DrugPatentWatch Database Preview
« Back to Dashboard
Summary for Patent: 7,834,020
|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 Patent Gesellschaft (Darmstadt, DE)|
|Patent Litigation and PTAB cases:||See patent lawsuits and PTAB cases for patent 7,834,020|
1. 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),
wherein said compound exhibits the following XRD data: TABLE-US-00003 No. d (.ANG.) 2.theta. I/I.sub.0 1 9,732 9.08 22 2 6,885 12.85 10 3 6,102 14.50 22 4 5,246 16.89 9 5 4,695 18.89 100 6 4,344 20.43 20 7 4,088 21.72 12 8 3,615 24.61 67 9 3,258 27.35
17 10 3,164 28.18 12.
2. 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, undesired puerperal lactation, or combinations thereof, comprising administering to said patient a compound according to claim 1.
3. A process for preparing 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride anhydrate in crystalline Form IV according to claim 1, wherein said process comprises: (1) drying Form XI of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monomethanolate at temperatures between 55.degree. and 65.degree. C., wherein said Form XI of 1-[4-5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride monomethanolate exhibits the following XRD data: TABLE-US-00004 No. d (.ANG.) 2.theta. I/I.sub.0 1 10,348 8.54 39 2 7,077 12.50 25 3 6,717 13.17 28 4 4,778 18.56 23 5 4,599 19.28 34 6 4,490 19.76 100 7 4,239 20.94 51 8 4,186 21.21 18 9 3,504 25.40 66 10 3,391 26.26 69.
4. A method according to claim 2, wherein said patient is suffering from a depressive disorder.
5. A method according to claim 2, wherein said patient is suffering from major depressive disorder.
6. A method according to claim 2, wherein said patient is suffering from dysthymic disorder.
7. A method according to claim 2, wherein said patient is suffering from adolescent depression.
For more information try a trial or see the plans and pricing
Serving hundreds of leading biopharmaceutical companies globally:
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 verifification 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.