6,7-unsaturated-7-carbamoyl-substituted morphinan derivative

Details 6,7-unsaturated-7-carbamoyl-substituted morphinan derivative 6,7-unsaturated-7-carbamoyl-substituted morphinan derivative

C - Chemistry, Metallurgy

07

D

C07D 489/08 (2006.01) A61K 31/485 (2006.01) A61P 1/08 (2006.01) A61P 1/10 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2609733

A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. A compound represented by the formula (I): [Chemical formula I] (see formula I) wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.

Nouveaux composés qui sont utiles comme agent thérapeutique et/ou préventif pour les nausées, les vomissements et/ou la constipation. L'invention concerne des composés, leurs sels acceptables du point de vue pharmaceutique et des hydrates de ceux-ci, les composés étant représentés par la formule : (I) dans laquelle chacun de R1 et R2 est indépendamment un hydrogène, un alkyle inférieur facultativement substitué, un alcényle inférieur facultativement substitué, un cycloalkyle facultativement substitué, un aryle facultativement substitué, etc. ; R3 est un hydrogène, un hydroxyle, un alkyle inférieur facultativement substitué, un alcényle inférieur facultativement substitué, un alcynyle inférieur facultativement substitué, un alcoxy inférieur facultativement substitué, etc. ; R4 est un hydrogène ou un alkyle inférieur ; et R5 est un hydrogène, un alkyle inférieur, un alkyle inférieur cycloalkylé ou un alcényle inférieur.

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