Labile derivatives of ketone analogs of 3-substituted-1-alkylami

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

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5142362, 514312, 514415, 514439, 514467, 514469, 514470, 514524, 514546, 514597, 514620, 514625, 514630, 514639, 514651, 544134, 546158, 549466, 549468, 549450, 549451, 549 30, 548182, 548146, 548200, 548201, 548503, 558422, 560142, 564 51, 564165, 564220, 564251, 564256, 564257, 564258, 564265, 564344, A61K 3115, C07C25138

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050176188

ABSTRACT:
Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.

REFERENCES:
patent: 4521414 (1985-06-01), Chiou et al.
Bodor et al, J. Med. Chem., vol. 31, No. 1, 1988, 100-106.
Ahmed et al, J. Pharm. Belg. 37(3), 214-217 (1982), abstracted in Chem. Abstracts, vol. 97, 188158n (1982).
Gnit'ko et al, Zh. Evol Biokhim Fiziol., 1972, 8(2), 194-201, abstracted in Chem. Abstracts, vol. 77, 70809j (1972).

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