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Claims for Patent: 8,673,921

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Claims for Patent: 8,673,921

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)
Application Number:14/032,183
Patent Claims: 1. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride in its crystalline modification, wherein the compound is an anhydrate, hydrate, solvate or dihydrochloride.

2. The compound of claim 1, wherein the compound is an anhydrate in crystalline modification III.

3. The compound of claim 1, wherein the compound is an anhydrate in crystalline modification VII.

4. The compound of claim 1, wherein the compound is a solvate in crystalline modification XI.

5. A pharmaceutical composition comprising 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in its crystalline modification IV and one or more hydrated forms of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.

6. A pharmaceutical composition according to claim 5, wherein the composition comprises 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monohydrate in its crystalline modification Form V.

7. A pharmaceutical composition according to claim 6, wherein Form IV and Form V are in a molar ratio of about 100 to 1 to 10 to 1.

8. A pharmaceutical composition according to claim 6 comprising an active ingredient consisting essentially of a mixture of Form IV and Form V.

9. A pharmaceutical composition according to claim 8, wherein Form IV and Form V are in a molar ratio of about 100 to 1 to 10 to 1.

10. 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 and undesired puerperal lactation, or combinations thereof, comprising administering to the patient in need thereof the pharmaceutical composition of claim 6.

11. A pharmaceutical composition comprising a compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in its crystalline modification IV, and one or more conventional auxiliary substances and/or carriers.

12. 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 and undesired puerperal lactation, or combinations thereof, comprising administering to the patient in need thereof the pharmaceutical composition of claim 11.

13. 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 and undesired puerperal lactation, or combinations thereof, comprising administering to the patient in need thereof an effective amount of a compound, wherein the compound is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monohydrate in its crystalline modification (V).

14. 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 and undesired puerperal lactation, or combinations thereof, comprising administering to the patient in need thereof an effective amount of a compound of claim 1.

15. A pharmaceutical composition comprising a compound according to claim 1, and one or more conventional auxiliary substances and/or carriers.
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