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Combination of a nicotinic receptor partial agonist and of an acetylcholinesterase inhibitor, pharmaceutical composition containing same and use thereof in the treatment of cognitive disorders

A technology of acetylcholinesterase and agonist, applied in the combination of a nicotinic receptor partial agonist and an acetylcholinesterase inhibitor, a pharmaceutical composition containing the combination and the field of use thereof in the treatment of cognitive impairment, It can solve problems such as adverse side effects and inability to accept the best therapeutic dose, and achieve the effect of reducing gastrointestinal side effects and good tolerance

Inactive Publication Date: 2011-05-04
SANOFI AVENTIS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] One difficulty with treating cognitive impairment associated with Alzheimer's disease with acetylcholinesterase inhibitors is that with repeated dosing, many treated patients gradually develop unwanted side effects
Thus, 10-15% of treated patients had to discontinue treatment due to gastrointestinal side effects (nausea, vomiting, diarrhea) and 40% of treated patients could not receive optimal therapeutic dose due to these side effects

Method used

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  • Combination of a nicotinic receptor partial agonist and of an acetylcholinesterase inhibitor, pharmaceutical composition containing same and use thereof in the treatment of cognitive disorders
  • Combination of a nicotinic receptor partial agonist and of an acetylcholinesterase inhibitor, pharmaceutical composition containing same and use thereof in the treatment of cognitive disorders
  • Combination of a nicotinic receptor partial agonist and of an acetylcholinesterase inhibitor, pharmaceutical composition containing same and use thereof in the treatment of cognitive disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0046] Example : Preparation of 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (2E)-but-2-enedioate

[0047] 232.45 g of 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate (WO 00 / 58311 ) were placed in 2331 ml of ethanol in a 6 L jacketed reactor. The reaction medium is brought to 60°C. A solution of 87.17 g of fumaric acid in 1000 ml of ethanol and 97 ml of water (preheated to 60° C.) was then added. Subsequently 1900 ml of solvent were distilled off, and the reaction medium was then cooled to 20° C. over 2.5 hours. After contacting at 20°C for 2.5 hours, filter 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate (2E)-but-2-enedioate with Wash twice with 400 ml of ethanol, then dry under vacuum at 50°C.

[0048] Melting point (DSC): 175°C.

[0049] 1H NMR (400MHz, DMSO-d6) δ (ppm): 1.80 (bs (a) , 2H), 2.10(bs, 2H), 3.10(bs, 6H), 3.71(bs, 1H), 3.84(bs, 1H), 4.25(bs, 0.5H), 4.40(bs, 0.5H), 6.58( s, 2H), 7.14 (m, 2H), 7.57 (m, 2H), 11 (b...

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Abstract

he present invention relates to the combination of an alpha-7 nicotinic receptor partial agonist and of an acetylcholinesterase inhibitor. The invention also relates to a pharmaceutical composition comprising the combination according to the invention and to the use thereof in the treatment of cognitive disorders.

Description

technical field [0001] The present invention relates to a combination of an alpha-7 nicotinic receptor partial agonist and an acetylcholinesterase inhibitor, a pharmaceutical composition containing the combination of the invention and its usefulness in the treatment of cognitive disorders and more particularly in relation to Alzheimer's disease Use in cognitive impairment. Background technique [0002] The term "cognitive impairment" is intended to denote a deficit in higher intellectual functioning involving, inter alia, impairment of short- and long-term memory, impairment of working memory, impairment of attention and vigilance processes, impairment of semantic memory, impairment of spatial memory and higher executive functions (abstraction, planning and Judgment) Obstacles. [0003] Patients with cognitive impairment associated with Alzheimer's disease are currently treated by administering acetylcholinesterase inhibitors. [0004] One difficulty with treating cognitiv...

Claims

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Application Information

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IPC IPC(8): A61K31/27A61K31/445A61K31/551A61K45/06A61P25/28
CPCA61K31/27A61K31/445A61K31/551A61K45/06A61P25/00A61P25/28A61P43/00A61K2300/00A61K31/085A61K31/439A61K31/13
Inventor 奥利维尔·伯吉斯菲利普·皮查特亚历山大·乌拉尼
Owner SANOFI AVENTIS SA
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