Organic compound

Patent metadata

Field	Value
Publication number	US-2025092045-A1
Application number	US-202418968542-A
Country	US
Kind code	A1
Filing date	Dec 4, 2024
Priority date	Dec 17, 2018
Publication date	Mar 20, 2025
Grant date	—

Abstract

The invention relates to a particular substituted heterocycle fused gamma-carboline, in free, or 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, the serotonin transporter (SERT), and/or pathways involving the dopamine D 1 and D 2 receptor signaling system.

First claim

1 . (canceled)

2 . (canceled)

3 . (canceled)

4 . (canceled)

5 . (canceled)

6 . A method for the treatment or prophylaxis of a central nervous system disorder, comprising administering to a patient in need thereof a compound

in free or pharmaceutically acceptable salt form, or a pharmaceutical compostion comprising the compound of Formula I in admixture with a pharmaceutically acceptable diluent or carrier; wherein the central nervous system disorder is a disorder selected from the group consisting of anxiety, depression, mood disorders, general anxiety disorder, social anxiety disorder, and panic disorder.

7 . (canceled)

8 . The method according to claim 6 , wherein the central nervous system disorder is a disorder selected from the group consisting of depression and mood disorders.

9 . The method according to claim 6 , wherein the central nervous system disorder is a disorder selected from refractory depression and major depressive disorder.

10 . (canceled)

11 . The method according to claim 6 , wherein the central nervous system disorder is depression.

12 . The method according to claim 11 , wherein the depression is acute depression.

13 . (canceled)

14 . The method according to claim 12 , wherein the depression is an acute major depressive episode, acute short-duration depressive episode, or acute recurrent brief depressive episode.

15 . The method according to claim 12 , wherein the depression is treatment resistant depression which has not responded to treatment with an antidepressant agent selected from a selective serotonin reuptake inhibitor (SSRI), a serotonin reuptake inhibitor (SRI), a tricyclic antidepressant, a monoamine oxidase inhibitor, a norepinephrine reuptake inhibitor (NRI), a dopamine reuptake inhibitor (DRI), an SRI/NRI, an SRI/DRI, an NRI/DRI, an SRI/NRI/DRI (triple reuptake inhibitor), a serotonin receptor antagonist, or any combination thereof.

16 . The method according to claim 6 , wherein said patient is not responsive to or cannot tolerate the side effects from, treatment with selective serotonin reuptake inhibitors (SSRIs), such as citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline.

17 . The method according to claim 6 , wherein said patient is not responsive to or cannot tolerate the side effects from, treatment with serotonin-norepinephrine reuptake inhibitors (SNRIs), such as venlafaxine, sibutramine, duloxetine, atomoxetine, desvenlafaxine, milnacipran, and levomilnacipran.

18 . The method according to claim 6 , wherein said patient is not responsive to or cannot tolerate the side effects from, treatment with antipsychotic agents, such as clomipramine, risperidone, quetiapine and olanzapine.

19 . (canceled)

20 . The method according to claim 6 , wherein the compound of Formula I is in pharmaceutically acceptable acid addition salt form with an acid selected from hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric, acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, and isethionic acid.

21 . The method according to claim 6 , wherein the compound of Formula I is in toluenesulfonic acid addition salt form.

22 . The method according to claim 6 , wherein the method comprises administering a tablet or capsule for oral administration comprising 1 mg to 100 mg of the Compound of Formula I in free or pharmaceutically acceptable salt form, based on the equivalent amount of free base form.

23 . The method according to claim 22 , wherein the tablet or capsule comprises 2.5 to 50 mg of the Compound of Formula I in free or pharmaceutically acceptable salt form, based on the equivalent amount of free base form.

24 . The method according to claim 6 , wherein the treatment provides an acute response within less than 1 week, or from 1 to 7 days, or from 1 to 5 days, or from 1 to 3 days, after initial dosing of the compound.

Assignees

• Intra Cellular Therapies Inc

Inventors

• Li Peng
• Zhang Qiang
• Davis Robert E

Classifications

• A61K9/1647

  Polyesters, e.g. poly(lactide-co-glycolide) · CPC title

• A61P25/22

  Anxiolytics · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61K9/0019

  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) · CPC title