Methods of treatment using selective 5-HT2A inverse agonists

Patent metadata

Field	Value
Publication number	US-9765053-B2
Application number	US-201113053079-A
Country	US
Kind code	B2
Filing date	Mar 21, 2011
Priority date	Mar 6, 2000
Publication date	Sep 19, 2017
Grant date	Sep 19, 2017

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.

First claim

What is claimed is:

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:

wherein
Z is

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 1 is methylene, vinylene, or an NH or N(lower alkyl) group;
X 2 is methylene, or when X 1 is methylene or vinylene, X 2 is methylene or a bond; or when X 1 is methylene, X 2 is O, S, NH, or N(lower alkyl) or a bond;
Y 1 is methylene and Y 2 is methylene, vinylene, ethylene, propylene, or a bond; or
Y 1 is a bond and Y 2 is vinylene; or
Y 1 is ethylene and Y 2 is O, S, NH, or N(lower alkyl);
Ar 1 and Ar 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.

Assignees

• Andersson Carl-Magnus A
• Croston Glenn
• Hansen Eva Louise
• Uldam Allan Kjaersgaard
• Acadia Pharm Inc

Inventors

• Andersson Carl-Magnus A
• Croston Glenn
• Hansen Eva Louise
• Uldam Allan Kjaersgaard

Classifications

• A61P9/08

  Vasodilators for multiple indications · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title