NOVEL POLYMORPHOUS FORMS OF LESOPITRON DIHYDROCHLORIDE AND HYDRATE FORMS THEREOF, PREPARATION METHODS, AND COMPOSITIONS BASED ON THEM Russian patent published in 2002 - IPC

Abstract RU 2178789 C2

FIELD: biologically active compounds. SUBSTANCE: invention relates to novel polymorphous forms of lesopitron (2-[4-[4-(chloropyrazol-1-yl] - 1- piperazinyl] pyrimidine) dihydrochloride showing activity relating central nervous system and particularly exhibiting anxiolytic, tranquillizing and antidepressant effects. Polymorphous forms are characterized by X-ray spectra of powder diffraction and IR spectra of scattered reflection. Indicated forms are prepared by crystallization of lesopitron dihydrochloride solution in mono-or polyatomic C1-C4-alcohol involving stepwise cooling followed by drying. Different polymorphous forms, I or II, are obtained depending on cooling conditions. Form I can also be prepared from form II. Lesopitron dihydrochloride hydrates are prepared in air oven at room temperature with air circulation providing required humidity, which depends on hydrate to be obtained. EFFECT: optimized preparation procedure. 17 cl, 8 dwg, 4 tbl, 6 ex

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RU 2 178 789 C2

Authors

Pilar Lupon Roses

Khajme Tomas Navarro

Sal'Vador Puig Torres

Khordi Frigola Konstansa

Dates

2002-01-27Published

1996-05-29Filed