Novel basic derivatives of benz[e]isoindol-1-ones and...

C - Chemistry – Metallurgy – 07 – D

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C07D 519/00 (2006.01) A61K 31/439 (2006.01) A61K 31/46 (2006.01) A61K 31/4745 (2006.01) C07D 451/04 (2006.01) C07D 453/02 (2006.01)

Patent

CA 2285817

Novel basic derivatives of benz[e]isoindol-l-ones and pyrrolo[3,4-c]quinolin-l-ones which can be represented by the general formula (I) indicated below are described: (see formula I) in which - X is CH or N, - R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, - Het is the 3-endotropyl group (that is, the 8-methyl-8--azadicyclo[3.2.1]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.

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