Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...
Patent
1980-05-06
1982-04-06
Milestone, Norma S.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Parasitic organism or component thereof or substance...
260239A, 2603264, 546226, 424274, C07D20504, C07D20716, C07D21160, C07D21162, A61K 31395, A61K 3140, A61K 31445
Patent
active
043235751
ABSTRACT:
The invention concerns compounds of the formula:- R.sup.1.CH(OH).CH.sub.2 NH.CR.sup.2 R.sup.3.A.sup.1. NH.CO.CHR.sup.4.A.sup.2.NR.sup.5. Q I wherein R.sup.1 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; R.sup.2 and R.sup.3 are independently hydrogen or (1-4C) alkyl; A.sup.1 is (1-4C) alklylene; A.sup.2 is a direct bond or (1-4C) alkylene; R.sup.4 is hydrogen, (1-6C)alkyl, phenyl-(1-4C)alkyl or halogenophenyl-(1-4 C)alkyl; and R.sup.5 is (1-6C)alkyl; or R.sup.4 and R.sup.5 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-ethy lamino}ethanol.
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patent: 3639476 (1972-02-01), Eberle et al.
patent: 3933911 (1976-01-01), Main
patent: 3944611 (1976-03-01), Smith
patent: 3957870 (1976-05-01), Main
patent: 4041075 (1977-08-01), Smith
patent: 4211878 (1980-07-01), Smith
Imperial Chemical Industries Limited
Milestone Norma S.
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