Discovery of (3 S, 3a R)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3, 3a, 4, 5-tetrahydro-2 H-benzo [g] indazole-7-carboxylic Acid (PF-3882845), an Orally Efficacious …

MJ Meyers, GB Arhancet, SL Hockerman…

Index: Meyers, Marvin J.; Arhancet, Graciela B.; Hockerman, Susan L.; Chen, Xiangyang; Long, Scott A.; Mahoney, Matthew W.; Rico, Joseph R.; Garland, Danny J.; Blinn, James. R.; Collins, Joe T.; Yang, Shengtian; Huang, Horng-Chih; McGee, Kevin F.; Wendling, Jay M.; Dietz, Jessica D.; Payne, Maria A.; Homer, Bruce L.; Heron, Marcia I.; Reitz, David B.; Hu, Xiao Journal of Medicinal Chemistry, 2010 , vol. 53, # 16 p. 5979 - 6002

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Citation Number: 59

Abstract

We have discovered a novel class of nonsteroidal pyrazoline antagonists of the mineralocorticoid receptor (MR) that show excellent potency and selectivity against other nuclear receptors. Early analogues were poorly soluble and had a propensity to inhibit the ...