Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.

Casey McComas,Jeffrey Cohen,Christine Huselton,Michael Marella,Edward Melenski,Cheryl Mugford,Ov Slayden,Richard Winneker,Jay Wrobel,Matthew R Yudt,Andrew Fensome

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

We have developed a new series of progesterone receptor modulators based upon the 4-aryl-phenylsulfonamide. Initial work in the series afforded potent compounds with good properties, however an advanced intermediate proved to be genotoxic in a non-GLP Ames assay following metabolic activation. We subsequently solved this problem and identified advanced leads which demonstrated oral efficacy in rhesus monkey pharmacodynamic and kinetics models.

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关键词

Progesterone modulator,Progesterone antagonist,Endometriosis,Uterine fibroids

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