Therapeutic or prophylactic agent for preventing nausea and...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 491/18 (2006.01) A61K 31/485 (2006.01) A61K 45/00 (2006.01) A61P 1/08 (2006.01) A61P 25/00 (2006.01) C07D 491/08 (2006.01) C07D 491/22 (2006.01)

Patent

CA 2492694

A therapeutic or preventive agent for nausea/vomiting which contains as an active ingredient either a morphinane derivative represented by the general formula (I): (I) (wherein R1 represents cyclopropylmethyl, etc.; R2 and R3 each represents hydroxy, methoxy, etc.; R4 and R5 are bonded to each other to form -O-, etc.; R6 represents hydrogen, etc.; and Q represents (II) which has been optionally substituted, etc., provided that X represents NH, NMe, etc.) or a pharmacologically acceptable acid addition salt thereof. The compound or salt is useful in a medicine widely applicable to vomiting caused by drugs having emetic activity, especially in a therapeutic or preventive agent for nausea/vomiting induced by ~ agonists represented by morphine.

La présente invention a trait à un agent thérapeutique ou préventif pour la nausée/le vomissement contenant en tant que principe actif soit un dérivé de morphinane de formule générale (I), dans laquelle R?1¿ représente cyclopropylméthyle ; R¿2? et R?3¿ représentent chacun hydroxy, méthoxy ; R?4¿ et R?5¿ forment ensemble -O- ; R?6¿ représente hydrogène ; et Q représente (II) éventuellement substitué, à condition que X représente NH, NMe, ou un sel d'addition à un acide pharmaceutiquement acceptable. Le composé ou sel est utile dans le domaine médical pour des applications variées contre le vomissement provoqué par des médicaments ayant une activité émétique, particulièrement dans un agent thérapeutique ou préventif pour la nausée/le vomissement induits par des agonistes µ représentés par la morphine.

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