Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372496 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The basic pyrrolidine amine was intentionally converted to a sulfonamide, carbamate, or amide to address these liabilities. The evaluation of the degree of partial agonism for these non-basic pyrrolidine derivatives and demonstration of their efficacy in an in vivo model of endometriosis is disclosed herein.
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Organic Chemistry
Authors
Lara S. Kallander, David G. Washburn, Tram H. Hoang, James S. Frazee, Patrick Stoy, Latisha Johnson, Qing Lu, Marlys Hammond, Linda S. Barton, Jaclyn R. Patterson, Leonard M. Azzarano, Rakesh Nagilla, Kevin P. Madauss, Shawn P. Williams,