neurotrophin antagoniste for treatment of epilepsy, alzheimer's disease and pain education

摘要

A pharmaceutical composition comprising a compound of Formula I wherein RSUP1 /SUPis selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(RSUP5/SUP)(RSUP6/SUP) wherein one of RSUP5 /SUPand RSUP6 /SUPis selected from H and and the other is selected from carboxy, carboxy-loweralkyl and lower alkoxycarbonyl; NHCHSUB2/SUBCHSUB2/SUBOX wherein X represents an in vivo hydrolyzable ester; and RSUP2 /SUPand RSUP3 /SUPare independently selected from H, NOSUB2/SUB, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S-, loweralkyl, and Z(O)ORSUP7 /SUPwherein Z is selected from C and S and RSUP7 /SUPis selected from H, lower alkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described. The compositions are useful to inhibit undesirable neurotrophin-mediated activity such as the neurite outgrowth that occurs in some neurodegenerative disease states.