Acid addition salts of thienopyrancarboxamide derivatives
AssigneeRecordati Ireland Limited
InventorsAmedeo Leonardi, Gianni Motta
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Abstract
The invention relates to novel addition salts of N-{3-[4-(2-Methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide, comprising N-{3-[4-(2-Methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide and an acid counterion wherein the acid counterion is selected from the group consisting of: (i) inorganic acids and (ii) sulfonic acids.
Claims25
An acid addition salt of N-{3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide selected from the group of consisting of inorganic, sulfonic, monocarboxylic, and aromatic addition salts of N-{3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide.
A crystalline mesylate salt of N-{3-[4-(2-Methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide, having at least one significant x-ray powder diffraction peak at a 2θ value selected from the group consisting of 10.97, 14.67, 15.73, 16.49, 18.75, 20.76, 22.07, 22.73, 24.35, 26.65, and 27.74.
A method for preparing an acid addition salt of N-{3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide comprising, reacting the free base of N-{3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl}-7-oxo-5-trifluoromethyl-7H-thieno[3,2-b]pyran-3-carboxamide with an acid in an organic solvent to form the acid addition salt.
Dependencies are inferred from the claim text.