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10,10-DIALKYL PROSTANOIC ACID DERIVATIVES AS AGENTS FOR LOWERING INTRAOCULAR PRESSURE
专利权人:
发明人:
申请号:
HK11112208.0
公开号:
HK1157771A
申请日:
2011.11.11
申请国别(地区):
HK
年份:
2012
代理人:
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 chemistry chemdraw filechemistry mol filewherein the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the &agr (down) configuration, and the solid triangle indicates the &bgr (up) configurationB is a single, double, or triple covalent bondn is 0-6X is CH2, S or OY is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or chemistry chemdraw filechemistry mol fileR is H, C1-6 alkyl or C2-6 alkenylR2 and R3 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 attachedR4 is hydrogen, R, C(&boxHO)R, or any group that is easily removed under physiological conditions such that R4 is effectively hydrogenR5 is hydrogen or RR6 isiv) hydrogenv) 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 orvi) 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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