FIELD: chemistry.
SUBSTANCE: invention relates to a polymorphic form I 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid, which is characterised by powder diffraction pattern, produced by X-ray phase analysis (XPA) when exposed to radiation of Cu-Kα, comprising following main peaks 2θ(°): 5.9, 9.3, 9.8, 11.9, 13.7, 14.3, 15.0, 17.8, 18.2–19.3, 19.7, 22.6, 23.4–24.5 and 24.9 +/-0.2. Polymorphic form I is obtained by recrystallisation 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid from ethyl acetate for 24 hours at 40 °C and 5 days at room temperature. Polymorphic form I is intended for preparing a pharmaceutical composition or for use as a medicinal agent, having antagonistic activity on 5-HT4 receptor.
EFFECT: polymorphic form 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid, having improved characteristics of stability and hygroscopicity.
7 cl, 1 tbl, 5 dwg, 6 ex
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