POLYMORPHOUS FORMS OF 1-[4-(5-CYANOINDOLE-3-YL)BUTYL]-4-(2-CARBAMOYLBENOFURAN-5-YL)-PIPERAZINE HYDROCHLORIDE

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)-piper...

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Hauptverfasser: KHEL'FERT BERND, NOJENFEL'D SHTEFFEN, BARTEL'S MATTIAS, RUDOL'F ZUZANNE, BATE ANDREAS, KNIL' KHAJKE, BETTKHER KHENNING
Format: Patent
Sprache:eng ; rus
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Zusammenfassung: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