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|Title:||Polymorphic forms of 1-'4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride|
|Abstract:||The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- , crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.|
|Inventor(s):||Bathe; Andreas (Darmstadt, DE), Helfert; Bernd (Ober-Ramstadt, DE), Neuenfeld; Steffen (Messel, DE), Kniel; Heike (Heppenheim, DE), Bartels; Matthias (Darmstadt, DE), Rudolph; Susanne (Dieburg, DE), Bottcher; Henning (Darmstadt, DE)|
|Assignee:||Merck Patentgesellschaft mit Beschrankter Haftung (Darmstadt, DE)|
|Filing Date:||Jun 05, 2002|
|Claims:||1. A process for preparing 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in its crystalline modification IV, having characteristic x-ray diffraction peaks at 6,102, 5,246, 4,695, and 3,615 d(.ANG.), comprising: drying Form V of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monohydrate, having characteristic x-ray diffraction peaks at 6,807, 4,563, 4,416, and 3,503 d(.ANG.), in vacuo at temperatures of 85.degree. to 90.degree. C. |
2. A process according to claim 1, wherein Form V is prepared by: (1) dispersing 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine in tetrahydrofuran (2) converting the 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine base, by addition of aqueous hydrochloric acid into the hydrochloride salt (3) precipitation of Form V at room temperature (4) recovering the precipitated 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monohydrate by filtration.
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