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Methods of treating addiction

A technology of addiction and opioid substances, applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve problems such as inability to effectively prevent relapse

Pending Publication Date: 2021-08-31
INTRA CELLULAR THERAPIES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] Existing treatments for opiate addiction often not effective in preventing relapse

Method used

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  • Methods of treating addiction
  • Methods of treating addiction
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0160] In a further embodiment of the first aspect, the present disclosure provides a further embodiment of Method 1 as follows:

[0161] 1.83 Approach 1 or any of Approaches 1.1-1.82, wherein the patient suffers from anxiety (including general anxiety, social anxiety, and panic disorder), depression (eg, treatment-resistant depression and MDD), psychosis (including dementia-related psychosis, such as hallucinations in advanced Parkinson's disease or paranoid delusions), schizophrenia, migraine, pain and pain-related conditions including headache, idiopathic pain, chronic pain (such as moderate to moderately severe chronic pain , such as in patients requiring 24-hour extended treatment for other diseases), neuropathic pain, toothache, fibromyalgia, other drug dependence, such as stimulant dependence and / or alcohol dependence.

[0162] 1.84 Approach 1 or any of 1.1-1.83, wherein the patient has been diagnosed with a substance use disorder or substance abuse disorder such as opi...

Embodiment 1

[0244] Example 1: (6bR,10aS)-8-(3-(4-fluorophenoxy)propyl)-6b,7,8,9,10,10a-hexahydro-1H-pyrido[3', Synthesis of 4':4,5]pyrrolo[1,2,3-de]quinoxalin-2(3H)-one

[0245]

[0246] (6bR,10aS)-6b,7,8,9,10,10a-hexahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de ]quinoxalin-2(3H)-one (100 mg, 0.436 mmol), 1-(3-chloropropoxy (proxy))-4-fluorobenzene (100 μL, 0.65 mmol) and potassium iodide (KI) (144 mg, A mixture of 0.87 mmol) in dimethylformamide (DMF) (2 mL) was degassed for 3 minutes, and N,N-diisopropylethylamine (DIPEA) (150 μL, 0.87 mmol) was added. The resulting mixture was heated to 78°C and stirred at this temperature for 2 hours. The mixture was cooled to room temperature, then filtered. The filter cake was purified by silica gel column chromatography using 7N NH in methanol / in methanol 3 A gradient of 0-100% ethyl acetate in a mixture of (1:0.1 v / v) as eluent yielded a partially purified product which was further purified with a semi-preparative HPLC system using 0-100% eth...

Embodiment 2

[0247] Example 2: (6bR,10aS)-8-(3-(6-fluoro-1H-indazol-3-yl)propyl)-6b,7,8,9,10,10a-hexahydro-1H- Synthesis of pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-2(3H)-one

[0248]

[0249] Step 1: Stirring BCl at 0-5 °C 3 3-Fluoroaniline (5.6 mL, 58 mmol) was added to a solution of MeS (10.8 g, 60 mmol) in toluene, followed by 4-chlorobutyronitrile (7.12 g, 68.73 mmol) and aluminum chloride (AlCl 3 ) (8.0 g, 60.01 mmol). The mixture was stirred overnight at 130°C and cooled to 50°C. Hydrochloric acid (3N, 30 mL) was added cautiously, and the resulting solution was stirred at 90 °C overnight. The resulting brown solution was cooled to room temperature and evaporated to dryness. The residue was dissolved in dichloromethane (DCM) (20 mL), and washed with saturated Na 2 CO 3 Alkaline to pH=7-8. The organic phase was separated and washed with Na 2 CO 3 Dried and concentrated. Purification of the residue by column chromatography on silica gel using a gradient of 0-20% ethyl ...

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Abstract

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, for use in methods for the treatment or prevention of opiate addiction relapse.

Description

[0001] Cross References to Related Applications [0002] This application is an international application claiming the benefit of and priority to U.S. Provisional Application Serial No. 62 / 795,899, filed January 23, 2019, the contents of which are hereby incorporated by reference in their entirety. [0003] field of invention [0004] The present invention relates to specific substituted heterocyclic fused gamma-carbolines as described herein in free or pharmaceutically acceptable salt and / or in substantially pure form, pharmaceutical compositions thereof for use in the treatment and / or prophylaxis Use in opiate addiction relapse. [0005] Background of the invention [0006] Substituted heterocyclic fused gamma-carbolines known to be 5-HT in the treatment of central nervous system disorders 2 receptors especially 5-HT 2A Agonists or antagonists of receptors. These compounds have been described in U.S. Patent Nos. 6,548,493; 7,238,690; 6,552,017; 6,713,471; 7,183,282; 2A N...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51C07D471/14
CPCA61K31/4985A61K9/0004A61P25/36C07D471/14
Inventor 李鹏姚伟R·戴维斯S·梅特斯K·瓦诺维尔G·斯奈德
Owner INTRA CELLULAR THERAPIES INC
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