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Details for Patent: 8,927,552

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Details for Patent: 8,927,552

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:Oct 23, 2012
Application Number:13/658,088
Claims:1. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII) having 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 compound of claim 1, wherein the compound has at least three characteristic peaks selected from 2Theta values corresponding to 13.26.+-.0.1, 16.89.+-.0.1, 19.82.+-.0.1, 20.49.+-.0.1 and 23.74.+-.0.1 degrees.

3. The compound of claim 1, wherein the compound has characteristic peaks at 2Theta values corresponding to 13.26.+-.0.1, 16.89.+-.0.1, 19.82.+-.0.1, 20.49.+-.0.1 and 23.74.+-.0.1 degrees.

4. The compound of claim 3, wherein the compound further has at least one characteristic peak selected from 2Theta values corresponding to 11.55.+-.0.1, 13.53.+-.0.1, 15.48.+-.0.1, 18.87.+-.0.1, and 27.50.+-.0.1 degrees.

5. The compound of claim 4, wherein the compound has characteristic peaks at a 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.

6. The compound of claim 1, wherein the compound has a solubility in water of about 0.10 .mu.g/mL.

7. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII) having characteristic peaks at 2Theta values corresponding to those exhibited in FIG. 20.

8. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII) having an IR spectrum with wavenumbers corresponding to the wavenumbers exhibited in FIG. 8.

9. A composition comprising a compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride hemihydrate in crystalline modification VIII (Form VIII) having: (a) 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; (b) characteristic peaks at 2Theta values corresponding to those exhibited in FIG. 20; or (c) an IR spectrum with wavenumbers corresponding to the wavenumbers exhibited in FIG. 8; and one or more conventional auxiliary substances and/or carriers.

10. The composition of claim 9, further comprising 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine- -hydrochloride anhydrate in crystalline modification IV (Form IV).

11. The composition of claim 9, further comprising 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).
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