IP Library Granted Patent US 9,708,322
Granted Patent B2
US 9,708,322 · App. 14/777,466 · Granted Jul 18, 2017

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

Inventors: Peng Li (New York, NY); Qiang Zhang (New York, NY); Robert Davis (New York, NY); Lawrence P. Wennogle (New York, NY)
Assignee: INTRA-CELLULAR THERAPIES, INC.
C07D471/16A61K9/4825A61K9/4891A61K9/5031A61K31/4985A61K47/34A61K47/38C07D471/14
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Quick Facts
Patent No.
US 9,708,322
App. No.
14/777,466
Granted
Jul 18, 2017
Kind
B2
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.

Claims (13)

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.

Continuity (2)
Provisional Application 61799405 · Mar 15, 2013
Related Publication 20160031885A1 · Feb 4, 2016