C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/292, 260/325
C07D 207/16 (2006.01) C07D 205/04 (2006.01) C07D 211/60 (2006.01)
Patent
CA 1149804
ABSTRACT The invention concerns compounds of the formula:- R1.CH(OH).CH2NH.CR2R3.A1.NH.CO.CHR4.A2.NR .Q I wherein R1 is 3,4-bis[(3-8C)alkanoyloxy]-phenyl, 3,5- 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)alkylene; A2 is a direct bond or (1-4C)- alkylene; R4 is hydrogen,(1-6C)alkyl, phenyl-(1-4C)alkyl or halogenophenyl-(1-4C)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, phenoxy- acetyl, benzoyl or benzyloxycarbonyl, the phenyl rings of which may optionally bear a substituent selected from halogeno, (1-4C)alkyl, (1-4C)alkoxy and trifluoromethyl; 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 compounds is 1-[3,4- bis(pivaloyloxy)phenyl]-2-{2-[(N-phenylacetyl-prolyl)- amino]-1,1-dimethyl-ethylamino}ethanol.
351309
Imperial Chemical Industries Limited
Smart & Biggar
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