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Last Updated: March 29, 2024

Details for Patent: 8,377,959


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Title:Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
Inventor(s): Weiner; David M. (San Diego, CA), Davis; Robert E. (San Diego, CA), Brann; Mark R. (Rye, NH), Andersson; Carl-Magnus A. (Hjarup, SE), Uldam; Allan K. (Vaerloese, DK)
Assignee: ACADIA Pharmaceuticals, Inc. (San Diego, CA)
Filing Date:Jun 29, 2012
Application Number:13/539,011
Claims:1. A method of treating Lewy Body Dementia in a patient, comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (I): ##STR00010## or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein the salt is a tartrate salt.

3. The method of claim 1, wherein the amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, is from about 0.001 mg to about 50 mg.

4. The method of claim 1, wherein the amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, is from about 1 mg to about 10 mg.

5. The method of claim 1, wherein the amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, is about 10 mg.

6. The method of claim 1, wherein the amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, is about 25 mg.

7. The method of claim 1, wherein the amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, is about 50 mg.

8. The method of claim 1, wherein the compound of formula (I) is administered daily.

9. The method of claim 1, wherein the compound of formula (I) is administered once daily.

10. The method of claim 1, wherein the compound is administered in combination with an anti-psychotic agent.

11. The method of claim 10, wherein the anti-psychotic agent selected from the group consisting of chloropromazine, haloperidol, molindone, thioridazine, a phenothiazine, a butyrophenone, diphenylbutylpiperidine, a thioxanthine, fluphenthixol, a substituted benzamide, sulpiride, sertindole, amisulpride, risperidone, clozapine, olanzapine, ziprasidone, aripirazole, N-desmethylclozapine, N-desmethylolanzapine, and 9-OH-risperidone.

12. The method of claim 10, wherein the anti-psychotic agent is haloperidol or risperidone.

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