1-Phenyl-2-aminoethanol derivatives
AssigneeImperial Chemical Industries PLC
InventorGeraint Jones
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AssigneeImperial Chemical Industries PLC
InventorGeraint Jones
Estimating the term…
The invention concerns new topical anti-inflammatory 1-phenyl-2-aminoethanol derivatives of the general formula: R.sup.1 .multidot.CH(OH).multidot.CH.sub.2 NH.multidot.CR.sup.2 R.sup.3 .multidot.A.sup.1 .multidot.NH[CO.multidot.Y.multidot.NH].sub.n .multidot.Q wherein R.sup.1 is a phenyl bearing specific combinations of (2-12C)alkanoyloxy,[(2-12C)alkanoyloxy]methyl,chloro and amino substituents, R.sup.2 and R.sup.3 are independently hydrogen or (1-4C)alkyl, A.sup.1 is a (1-4C)alkylene, Y is a (1-4C)alkylene optionally bearing a (1-4C)alkyl or benzyl, n is an integer from 1 to 4, and Q is an optionally substituted benzoyl, phenylacetyl, or phenoxyacetyl together with the acid-addition salts thereof; and the pharmaceutical compositions thereof, for use in the treatment of inflammatory skin diseases and conditions. The invention also concerns processes for the manufacture of derivatives of formula I. A representative compound of the invention is 1-[3,4-bis(pivaloyloxy)phenyl]-2-{2-[(N-benzoylglycyl)amino]-1,1-dimethyl- ethylamino}ethanol.
A 1-phenyl-2-aminoethanol derivative of the formula:
A 1-phenyl-2-aminoethanol derivative selected from the group consisting of 1-[3,4-bis(pivaloyloxy)phenyl]-2-{2-[(N-benzoyl-glycyl)amino]-1,1-dimethyl ethylamino}ethanol, 1-[3,4-bis(pivaloyloxy)phenyl]-2-{2-[(N-phenylacetyl-glycyl)amino]-1,1-dim ethyl-ethylamino}ethanol, 1-[3,4-bis(pivaloyloxy)phenyl-2-{2-[(N-phenylacetylglycyl)glycyl-amino]-1, 1-dimethyl-ethylamino}ethanol, 1-(3,5-dichloro-4-aminophenyl)-2-{2-[(N-phenoxyacetyl-glycyl)amino]-1,1-di methyl-ethylamino}-ethanol, 1-(3,5-dichloro-4-aminophenyl)-2-{2-[(N-phenylacetyl-glycyl)glycyl-amino]- 1,1-dimethyl-ethylamino}-ethanol, and the pharmaceutically acceptable acid-addition salts thereof.
A method of treatment of an area of inflammation affecting the skin of a warm blooded animal which comprises topically administering to said area an effective amount of a compound of formula I, or a pharmaceutically acceptable acid-addition salt thereof:
Dependencies are inferred from the claim text.