1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea salt
OwnerJorg Velker, Michael Scherz +1inventors
InventorsJorg Velker, Michael Scherz, Thomas Weller
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Abstract
The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline salt or a non defined salt hydrate thereof 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 salt alone or in combination with other compounds or formulations of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline salt in the preparation of pharmaceutical compositions. The invention also relates to the use of such salts in formulations as neurohormonal antagonists.
Claims23
The compound, 1-[2-(4-Benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea of formula I in the form of a crystalline salt or non-defined crystalline salt hydrate.
A process for preparing 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea of formula I as a salt, comprising:
- a. mixing 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea of formula I with an organic solvent and adding an acid, a solution of an acid in water, a solution of an acid in an organic solvent, or a solution of an acid in a mixture of water with an organic solvent, and stirring the mixture;
- or
- b. mixing 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea of formula I with a mixture of an organic solvent with water and adding an acid, a solution of an acid in water, a solution of an acid in an organic solvent, or a solution of an acid in a mixture of water with an organic solvent, and stirring the mixture;
- or
- c. adding 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea of formula I as a solid, or dissolved in a mixture of an organic solvent with water to an acid, to a solution of an acid in water, to a solution of an acid in an organic solvent, or to a solution of an acid in a mixture of water with an organic solvent, and stirring the mixture;
- or
- d. adding 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea of formula I as a solid, or dissolved in an organic solvent to an acid, to a solution of an acid in water, to a solution of an acid in an organic solvent, or to a solution of an acid in a mixture of water with an organic solvent, and stirring the mixture.
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