POLYMORPHOUS FORMS OF 1-[4-(5-CYANOINDOLE-3-YL)BUTYL]-4-(2-CARBAMOYLBENOFURAN-5-YL)-PIPERAZINE HYDROCHLORIDE Russian patent published in 2007 - IPC C07D405/12 A61K31/501 A61P25/00 

Abstract RU 2303598 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel crystalline modifications of 1-[4-(5-cyanoindole-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)-piperazine hydrochloride, crystalline modification of 1-[4-(5-cyanoindole-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)-piperazine hydrochloride hydrate (forms V, VI, VIII) and 1-[4-(5-cyanoindole-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)-piperazine hydrochloride anhydrate (forms IV, III, VII, IX). Proposed forms can be used in preparing solid medicinal formulations for treatment of or prophylaxis of depressive states, anxiety disorders, maniacal-depressive disorders, maniacal syndrome, dementia, disorders associated with substrates deficiency, disorder in sexual function, alimentary disorders, obesity, fibromyalgia, insomnia, psychiatric disorders, brain infarction, hypertension, in treatment of adverse effects in treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesirable post-delivery lactation. Also, invention relates to methods for synthesis of forms V and IV and to pharmaceutical compositions and pharmaceutical preparation based on thereof. Invention provides the improved solubility, reduced hygroscopicity and increased storage time of synthesized compounds and the preparation based on thereof.

EFFECT: improved and valuable properties of forms.

13 cl, 46 dwg, 2 tbl, 16 ex

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RU 2 303 598 C2

Authors

Bate Andreas

Khel'Fert Bernd

Nojenfel'D Shteffen

Knil' Khajke

Bartel'S Mattias

Rudol'F Zuzanne

Bettkher Khenning

Dates

2007-07-27Published

2002-06-05Filed