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Hydrolysis-promoting hydrophobic taxane derivatives

  • US 6,392,063 B1
  • Filed: 07/19/2000
  • Issued: 05/21/2002
  • Est. Priority Date: 09/12/1995
  • Status: Expired due to Fees
First Claim
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1. A taxane having the formula:

  • embedded imagewherein;

    A1 is H or a group having the formula Z—

    C(O)NHCH(C6H5)CH(OR)—

    C(O)—

    , A2 is H, or CH3C(O)— and

    A3 is H or OH;

    Z is phenyl, benzyloxy, (CH3)3CO—

    or CH(CH3)═

    C(CH3)—

    ;

    each of R and R1 is H or an acyl group having the formula Y1Y2, provided that (a) when R1 is H, A1 is Z—

    C(O)NHCH(C6H5)CH(OR)C(O)— 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 —

    CH3;

    wherein the α

    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.

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