Oculoselective beta-blockers as antiglaucoma agents

C - Chemistry – Metallurgy – 07 – C

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C07C 233/00 (2006.01) A61K 31/24 (2006.01) C07C 233/36 (2006.01) C07C 233/37 (2006.01) C07C 233/40 (2006.01) C07C 233/62 (2006.01) C07C 233/78 (2006.01) C07C 235/50 (2006.01) C07C 235/60 (2006.01) C07D 295/215 (2006.01) C07D 307/24 (2006.01) C07D 307/68 (2006.01)

Patent

CA 2005371

-33- TITLE OCULOSELECTIVE BETA-BLOCKERS AS ANTIGLAUCOMA AGENTS ABSTRACT OF THE DISCLOSURE In accordance with the present invention, disclosed herein are compounds of the formula Image wherein R is hydrogen, straight or branched loweralkyl, cycloalkyl, amino, loweralkoxy or acylamino, and R1 is straight or branched loweralkyl, amino, cyclohexyl, morpholino, piperidino, tetrahydrofuranyl, dihydrofuranyl, furanyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolidinyl, tetrahydrooxazolyl, and dihydrooxazolyl, R2 is hydrogen or -COR3 wherein R3 is straight or branched loweralkyl, provided, however, when R1 is loweralkyl or cyclohexyl, R2 is not hydrogen, and pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of glaucoma.

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