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Generated: July 23, 2017

DrugPatentWatch Database Preview

Details for Patent: 8,318,744

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Details for Patent: 8,318,744

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:Apr 12, 2011
Application Number:13/085,117
Claims:1. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification III (Form III) having at least five characteristic peaks selected from the 2Theta values corresponding to 5.82 .+-.0.1, 11.00 .+-.0.1, 14.89 .+-.0.1, 16.96 .+-.0.1, 17.41 .+-.0.1, 17.97 .+-.0.1, 21.16 .+-.0.1, 22.05 .+-.0.1, 25.28 .+-.0.1 and 28.03 .+-.0.1 degrees.

2. The compound of claim 1, having characteristic peaks at a 2Theta value corresponding to 14.89 .+-.0.1, 17.41 .+-.0.1, 17.97 .+-.0.1, 22.05 .+-.0.1 and 25.28 .+-.0.1 degrees.

3. The compound according to claim 1, wherein the compound has a solubility in water of about 0.12 .mu.g/mL.

4. The compound of claim 1 having characteristic peaks at 2Theta values corresponding to 5.82 .+-.0.1, 11.00 .+-.0.1, 14.89 .+-.0.1, 16.96.+-.0.1, 17.41 .+-.0.1, 17.97 .+-.0.1, 21.16 .+-.0.1, 22.05 .+-.0.1, 25.28 .+-.0.1 and 28.03 .+-.0.1 degrees.

5. A compound which is 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification III (Form III) having characteristic peaks at 2Theta values corresponding to those exhibited in FIG. 22.

6. A compound which is 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification III (Form III) having an IR spectrum with wavenumbers corresponding to the wavenumbers exhibited in FIG. 10.

7. A method of treating a patient suffering from a depressive disorder comprising administering to said patient a compound according to claim 1.

8. The method of claim 7, wherein the depressive disorder is major depressive disorder.

9. A method of treating a patient suffering from major depressive disorder comprising administering to the patient the compound of claim 4.

10. A compound which is 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline modification III (Form III) having a Raman spectrum with wavenumbers corresponding to the wavenumbers exhibited in FIG. 44.
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Serving 500+ biopharmaceutical companies globally:

Teva
Queensland Health
Novartis
Deloitte
Citi
Mallinckrodt
Harvard Business School
Boehringer Ingelheim
Merck
Fish and Richardson

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