Esters of 3-(3-substituted-amino-2-hydroxypropoxy)-4-substituted

Details Esters of 3-(3-substituted-amino-2-hydroxypropoxy)-4-substituted Esters of 3-(3-substituted-amino-2-hydroxypropoxy)-4-substituted

1982-12-22

1985-04-02

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548135, C07D28510, A61K 3141

Patent

active

045087253

ABSTRACT:
Novel compounds are disclosed having the formula ##STR1## wherein R is lower alkyl, lower cycloalkyl, lower haloalkyl, lower alkylcarboxymethyl, arylcarboxymethyl, lower alkenyl, lower alkynyl, aryl having from 6 to about 10 carbon atoms, or aralkyl; R.sub.1 is lower alkyl, lower hydroxyalkyl, lower alkenyl, lower alkynyl, aralkyl, or --WB; where W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.2 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group; A is a direct bond, lower alkylene, or lower alkene having from 1 to about 10 carbon atoms; and the pharmaceutically acceptable salts thereof. These compounds are useful as .beta.-adrenergic blocking agents and for the treatment of glaucoma.

REFERENCES:
patent: 3655663 (1972-04-01), Wasson
patent: 3729469 (1973-04-01), Wasson
patent: 3729477 (1973-04-01), Wasson
patent: 3891639 (1975-06-01), Wasson
patent: 4011217 (1977-03-01), Wasson
patent: 4051144 (1977-09-01), Weinstock et al.
patent: 4076939 (1978-02-01), Belanger
patent: 4127674 (1978-11-01), Leopold

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