CRYSTALLINE SOLID FORM OF (2S,5Z)-2-AMINO-7-(ETHANEIMIDOYLAMINO)-2-METHYLHEPT-5-ENOIC ACID 1.5 HYDROCHLORIDE, METHOD FOR ITS PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2008 - IPC C07C257/14 A61K31/155 

FIELD: organic chemistry, chemical technology, pharmacy.

SUBSTANCE: invention relates to a crystalline form of (2S,5Z)-2-amino-7-(ethaneimidoylamino)-2-methylhept-5-enoic acid 1.5 hydrochloride formula 1and its using as a medicinal agent for prophylaxis or treatment of clinical state wherein NO-synthase inhibitor is desirable. Also, invention relates to a pharmaceutical composition possessing the inhibitory effect on activity of NO-synthase and comprising the effective dose of (2S,5Z)-2-amino-7-(ethaneimidoylamino)-2-methylhept-5-enoic acid 1.5 hydrochloride in combination with a pharmaceutically acceptable carrier. Method for preparing crystalline (2S,5Z)-2-amino-7-(ethaneimidoylamino)-2-methylhept-5-enoic acid 1.5 hydrochloride involves the following steps: (a) preparing noncrystalline form of (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid and at least one of steps (b)-(d) and namely, (b) addition of hydrochloric acid up to equivalent 1.5 HCl as a component of (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid, or (c) regulation of the hydrochloric acid concentration with a suitable base up to equivalent 1.5 HCl as a component of (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid, or (d) removing other counter-ions of salt from (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid and addition of hydrochloric acid up to equivalent 1.5 hydrochloride as a component of (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid, and (e) priming (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid 1.5 hydrochloride prepared from crystalline (2S,5Z)-2-amino-2-methyl-7-[(1-iminoethyl)amino]-5-heptenoic acid 1.5 hydrochloride, and (f) optional addition of a solvent. Invention provides preparing crystalline salt of (2S,5Z)-2-amino-7-(ethaneimidoylamino)-2-methylhept-5-enoic acid 1.5 hydrochloride that inhibit or modulates synthesis of nitrogen oxide.

EFFECT: improved preparing method.

7 cl, 4 tbl, 3 ex