH(OR)C(O)â€” and R is said acyl group, (b) when R is H, R1 is said acyl group and (c) when A1 is H, R1 is said acyl group.