Labile ketone derivatives of 3-substituted-1-alkylamino...

C - Chemistry – Metallurgy – 07 – C

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C07C 251/40 (2006.01) A61K 31/15 (2006.01) C07C 251/38 (2006.01) C07D 215/227 (2006.01) C07D 285/10 (2006.01) C07D 413/04 (2006.01)

Patent

CA 1335286

Compounds having the formula Image (I) and their pharmaceutically acceptable acid addition salts, wherein -X- is -O-, -CH2- or -; =Y is =O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms, the aralkyl group optionally bearing methoxy substituents on the aryl portion thereof; and Ar is the 3-aromatic or heterocyclic residue of a 1- alkylamino-2-propanol having an optionally substituted 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 for ophthalmic use in the treatment of glaucoma or for lowering intraocular pressure.

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