Substituted pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines for inhibiting serotonin reuptake transporter activity

Patent metadata

Field	Value
Publication number	US-9708322-B2
Application number	US-201414777466-A
Country	US
Kind code	B2
Filing date	Mar 15, 2014
Priority date	Mar 15, 2013
Publication date	Jul 18, 2017
Grant date	Jul 18, 2017

Abstract

The invention relates to substituted heterocycle fused gamma-carbolines of the Formula Q as described herein, in free base or pharmaceutically acceptable salt form, and/or pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT 2A receptor pathway, the serotonin transporter (SERT) pathway and/or the dopamine D 2 receptor pathway signaling systems.

First claim

The invention claimed is:

1. A method for inhibiting serotonin reuptake transporter activity in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising:
(i) a compound of Formula Q:

wherein:
X is —N(H)— or —N(CH 3 )—; and
Y is —C(═O)— or —O—;

in free base or pharmaceutically acceptable salt form, and

(ii) a polymeric matrix which comprises polymers selected from a group consisting of poly(glycolic acid), poly-D,L-lactic acid and poly-L-lactic acid, or copolymers thereof.

2. The method according to claim 1 , wherein said patient has a disorder involving the serotonin (5-hydroxytryptamine) 2A pathway, the dopamine D2 receptor pathway and/or the serotonin reuptake transporter pathway.

3. The method according to claim 2 , wherein said disorder is selected from a group consisting of (1) psychosis in a patient suffering from depression, (2) depression in a patient suffering from psychosis, (3) a mood disorder associated with psychosis, and (4) a sleep disorder associated with psychosis.

4. The method according to claim 1 , wherein said patient has a disorder selected from a group consisting of obesity, anxiety, depression, psychosis, schizophrenia, migraine, a sleep disorder, a sexual disorder, a gastrointestinal disorder, a condition associated with cephalic pain, a social phobia, an agitation in dementia and an agitation in autism and related autistic disorders.

5. The method according to claim 4 , wherein the disorder is depression.

6. The method according to claim 4 , wherein the disorder is psychosis.

7. The method according to claim 4 , wherein the disorder is schizophrenia.

Assignees

• Intra Cellular Therapies Inc

Inventors

• Li Peng
• Zhang Qiang
• Davis Robert
• Wennogle Lawrence P

Classifications

• C07D471/14

  Ortho-condensed systems · CPC title

• A61K9/4891

  Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004) · CPC title

• A61K31/4985

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

• A61K9/4825

  Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816) · CPC title

• A61K9/5031

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide) · CPC title