Generated: May 29, 2017
|Title:||1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine as a compound with combined serotonin reuptake, 5-HT.sub.3 and 5-HT.sub.1A activity for the treatment of cognitive impairment|
|Abstract:||1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT.sub.3 and 5-HT.sub.1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients. ##STR00001##|
|Inventor(s):||Bang-Andersen; Benny (Copenhagen S, DK), Mork; Arne (Malov, DK), Stensbol; Tine Bryan (Vaerlose, DK), Faldt; Andre (Ishoj, DK), Holm; Rene (Jyllinge, DK), de Diego; Heidi Lopez (Naerum, DK)|
|Assignee:||H. Lundbeck A/S (Copenhagen-Valby, DK)|
|Filing Date:||Apr 01, 2014|
|Claims:||1. A method of treating cognitive impairment involving decline in speed of processing, executive function, attention, or verbal learning and memory in a patient diagnosed with depression, the method comprising: administering a therapeutically effective amount of Compound I or a pharmaceutically acceptable salt thereof to the patient, wherein Compound I is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine, Compound I or a pharmaceutically acceptable salt thereof is crystalline and is administered at a daily dose of 1-20 mg, and the method alleviates a symptom or complication of the cognitive impairment or delays the progression of the cognitive impairment. |
2. The method of claim 1, wherein Compound I or a pharmaceutically acceptable salt thereof is a hydrobromide salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine.
3. The method of claim 2, wherein the hydrobromide salt is characterized by XRPD reflections at 6.89, 9.73, 13.78 and 14.64+/- 0.10.degree. 2.theta..
4. The method of claim 3, wherein the hydrobromide salt is characterized by an XRPD as shown in FIG. 3.
5. The method of claim 3, wherein the hydrobromide salt has a particle size distribution corresponding to: D98%: 650-680 .mu.m; D50%: 230-250 .mu.m; and D5%: 40-60 .mu.m; D98%: 370-390 .mu.m; d50%: 100-120 .mu.m; and D5%: 5-15 .mu.m; D98%: 100-125 .mu.m; D50%: 15-25 .mu.m; and D5%: 1-3 .mu.m; or D98%: 50-70 .mu.m; D50%: 3-7 .mu.m; and D5%: 0.5-2 .mu.m.
6. The method of claim 1, wherein the depression is generalized depression.
7. The method of claim 1, wherein the depression is major depressive disorder.
8. The method of claim 1, wherein the depression is postnatal depression.
9. The method of claim 1, wherein the depression is a depression associated with bipolar disorder.
10. The method of claim 1, wherein the depression is a treatment resistant depression.
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