Fumarate salts of a histamine H3 receptor antagonist
The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof.
1. A compound 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide difumarate monohydrate in the crystalline Form I.
2. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.
3. A pharmaceutical composition prepared by formulating a compound according to claim 1 with one or more pharmaceutically acceptable carriers.
4. A process for preparing a pharmaceutical composition comprising formulating a compound according to claim 1 with one or more pharmaceutically acceptable diluents.
5. A process for the manufacture of the 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide difumarate monohydrate according to claim 1 comprising the steps of contacting, under elevated temperature or at ambient temperature, 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide dissolved in a suitable solvent or in a mixture of solvents, with fumaric acid, optionally dissolved in a solvent or in a mixture of solvents; and isolating the precipitated solid.
6. The pharmaceutical composition according to claim 3 , which is in a solid dosage form.