×

C-21 modified epothilones

  • US 6,262,094 B1
  • Filed: 02/17/2000
  • Issued: 07/17/2001
  • Est. Priority Date: 02/22/1999
  • Status: Expired due to Term
0
Associated Cases
0
Associated Defendants
0
Product Citations
0
Petitions
105
Forward Citations
2
Assignments
First Claim
Patent Images

1. Compound having the general formula I where:

  • P—

    Q is a C, C double bond or an epoxide;

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

    R1 is selected from the group consisting of G1 is selected from the group of H, halogen, CN, alkyl and substituted alkyl;

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

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

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

    O, Z4SO2, and optionally substituted glycosyl;

    G5 is selected from the group of halogen, N3, NCS, SH, CN, NC, N(Z1)3+ and heteroaryl;

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

    G7 is CZ7 or N;

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

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

    NH—

    NH— and

    —

    N═

    N—

    ;

    G10 is N or CZ12;

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

    Z1, Z6, Z9, and Z11 are independently selected from the group H, alkyl, substituted alkyl, acyl, and substituted acyl;

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

    Z3, Z5, Z8, and Z10 are independently selected from the group H, alkyl, substituted alkyl, acyl, substituted acyl, aryl, and substituted aryl;

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

    Z7 is selected from the group of H, halogen, alkyl, substituted alkyl, aryl, substituted aryl, OZ8, SZ8, and NZ8Z9; and

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

    with the proviso that when R1 is G1, G2, G3 and G4 cannot simultaneously have the following meanings;

    G1 and G2=H, G3=O and G4=H or Z2C═

    O where Z2=alkyl group and with the proviso that when R1 is  

    G1, G2, and G5 cannot simultaneously have the following meanings;

    G1 and G2=H, and G5=F.

View all claims
  • 2 Assignments
Timeline View
Assignment View
    ×
    ×