SOLID FORMS CONTAINING (-)-O-DESMETHYLVENLAFAXINE AND USE THEREOF Russian patent published in 2013 - IPC C07C215/64 A61K31/137 A61P15/12 A61P25/14 A61P29/00 A61P25/22 

Abstract RU 2477269 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of desmethylvenlafaxine of formula in form of a hydrochloride salt of a stereomerically pure compound which is suitable for treating, preventing or managing a disease selected from depression, pain, anxiety, incontinence or vasomotor symptoms caused by menopause. The crystalline form contains water in amount of about 4% to about 8% of the total weight of the sample, and molar ratio of the water to the hydrochloride salt is about 1:1, and the crystalline form has X-ray powder diffraction peaks at positions of about 12.7, 14.5, 19.1, 21.4, 23.0, 25.5 and 27.3°2θ, and is characterised by the following corresponding unit cell parameters measured at 150 K: a=6.78 A; b=9.29 A; c=27.65 A; α=90°; β=90°; γ=90°. The crystalline form is characterised by weight loss during thermal gravimetric analysis of about 4% to about 8%, primarily about 5.6% of the total weight of the sample when heated from about 25°C to about 110°C and endothermic effect during differential scanning calorimetry with onset temperature of the effect of about 50°C to about 125°C, primarily about 93°C. The crystalline form is non-hygroscopic at relative humidity from about 5% to about 85% and absolute form.

EFFECT: obtaining a compound which is suitable for treating, preventing or managing a disease selected from depression, pain, anxiety, incontinence or vasomotor symptoms caused by menopause.

20 cl, 58 dwg, 7 tbl, 18 ex

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RU 2 477 269 C2

Authors

Sizenski Majkl

Uilkinson Kharold S.

Snunian Dzhon

Kim Norman

Laflin Sharon M.

Bekejl Rodzher P.

Plankett Kevin

Mauso Patrik

Dates

2013-03-10Published

2008-02-21Filed