Esters of aryloxypropanolamine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/477, 260/387

C07D 295/20 (2006.01) C07C 275/14 (2006.01) C07C 275/28 (2006.01) C07D 285/10 (2006.01) C07D 295/215 (2006.01) C07D 303/22 (2006.01) C07D 333/34 (2006.01) C07D 333/38 (2006.01)

Patent

CA 1201437

Abstract of the Disclosure Novel compounds of the general formula Image wherein R1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxy- methyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the Image group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic sub- stituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is -NR2COR3, -NR2CONR3R4, -NR2SO2R3, -NR2SO2NR3R4, or -NR2COOR5, wherein R2, R3, R4 and R5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R3 and R5 are not hydrogen when B is -NR2SO2R3 or -NR2COOR5, or R3 and R4 may together With N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds have .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.

415312

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