Compounds and methods

Patent metadata

Field	Value
Publication number	US-12565499-B2
Application number	US-202418601923-A
Country	US
Kind code	B2
Filing date	Mar 11, 2024
Priority date	Apr 14, 2012
Publication date	Mar 3, 2026
Grant date	Mar 3, 2026

Abstract

The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.

First claim

What We claim is:

1 . A method for the treatment of cognitive impairments and/or memory impairments associated with dementia, wherein the dementia is selected from mild cognition impairment, senile dementia, Alzheimer's disease, Pick's disease, frontotemporal dementia, dementia with Lewy bodies, and vascular dementia, wherein the patient suffers from a co-morbid disorder selected from psychosis and depression, comprising administering to a patient in need thereof, a therapeutically effective amount of a compound of Formula I:

wherein:
X is —N(CH 3 )—; and
Y is —C(═O);
in tosylate salt form.

2 . The method according to claim 1 , wherein the dementia is Alzheimer's disease.

3 . The method according to claim 1 , wherein the dementia is mild cognition impairment.

4 . The method according to claim 1 , wherein the co-morbid disorder is psychosis.

5 . The method according to claim 1 , wherein the co-morbid disorder is depression.

6 . The method according to claim 1 , wherein the dosage of the Compound of Formula I in tosylate salt form is about 10-100 mg, measured as the amount of equivalent free base form.

7 . The method according to claim 1 , wherein the method treats cognitive impairments.

8 . The method according to claim 1 , wherein the method treats memory impairments.

9 . The method according to claim 6 , wherein the dosage of the Compound of Formula I in tosylate salt form is about 1-10 mg, measured as the amount of equivalent free base form.

10 . The method according to claim 1 , wherein the method is effective in alleviating cognitive impairment or improving cognition.

11 . The method according to claim 1 , wherein the method is effective in alleviating memory impairment or improving memory.

12 . The method according to claim 1 , wherein the dementia is selected from mild cognition impairment, senile dementia, Alzheimer's disease, and frontotemporal dementia.

13 . The method according to claim 1 , wherein the dementia is selected from mild cognition impairment, Alzheimer's disease, and frontotemporal dementia.

Assignees

• Intra Cellular Therapies Inc

Inventors

• Mates Sharon
• Davis Robert
• Vanover Kimberly
• Wennogle Lawrence

Classifications

• A61K31/445 Primary

  Non condensed piperidines, e.g. piperocaine · CPC title

• C07D471/16

  Peri-condensed systems · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61K31/4985 Primary

  Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K31/5383

  ortho- or peri-condensed with heterocyclic ring systems · CPC title