DERIVATIVES OF EPOTHILONE Russian patent published in 2003 - IPC

Abstract RU 2213741 C2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of epothilone of the formula: wherein Q is taken among group including: wherein R8 is hydrogen atom, alkyl; G is R11 wherein R12 is alkyl, heterocycle; is hydrogen atom; W represents oxygen atom or NR15 wherein R15 is hydrogen atom; Y = X and represents oxygen atom; Z1 and Z2 represent -CH2; B1 and B2 mean OH; R1-R7 mean hydrogen atom, alkyl. Invention relates also to their pharmaceutically acceptable salts, geometrical, optical isomers and stereoisomers under condition that compounds where W and X both represent oxygen atom and R1,R2,R7 represent hydrogen atom; R3,R4,R6 represent methyl group; R8 re[resents hydrogen atom or methyl group; Z1 and Z2 represent CH2; G represents 1-methyl-3-(substituted-3- thiazolyl)- ethenyl; Q as indicated above are excluded. Invention relates also to method for cancer treatment, diseases associated with hyperproliferation of cells and to method providing anti- angiogenesis effect in patient. EFFECT: valuable medicinal properties of compounds. 6 cl, 2 tbl, 2 dwg, 8 ex

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RU 2 213 741 C2

Authors

Vajt Gregori D.

Borzilleri Robert M.

Kim Sung-Khun

Dzhonson Dzhejms A.

Dates

2003-10-10Published

1998-06-16Filed