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Phosphonooxymethyl ethers of taxane derivatives

  • US 5,646,176 A
  • Filed: 05/19/1995
  • Issued: 07/08/1997
  • Est. Priority Date: 12/24/1992
  • Status: Expired due to Term
First Claim
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1. A compound having the formula ##STR113## wherein R1 is hydroxy, --OCH2 (OCH2)m OP(O)(OH)2, --OC(O)Rx or --OC(O)ORx ;

  • R2'"'"' is hydrogen, and R2 is hydrogen, hydroxy, --OCH2 (OCH2)m OP(O)(OH)2, --OC(O)Rx or --OC(O)ORx ;

    R3 is hydrogen, hydroxy, C1-6 alkyloxy, --OC(O)Rx, --OCH2 (OCH2)m OP(O)(OH)2 or --OC(O)ORx ;

    one of R6 or R7 is hydrogen and the other is hydroxy, C1-6 alkanoyloxy, or --OCH2 (OCH2)m OP(O)(OH2);

    or R6 and R7 together form an oxo group;

    with the proviso that at least one of R1, R2, R3, R6 or R7 is --OCH2 (OCH2)m OP(O)(OH)2 ;

    m is zero or an integer one to six inclusive;

    R4 and R5 are independently C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or --Z--R6 ;

    Z is a direct bond, C1-6 alkyl or C2-6 alkenyl;

    R6 is aryl, substituted aryl, C3-6 cycloalkyl, or heteroaryl;

    p is 0 or 1; and

    Rx is C1-6 alkyl optionally substituted with one to six same or different halogen atoms, C3-6 cycloalkyl, C2-6 alkenyl or hydroxy;

    or Rx is a radical of the formula ##STR114## wherein D is a bond or C1-6 alkyl; and

    Ra, Rb and Rc are independently hydrogen, amino, C1-6 alkylamino, di-C1-6 alkylamino, halogen, C1-6 alkyl, or C1-6 alkoxy.

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