Next-generation contraceptives: The discovery of non-steroidal progesterone receptor modulators

MEDI 18

Andrew Fensome, fensoma@wyeth.com1, Andrea Adams2, William Adams2, Reinhold Bender1, Thomas Berrodin3, Rajiv Chopra1, Jeff Cohen3, Mark A. Collins1, Lin Deng2, Horace Fletcher III1, Phyllis Gallucci4, Valerie Hudak1, Christine Huselton2, Susan Lockhead2, Karl Malakian1, Michael Marella, marellm@wyeth.com1, Edward Melenski, melense@wyeth.com1, Casey C. McComas, mccomac@wyeth.com1, Cheryl Mugford2, Layne Norlund4, Andrea Olland1, David Ruble4, Louise Russo3, Ov Slayden5, Kristine Svenson1, Eugene A. Terefenko, terefee@wyeth.com1, Raymond Unwalla1, Jianyao Wang2, James Wilhelm1, Scott Wolfrom1, David Yates4, Matthew Yudt3, Zhiming Zhang3, Puwen Zhang, zhangp@wyeth.com1, Richard C. Winneker3, and Jay Wrobel1. (1) Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, (2) Biotransfomation Division, Drug Safety and Metabolism, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, (3) Women's Health and Musculoskeletal Biology, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, (4) BioResources, Wyeth Research, 500 Arcola Road, Collegeville, PA, (5) Division of Reproductive Sciences, Oregon National Primate Research Center, Oregon Health and Science University, Beaverton, OR
Oral contraceptives (OC) have been widely used for the past four decades; however, currently available therapies are not appropriate for all women. Contraindication, due to the small increased risk of thromboembolism for example, prevents some women from starting on these therapies; still others who begin using OC's discontinue their use due to hormonal side effects, commonly associated with the estrogenic component of the drug regimen. Hence there is still a need to provide improved medications for wider general use than the currently available OC's.

We have pursued the discovery of non-steroidal progesterone receptor (PR) modulators as a single therapeutic agent with potential for use in contraception and reproductive disorders. Several of these compounds have moved into development, including Tanaproget, the first non-steroidal PR modulator studied in the clinic.

This talk will focus on the discovery, SAR and pharmacological characterization of PR modulators, including both agonists and antagonists, which have progressed into the Development Pipeline at Wyeth for use in contraception.

 

Medicinal Chemistry Award Symposium
1:30 PM-4:20 PM, Sunday, August 19, 2007 BCEC -- 210B, Oral

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007