Acetylcholine enhancers

Details Acetylcholine enhancers Acetylcholine enhancers

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/44 (2006.01) C07D 209/00 (2006.01) C07D 221/00 (2006.01)

Patent

CA 2331794

Disclosed herein are quinoline derivatives having dual mechanistic properties, referred to in this patent document as "acetylcholine enhancers", i.e., compounds which evidence acetylcholinesterase (AChE) inhibition activity, and 5-HT3 receptor antagonist activity. A particularly preferred compound is 2-[2- (1-benzylpiperizin-4-yl)ethyl]-2,3-dihydro-9-methoxy-1H-pyrrolo[3,4-b]quinolin- 1-one hemifumarate, referred to herein as Compound A ("Cm.A").

L'invention concerne des dérivés de quinoline possédant des propriétés mécanistes doubles, ces dérivés étant dénommés dans ce document de brevet "activateurs d'acétylcholine", c.-à-d. des composés qui attestent de l'activité d'inhibition de l'acétylcholinestérase (AChE), et de l'activité d'antagoniste du récepteur de 5-HT3. Un composé particulièrement préféré est 2-[2-(1-benzylpipérizin-4-yl) éthyl]-2,3-dihydro-9-méthoxy-1H-pyrrolo [3,4-b] quinolin-1-one hemifumarate, ci-après dénommé Composé A ("Cm.A").

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