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Last Updated: May 5, 2024

Claims for Patent: 10,464,938


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Summary for Patent: 10,464,938
Title:Pharmaceutical compositions comprising ((6bR,10aS)-1-(4-fluorophenyl)-4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-p- yrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)butan-1-one or pharmaceutically acceptable salts thereof
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: ##STR00001##
Inventor(s): Tomesch; John Charles (Succasunna, NJ), Li; Peng (New Milford, NJ), Yao; Wei (New Milford, NJ), Zhang; Qiang (Somerset, NJ), Beard; James David (New York, NY), Thompson; Andrew S. (Mountainside, NJ), Cheng; Hua (Plainsboro, NJ), Wennogle; Lawrence P. (Hillsborough, NJ)
Assignee: INTRA-CELLULAR THERAPIES, INC. (New York, NY)
Application Number:16/439,361
Patent Claims: 1. A pharmaceutical composition comprising toluenesulfonic acid and the compound of Formula 2J: ##STR00099## or a pharmaceutically acceptable salt thereof, wherein: k is 1; m is 1; n is 1; R.sup.1 is 4-(4-fluorophenyl)-4-oxobutyl; R.sup.5 is H; R.sup.6a and R.sup.6b are independently H; R.sup.7, R.sup.8 and R.sup.9 are independently H; R.sup.10 is CH.sub.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: ##STR00100## wherein: k is 1; m is 1; n is 1; R.sup.1 is 4-(4-fluorophenyl)-4-oxobutyl; R.sup.5 is H; R.sup.6a and R.sup.6b are independently H; R.sup.7, R.sup.8 and R.sup.9 are independently H; R.sup.10 is CH.sub.3; and X is --N--.

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