Epibatidine and derivatives, compositions and methods of treatin

Details Epibatidine and derivatives, compositions and methods of treatin Epibatidine and derivatives, compositions and methods of treatin

1992-03-03

1994-05-24

Fan, Jane T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546272, 548466, 548452, 5483121, 544405, 544333, 514413, 514397, 514253, 514256, C07D40104, A61K 3144

Patent

active

053148991

ABSTRACT:
The present invention is directed to compounds, compositions and methods of treating pain, and derivatives that have potent analgetic activity. The compounds have the formula: ##STR1## wherein R.sup.1 is selected from H, lower alkyl, C.sub.3 -C.sub.9 cycloalkyl, acyl, and C.sub.3 -C.sub.9 cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, or C.sub.3 -C.sub.8 cycloalkenyl or C.sub.3 -C.sub.8 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, C.sub.1 -C.sub.6 lower alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 lower alkoxyl, halo, C.sub.1 -C.sub.6 haloalkyl, amino, C.sub.1 -C.sub.6 alkylamino and C.sub.2 -C.sub.10 dialkylamino, and sulfonamido or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 4499099 (1985-02-01), Watts
patent: 5015655 (1991-05-01), Galliani et al.
Fraser et al. Canadian Jour. of Chem. vol. 48. 1970 pp. 2065-2074.
Kricka et al. Advances in Heterocyclic Chemistry vol. 16. pp. 87-121. 1974.
Aceto et al. Problems of Drug Dependence, 1992: Proceedings of the 54th Annual Scientific Meeting. pp. 460-516.

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