Modulators of dopamine neurotransmission
View Patent ↗A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of the following formula: wherein R 1 is selected from the group consisting of OSO 2 CF 3 , OSO 2 CH 3 , SO 2 R 3 , COCF 3 , COCH 3 and COCH 2 CH 3 , wherein R 3 is as defined hereafter; R 2 is selected from the group consisting of C 1 -C 4 alkyls, allyl, CH 2 CH 2 CH 2 F, CH 2 CF 3 , 3,3,3-trifluoropropyl and 4,4,4-trifluorobutyl; R 3 is selected from the group consisting of C 1 -C 3 alkyls, CF 3 , and N(CH 3 ) 2 ; with the proviso that when R 1 is SO 2 R 3 and R 3 is a C 1 -C 3 alkyl, then R 2 is not CH 2 CH 2 OCH 3 ; or a pharmaceutically acceptable salt thereof are provided. Also, pharmaceutical compositions comprising the above compound and methods wherein the above compound is used for the treatment of various disorders are provided.
1. A 3-substituted 4-(phenyl-N-alkyl)-piperazine compound of Formula 1:
wherein:
R 1 is selected from the group consisting of OSO 2 CF 3 , OSO 2 CH 3 , SO 2 R 3 , COCF 3 , COCH 3 and COCH 2 CH 3 , wherein R 3 is as defined below;
R 2 is selected from the group consisting of C 1 -C 4 alkyls, allyl, CH 2 CH 2 CH 2 F, CH 2 CF 3 , 3,3,3-trifluoropropyl and 4,4,4-trifluorobutyl;
R 3 is selected from the group consisting of C 1 -C 3 alkyls, CF 3 , and N(CH 3 ) 2 ;
with the proviso that when R 1 is SO 2 R 3 and R 3 is a C 1 -C 3 alkyl, then R 2 is not CH 2 CH 2 OCH 3 ;
or a pharmaceutically acceptable salt thereof.
2. A compound according to claim 1 , wherein R 1 is selected from the group consisting of OSO 2 CF 3 , OSO 2 CH 3 , SO 2 CH 3 , SO 2 CF 3 , COCH 3 and SO 2 N(CH 3 ) 2 .
3. A compound according to claim 1 , wherein R 2 is selected from the group consisting of n-propyl and ethyl.
4. A pharmaceutical composition comprising a compound according claim 1 and one or more pharmaceutically acceptable carriers or diluents.
5. A pharmaceutical composition according to claim 4 , formulated for oral administration.
6. A pharmaceutical composition according to claim 5 , formulated as a tablet.
7. A pharmaceutical composition according to claim 5 , formulated as a capsule.
8. A pharmaceutical composition according to claim 4 , formulated for administration by injection.