1208123-17-4Relevant articles and documents
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
Kallander, Lara S.,Washburn, David G.,Hoang, Tram H.,Frazee, James S.,Stoy, Patrick,Johnson, Latisha,Lu, Qing,Hammond, Marlys,Barton, Linda S.,Patterson, Jaclyn R.,Azzarano, Leonard M.,Nagilla, Rakesh,Madauss, Kevin P.,Williams, Shawn P.,Stewart, Eugene L.,Duraiswami, Chaya,Grygielko, Eugene T.,Xu, Xiaoping,Laping, Nicholas J.,Bray, Jeffrey D.,Thompson, Scott K.
scheme or table, p. 371 - 374 (2010/04/24)
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 in