Antiglaucoma agents

A - Human Necessities – 61 – K

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A61K 31/33 (2006.01) C07D 491/18 (2006.01)

Patent

CA 1084841

ANTIGLAUCOMA AGENTS Abstract of the Disclosure A method of reducing intra-ocular pressure in mammalian patients comprising administering to a glaucoma patient a therapeutically effective amount of a compound of the formula Image Image wherein, in the C ring, X is CH2, S, or NR4 where R4 is H, loweralkyl, loweralkenyl, loweralkynyl or loweralkanoyl; n is an integer of 0 to 3; m is an integer of 0 to 3, or the C ring is a quinuclidine ring Image ; each R1 is loweralkyl, and when taken together, the substituents R1R1 form oxygen; R2 is a C1-C20 straight or branched chain alkyl, cycloalkyl, or Image wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms, and each R5, R6 and R7 are the same or different members of the group consisting of H, halo or loweralkyl; R3 is H or Image wherein Y' is a straight or branched chain alkylene group having 1 to 8 carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH2, O, S or NR9 where Rg is H or loweralkyl, with the provision that when Z is 0, S or NR9, the sum of a and b is 3 or 4, and R8 is H or lower- alkyl; and the pharmaceutically acceptable salts thereof. -2-

283535

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