Pharmaceutical compositions comprising ((6bR,10aS)-1-(4-fluorophenyl)-4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)butan-1-one or pharmaceutically acceptable salts thereof

Patent metadata

Field	Value
Publication number	US-10464938-B2
Application number	US-201916439361-A
Country	US
Kind code	B2
Filing date	Jun 12, 2019
Priority date	Mar 12, 2007
Publication date	Nov 5, 2019
Grant date	Nov 5, 2019

Abstract

The present invention provides pharmaceutical compositions comprising certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, and as further defined herein:

First claim

What is claimed is:

1. A pharmaceutical composition comprising toluenesulfonic acid and the compound of Formula 2J:

or a pharmaceutically acceptable salt thereof,
wherein:
k is 1;
m is 1;
n is 1;
R 1 is 4-(4-fluorophenyl)-4-oxobutyl;
R 5 is H;
R 6a and R 6b are independently H;
R 7 , R 8 and R 9 are independently H;
R 10 is CH 3 ; and
X is —N—.

2. The pharmaceutical composition according to claim 1 , wherein the compound of Formula 2J is a free base of the compound of Formula 2J.

3. The pharmaceutical composition according to claim 1 , wherein the compound of Formula 2J is a pharmaceutically acceptable salt of the compound of Formula 2J.

4. The pharmaceutical composition according to claim 3 , wherein the pharmaceutically acceptable salt of the compound of Formula 2J is the toluenesulfonic acid addition salt.

5. The pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition comprises the toluenesulfonic acid and the compound of Formula 2J in a stoichiometric ratio.

6. A method for antagonizing 5-hydroxytryptamine 2 receptors in a patient, comprising administering to the patient in need thereof an effective amount of the pharmaceutical composition according to claim 2 .

7. A method for antagonizing 5-hydroxytryptamine 2 receptors in a patient, comprising administering to the patient in need thereof an effective amount of the pharmaceutical composition according to claim 3 .

8. A method for antagonizing 5-hydroxytryptamine 2 receptors in a patient, comprising administering to the patient in need thereof an effective amount of the pharmaceutical composition according to claim 4 .

9. A method for modulating 5-hydroxytryptamine receptor 2A activity in a patient, comprising administering to the patient in need thereof an effective amount of the pharmaceutical composition according to claim 2 .

10. A method for modulating 5-hydroxytryptamine receptor 2A activity in a patient, comprising administering to the patient in need thereof an effective amount of the pharmaceutical composition according to claim 3 .

11. A method for modulating 5-hydroxytryptamine receptor 2A activity in a patient, comprising administering to the patient in need thereof an effective amount of the pharmaceutical composition according to claim 4 .

12. A pharmaceutical composition comprising a toluenesulfonic acid addition salt of the compound of Formula 2J:

wherein:
k is 1;
m is 1;
n is 1;
R 1 is 4-(4-fluorophenyl)-4-oxobutyl;
R 5 is H;
R 6a and R 6b are independently H;
R 7 , R 8 and R 9 are independently H;
R 10 is CH 3 ; and
X is —N—.

Assignees

• Intra Cellular Therapies Inc

Inventors

• Tomesch John Charles
• Li Peng
• Yao Wei
• Zhang Qiang
• Beard James David
• Thompson Andrew S
• Cheng Hua
• Wennogle Lawrence P

Classifications

• A61P43/00

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

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61P25/26

  Psychostimulants, e.g. nicotine, cocaine · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61P25/22

  Anxiolytics · CPC title