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Details for Patent: 9,211,289

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Details for Patent: 9,211,289

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:Nov 10, 2014
Application Number:14/537,793
Claims:1. A method for treating side-effects caused or exacerbated by a dopaminergenic agent-associated therapy comprising administering an therapeutically effective amount of a serotonin 2A or 2C receptor inverse agonist to a patient on a dopaminergenic agent, wherein the serotonin 2A or 2C receptor inverse agonist is a compound of Formula (I) or a salt thereof: ##STR00010##

2. The method of claim 1, wherein the serotonin 2A or 2C receptor inverse agonist is a tartrate salt of the compound of Formula (I).

3. The method of claim 2, wherein the therapeutically effective amount of the tartrate salt of the compound of Formula (I) is from 10 mg to 50 mg.

4. The method of claim 2, wherein the therapeutically effective amount of the tartrate salt of the compound of Formula (I) is 10 mg.

5. The method of claim 2, wherein the therapeutically effective amount of the tartrate salt of the compound of Formula (I) is 25 mg.

6. The method of claim 2, wherein the therapeutically effective amount of the tartrate salt of the compound of Formula (I) is 50 mg.

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

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

9. The method of claim 1, wherein the salt of compound of formula (I) is formulated for oral administration as a unit dose.

10. The method of claim 9, wherein the unit dose is a tablet.

11. The method of claim 1, wherein the dopaminergenic agent is selected from the group consisting of levodopa, bromocriptine, pergolide, ephedrine sulfate, pemoline, mazindol, d,l-.alpha.-methylphenethylamine, methylphenidate, pramipexole, modafinil, and ropinirole.

12. The method of claim 1, wherein the therapeutically effective amount of serototonin 2A or 2C receptor inverse agonist is from 0.01 .mu.g/kg of body weight per day to 1.0 g/kg of body weight per day.

13. The method of claim 1, wherein the therapeutically effective amount of serototonin 2A or 2C receptor inverse agonist is from 0.01 mg/kg of body weight per day to 100 mg/kg of body weight per day.
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