Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases

Patent metadata

Field	Value
Publication number	US-10028944-B2
Application number	US-201715397582-A
Country	US
Kind code	B2
Filing date	Jan 3, 2017
Priority date	Jan 16, 2003
Publication date	Jul 24, 2018
Grant date	Jul 24, 2018

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.

First claim

What is claimed is:

1. A method for treating a neuropsychiatric disease, or a symptom thereof comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (I) or a salt thereof:

2. The method of claim 1 , wherein the neuropsychiatric disease is selected from the group consisting of schizophrenia, schizoaffective disorders, mania, behavioral disturbances associated with dementia and psychotic depression.

3. The method of claim 2 , wherein the neuropsychiatric disease is psychotic depression.

4. The method of claim 1 , wherein the neuropsychiatric disease is an affective disorder, and wherein the affective disorder is major depression.

5. The method of claim 1 , wherein a tartrate salt of the compound of Formula (I) is administered to the patient.

6. The method of claim 5 , wherein the tartrate salt of the compound of Formula (I) in an amount of about 0.001 mg to about 50 mg is administered to the patient.

7. The method of claim 5 , wherein the tartrate salt of the compound of Formula (I) in an amount of about 15 mg is administered to the patient.

8. The method of claim 5 , wherein the tartrate salt of the compound of Formula (I) in an amount of about 25 mg is administered to the patient.

9. The method of claim 5 , wherein the tartrate salt of the compound of Formula (I) in an amount of about 50 mg is administered to the patient.

10. The method of claim 5 , wherein the tartrate salt of the compound of Formula (I) is administered daily.

11. The method of claim 5 , wherein the tartrate salt of compound of Formula (I) is administered once daily.

12. The method of claim 5 , wherein the tartrate salt of compound of Formula (I) is administered two times daily.

13. The method of claim 5 , wherein the tartrate salt of compound of Formula (I) is formulated for oral administration as a unit dose.

14. The method of claim 13 , wherein the unit dose is a tablet.

15. The method of claim 1 , wherein the therapeutically effective amount of the compound of Formula (I) or a salt thereof is from 0.01 mg/kg of body weight per day to 100 mg/kg of body weight per day.

Assignees

• Acadia Pharm Inc

Inventors

• Weiner David M
• Davis Robert E
• Brann Mark R
• Andersson Carl-Magnus A
• Uldam Allan K

Classifications

• 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

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title