CRYSTALLINE FORMS OF (6R)-L-ERYTHRO-TETRAHYDROBIOPTERIN DIHYDROCHLORIDE Russian patent published in 2011 - IPC C07D475/04 A61K31/522 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel crystalline forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and/or solvates (versions) thereof, for which characteristic powder diffraction patterns with radiation Cu_Kα1 are given, with characteristic peaks expressed in values of d (Å). Said modifications can be used to treat neurological disorder. The invention also relates to pharmaceutical compositions (versions) which may additionally contain folate, separately or together with arginine in an effective amount. The folate is folic acid or tetrahydrofolate selected from tetrahydrofolic acid, 5,10-methylene-tetrahydrofolic acid, 10-formyl-tetrahydrofolic acid, 5-formyl-tetrahydrofolic acid or 5-methyl-tetrahydrofolic acid, or polyglutamate thereof or pharmaceutically acceptable salt thereof. The invention also relates to methods of producing (versions) said crystalline modifications. For example, the method of producing crystalline form A of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride involves dissolving (6R)-L-erythro-tetrahydrobiopterin dihydrochloride in water at ambient temperature, and (1) cooling the solution to a low temperature with solidification of the solution, and removing water at pressure ranging from 0.01 to 1 mbar, or (2) removing water from said aqueous solution by filtering and drying with evaporation of water, and extracting said crystalline form.

EFFECT: improved properties of compounds.

42 cl, 18 tbl, 15 dwg, 6 ex