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Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
Meyers MJ, Arhancet GB, Hockerman SL, Chen X, Long SA, Mahoney MW, Rico JR, Garland DJ, Blinn JR, Collins JT, Yang S, Huang HC, McGee KF, Wendling JM, Dietz JD, Payne MA, Homer BL, Heron MI, Reitz DB, Hu X. Meyers MJ, et al. Among authors: yang s. J Med Chem. 2010 Aug 26;53(16):5979-6002. doi: 10.1021/jm100505n. J Med Chem. 2010. PMID: 20672822
Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design.
Walker DP, Arhancet GB, Lu HF, Heasley SE, Metz S, Kablaoui NM, Franco FM, Hanau CE, Scholten JA, Springer JR, Fobian YM, Carter JS, Xing L, Yang S, Shaffer AF, Jerome GM, Baratta MT, Moore WM, Vazquez ML. Walker DP, et al. Among authors: yang s. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1120-6. doi: 10.1016/j.bmcl.2012.11.107. Epub 2012 Dec 12. Bioorg Med Chem Lett. 2013. PMID: 23298810
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