Pharmaceutical compositions based on aminomethylindoles and...

Details Pharmaceutical compositions based on aminomethylindoles and... Pharmaceutical compositions based on aminomethylindoles and...

A - Human Necessities

61

K

A61K 31/40 (2006.01) C07D 209/14 (2006.01)

Patent

CA 2187460

Pharmaceutical compositions containing active ingredients derived from 2-aminomethyl-5-benzyloxyindols, including their N-propinyl, N-2-butinyl- and N-2,3-butadienil derivatives, which are potent inhibitors of monoamine oxidase types A and B in rat liver and brain, as well as in human brain, with a marked selectivity for the inhibition "in vitro" and "in vivo" of monoamine oxidase B in preference to A. Based on this selectivity for inhibition of monoamine oxidase B, as well as the capacity to neutralise the neurotoxic action of MPTP and other neurotoxins in laboratory animals, the above compounds are useful for the treatment of cerebral neurodegenerative processes and in particular for the treatment of Parkinsonism and Alzheimer's disease.

Compositions pharmaceutiques contenant comme composants actifs des dérivés de 2-aminométhyl-5-benzyloxyindoles, y compris les dérivés N-propynyl, N-2-butynyl et N-2,3-butidinyle, qui sont de puissants inhibiteurs des monoaminoxydases A et B du foie et du cerveau de rat, ainsi que du cerveau humain, avec une sélectivité marquée pour l'inhibition in vitro et in vivo de la monoaminoxydase B, avec une préférence sur la A. En raison de cette sélectivité d'inhibition de la monoaminoxydase B, ainsi que de leur capacité à neutraliser chez des animaux de laboratoire l'action neurotoxique de la MPTP et autres neurotoxines, les composés de l'invention sont utiles pour le traitement de processus neurodégénératifs cérébraux et en particulier pour le traitement des maladies de Parkinson et d'Alzheimer.

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