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Last Updated: March 28, 2024

Claims for Patent: 9,765,053


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Summary for Patent: 9,765,053
Title:Methods of treatment using selective 5-HT2A inverse agonists
Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.
Inventor(s): Andersson; Carl-Magnus A. (Glostrup, DK), Croston; Glenn (San Diego, CA), Hansen; Eva Louise (Glostrup, DK), Uldam; Allan Kjaersgaard (Glostrup, DK)
Assignee: ACADIA Pharmaceuticals Inc. (San Diego, CA)
Application Number:13/053,079
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,765,053
Patent Claims: 1. A method for the treatment of psychosis, comprising administering an effective amount of a selective 5-HT2A inverse agonist to a human in need of such treatment, wherein the compound is selected from: ##STR00010## wherein Z is ##STR00011## in which R is hydrogen, a cyclic or straight-chained or branched acyclic organyl group, a lower hydroxyalkyl group, a lower aminoalkyl group, or an aralkyl or heteroaralkyl group; n is 0, 1 or 2; X.sub.1 is methylene, vinylene, or an NH or N(lower alkyl) group; X.sub.2 is methylene, or when X.sub.1 is methylene or vinylene, X.sub.2 is methylene or a bond; or when X.sub.1 is methylene, X.sub.2 is O, S, NH, or N(lower alkyl) or a bond; Y.sub.1 is methylene and Y.sub.2 is methylene, vinylene, ethylene, propylene, or a bond; or Y.sub.1 is a bond and Y.sub.2 is vinylene; or Y.sub.1 is ethylene and Y.sub.2 is O, S, NH, or N(lower alkyl); Ar.sub.1 and Ar.sub.2 independently are unsubstituted or substituted aryl or heteroaryl groups; W is oxygen or sulfur; or a pharmaceutically acceptable salt, or ester, thereof; and wherein the compound has substantially no activity at 5-HT1A, 5-HT1B, dopaminergic, histaminergic, adrenergic or muscarinergic receptors.

2. The method of claim 1, wherein the disease or disorder is psychosis associated with Parkinsonism.

3. The method of claim 1, wherein the compound or pharmaceutical composition is in the form of a dosage unit that contains from about 0.01 mg to about 50 mg of the selective 5-HT2A receptor inverse agonist.

4. The method of claim 3, wherein the dosage unit that contains from about 1 mg to about 10 mg of the selective 5-HT2A receptor inverse agonist.

5. The method of claim 3, wherein about 0.001 mg/kg to about 10 mg/kg of body weight per day of the selective 5-HT2A receptor inverse agonist is administered.

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