Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Method of treating depression with delta receptor agonist compounds

A compound and composition technology, applied in the direction of drug combination, organic chemistry, pharmaceutical formulation, etc., can solve problems such as lack of treatment methods

Inactive Publication Date: 2005-03-16
VERSI GRP LLC
View PDF0 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such treatments are lacking in the prior art

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method of treating depression with delta receptor agonist compounds
  • Method of treating depression with delta receptor agonist compounds
  • Method of treating depression with delta receptor agonist compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0127]

[0128] 4-((α-R)-α((2S,5R)-2,5-Dimethyl-4-(4-fluorobenzyl)-1-piperazinyl)-3-hydroxy Benzyl)-N,N-diethylbenzamide

[0129] A solution of 3-bromophenol (400 g, 2.31 mol), tert-butylchlorodimethylsilane (391 mg, 2.54 mol) and imidazole (346 g, 5.08 mol) in 5000 mL of dichloromethane was stirred overnight at room temperature. The reaction solution was poured into 2000 mL of water, and the layers were separated. The organic layer was washed with 1 N aqueous sodium hydroxide solution (3 x 1500 mL) and water (2 x 1500 mL) before passing through a pad of silica gel (400 g, silica 60, 230-400 mesh). The silica gel was washed with dichloromethane (2 x 500 mL), the filtrates were combined, and the solvent was removed under reduced pressure to afford 669 g (98.4%) of 3-(bromophenoxy)-tert-butyldimethyl base silane. NMR (300MHz, CDCl 3 ): δ0.2(s, 6H); 1.0(s, 9H); 6.75(m, 1H); 7.0(br s, 1H); 7.1(m, 2H).

[0130] A solution of 3-bromophenoxy-tert-butyldimethylsilane (27.3 ...

Embodiment 2

[0137]

[0138] 4-(α-R)-α((2S,5R)-2,5-Dimethyl-4-(3-fluorobenzyl)-1-piperazinyl)-3-hydroxy Benzyl)-N,N-diethylbenzamide

[0139] A solution of 3-bromophenol (400 g, 2.31 mol), tert-butylchlorodimethylsilane (391 mg, 2.54 mol) and imidazole (346 g, 5.08 mol) in 5000 mL of dichloromethane was stirred overnight at room temperature. The reaction solution was poured into 2000 mL of water, and the layers were separated. The organic layer was washed with 1 N aqueous sodium hydroxide solution (3 x 1500 mL) and water (2 x 1500 mL) before passing through a pad of silica gel (400 g, silica 60, 230-400 mesh). The silica gel was washed with dichloromethane (2 x 500 mL), the filtrates were combined and the solvent was removed under reduced pressure to afford 669 g (98.4%) of 3-(bromophenoxy)-tert-butyldimethyl silane. NMR (300MHz, CDCl 3 ): δ0.2(s, 6H); 1.0(s, 9H); 6.75(m, 1H); 7.0(br s, 1H); 7.1(m, 2H).

[0140] A solution of 3-bromophenoxy-tert-butyldimethylsilane (27.3 g, 92.6...

Embodiment 3

[0149]

[0150] 4-((α-R)-α-((2S,5R)-2,5-Dimethyl-4-(2-fluorobenzyl)-1-piperazinyl)-3-hydroxybenzyl) -N,N-Diethylbenzamide

[0151] 4-((α-R)-α-((2S,5R)-2,5-dimethyl-1-piperazinyl)-3-trifluoromethylsulfonyloxybenzyl)-N,N -Diethylbenzamide (from Example 1, 527.6 mg, 1.0 mmol) was dissolved in acetonitrile (4.0 mL) and sodium iodide (15 mg, 0.1 mmol) was added. The suspension was stirred during the addition of triethylamine (500 μL (363 mg), 3.59 mmol) followed by 2-fluorobenzyl bromide (241 μL (378 mg), 2.0 mmol). The reaction mixture was sealed under nitrogen and stirred overnight at room temperature. The reaction mixture was evaporated to dryness and partitioned between ethyl acetate (10 mL) and saturated aqueous sodium bicarbonate (2.5 mL). The supernatant organic layer was removed, and the water-soluble fraction was washed with ethyl acetate (3 x 10 mL). The combined organic extracts and washings were dried over anhydrous sodium sulfate and evaporated to a golden oil. ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

Compositions and methods for treatment of depression or other affective mood disorders or pathological mental and / or emotional states, by administration to a subject suffering or susceptible to same, of therapeutically effective delta receptor agonist compund(s), optionally in combination with other mood disorder-combating agents.

Description

Background of the invention [0001] field of invention [0002] The present invention relates to compositions and methods for the treatment of depression or other affective mood disorders or pathological mental and / or emotional states by administering a delta opioid receptor agonist compound and optionally other agents for therapeutic purposes. [0003] Related technical description [0004] Depression is a difficult psychological disorder to treat. Patients with this condition are often reluctant to seek the medical treatment necessary to diagnose the condition. This reluctance is often related to the patient's fear of stigma in seeking psychiatric help, or to the patient's feelings of worthlessness associated with depression. Furthermore, once the patient seeks appropriate psychiatric help, it is difficult to successfully treat the disorder with a single psychiatric approach. [0005] In the Diagnostic and Statistical Manual of Mental Disorders, 4th Edition (DSM IV), ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/14A61K9/70A61K31/495A61K31/496A61K31/497A61P25/24A61P43/00C07D401/06
CPCA61K31/497A61P25/24A61P43/00
Inventor 张宽仁威廉·彭德格斯特彼得·J·真戈
Owner VERSI GRP LLC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com