Details for Patent: 8,921,375
✉ Email this page to a colleague
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 hypertension, cerebral disorders, chronic pain, acromegaly, 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: | May 30, 2014 |
Application Number: | 14/291,931 |
Claims: | 1. A method of treating a patient suffering from a depressive disorder, the method comprising administering to the patient an effective amount of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII), wherein the crystalline modification VIII is characterized by at least three characteristic peaks selected from the 2Theta values corresponding to 11.55.+-.0.1, 13.26.+-.0.1, 13.53.+-.0.1, 15.48.+-.0.1, 16.89.+-.0.1, 18.87.+-.0.1, 19.82.+-.0.1, 20.49.+-.0.1, 23.74.+-.0.1 and 27.50.+-.0.1 degrees. 2. The method of claim 1, wherein the crystalline modification VIII is characterized by characteristic peaks at 2Theta values corresponding to those exhibited in FIG. 20. 3. The method of claim 1, wherein the compound is administered in the form of a pharmaceutical composition comprising an effective amount of the compound and one or more conventional auxiliary substances and/or carriers. 4. The method of claim 3, wherein the composition comprises 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride anhydrate in crystalline modification IV (Form IV). 5. The method of claim 3, wherein the composition comprises 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride anhydrate in crystalline modification IV (Form IV) and 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride monohydrate in crystalline modification V (Form V). 6. The method of claim 1, wherein the depressive disorder is major depressive disorder. 7. A method of treating a patient suffering from a depressive disorder, the method comprising administering to the patient an effective amount of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII), wherein the crystalline modification VIII is characterized by an IR spectrum with wavenumbers corresponding to the wavenumbers exhibited in FIG. 8. 8. The method of claim 7, wherein the compound is administered in the form of a pharmaceutical composition comprising an effective amount of the compound and one or more conventional auxiliary substances and/or carriers. 9. The method of claim 8, wherein the composition comprises 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride anhydrate in crystalline modification IV (Form IV). 10. The method of claim 8, wherein the composition comprises 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride anhydrate in crystalline modification IV (Form IV) and 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride monohydrate in crystalline modification V (Form V). 11. The method of claim 7, wherein the depressive disorder is major depressive disorder. |