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10,10-DIALKYL PROSTANOIC ACID DERIVATIVES AS AGENTS FOR LOWERING INTRAOCULAR PRESSURE
专利权人:
ALLERGAN; INC.
发明人:
DONDE YARIV,NGUYEN JEREMIAH H.
申请号:
SI200431931
公开号:
SI1608309T1
申请日:
2004.02.06
申请国别(地区):
SI
年份:
2012
代理人:
摘要:
The present invention relates to a method of making compounds of Formula V wherein part of the synthesis comprises reducing a compound of Formula VI to a compound of Formula VII in the presence of Bakers yeast wherein the dashed lines indicate the presence or absence of a bond, the hatched wedges indicate the ±(down) configuration, and the solid triangles indicate the ²(up) configuration B is a single, double, or triple covalent bond n is 0-6 X is CH 2 , S or O Y is any pharmaceutically acceptable salt of CO 2 H, CO 2 R, CONR 2 , CONHCH 2 CH 2 OH, CON(CH 2 CH 2 OH) 2 , CH 2 OR, P(O)(OR) 2 , CONRSO 2 R, SONR 2 , or R is H, C 1-6 alkyl or C 2-6 alkenyl R 2 and R 3 are C 1-6 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 5 is hydrogen or R and R 6 is i) hydrogen ii) 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 iii) aryloxy, heteroaryloxy, C 3-8 cycloalkyloxy, C 3-8 cycloalkyl, C 6-10 aryl or C 3-10 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, C 6-10 aryl, C 3-10 heteroaryl, aryloxy, heteroaryloxy, C 1-6 alkyl, OR, SR, and SO 2 R.
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