Epibatidine and derivatives, compositions and methods of...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/08 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01)

Patent

CA 2131365

The present invention is directed to compounds, compositions and methods of treating pain, and derivatives that have potent analgetic activity. The compounds have formula (I) wherein R1 is selected from H, lower alkyl, C3-C9 cycloalkyl, acyl, and C3-C9 cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, or C3-C8 cycloalkenyl or C3-C8 cycloalkynyl; and wherein R is selected from cycloalkyl, aryl, heteroaryls (selected from the group consisting of pyridyl, thienyl, furanyl, imidazolyl, pyrazinyl, and pyrimidyl) or phenoxy and wherein said R groups can be substituted with hydroxyl, C1-C6 lower alkyl, C2-C6 alkenyl, C1-C6 lower alkoxyl, halo, C1-C6 haloalkyl, amino, C1-C6 alkylamino and C2-C10 dialkylamino, and sulfonamido or a pharmaceutically acceptable salt thereof.

Composés , compositions et méthodes pour traiter la douleur; dérivés possédant des propriétés analgésiques. Les composés correspondent à la formule (I), dans laquelle R1 est choisi parmi H, un alkyle inférieur, un cycloalkyle C3-C9, un acyle, un cycloalkylalkyle C3-C9, un haloalkyle, un alcényle, un alcynyle, un hydroxyalkyle ou un cycloalcényle C3-C8 ou un cycloalcynyle C3-C8; R est choisi parmi un groupe cycloalkyle, aryle, hétéroaryle (choisi parmi les groupes pyridyle, thiényle, furanyle, imidazolyle, pyrazinyle et pyrimidyle) ou phénoxy et où les groupes R peuvent faire l'objet d'un substitution par un groupe hydroxyle, alkyle inférieur C1-C6, alcényle C2-C6, alcoxy inférieur C1-C6, halo, haloalkyle C1-C6, amino, alkylamino C1-C6 et dialkylamino C2-C10 et sulfonamido; ou sels de ces composés acceptables en pharmacie.

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