POLYMORPHIC MODIFICATIONS OF EPOTILONE ANALOG, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITIONS BASED ON THEREOF Russian patent published in 2006 - IPC C07D491/04 A61K31/427 A61P35/00 

Abstract RU 2272039 C2

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to crystalline polymorphic modifications of strong acting epotilone analog of forma A and forma B represented by the formula (I): Invention proposes a crystalline substance representing a mixture of form A and form B of epotilone analogs. Invention proposes two variants of a method for preparing crystalline polymorphic modification representing form A. Also, invention proposes a pharmaceutical composition inhibiting angiogenesis and comprising an active component that represents crystalline polymorphic modification of epotilone analog of form A, form B or a crystalline polymorphic modification of epotilone analog of the formula (I) wherein this modification has no amorphous component, and a pharmaceutically acceptable carrier. Also, invention proposes a method for treatment of cancer comprising administration in mammal the effective dose of crystalline polymorphic modification of epotilone analog. Invention provides preparing crystalline polymorphic modifications of strong acting epotilone analog of the formula (I) characterizing by improved properties for using in therapy of cancer species.

EFFECT: improved preparing methods, valuable medicinal properties of compounds and composition.

16 cl, 9 dwg, 7 tbl, 5 ex

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RU 2 272 039 C2

Authors

Dimarko Dzhon D.

Gugutas Dzhek Z.

Vitez Imre M.

Davidovich Marta

Galella Majkl

Mehlloj Timoti M.

Guo Zkhenrong

Favro Deni

Dates

2006-03-20Published

2001-08-01Filed