Quinolinomorphinan derivative and medical use thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 489/09 (2006.01) A61K 31/485 (2006.01) C07D 489/00 (2006.01) C07D 491/20 (2006.01)

Patent

CA 2256336

The present invention provides a quinolinomorphinan derivative or a pharmacologically acceptable acid addition salt thereof, and an agent for curing or preventing cerebral disorders composed of the derivative and salt thereof, which is represented by the following formula (I) : (see formula I) [wherein R1 represents cyclopropylmethyl or the like; R2 and R3 independently represent hydroxy, methoxy, or the like; R4 represents hydrogen, methyl, amino, or the like; and (R5)m represents hydrogen, substituted benzo, or the like] . The compounds of the present invention have the excellent effect of preventing damages of the cerebral nerve cells. Therefore, the compounds of the present invention are useful as medicines used for curing or preventing various cerebral diseases such as cerebral stroke, traumatic cerebral diseases, cerebral edema, and cerebral neurodegenerative diseases, ameliorating aftereffects thereof, and preventing the recurrence thereof by inhibiting various ischemic, hemorrhagic or traumatic cerebral

L'invention concerne des dérivés de quinolinomorphinane représentés par la formule générale (I), ou des sels acides d'addition de ces derniers acceptables du point de vue pharmacologique, ainsi que des remèdes et préventifs destinés aux maladies neurodégénératives et contenant ces dérivés. Dans la formule générale (I), R<1> représente cyclopropylméthyle, etc.; R<2> et R<3> représentent chacun hydroxy, méthoxy, etc.; R<4> représente hydrogène, méthyle, amino, etc.; et (R<5>)m représente hydrogène, benzo substitué, etc. Parce qu'ils ont des effets préventifs excellents sur les troubles des cellules des nerfs crâniens, ces composés inhibent plusieurs troubles ischémiques, hémorragiques, ou traumatiques du cerveau et troubles des cellules des nerfs crâniens provoqués par différentes dégénérescences des nerfs et s'utilisent donc comme médicaments dans le traitement de plusieurs maladies neurodégénératives telles que l'attaque cérébrale, des affections traumatiques du cerveau, l'oedème cérébral et des affections dégénératives du nerf crânien; ces composés permettent d'améliorer les séquelles de ces affections et de prévenir leur récurrence.

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