85515-51-1Relevant academic research and scientific papers
2-hydroxypropylamine heteroaryl ester derivatives
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, (2008/06/13)
The present invention relates to compounds of the general formula STR1 wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR2 COR1, --NR2 CONR1 R3, --NR2 SO2 R1, NR2 SO2 NR1 R3, or --NR2 COOR1, wherein R1, R2 and R3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R1 is not hydrogen when B is --NR2 SO2 R1 or --NR2 COOR1, or R1 and R3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.
AROMATIC AND ESTERS OF HYDROXYPROPYLAMINES
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, (2008/06/13)
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 2 COR 1,--NR 2 CONR 1 R 3,--NR 2 SO 2 R. sub.1,--NR 2 SO 2 NR 1 R 3, or--NR 2 COOR 1 wherein R. sub.1, R 2 and R 3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R 1 is not hydrogen when B is--NR 2 SO 2 R 1 or--NR 2 COOR 1, or R 1 and R 3 may together with N form a 5 to 7 momoered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit β-adrenergic blocking activity and are also useful in the treatment of glaucoma.
propanolamines. 1. Novel β-Blockers with Ultrashort Duration of Action
Kam, Sheung-Tsam,Matier, William L.,Mai, Khuong X.,Barcelon-Yang, Cynthia,Borgman, Robert J.,et al.
, p. 1007 - 1016 (2007/10/02)
Novel propanolamines were synthesized and investigated as potential ultrashort-acting β-adrenergic receptor blockers.Many of these analogues exhibited good potency and short duration.The N-ureidoalkyl analogue 85 (ACC-9089) has a potency equal to propranolol and a duration of action of about 21 min in the dog.It has been selected as a candidate for further clinical study.Structure-activity relationships and structure-duration relationships for these new β-blockers are also discussed.
Method for treating glaucoma by the topical administration of selectively metabolized beta-blocking agents
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, (2008/06/13)
A method for the treatment of glaucoma or lowering intraocular pressure in a mammal, involving topically administering to the eye of such mammal a selectively metabolized beta-blocking compound of the formula STR1 wherein R may be lower alkyl, lower hydroxyalkyl, lower alkynyl, aralkyl, or an ester-containing group and Ar may be substituted or unsubstituted aromatic; or a pharmaceutically acceptable salt thereof. Because of a relatively long duration of action of such compounds in ocular fluids and a relatively short duration of action in the systemic circulation, such compounds are useful for the treatment of excessive intraocular pressure without substantial systemic effects.
