Aromatic and esters of hydroxypropylamines

Details Aromatic and esters of hydroxypropylamines Aromatic and esters of hydroxypropylamines

1981-11-12

1986-04-15

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

560110, 560 24, 560 10, 560 20, 560 49, 560 56, 560 67, 560 74, 560100, 560146, 560196, 560160, 549 65, 549 66, 549 68, 549 69, 548337, 548225, 548233, 548469, 548538, 548542, 546245, 546248, 544383, 544390, 544160, 544176, 544 581, 544 584, 514522, 514533, 514535, 514540, 514534, 514478, 514481, 514482, 564 48, 564 59, 564 90, 564 94, 514486, 558416, C07C 6976, C07C12506, C07D33332, C07D33336

Patent

active

045828555

ABSTRACT:
Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 momoered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.

REFERENCES:
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patent: 3501769 (1970-03-01), Crowther et al.
patent: 4387103 (1983-06-01), Erhardt et al.
patent: 4405642 (1983-09-01), Kam et al.
Gorczynski; R. F., Cardiovascular Pharmacology of ACC 9089, (unpublished).
Tatsuno et al., J. Med. Chem., vol. 20, No. 3, pp. 394-397, (1977).
Howe, J. Med. Chem., vol. 11, pp. 1000-1008, 1968.
Frishman, W. H., Amer. Heart Journal, 99, 528-536, (1980).
Kenakin, T., Can. J. Physiol. Pharmacol., vol. 60, p. 249, 1982.

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