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Serving hundreds of leading biopharmaceutical companies globally:

Harvard Business School
Daiichi Sankyo
Fish and Richardson

Generated: June 24, 2018

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Claims for Patent: 8,236,804

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Summary for Patent: 8,236,804
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)
Application Number:13/100,948
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,236,804
Patent Claims: 1. A method of treating a major depressive disorder, the method comprising: administering to a patient in need thereof a pharmaceutical composition comprising an effective amount of 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) having at least five characteristic peaks selected from the degrees two-theta values corresponding to 9.08.+-.0.1, 12.85.+-.0.1, 14.50.+-.0.1, 16.89.+-.0.1, 18.89.+-.0.1, 20.43.+-.0.1, 21.72.+-.0.1, 24.61.+-.0.1, 27.35.+-.0.1 and 28.18.+-.0.1 and one or more conventional auxiliary substances and/or carriers, wherein the major depressive disorder is treated in the patient.

2. The method of claim 1, wherein the compound has at least five characteristic peaks selected from the degrees two-theta values corresponding to 12.85.+-.0.1, 14.50.+-.0.1, 20.43.+-.0.1, 21.72.+-.0.1, 27.35.+-.0.1 and 28.18.+-.0.1.

3. The method of claim 1, wherein the compound has characteristic peaks at the degrees two-theta values corresponding to 9.08.+-.0.1, 14.50.+-.0.1, 18.89.+-.0.1, 20.43.+-.0.1 and 24.61.+-.0.1.

4. The method of claim 1, wherein, the compound has a solubility in water of about 0.33 .mu.g/mL.

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