Epibatidine and derivatives, compositions and methods of treating pain

A compound having the formula:

• ##STR9## wherein R.sub.1 is selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.9 cycloalkyl, C.sub.1 -C.sub.7 acyl, C.sub.4 -C.sub.9 cycloalkylalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 hydroxyalkyl, and C.sub.3 -C.sub.8 cycloalkenyl;
• and wherein R is pyridyl, which is unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 alkoxyl, halo, C.sub.1 -C.sub.6 haloalkyl, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.10 dialkylamino, and sulfonamido;
• or a pharmaceutically acceptable salt thereof;
• with the proviso that R is not 6-chloro-3-pyridyl when R.sub.1 is H.

A method of treating pain which comprises administering to a host in need thereof, an effective amount of a compound having the formula:

• ##STR11## wherein R.sub.1 is selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.9 cycloalkyl, C.sub.1 -C.sub.7 acyl, C.sub.4 -C.sub.9 cycloalkylalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 hydroxyalkyl, and C.sub.3 -C.sub.8 cycloalkenyl;
• and wherein R is pyridyl, which is unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 alkoxyl, halo, C.sub.1 -C.sub.6 haloalkyl, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.10 dialkylamino, and sulfonamido;
• or a pharmaceutically acceptable salt thereof;
• with the proviso that R is not 6-chloro-3-pyridyl when R.sub.1 is H.