| 摘要 |
Aralkylamine derivatives of formula (I) and their salts are new: A1 = CH2R6, OR6, NR6R7, SOeR13, (CR6R7)qOR6, (CR6R7)qNR6R7 or (CR6R7)qSOeR13; q = 1-6; A2 = H; or A1+A2 = O, CR6R7, NOR6 or S; Q = R5-phenyl, R5-naphthyl, SR6, NR6R7, OR6 or R5-heteroaryl; T = H, R4-aryl, R4-heterocycloalkyl, R4-heteroaryl, R4-cycloalkyl or R10-bridged cycloalkyl; b = 0-2; b1 = 1-2; X = a bond, CO, O, NR6, SOe, NR6CO, CONR6, OC(O)NR6, OC(S)NR6, NR6C(S)O, C(=NOR6), SO2NR6, NR6SO2, NR6CO2 or OC(O); R4, R5 = 1-3 of H, halo, OR6, OC(O)R6, OC(O)NR6R7, NR6R7, 1-6C alkyl, CF3, C2F5, COR6, CO2R6, CONR6R7, SOeR13, CN, OCF3, NR6CO2R16, NR6COR7, NR8CONR6R7, R15-phenyl, R15-benzyl, NO2, NR6SO2R13 or SO2NR6R7; or adjacent R4 substituents or adjacent R5 substituents can form OCH2O; or R4 = R15-heteroaryl; R6, R7, R8, R8a, R13 = H, 1-6C alkyl, 2-6C hydroxyalkyl, 1-6C alkoxy-1-6C alkyl, R15-phenyl or R15-benzyl or NR6R7 = 5-6 membered ring containing 1-2 of O, S and/or NR19; R9, R9a = R6 or OR6; provided that when R9 = OH, then X = a bond, CO, NR6CO or C(=NOR6); R10 = H or 1-6C alkyl; R15 = 1-3 of H, 1-6C alkyl, 1-6C alkoxy, 1-6C alkylthio, halo, CF3, C2F5, COR10, CO2R10, CON(R10)2, SOeR10, CN, N(R10)COR10, N(R10)CON(R10)2 or NO2; R16 = 1-6C alkyl, R15-phenyl or R15-benzyl; R19 = H, 1-6C alkyl, CON(R10)2, CO2R10, (CR8R9)fCO2R10 or (CR8R9)uC(O)N(R10)2; f = 1-6; u = 0-6; Z = a group of formula (a)-(c): g, j = 0-3; h, k = 1-4, provided that h +g = 1-7; J = (H, H), O, S, NR9 or NOR9; L, L1 = H, 1-6C alkyl, 1-6C alkenyl, CH2-cycloalkyl, R15-benzyl, R15-heteroaryl, COR6, (CH2)mOR6, (CH2)mNR6R7, (CH2)mCO2R6 or (CH2)mCONR6R7; m = 0-4; provided that when j = 0 then m = 1-4; R25 = H, 1-6C alkyl, CN, R15-phenyl or R15-benzyl; R26, R27 = H, 1-6C alkyl, R4-aryl or R4-heteroaryl or R26 = H, 1-6C alkyl, R4-aryl or R4-heteroaryl and R27 = COR6, CONR6R7, COR4-aryl, COR4-heteroaryl, SO2R13 or SO2R4-aryl; R28 = H, (CR6R19)tG or (CR6R7)vG2; t, v = 0-3; provided that when j = 0 then t = 1-3; R29 = H, 1-6C alkyl, C(R10)2SOeR6, R4-phenyl or R4-heteroaryl; G = H, R4-aryl, R4-heterocycloalkyl, R4-heteroaryl, R4-cycloalkyl, OR6, NR7R6, COR6, CO2R6, CONR7R9, SOeR13, NR6CO2R16, NR6COR7, NR8CONR6R7, NR6SO2R13, SO2NR6R7, OC(O)R6, OC(O)NR6R7, C(=NOR8)NR6R7, C(=NR25)NR6R7, NR8C(=NR15)NR6R7, CN, C(O)NR6OR7 or C(O)N(R9)-(R4-heteroaryl), provided that when n = 1 and u = 0 or when R9 = OR6 then G is not OH or NR6R7 and G2 = R4-aryl, R4-heterocycloalkyl, R4-heteroaryl, R4-cycloalkyl, COR6, CO2R16, SO2NR6R7 or CONR6R7. 15 Compounds (I) are specifically claimed e.g: N-(2-(3,4-dichlorophenyl)-3-hydroxy-4-(4-hydroxy-4-phenyl-1-piperidinyl)butyl)-N-methyl benzamide. |
