1-phenyl-2-aminoethanol derivatives

Details 1-phenyl-2-aminoethanol derivatives 1-phenyl-2-aminoethanol derivatives

C - Chemistry, Metallurgy

07

K

530/5.06, 260/55

C07K 5/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1137978

ABSTRACT The invention concerns new topical anti- inflammatory 1-phenyl-2-aminoethanol derivatives of the general formula:- R1.CH(OH).CH2NH.CR2R3.A1.NH[CO.Y.NH]n.Q wherein R1 is a phenyl bearing specific combinations of (2-12C)alkanoyloxy,[(2-12C)alkanoyloxy]methyl,chloro and amino substituents, R2 and R3 are independently hydrogen or (1-4C)alkyl, A1 is a (1-4C)alkylene, Y is a (1-4C)alkyene optionally bearing a (1-4C)alkyl or benzyl, n is an integer from 1 to 4, and Q is an opeionally substituted benzoyl, phenylacetyl, or phenoxyacetyl together with the acid-addition salts thereof; and the pharmaceutical compositions thereor, 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-benzoyl- glycyl)amino]-l,l-dimethyl-ethylamino}ethanol.

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