IP Library Granted Patent US 10,464,938
Granted Patent B2
US 10,464,938 · App. 16/439,361 · Granted Nov 5, 2019

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

Inventors: John Charles Tomesch (Succasunna, NJ); Peng Li (New Milford, NJ); Wei Yao (New Milford, NJ); Qiang Zhang (Somerset, NJ); James David Beard (New York, NY); Andrew S. Thompson (Mountainside, NJ); Hua Cheng (Plainsboro, NJ); Lawrence P. Wennogle (Hillsborough, NJ)
Assignee: INTRA-CELLULAR THERAPIES, INC.
C07D471/16C07D471/04
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Quick Facts
Patent No.
US 10,464,938
App. No.
16/439,361
Granted
Nov 5, 2019
Kind
B2
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:

Claims (33)

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—.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 21, 2022
From: WENNOGLE, LAWRENCE P.
To: INTRA-CELLULAR THERAPIES, INC.
Reel/Frame 059666/0753 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2022
From: TOMESCH, JOHN CHARLES; LI, PENG; YAO, WEI; ZHANG, QIANG; BEARD, JAMES DAVID; THOMPSON, ANDREW; CHENG, HUA
To: INTRA-CELLULAR THERAPIES, INC.
Reel/Frame 059653/0620 →
Continuity (8)
Continuation 16244796 · Jan 10, 2019
Continuation 15660762 · Jul 26, 2017
Continuation 15066962 · Mar 10, 2016
Continuation 14323545 · Jul 3, 2014
Continuation 13593097 · Aug 23, 2012
Division 12531016
Provisional Application 60906473 · Mar 12, 2007
Related Publication 20190292185A1 · Sep 26, 2019
Cited By (19)
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