Morphinan derivatives and pharmaceutical use thereof

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 489/08 (2006.01) A61K 31/485 (2006.01) C07D 489/00 (2006.01)

Patent

CA 2143864

A morphinan derivative or its pharmaceutically acceptable acid addition salt represented with, for example, (see formula I) and an analgesic, diuretic, antitussive and brain cell protector having its derivative or its salt as the active ingredient are described. The compound of the present invention possesses strong analgesic activity, diuretic action and antitussive action as a highly selective .KAPPA.-opioid agonist, allowing it to be used as a useful analgesic, diuretic and antitussive. On the other hand, the compound of the present invention also possesses remarkable cerebro-neuroprotective activity, thus allowing it be used as a useful cerebro-neuroprotective agents.

Dérivé de morphinane représenté par la formule (1) ou sel dérivé à addition d'acide, acceptable du point de vue pharmaceutique, et agents analgésiques, diurétiques, antitussifs et agents protecteurs des cellules cérébrales, contenant chacun ledit dérivé ou ledit sel en tant que composant actif. Ces composés ont, en tant qu'agoniste kappa -opioïde hautement sélectif, des effets analgésiques, diurétiques et antitussifs. En outre, ils ont un effet protecteur important sur les cellules cérébrales et servent donc d'agents protecteurs de ces cellules.

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