申请人:Pfizer Inc.
公开号:US06300363B1
公开(公告)日:2001-10-09
This invention provides a compound of the following formula:
and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4 alkylidene; Q is C1-6 alkyl, C3-7 cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1 is hydrogen, C1-6 alkyl or the like; R2 is hydrogen, C1-4 alkyl, C(O)R5 wherein R5 is C1-22 alkyl or C2-22 alkenyl, halosubstituted C1-8 alkyl, halosubstituted C2-8alkenyl, —Y—C3-7 cycloalkyl, —Y—C3-7 cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4 alkyl, hydroxy, C1-4 alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula —Y—Q is not methyl or ethyl when X is hydrogen; L is oxygen; R1 is hydrogen; and R2 is acetyl.
This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.
这项发明提供了以下公式的化合物及其药物可接受的盐,其中L为氧或硫;Y为直接键或C1-4烷基亚甲基;Q为C1-6烷基,C3-7环烷基,苯基,萘基,杂环芳基或类似物;R1为氢,C1-6烷基或类似物;R2为氢,C1-4烷基,C(O)R5,其中R5为C1-22烷基或C2-22烯基,卤素取代的C1-8烷基,卤素取代的C2-8烯基,-Y-C3-7环烷基,-Y-C3-7环烯基,苯基,萘基,杂环芳基或类似物;X为卤素,C1-4烷基,羟基,C1-4烷氧基或类似物;n为0,1,2或3,但当X为氢时,公式-Y-Q的基团不是甲基或乙基;L为氧;R1为氢;R2为乙酰基。这项发明还提供了一种制备用于治疗前列腺素作为病原体的医疗状况的药物组合物。