- Novel progesterone receptor modulators: 4-Aryl-phenylsulfonamides
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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 Ame
- McComas, Casey,Cohen, Jeffrey,Huselton, Christine,Marella, Michael,Melenski, Edward,Mugford, Cheryl,Slayden, Ov,Winneker, Richard,Wrobel, Jay,Yudt, Matthew R.,Fensome, Andrew
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p. 7119 - 7122
(2013/01/15)
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- Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)- 1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348)
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We have continued to explore the 3,3-dialkyl-5-aryloxindole series of progesterone receptor (PR) modulators looking for new agents to be used in female healthcare: contraception, fibroids, endometriosis, and certain breast cancers. Previously we reported
- Fensome, Andrew,Adams, William R.,Adams, Andrea L.,Berrodin, Tom J.,Cohen, Jeff,Huselton, Christine,Illenberger, Arthur,Kern, Jeffrey C.,Hudak, Valerie A.,Marella, Michael A.,Melenski, Edward G.,McComas, Casey C.,Mugford, Cheryl A.,Slayden, Ov D.,Yudt, Matthew,Zhang, Zhiming,Zhang, Puwen,Zhu, Yuan,Winneker, Richard C.,Wrobel, Jay E.
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p. 1861 - 1873
(2008/12/20)
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- Cyanopyrrole-phenyl progesterone receptor modulators and uses thereof
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Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein. These compounds are us
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Page/Page column 11
(2008/06/13)
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- Use of progesterone receptor modulators
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The use of compounds of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7, are as defined herein, for contraception, hormone replace
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Page/Page column 15
(2010/11/25)
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- Progesterone receptor modulators comprising pyrrole-oxindole derivatives and uses thereof
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Pyrrole-oxindole derivatives useful as progesterone receptor antagonists are provided. Pharmaceutical compositions containing these derivatives are described, as is the use thereof in contraception and hormone-related conditions.
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Page/Page column 8
(2010/02/15)
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- COUPLING PROCESS FOR GENERATING REACTIVE BORON- CONTAINING DERIVATIVES OF N-SUBSTITUTED PYRROLE-2- CARBONITRILES TO PRODUCE BIARYLS
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A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.
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Page/Page column 24
(2008/06/13)
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