• Patent

Cocaine receptor binding ligands

Novel compounds show high affinity for specific cocainereceptors in the brain, particularly dopamine transporter sites,and have the formula ##STR1## Wherein Y=CH.sub.2 R.sub.3, CO.sub.2R.sub.2 or ##STR2## R.sub.1 =hydrogen, C.sub.1-5 alkyl, R.sub.2=hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy,C.sub.1-6 alkynyl, halogen or amine, R.sub.3 =OH, hydrogen,C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, Cl Br, I,CN, NH.sub.2, NHC.sub.1-6 alkyl, NC.sub.1-6 alkyl, OCOC.sub.1-6alkyl, OCOC.sub.1-3 alkylaryl, A=S, 0 or NH X=H, C.sub.1-6 alkyl,C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen,amino, acylamido, and Z=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2,N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6alkyl , NR.sub.4 R.sub.5, NHCOR.sub.5, NHCO.sub.2 R.sub.6, whereinR.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.


Kuhar, MJ., Boja, JW., Carroll, F., Lewin, A., & Abraham, P. (1995). IPC No. U.S. Cocaine receptor binding ligands. (Patent No. 5380848).