C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) A61K 31/4709 (2006.01) A61P 9/02 (2006.01)
Patent
CA 2583845
The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2- methyl~-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the use of said 1-[2-(4-benzyl-4-hydroxy- piperidin-1-yl)-ethyl]-3-(2-methyl-~quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt alone or in combination with other compounds. Further, the present invention relates to formulations of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)~ethyl]-3-(2- methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt in the preparation of pharmaceutical compositions. The invention also relates to the use of such sulfate salts in formulations as neurohormonal antagonists.
L'invention porte sur une 1-[2-(4-benzyl-4-hydroxy-pipéridin-1-yl)-éthyl]-3-(2-méthyl-quinolin-4-yl)-urée utilisée comme sel de sulfate cristallin, stoichiométriquement défini et non hygroscopique, et sur un procédé de préparation de cette dernière. L'invention concerne en outre l'utilisation de ladite 1-[2-(4-benzyl-4-hydroxy-pipéridin-1-yl)-éthyl]-3-(2-méthyl-quinolin-4-yl)-urée comme sel de sulfate cristallin, stoichiométriquement défini et non hygroscopique, seule ou combinée à d'autres composés. L'invention se rapporte aussi à des formulations de la 1-[2-(4-benzyl-4-hydroxy-pipéridin-1-yl)-éthyl]-3-(2-méthyl-quinolin-4-yl)-urée précitée comme sel de sulfate cristallin, stoichiométriquement défini et non hygroscopique, dans la préparation de compositions pharmaceutiques. L'invention concerne enfin l'utilisation des sels de sulfate précités comme antagonistes neurohormonaux dans des formulations.
Bonard Jean Michel
Buchmann Stephan
Redey Stephane
Woinet Bertrand
Actelion Pharmaceuticals Ltd
Gowling Lafleur Henderson Llp
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