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Generated: November 18, 2017

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Claims for Patent: 7,659,285

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Claims for Patent: 7,659,285

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. (Ballerup, DK)
Assignee: Acadia Pharmaceuticals, Inc. (San Diego, CA)
Application Number:11/416,855
Patent Claims: 1. A method of treating Parkinson's Disease psychosis in a patient, comprising administrating to a patient having Parkinson's Disease a therapeutically effective amount of N-(1-methylpiperidin-4-yl)-N-(4-flourophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide or a pharmaceutically acceptable salt thereof.

2. A method of treating Parkinson's Disease psychosis in a patient, composing administrating to a patient having Parkinson's Disease a pharmaceutical composition comprising from about 10 mg to about 50 mg of N-(1-methylpiperidin-4-yl)-N-(4-flourophenylmethyl)-N-'-(4-(2-methylpropy- loxy)phenylmethyl)carbamide or a pharmaceutically acceptable salt thereof.

3. Then method of claim 1, wherein about 10 mg of N-(1-methylpiperidin-4-yl)-N-(4-flourophenylmethyl)-N'-(4(2-methylpropylo- xy)phenylmethyl)carbamide of a pharmaceutically acceptable salt thereof is administered.

4. The method of claim 1, wherein about 25 mg of N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide or a pharmaceutically acceptable salt thereof is administered.

5. The method of claim 1, wherein about 50 mg of N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide or a pharmaceutically acceptable salt thereof is administered.

6. The method of claim 1 or 2, wherein the composition is administered once daily.

7. The method of claim 1, wherein about 0.01 mg/kg of body weight to about 1.5 mg/kg body weight of the compound is administered.

8. The method of claim 1, wherein the tartrate salt of N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide is administered.

9. The method of claim 2, wherein the tartrate salt of N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide is administered.

10. The method of claim 1, wherein the hydrochloride salt of N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide is administered.

11. The method of claim 2, wherein the hydrochloride salt of N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyl- oxy)phenylmethyl)carbamide is administered.
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Healthtrust
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Argus Health
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Fish and Richardson

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