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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:
EP10178294.4
公开号:
EP2263674B1
申请日:
2004.02.06
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
The present invention relates to a method of making compounds of Formula Vwherein part of the synthesis comprises reducing a compound of Formula VI to a compound of Formula VII in the presence of Bakers yeastwherein the dashed lines indicate the presence or absence of a bond, the hatched wedges indicate the α(down) configuration, and the solid triangles indicate the β(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, CO2R, CONR2, CONHCH2CH2OH, CON(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, orR 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 attachedR5 is hydrogen or R andR6 isi) hydrogenii) 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 oriii) 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.
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