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Last Updated: May 11, 2024

Claims for Patent: 11,458,134


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Summary for Patent: 11,458,134
Title:1-[2-(2,4-dimeihylphenylsulfanyl)-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-HTand 5-HTand may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
Inventor(s):Faldt André, Lopez de Diego Heidi, Holm Rene, Mealy Michael J.
Assignee:H. Lundbeck A/S
Application Number:US16502677
Patent Claims: 1. A pharmaceutical composition , comprising:{'figref': {'@idref': 'DRAWINGS', 'FIGS. 2-5'}, 'a HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine, wherein the HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine is a crystalline form characterized by an XRPD pattern as shown in any of ;'}mannitol;microcrystalline cellulose;sodium starch glycolate; andmagnesium stearate.2. The composition of claim 1 , wherein the composition comprises:the HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine in an amount of 2-30% by weight of the composition;the mannitol in an amount of 25-45% by weight of the composition;the microcrystalline cellulose in an amount of 22-27% by weight of the composition;the sodium starch glycolate in an amount of 4-5% by weight of the composition; andthe magnesium stearate in an amount of 0.25-5% by weight of the composition.3. The composition of claim 2 , wherein the magnesium stearate is in an amount of 0.25-2% by weight of the composition.4. The composition of claim 1 , wherein the composition comprises:the HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine in an amount of 20-22% by weight of the composition;the mannitol in an amount of 35-36% by weight of the composition;the microcrystalline cellulose in an amount of 24-25% by weight of the composition;the sodium starch glycolate in an amount of 3-4% by weight of the composition; andthe magnesium stearate in an amount of 0.25-1% by weight of the composition.5. The composition of claim 1 , wherein the composition comprises:the HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine in an amount of 12-13% by weight of the composition;the mannitol in an amount of 36-37% by weight of the composition;the microcrystalline cellulose in an amount of 24-25% by weight of the composition;the sodium starch glycolate in an amount of 3-4% by weight of the composition; andthe magnesium stearate in an amount of 0.25-1% by weight of the composition.6. The composition of claim 1 , wherein the composition comprises:the HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine in an amount of 25-27% by weight of the composition;the mannitol in an amount of 27-29% by weight of the composition;the microcrystalline cellulose in an amount of 24-25% by weight of the composition;the sodium starch glycolate in an amount of 3-5% by weight of the composition; andthe magnesium stearate in an amount of 0.25-1% by weight of the composition.7. The composition of claim 1 , wherein the composition comprises:the HBr salt of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine in an amount of 3-4% by weight of the composition;the mannitol in an amount of 40-42% by weight of the composition;the microcrystalline cellulose in an amount of 26-28% by weight of the composition;the sodium starch glycolate in an amount of 3-5% by weight of the composition; andthe magnesium stearate in an amount of 0.5% by weight of the composition.8. The composition of claim 1 , wherein the composition is a tablet.9. A method of treating a disease selected from the group consisting of affective disorders claim 1 , depression claim 1 , major depressive disorder claim 1 , anxiety claim 1 , general anxiety disorder claim 1 , social anxiety disorder claim 1 , obsessive compulsive disorder claim 1 , panic disorder claim 1 , and panic attacks claim 1 , the method comprising administering a therapeutically effective amount of the composition of to a patient in need thereof claim 1 ,wherein the method alleviates a symptom or complication of the disease, or delays the progression of the disease, in the patient.10. The method of claim 9 , wherein the disease is major depressive disorder.

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