Carbamoyl esters that inhibit cholinesterase and release...

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 271/40 (2006.01) A61K 31/27 (2006.01) A61K 31/407 (2006.01) A61K 31/4406 (2006.01) A61K 31/5365 (2006.01) A61P 25/00 (2006.01) C07D 213/64 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2543322

Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: Formula (I)wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

L'invention concerne des esters de carbamoyle inhibant l'activité de la cholinestérase et, lors d'une hydrolyse, libérant un agent pharmacologiquement actif. Dans un mode de réalisation, l'ester de carbamoyle présente la structure représentée par la formule (I), dans laquelle A est choisi dans le groupe constitué par un aryle non substitué, un aryle substitué, un hétéroaryle non substitué et un hétéroaryle substitué. Ces esters de carbamoyle sont utilisés dans des méthodes destinées à traiter un individu. L'agent pharmacologiquement actif obtenu par hydrolyse des esters de carbamoyle permet de traiter, par exemple, une affection du système nerveux, un déficience cholinergique et des affections ou des maladies associées à une carence en un agent pharmacologiquement actif, tel que l'acétylcholine.

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