Claims for Patent: 12,122,792

Summary for Patent: 12,122,792

Title:	Pharmaceutical compositions comprising 4-((6bR,10aS)-3-methyl2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin8(7H)-yl)-1-(4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)phenyl)butan-1-one for treating conditions of the central nervous system and cardiac disorders
Abstract:	The invention relates to pharmaceutical compositions comprising the compound of Formula I, and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.
Inventor(s):	Peng Li, Robert E DAVIS, Kimberly Vanover
Assignee:	Intra Cellular Therapies Inc
Application Number:	US18/240,951
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,122,792
Patent Claims:	1. A pharmaceutical composition comprising a pharmaceutically acceptable diluent or carrier in admixture with: (i) a compound of Formula I: in free base or pharmaceutically acceptable salt form; and (ii) a compound of Formula II: in free base or pharmaceutically acceptable salt form. 2. The pharmaceutical composition according to claim 1, wherein the compound of Formula II is in toluenesulfonic acid addition salt form. 3. The pharmaceutical composition according to claim 2, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:200 to 1:2000. 4. The pharmaceutical composition according to claim 2, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:245 to 1:1000. 5. The pharmaceutical composition according to claim 2, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:250 to 1:550. 6. The pharmaceutical composition according to claim 2, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:300 to 1:500. 7. The pharmaceutical composition according to claim 2, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:285 to 1:400. 8. The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is formulated as a sustained release composition or delayed release composition. 9. The pharmaceutical composition according to claim 8, wherein the sustained release composition or delayed release composition is an injectable depot. 10. The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition further comprises a polymeric matrix. 11. The pharmaceutical composition according to claim 10, wherein the polymeric matrix comprises a biodegradable poly(D,L-lactide-co-glycolide) polymer. 12. The pharmaceutical composition according to claim 11, wherein the polymeric matrix is comprised within a microsphere. 13. A method for (a) inhibiting serotonin (5-hydroxytryptamine) receptor activity, (b) modulating dopamine D2 receptor function, (c) inhibiting serotonin reuptake transporter activity, (d) inhibiting norepinephrine reuptake transporter activity, or (e) inhibiting sodium ion channel activity each in a patient in need thereof, wherein the method comprises administering to the patient a therapeutically effective amount of the pharmaceutical composition according to claim 1. 14. The method according to claim 13, wherein the patient has a cardiac disorder or a central nervous system disorder involving the serotonin (5-hydroxytryptamine) receptor, the dopamine D2 receptor system, the serotonin reuptake transporter, the norepinephrine reuptake transporter (NET), and/or the sodium ion channel. 15. The method according to claim 14, wherein the cardiac disorder is selected from the group consisting of an arrhythmia, myocardial infarction, a recurrent tachyarrhythmia, and a ventricular tachycardia. 16. The method according to claim 15, wherein the arrhythmia is selected from the group consisting of an increased QT interval, a paroxysmal atrial fibrillation, a recurrent atrial fibrillation, a ventricular arrhythmia, and Wolff-Parkinson-White syndrome. 17. The method according to claim 14, wherein the central nervous system disorder is selected from the group consisting of an agitation in autism, an agitation in dementia, agoraphobia, anxiety, attention deficit disorder, body dysmorphic disorder, compulsive eating disorder, compulsive gambling disorder, dementia, depression, a gastrointestinal disorder, hypochondriasis, impulse control disorder, kleptomania, migraine, a mood disorder, a neurodegenerative disorder, obesity, an obsessive-compulsive disorder, orthostatic intolerance, a pain disorder, pathological grooming disorder, psychosis, pyromania, schizophrenia, a seizure disorder, a sexual disorder, a sleep disorder, a social phobia, and a substance abuse disorder, or a combination thereof. 18. The method according to claim 17, wherein the central nervous system disorder is anxiety or depression, or a combination thereof. 19. The method according to claim 18, wherein the anxiety or depression is acute anxiety or acute depression. 20. The method according to claim 19, wherein the acute anxiety is selected from the group consisting of a short-duration anxious episode associated with generalized anxiety disorder, a short-duration anxious episode associated with panic disorder, a short-duration anxious episode associated with social anxiety disorder, a short-duration anxious episode associated with social avoidance, and a short-duration anxious episode associated with a specific phobia. 21. The method according to claim 19, wherein the acute depression is selected from the group consisting of an acute major depressive episode, an acute recurrent brief depressive episode, and an acute short-duration depressive episode. 22. The method according to claim 19, wherein the acute depression is treatment resistant depression. 23. The method according to claim 22, wherein the treatment resistant depression is depression which has not responded to treatment with an antidepressant agent selected from the group consisting of a dopamine reuptake inhibitor (DRI), a monoamine oxidase inhibitor, a norepinephrine reuptake inhibitor (NRI), a norepinephrine reuptake inhibitor/dopamine reuptake inhibitor (NRI/DRI), a serotonin receptor antagonist, a serotonin reuptake inhibitor (SRI), and a tricyclic antidepressant, or a combination thereof. 24. The method according to claim 23, wherein the serotonin reuptake inhibitor (SRI) is selected from the group consisting of a selective serotonin reuptake inhibitor (SSRI), a serotonin reuptake/dopamine reuptake inhibitor (SRI/DRI), a serotonin reuptake/norepinephrine reuptake inhibitor (SRI/NRI), and a serotonin reuptake/norepinephrine reuptake/dopamine reuptake inhibitor (SRI/NRI/DRI). 25. The method according to claim 17, wherein the central nervous system disorder is a pain disorder. 26. The method according to claim 17, wherein the central nervous system disorder is schizophrenia. 27. The method according to claim 17, wherein the central nervous system disorder is a seizure disorder. 28. The method according to claim 17, wherein the depression is bipolar depression or major depressive disorder. 29. A pharmaceutical composition comprising: 1) a compound of Formula I: in free base or pharmaceutically acceptable salt form; and (ii) a compound of Formula II: in toluenesulfonic acid addition salt form; wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:200 to 1:2000. 30. The pharmaceutical composition according to claim 29, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:245 to 1:1000. 31. The pharmaceutical composition according to claim 29, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:250 to 1:550. 32. The pharmaceutical composition according to claim 29, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:300 to 1:500. 33. The pharmaceutical composition according to claim 29, wherein the pharmaceutical composition comprises the compound of Formula I and the compound of Formula II in a weight ratio in the range of from 1:285 to 1:400. 34. A method for treating a central nervous system disorder in a patient in need thereof, wherein the method comprises administering to the patient a therapeutically effective amount of the pharmaceutical composition according to claim 29; wherein the central nervous system disorder is selected from the group consisting of a bipolar disorder, major depressive disorder, and schizophrenia. 35. The method according to claim 34, wherein the bipolar disorder is bipolar depression.