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Epothilone derivatives for the treatment of refractory tumors

  • US 6,727,276 B2
  • Filed: 02/08/2002
  • Issued: 04/27/2004
  • Est. Priority Date: 02/20/2001
  • Status: Expired due to Fees
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First Claim
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1. A method of treating a tumor in a mammal, said tumor having demonstrated resistance to oncology therapy and sensitive to compounds of Formula I, comprising administering to said mammal an effective amount of a composition comprising a pharmaceutically acceptable carrier and an epothilone compound of formula I:

  • embedded imagewherein;

    P—

    Q is a carbon-carbon double bond or an epoxide;

    G is embedded imageR is selected from the group of H, alkyl, and substituted alkyl;

    R1 selected from the group consisting of embedded imageR2 is embedded imageG1 is selected from the group consisting of H, halogen, CN, alkyl and substituted alkyl;

    G2 is selected from the group consisting of H, alkyl, and substituted alkyl;

    G3 is selected from the group consisting of O, S, and NZ1;

    G4 is selected from the group consisting of H, alkyl, substituted alkyl, OZ2, NZ2Z3, Z2C═

    O, Z4SO2, and optionally substituted glycosyl;

    G5 is selected from the group consisting of halogen, N3, NCS, SH, CN, NC, N(Z1)3+ and heteroaryl, provided that if G1 and G2 are both hydrogen, G5 is not halogen;

    G6 is selected from the group consisting of H, alkyl, substituted alkyl, CF3, OZ5, SZ5, and NZ5Z6;

    G7 is CZ7 or N;

    G8 is selected from the group consisting of H, halogen, alkyl, substituted alkyl, OZ10, SZ10, NZ10Z11;

    G9 is selected from the group consisting of O, S, —

    NH—

    NH— and

    —

    N═

    N—

    ;

    G10 is N or CZ12;

    G11 is selected from the group consisting of H2N, substituted H2N, alkyl, substituted alkyl, aryl, and substituted aryl;

    each Z1, Z6, Z9, and Z11 is, independently, selected from the group consisting of H, alkyl, substituted alkyl, acyl, and substituted acyl;

    Z2 is selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, and heterocycle;

    each Z3, Z5, Z8, and Z10 is, independently, selected from the group consisting of H, alkyl, substituted alkyl, acyl, substituted acyl, aryl, and substituted aryl;

    Z4 is selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, and heterocycle;

    Z7 is selected from the group consisting of H, halogen, alkyl, substituted alkyl, aryl, substituted aryl, OZ8, SZ8, and NZ8Z9, provided that if G6 and G8 are both H, then Z7 is not also H; and

    Z12 is selected from the group consisting of H, halogen, alkyl, substituted alkyl, aryl, and substituted aryl;

    with the proviso that when R1 is embedded imageG1, G2, G3 and G4 cannot simultaneously have the following meanings;

    G1 and G2 are H, G3 is O, and G4 is H or Z2C═

    O wherein Z2 is an alkyl group, and pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof.

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