Organic compounds

Patent metadata

Field	Value
Publication number	US-12195463-B2
Application number	US-201917416997-A
Country	US
Kind code	B2
Filing date	Dec 20, 2019
Priority date	Dec 21, 2018
Publication date	Jan 14, 2025
Grant date	Jan 14, 2025

Abstract

The invention relates to a particular enantiomer of a substituted heterocycle fused gamma-carboline, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT 2A receptor, and pathways involving the dopamine D 1 and D 2 receptor signaling system.

First claim

What is claimed:

1. A compound of a Formula I:

in free or pharmaceutically acceptable salt form; and
wherein the compound is in isolated and purified form of at least 90% purity.

2. The compound according to claim 1 in the form of a pharmaceutically acceptable salt.

3. A pharmaceutical composition comprising a compound according to claim 1 , in free or pharmaceutically acceptable salt form, in admixture with a pharmaceutically acceptable diluent or carrier.

4. A method for the treatment or prophylaxis of a central nervous system disorder, comprising administering to a patient in need thereof a compound according to claim 1 , in free or pharmaceutically acceptable salt form.

5. The method according to claim 4 , wherein said disorder is selected from the group consisting of obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, agoraphobia, social phobias, agitation in dementia, agitation in autism, dementia, mood disorders, substance use disorder and/or substance abuse disorder, drug dependencies, co-morbidities associated with drug dependencies, binge eating disorder, obsessive-compulsive disorder (OCD), obsessive-compulsive personality disorder (OCPD); and stimulant use disorder (SUD).

6. The method according to claim 4 , wherein said disorder is a disorder involving the serotonin 5-HT 2A , serotonin reuptake transporter (SERT), dopamine D1 and/or D2 pathways.

7. The method according to claim 4 , wherein said disorder is a disorder selected from the following: (1) psychosis, in a patient suffering from depression; (2) depression in a patient suffering from psychosis; (3) mood disorders associated with psychosis; (4) sleep disorders associated with psychosis; and (5) substance addiction, substance use disorders and/or substance-induced disorders.

8. The method according to claim 4 , wherein said central nervous system disorder is a disorder selected from obsessive-compulsive disorder (OCD), obsessive-compulsive personality disorder (OCPD), general anxiety disorder, social anxiety disorder, panic disorder, agoraphobia, compulsive gambling disorder, compulsive eating disorder, body dysmorphic disorder, hypochondriasis, pathological grooming disorder, kleptomania, pyromania, attention deficit-hyperactivity disorder (ADHD), attention deficit disorder (ADD), impulse control disorder, and combination thereof.

9. The compound according to claim 1 , wherein the compound is in solid crystal form.

10. The compound according to claim 1 , wherein the compound has a diastereomeric excess greater than 90%.

11. The compound according to claim 10 , wherein the compound is in isolated or purified form of at least 98% purity.

12. The compound according to claim 2 , wherein the pharmaceutically acceptable salt is a hydrochloric or toluenesulfonic acid salt.

13. The method according to claim 5 , wherein said disorder is selected from the group consisting of general anxiety, social anxiety, panic disorders, refractory depression, major depressive disorder, psychosis associated with dementia, agitation in Alzheimer's disease, dementia of Alzheimer's disease, dementia of Parkinson's disease, cocaine dependency, amphetamine dependency, and withdrawal from drug dependency.

14. The compound according to claim 1 , wherein the compound has an enantiomeric excess greater than 90%.

Assignees

• Intra Cellular Therapies Inc

Inventors

• Li Peng
• Vanover Kimberly
• Davis Robert

Classifications

• A61P25/00 Primary

  Drugs for disorders of the nervous system · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61P25/28

  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 · CPC title

• A61P25/22

  Anxiolytics · CPC title