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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 Patent Gesellschaft (Darmstadt, DE)|
1. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification IV (Form IV),
wherein said compound exhibits the following XRD data: TABLE-US-00003 No. d (.ANG.) 2.theta. I/I.sub.0 1 9,732 9.08 22 2 6,885 12.85 10 3 6,102 14.50 22 4 5,246 16.89 9 5 4,695 18.89 100 6 4,344 20.43 20 7 4,088 21.72 12 8 3,615 24.61 67 9 3,258 27.35
17 10 3,164 28.18 12.
2. A method of treating a patient suffering from a depressive disorder, an anxiety disorder, a bipolar disorder, mania, dementia, a substance-related disorder, a sexual dysfunction, an eating disorder, obesity, fibromyalgia, a sleeping disorder, a psychiatric disorder, cerebral infarct, tension, side-effects in the treatment of hypertension, a cerebral disorder, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome, undesired puerperal lactation, or combinations thereof, comprising administering to said patient a compound according to claim 1.
3. A process for preparing 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline Form IV according to claim 1, wherein said process comprises: (1) drying Form XI of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monomethanolate at temperatures between 55.degree. and 65.degree. C., wherein said Form XI of 1-[4-5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monomethanolate exhibits the following XRD data: TABLE-US-00004 No. d (.ANG.) 2.theta. I/I.sub.0 1 10,348 8.54 39 2 7,077 12.50 25 3 6,717 13.17 28 4 4,778 18.56 23 5 4,599 19.28 34 6 4,490 19.76 100 7 4,239 20.94 51 8 4,186 21.21 18 9 3,504 25.40 66 10 3,391 26.26 69.
4. A method according to claim 2, wherein said patient is suffering from a depressive disorder.
5. A method according to claim 2, wherein said patient is suffering from major depressive disorder.
6. A method according to claim 2, wherein said patient is suffering from dysthymic disorder.
7. A method according to claim 2, wherein said patient is suffering from adolescent depression.
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