Claims for Patent: 10,960,009

Summary for Patent: 10,960,009

Title:	Methods of treating schizophrenia and depression
Abstract:	The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Inventor(s):	Vanover; Kimberly (New York, NY), Li; Peng (New Milford, NJ), Mates; Sharon (New York, NY), Davis; Robert (San Diego, CA), Wennogle; Lawrence P. (Hillsborough, NJ)
Assignee:	INTRA-CELLULAR THERAPIES, INC. (New York, NY)
Application Number:	16/392,409
Patent Claims:	1. A method for the treatment of the negative symptoms of schizophrenia comprising administering to a schizophrenic patient in need thereof an effective amount ##STR00015## of a Compound of Formula wherein: X is --N(CH.sub.3)-- and Y is --C(O)--; in free or pharmaceutically acceptable salt form, wherein the effective amount of the Compound of Formula I is 40 mg to 60 mg per day, measured as the weight of the corresponding free base form of the Compound. 2. The method according to claim 1, wherein the compound of Formula I is in pharmaceutically acceptable salt form. 3. The method according to claim 1, wherein the compound of Formula I is in toluene sulfonic acid addition salt form. 4. The method according to claim 1, wherein the negative symptoms are selected from emotional withdrawal, passive social withdrawal, apathetic social withdrawal, lack of spontaneity, stereotyped thinking, and active social avoidance. 5. The method according to claim 1, wherein the method improves the positive symptoms and the negative symptoms of schizophrenia. 6. The method according to claim 1, wherein the method improves social integration and social function of the patient. 7. The method according to claim 1, wherein the patient has prominent negative symptoms of schizophrenia at the initiation of treatment. 8. The method according to claim 1, wherein the patient has co-morbid anxiety, cognitive dysfunction, and/or insomnia. 9. The method according to claim 8, wherein the method is effective to reduce the patient's symptoms of anxiety, cognitive impairment and/or insomnia. 10. The method according to claim 1, wherein the effective amount of the Compound of Formula I is about 40 mg per day, measured as the weight of the corresponding free base form of the Compound. 11. The method according to claim 1, wherein the compound is in toluenesulfonic acid addition salt form and the effective amount of the Compound of Formula I is 60 mg of the salt form administered once per day (equivalent to about 41.7 mg of the free base). 12. The method according to claim 1, wherein the patient still suffers from negative symptoms of schizophrenia after treatment with another antipsychotic agent. 13. The method according to claim 1, wherein the patient has previously not responded adequately to treatment with another antipsychotic agent. 14. A method for the treatment of schizophrenia without hyperprolactinemia, EPS/akathisia, weight gain or cardiovascular side effects comprising administering to a patient in need thereof an effective amount of a Compound of Formula I: ##STR00016## wherein: X is --N(CH.sub.3)-- and Y is --C(O)--; in free or pharmaceutically acceptable salt form, wherein the effective amount of the Compound of Formula I is 40 mg to 60 mg per day, measured as the weight of the corresponding free base form of the Compound. 15. The method according to claim 14, wherein the compound is in toluenesulfonic acid addition salt form and the effective amount of the Compound of Formula I is 60 mg of the salt form administered once per day (equivalent to about 41.7 mg of the free base). 16. A method for the treatment of schizophrenia comprising administering to a patient in need thereof an effective amount of a Compound of Formula I: ##STR00017## wherein: X is --N(CH.sub.3)-- and Y is --C(O)--; in free or pharmaceutically acceptable salt form, wherein the patient has co-morbid depression, and wherein the patient has prominent negative symptoms of schizophrenia at the initiation of treatment and after treatment with another antipsychotic agent, wherein the effective amount of the Compound of Formula I is 40 mg to 60 mg per day, measured as the weight of the corresponding free base form of the Compound. 17. The method according to claim 16, wherein the patient has a Calgary Depression Scale for Schizophrenia (CDSS) score of greater than 6 at the initiation of treatment. 18. The method according to claim 16, wherein the method is effective to significantly reduce the patient's symptoms of depression. 19. The method according to claim 16, wherein the compound is in toluenesulfonic acid addition salt form and the effective amount of the Compound of Formula I is 60 mg of the salt form administered once per day (equivalent to about 41.7 mg of the free base).