Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|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%.
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.