| 摘要 |
<p>A compound of Formula (I), wherein R1 represents hydrogen, C¿1?-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, or (CH2)nAr; W represents C(O), C(O)O, C(O)NR?6¿, or a bond; R2 represents hydrogen, Ar, or (CH¿2?)pCH[(CH2)qR?7](CH¿2)tR8; or together R?2 and R6¿ represent (CH¿2?)jY(CH2)k; R?3 and R5¿ independently represent hydrogen, halogen, or C¿1?-C4 alkyl; X represents oxygen, or NH; R?4¿ represents hydrogen, C¿1?-C4 alkyl(CH2)uAr, R?9¿CO, or R9SO2; R6 represents hydrogen, C¿1?-C4 alkyl, aryl or heteroaryl, or together R?2 and R6¿ represent (CH¿2?)jY(CH2)k; R?7 and R8¿ independently represent hydrogen, halogen, CN, -C CH, N¿3?, CF3, NO2, Ar, OR?10, NR10R11¿, C(O)OR10, OC(O)R10, C(O)NR?10R11, NR10C(O)R11, SO¿2NR?10R11, or NR10SO¿2R11; R9 represents C¿1?-C4 alkyl, or Ar; Ar represents phenyl, naphthyl, or a 5- or 6-membered heterocyclic ring containing 0-3 nitrogens, 0-1 sulfurs and 0-1 oxygens; Ar is optionally substituted with one or more substituents independently selected from: hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, (CH2)naryl, CN, NO2, CF3, OR?12, NR12R13¿ and COOR?12; R10, R11, R12 and R13¿ independently represent hydrogen, C¿1?-C4 alkyl, aryl, or heteroaryl; or together R?10 and R11¿ and/or R?12 and R13¿ independently represent (CH¿2?)jY(CH2)k; Y represents oxygen, sulfur, NR?14¿, or a bond; j is 2-4; k, m, n, p, q, t and u are independently 0-2; R14 represents hydrogen, C¿1?-C4 alkyl, aryl or heteroaryl; or an enantiomer thereof,and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission. The compounds of the invention enhance the efficacy of agonists at nicotinic receptors.</p> |
