You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 19, 2024

Details for Patent: 8,318,744


✉ Email this page to a colleague

« Back to Dashboard


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.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.