SOLID ORAL FORMULATIONS AND CRYSTALLINE FORMS OF APOPTOSIS PROTEIN INHIBITOR Russian patent published in 2016 - IPC C07D417/04 A61K31/427 A61K9/20 A61K9/28 

Abstract RU 2574405 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a crystalline semihydrate form of HA (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluorobenzoyl)thiazol-2-yl]pyrrolidin-1-yl}-2-oxoethyl)-2-methylamino-propionamide described by formula chiral (I)

and being an apoptosis protein inhibitor, which protects cancer cells from apoptosis-caused death. The crystalline semihydrate form of HA compound (I) is characterised by an X-ray powder diffraction pattern containing three or more 2θ values specified in a group consisting of 8.3±0.2, 9.5±0.2, 13.5±0.2, 17.3±0.2, 18.5±0.2 and 18.9±0.2 at room temperature. The crystalline semihydrate form of HA compound (I) is also characterised by an X-ray powder diffraction pattern, a heat pattern of differential scanning calorimetry and a thermographic analysis pattern.

EFFECT: non-hygroscopic and stable polymorphic form of (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluorobenzoyl)thiazol-2-yl]pyrrolidin-1-yl}-2-oxoethyl)-2-methylaminopropionamide.

5 cl, 18 dwg, 10 tbl, 17 ex

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RU 2 574 405 C2

Authors

Dzhivan Tkhakur

Don Jan

Lili Fehn

Dates

2016-02-10Published

2010-08-11Filed