Details for Patent: 8,193,195

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 (Darmstadt, DE)
Filing Date:	Nov 12, 2010
Application Number:	12/945,272
Claims:	1. A method of treating a depressive disorder, the method comprising: administering to a patient in need thereof an effective amount of a compound which is a crystalline hydrochloride salt of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- , wherein a depressive disorder is treated in the patient. 2. The method of claim 1, wherein said compound is administered in the form of a pharmaceutical composition comprising an effective amount of said compound and one or more conventional auxiliary substances and/or carriers. 3. The method of claim 2, wherein the compound is an anhydrate of the hydrochloride salt of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- . 4. The method of claim 2, wherein the compound is a hydrate of the hydrochloride salt of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- . 5. The method of claim 4, wherein the hydrate is a monohydrate. 6. The method of claim 4, wherein the hydrate is a hemihydrate. 7. The method of claim 2, wherein, the compound is selected from: 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification III (Form III); 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification IV (Form IV); 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monohydrate in crystalline modification V (Form V); 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII); and a combination thereof. 8. The method of claim 7, wherein the composition comprises Form IV. 9. The method of claim 7, wherein the composition comprises Form IV and Form V. 10. The method of claim 9, wherein the composition comprises Form IV and Form V in a molar ratio of 100 to 1 to 10 to 1. 11. The method of claim 7, wherein the composition comprises Form V. 12. The method of claim 7, wherein the composition comprises Form VIII. 13. The method of claim 7, wherein the compound consists essentially of Form IV and Form V. 14. The method of claim 13, wherein the compound consists essentially of Form IV and Form V in a molar ratio of 100 to 1 to 10 to 1. 15. The method of claim 7, wherein the composition comprises Form III. 16. The method according to any one of the preceding claims, wherein the depressive disorder is major depressive disorder.