| 摘要 |
A process for preparing arylethanoldiamines of Formula (IA) or a pharmaceutically acceptable salt thereof: (see formula IA) R1 represents an aryl or phenoxymethyl group, optionally substituted by one or more substituents; R2 represents hydrogen or C1-6alkyl; R3 represents hydrogen or C1-6alkyl; X1 and X2 independently represent (a) hydrogen, (b) C1-6alkylCO, or (c) an aryl CO group optionally substituted, with the proviso that when one is (b) or (c) the other is hydrogen (a); R4 represents a group (W): (see formula W) wherein A represents aryl or heteroaryl groups; R5 represents cyano, tetrazol-5-yl, -CO2H or --CO2R8; R6 and R7 independently represent hydrogen, C1-6alkyl, -CO2H, -CO2R8, cyano, tetrazol-5-yl, halogen, trifluoromethyl or C1-6alkoxy, or when R6 and R7 are bonded to adjacent carbons, may be fused 5- or 6- membered ring; each R12 independently represents substituents; and n represents an integer from 0-4; and R8 and R9 independently represent C1-6alkyl. Compounds (IA) are agonists at atypical beta-adrenoceptors. |
