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

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

C - Chemistry, Metallurgy

07

D

260/301, 260/308

C07D 285/10 (2006.01) C07D 417/12 (2006.01)

Patent

CA 1230879

-1- ESTERS OF 3-(3-SUBSTITUTED-AMINO-2-HYDROXYPROPOXY)- 4-SUBSTITUTED-1,2,5-THIADIAZOLE DERIVATIVES Abstract of the Disclosure Novel compounds are disclosed having the formula Image 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; R1 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 -NR2COR3, -NR2CONR3R4, -NR2SO2R3, -NR2SO2NR3R4, or -NR2COOR5, where 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; 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.

443183

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