摘要 |
<p>A compound of Formula (I), wherein R1 represents hydrogen, C1 C4 alkyl, C2 C4 alkenyl, C2 C4 alkynyl, or (CH2)nAr; W represents C(O), C(O)O, C(O)NR6, or a bond; R2 represents hydrogen, Ar, or (CH2)pCH[(CH2)qR7](CH2)tR8; or together R2 and R6 represent (CH2)jY(CH2)k; R3 and R5 independently represent hydrogen, halogen, or C1 C4 alkyl; X represents oxygen, or NH; R4 represents hydrogen, C1 C4 alkyl(CH2)uAr, R9CO, or R9SO2; R6 represents hydrogen, C1 C4 alkyl, aryl or heteroaryl, or together R2 and R6 represent (CH2)jY(CH2)k; R7 and R8 independently represent hydrogen, halogen, CN, Cequiv;CH, N3, CF3, NO2, Ar, OR10, NR10R11, C(O)OR10, OC(O)R10, C(O)NR10R11, NR10C(O)R11, SO2NR10R11, or NR10SO2R11; R9 represents C1 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, OR12, NR12R13 and COOR12; R10, R11, R12 and R13 independently represent hydrogen, C1 C4 alkyl, aryl, or heteroaryl; or together R10 and R11 and or R12 and R13 independently represent (CH2)jY(CH2)k; Y represents oxygen, sulfur, NR14, or a bond; j is 2 4; k, m, n, p, q, t and u are independently 0 2; R14 represents hydrogen, C1 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> |