| 摘要 |
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the alpha (down) configuration, and the solid triangle indicates the beta (up) configuration; B is a single, double, or triple covalent bond; n is 0-6; X is CH2, S or O; Y is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl or C2-6 alkenyl; R<2 >and R<3 >are C1-6 linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached; R<4 >is hydrogen, R, C(=O)R, or any group that is easily removed under physiological conditions such that R<4 >is effectively hydrogen; R<5 >is hydrogen or R; R<6 >is iv) hydrogen; v) a linear or branched hydrocarbon containing between 1 and 8 carbon atoms, which may contain one or more double or triple bonds, or oxygen or halogen derivatives of said hydrocarbon, wherein 1-3 carbon or hydrogen atoms may be substituted by O or a halogen; or vi) aryloxy, heteroaryloxy, C3-8 cycloalkyloxy, C3-8 cycloalkyl, C6-10 aryl or C3-10 heteroaryl, wherein one or more carbons is substituted with N, O, or S; and which may contain one or more substituents selected from the group consisting of halogen, trihalomethyl, cyano, nitro, amino, hydroxy, C6-10 aryl, C3-10 heteroaryl, aryloxy, heteroaryloxy, C1-6 alkyl, OR, SR, and SO2R. Some of the compounds of the present invention and some of their methods of preparation are also novel an nonobvious.
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