Nicotinic receptor non-competitive antagonists
The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
1. A method for the treatment of nicotine addiction or smoking cessation comprising the administration of a compound of Formula I:
wherein
each of R 1 and R 2 individually is H, C 1-6 alkyl, or aryl-substituted C 1-6 alkyl, or R 1 and R 2 combine with the nitrogen atom to which they are attached to form a 3- to 8-membered ring, which ring may be optionally substituted with C 1-6 alkyl, aryl, C 1-6 alkoxy, or aryloxy substituents;
R 3 is H, C 1-6 alkyl, or C 1-6 alkoxy-substituted C 1-6 alkyl;
each of R 4 , R 5 , R 6 , and R 7 individually is H, C 1-6 alkyl, or C 1-6 alkoxy;
L 1 is a linker species selected from the group consisting of CR 8 R 9 , CR 8 R 9 CR 10 R 11 , and O;
L 2 is a linker species selected from the group consisting of CH 2 , CH 2 CH 2 , CH 2 CH 2 CH 2 , and CH 2 CH 2 CH 2 CH 2 ;
each of R 8 , R 9 , R 10 , and R 11 individually is hydrogen or C 1-6 alkyl; and
the dashed line indicates an optional double bond;
or a pharmaceutically acceptable salt thereof.
2. A method for the treatment of nicotine addiction or smoking cessation comprising the administration of a compound
or a pharmaceutically acceptable salt thereof.