| 摘要 |
The invention concerns compounds of the formula:- R1.CH(OH).CH2NH.CR2R3.A1. NH.CO.CHR4.A2.NR5. Q I wherein R1 is 3,4-bis[(3-8C)alkanoyloxy]-phenyl, 3,5- bis [(3-8C)alkanoyloxy]phenyl, 3-[(3-8C)alkanoyloxy]methyl-4-[(3-8C)alkanoyloxy]phenyl, 4-[(3-8C)alkanoyloxy]phenyl, 2-chlorophenyl or 3,5-dichloro-4-aminophenyl; R2 and R3 are independently hydrogen or (1-4C) alkyl; A1 is (1-4C) alklylene; A2 is a direct bond or (1-4C) alkylene; R4 is hydrogen, (1-6C)alkyl, phenyl-(1-4C)alkyl or halogenophenyl-(1-4 C)alkyl; and R5 is (1-6C)alkyl; or R4 and R5 together form (2-5C) alkylene; and Q is (3-12C) alkanoyl, [(3-6C)alkoxy]carbonyl, phenylacetyl, phenoxyacetyl, benzoyl or benzyloxycarbonyl, the phenyl rings of which may optionally bear a substitutent selected from halogeno, (1-4C)alkyl, (1-4C)alkoxy and trifuloromethyl; and the pharmaceutically acceptable acid-addition salts thereof; processes for their manufacture; and pharmaceutical compositions thereof. The compounds of formula I are topical anti-inflammatory agents. A representative compound is 1-[3,4-bis (pivaloyloxy)phenyl]-2-{2-[(N-phenylacetyl-proyly)amino]-1,1-dimethyl- ethylamino}ethanol. |
