摘要 |
Acetamide derivatives of formula (I) and their salts are new. R = phenyl optionally substituted by 1 or more A; A = halo, NO2, OH, lower alkoxy, lower alkyl or lower haloalkyl; R1 = aryl, heteroaryl, 1-6C alkyl or 3-6C cycloalkyl all optionally substituted by 1 or more A, 1 or more B or 1 or more G; B = ORa, COORa, CONRbR6, NRbRc, NRbCHO, NRbCORa, SO2Ra, SO2ORa, CONRbSO2Ra or P(O)(ORa)2; Ra-Rc = H, Alk, Ar-1-7C alkyl, Het-1-7C alkyl, Ar or Het; Ar = aryl optionally substituted by 1 or more A; Het = heteroaryl optionally substituted by 1 or more A; Alk = lower alkyl optionally substituted by 1 or more halo, NO2 or OH; G = 5 or 6 membered heterocyclyl containing 1-3 O or N and optionally substituted by 1 or more A; R2 = 1-8C alkyl (optionally substituted by B or G), aryl-17C alkyl heteroaryl-1-7C alkyl or aryl; R3 = H, D(CH2)nCO, DCOECO, DSO2ECO, D(CH2)n SO2, DCOESO2, RbRcNCO RbRcNCS or Ra; D =, 1-6C alkyl, 3-6C cycloalkyl, aryl, lower haloalkyl, lower haloalkoxy, amino, lower alkoxyamino, lower haloalkylamino, RbRcN, RbRcNO, RaO, Ra, RaOCO, RbRcNCO, RaSO2NRb, RaS or G; E = 1-6C divalent group; X, Y = N or C optionally substituted by Ra-Rc; Z = polymethylene optionally substituted by Ra-Rc. |