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|Title:||1-[2-(2,4-dimethylphenylsulfanyl)-phenyl] piperazine as a compound with combined serotonin reuptake, 5-HT3 and 5-HT1A 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), Faldt; Andre (Ishoj, DK), Mork; Arne (Malov, DK), Lopez de Diego; Heidi (Naerum, DK), Holm; Rene (Jyllinge, DK), Stensbol; Tine Bryan (Vaerlose, DK), Moore; Nicholas (Delmar, NY)|
|Assignee:||H. Lundbeck A/S (Valby, DK)|
1. Compound 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine or a pharmaceutically acceptable salt thereof in a crystalline form characterized by an XRPD pattern as
shown in any of FIGS. 1-17.
2. Compound 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine hydrobromide salt in a crystalline form which is characterized by XRPD reflections at 6.89, 9.73, 13.78 and 14.64 +/-0.10.degree. 2.theta..
3. The compound according to claim 2 wherein said crystalline form is characterized by an XRPD as shown in FIG. 3.
4. The compound according to claim 2, which compound 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.
5. A composition comprising a compound according to claim 2 and a pharmaceutically acceptable excipient.
6. The composition according to claim 5, said composition being a tablet prepared by wet granulation and comprising anhydrous calcium hydrogen phosphate, corn starch, PVP-VA copolymer, microcrystalline cellulose, sodium starch glycolate, talc and magnesium stearate.
7. The composition according to claim 6 comprising TABLE-US-00008 HBr salt 3-8% Anhydrous calcium hydrogen phosphate 35-45% Corn starch 15-25% PVP-VA copolymer 2-6% Microcrystalline cellulose 20-30% Sodium starch glycolate 1-3% Talc 2-6% Magnesium stearate 0.5-2% .
8. The composition according to claim 6 comprising TABLE-US-00009 HBr salt approximately 5% Anhydrous calcium hydrogen phosphate approximately 39% Corn starch approximately 20% PVP-VA copolymer approximately 3% Microcrystalline cellulose approximately 25% Sodium starch glycolate approximately 3% Talc approximately 4% Magnesium stearate approximately 1%.