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Methods for the treatment of alcohol abuse, addiction and dependency

A technology for alcohol abuse and alcohol dependence, which can be applied in pharmaceutical formulations, organic active ingredients, medical preparations containing active ingredients, etc., and can solve a large number of liver metabolism problems

Inactive Publication Date: 2009-12-30
JANSSEN PHARMA NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although atypical antipsychotics have been suggested as potential treatments for substance abuse, their administration in substance abuse patients is subject to substantial hepatic metabolism.

Method used

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  • Methods for the treatment of alcohol abuse, addiction and dependency
  • Methods for the treatment of alcohol abuse, addiction and dependency
  • Methods for the treatment of alcohol abuse, addiction and dependency

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] 1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-1,3,8-triaza-spiro[4.5]decane-4-one

[0066]

[0067] Step A: (8-Hydroxymethyl-naphthalen-1-yl)-methanol

[0068] 1,8-Naphthalic anhydride (200 g, 1.0 mol) in toluene (2.5 L) was charged at room temperature in a 12-L vessel equipped with a thermocouple, overhead stirrer, 2-L additional funnel, and condenser under nitrogen. -L4 neck flask. DIBAL-H (1.5 M in toluene, 2.664 L, 4 mol) was added via an additional funnel over 1.5 h while the reaction mixture was stirred. The solution was then heated to 95°C overnight, cooled to 15°C, and washed with ethyl acetate (2.2 L) and H 2 O (2 L) was diluted slowly, followed by the addition of conc. HCl (320 mL). The resulting suspension was stirred at room temperature for 30 min, filtered and air-dried on filter paper for 2 h. The resulting material was stirred in 95% ethanol (1.2 L) at 70°C for 2 h, filtered to obtain a wet solid, which was air-dried on filter paper ov...

Embodiment 2

[0087] 1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-3-(S)-oxiranylmethyl-1,3,8-triazine Hetero-spiro[4.5]decane-4-one

[0088]

[0089] 1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-1,3,8-triaza-spiro[4.5]-decane-4-one (2.0 g, 4.95 mmol) was dissolved in N,N-dimethylformamide (25.0 mL). Sodium hydride (60% in mineral oil, 238 mg, 5.94 mmol) was then added to the reaction mixture at 0°C under nitrogen atmosphere, and the reaction mixture was stirred at 0°C for one hour. Then (2R)-(-)-3-nitrobenzenesulfonic acid glycidyl ester (1.54 g, 5.94 mmol) was added to the reaction mixture at 0°C. The reaction mixture was stirred at 0°C for one hour, then at room temperature under nitrogen for 18 hours, and partitioned with water and ethyl acetate. The organic layer was washed with brine, washed with Na 2 SO 4 Dry, filter and evaporate the solvent in vacuo to give a crude oil. The crude oil was purified by flash chromatography (2.5% methanol / dichloromethane)...

Embodiment 3

[0093] 3-(3-Amino-2-(R)-hydroxy-propyl)-1-(4-fluoro-phenyl)-8-(8-methyl-naphthalene-1-ylmethyl base)-1,3,8-triaza-spiro[4.5]decane-4-one

[0094]

[0095] 1-(4-fluoro-phenyl)-8-(8-methyl-naphthalen-1-ylmethyl)-3-(S)-oxiranylmethyl-1,3,8-triazine Hetero-spiro[4.5]decan-4-one (0.06 g, 0.13 mmol) was dissolved in ethanol (2 mL) and methanol (0.4 mL). Concentrated ammonium hydroxide (1 mL) was then added to the solution and the reaction mixture was stirred in a pressure bottle at 40°C for two hours. The solvent was then evaporated in vacuo to give a crude oil. The crude oil was purified by flash chromatography (5.0% ammonia 2.0 M in methanol / dichloromethane) to afford the title compound as a foam.

[0096] 1 H NMR (400MHz, CDCl 3 )δ7.77-7.75 (1H, m), 7.71-7.68 (1H, m), 7.37-7.30 (4H, m), 6.97-6.91 (2H, m), 6.87-6.83 (2H, m), 4.74 ( 2H, s), 4.0 (2H, s), 3.79-3.74 (1H, m), 3.57-3.52 (1H, m), 3.41-3.36 (1H, m), 3.11 (3H, s), 2.91-2.74 ( 4H, m), 2.66-2.61 (1H, m), 2.30-2....

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PUM

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Abstract

The present invention is directed to methods for the treatment of alcohol abuse, addiction and / or dependency, alone and in combination with one or more anti-addiction agents.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Provisional Patent Application 60 / 861,378, filed November 28, 2006, which is hereby incorporated by reference in its entirety. field of invention [0003] The present invention relates to methods of treating alcohol abuse, alcohol addiction and / or alcohol dependence, alone or in combination with one or more detoxification agents. Background of the invention [0004] Alcohol abuse, typically characterized by the consumption of alcohol in an inappropriate manner resulting in clinically significant impairment or suffering, is a serious medical and social problem. Studies suggest that agents that cause a selective reduction in alcohol drinking in animals without similar reductions in water and food intake may be clinically effective in treating alcoholism in humans. Daidzin, the active ingredient in the Chinese herbal medicine Pueraria lobata (Radixpureariea) (RP), used in China f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/438A61P25/32
CPCA61K31/4468A61K31/438A61K31/145A61P25/32A61P43/00A61K31/4188
Inventor A·H·韦迪亚
Owner JANSSEN PHARMA NV
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