Epothilone Derivatives And Their Synthesis And Use

  • Published: Jan 10, 2007
  • Earliest Priority: Jun 22 1998
  • Family: 49
  • Cited Works: 50
  • Cited by: 0
  • Cites: 5
  • Additional Info: Cited Works Published

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The invention relates to epothilone analog represented by the formula I wherein (i) R 2 is absent or oxygen; "a" can be either a single or double bond; "b" can be either absent or a single bond; and "c" can be either absent or a single bond, with the proviso that if R 2 is oxygen then "b" and "c" are both a single bond and "a" is a single bond; if R 2 is absent then "b" and "c" are absent and "a" is a double bond; and if "a" is a double bond, then R 2 , "b" and "c" are absent; R 3 is a radical selected from the group consisting of hydrogen; lower alkyl; -CH=CH 2 ; -C‰¡CH; -CH 2 F; -CH 2 CI; -CH 2 -OH; -CH 2 -O-(C 1 -C 6 -alkyl); and -CH 2 -S-(C 1 -C 6 -alkyl); R 4 and R 5 are independently selected from hydrogen, methyl or a protecting group; and R 1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.


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Document History
  • Publication: Jan 10, 2007
  • Application: Jun 21, 1999
    EP EP 06118853 A
  • Priority: Jun 21, 1999
    EP EP 99931120 A
  • Priority: Jun 22, 1998
    US US 10260298 A

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