# US 11,026,951 B2 · Methods of treating bipolar disorder > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,026,951 B2 - Document ID: US11026951B2 - Status: Granted - Kind: B2 - Application number: 16/507,956 - Filed: 2019-07-10 - Published: 2019-10-31 - Granted: 2021-06-08 - Earliest claimed: 2013-12-03 - Assignees: Intra-Cellular Therapies, Inc. - Applicants: Intra-Cellular Therapies, Inc. - Inventors: Kimberly Vanover; Peng Li; Sharon Mates; Robert Davis; Lawrence P. Wennogle - Web page: https://patentgrep.com/patent/US11026951B2 ## CPC - A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)} - A61K 9/5153: {Polyesters, e.g. poly(lactide-co-glycolide)} - A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 25/20: Hypnotics; Sedatives - A61P 25/22: Anxiolytics - A61P 25/24: Antidepressants - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## 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. ## Claims ### Claim 1 A method for the treatment of bipolar disorder I and/or bipolar II disorder comprising administering to a patient in need thereof an effective amount of a Compound of Formula I: wherein: X is —N(CH3)— and Y is —C(O)—; in free or pharmaceutically acceptable salt form, wherein said Compound is not used in combination with another antipsychotic agent. ### Claim 2 (depends on 1) The method according to claim 1, wherein the compound of Formula I is in pharmaceutically acceptable salt form. ### Claim 3 (depends on 1) The method according to claim 1, wherein the compound of Formula I is in toluenesulfonic acid addition salt form. ### Claim 4 (depends on 1) The method according to claim 1, wherein the bipolar disorder is bipolar I disorder. ### Claim 5 (depends on 1) The method according to claim 1, wherein the bipolar disorder is bipolar II disorder. ### Claim 6 (depends on 1) The method according to claim 1, wherein the effective amount of the Compound of Formula I is 20 mg to 60 mg per day, measured as the weight of the corresponding free base form of the Compound. ### Claim 7 (depends on 1) The method according to claim 1, 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. ### Claim 8 (depends on 1) 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. ### Claim 9 (depends on 1) 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). ### Claim 10 (depends on 1) The method according to claim 1, wherein the patient has bipolar disorder with psychotic symptoms. ### Claim 11 (depends on 1) The method according to claim 1, wherein the patient has bipolar depression. ### Claim 12 (depends on 1) The method according to claim 1, wherein the method is effective in treating the symptoms of depression of bipolar disorder. ### Claim 13 (depends on 4) The method according to claim 4, wherein the method is effective in treating the symptoms of depression of bipolar disorder. ### Claim 14 (depends on 5) The method according to claim 5, wherein the method is effective in treating the symptoms of depression of bipolar disorder. ### Claim 15 (depends on 9) The method according to claim 9, wherein the bipolar disorder is bipolar I disorder. ### Claim 16 (depends on 15) The method according to claim 15, wherein the method is effective in treating the symptoms of depression of bipolar disorder. ### Claim 17 (depends on 9) The method according to claim 9, wherein the bipolar disorder is bipolar II disorder. ### Claim 18 (depends on 17) The method according to claim 17, wherein the method is effective in treating the symptoms of depression of bipolar disorder. ### Claim 19 (depends on 1) The method according to claim 1, wherein the Compound is administered as the sole therapeutic agent for the treatment of said bipolar disorder. ### Claim 20 (depends on 1) The method according to claim 1, wherein the method does not result in hyperprolactinemia, EPS/akathisia, weight gain or cardiovascular side effects. ### Claim 21 (depends on 9) The method according to claim 9, wherein the Compound is administered as the sole therapeutic agent for the treatment of said bipolar disorder. ### Claim 22 (depends on 9) The method according to claim 9, wherein the method does not result in hyperprolactinemia, EPS/akathisia, weight gain or cardiovascular side effects. ### Claim 23 (depends on 1) The method according to claim 1, wherein the method does not result in EPS/akathisia or weight gain. ### Claim 24 (depends on 9) The method according to claim 9, wherein the method does not result in EPS/akathisia or weight gain.