Epothilone derivatives and their synthesis and use

Details Epothilone derivatives and their synthesis and use Epothilone derivatives and their synthesis and use

2003-03-11

2009-08-25

Andres, Janet L. (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S187000, C548S194000

Reexamination Certificate

active

07579366

ABSTRACT:
The invention relates to epothilone analog represented by the formula Iwherein(i) R2is 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 R2is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent;R3is a radical selected from the group consisting of hydrogen; lower alkyl; —CH═CH2; —C≡CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl);R4and R5are independently selected from hydrogen, methyl or a protecting group; andR1is 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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Schiff,

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