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Last Updated: March 28, 2024

Details for Patent: 8,618,130


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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), Uldan; Allan K. (Vaerloese, DK)
Assignee: ACADIA Pharmaceuticals Inc. (San Diego, CA)
Filing Date:Jan 25, 2013
Application Number:13/750,778
Claims:1. A method of treating psychosis, or a symptom thereof, comprising administering to a patient suffering from psychosis, or a symptom thereof, 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 compound of formula (I) is administered in combination with an 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.

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

4. The method of claim 1, wherein the salt is a hydrochloride salt.

5. 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.

6. 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.

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

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

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

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

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

12. The method of claim 1, wherein the psychosis is associated with a neurodegenerative disorder.

13. The method of claim 1, wherein the psychosis is drug-induced.

14. The method of claim 1, wherein the psychosis is associated with dopaminergic therapy.

15. The method of claim 1, wherein the psychosis is associated with L-dopa therapy.

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