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Page 1
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: hockerman sl. J Med Chem. 2010 Aug 26;53(16):5979-6002. doi: 10.1021/jm100505n. J Med Chem. 2010. PMID: 20672822
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Becker DP, Barta TE, Bedell LJ, Boehm TL, Bond BR, Carroll J, Carron CP, Decrescenzo GA, Easton AM, Freskos JN, Funckes-Shippy CL, Heron M, Hockerman S, Howard CP, Kiefer JR, Li MH, Mathis KJ, McDonald JJ, Mehta PP, Munie GE, Sunyer T, Swearingen CA, Villamil CI, Welsch D, Williams JM, Yu Y, Yao J. Becker DP, et al. J Med Chem. 2010 Sep 23;53(18):6653-80. doi: 10.1021/jm100669j. J Med Chem. 2010. PMID: 20726512
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Becker DP, Villamil CI, Barta TE, Bedell LJ, Boehm TL, Decrescenzo GA, Freskos JN, Getman DP, Hockerman S, Heintz R, Howard SC, Li MH, McDonald JJ, Carron CP, Funckes-Shippy CL, Mehta PP, Munie GE, Swearingen CA. Becker DP, et al. J Med Chem. 2005 Oct 20;48(21):6713-30. doi: 10.1021/jm0500875. J Med Chem. 2005. PMID: 16220987
MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
Barta TE, Becker DP, Bedell LJ, Easton AM, Hockerman SL, Kiefer J, Munie GE, Mathis KJ, Li MH, Rico JG, Villamil CI, Williams JM. Barta TE, et al. Among authors: hockerman sl. Bioorg Med Chem Lett. 2011 May 15;21(10):2820-2. doi: 10.1016/j.bmcl.2011.03.099. Epub 2011 Apr 1. Bioorg Med Chem Lett. 2011. PMID: 21507637
alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1.
Becker DP, Barta TE, Bedell L, DeCrescenzo G, Freskos J, Getman DP, Hockerman SL, Li M, Mehta P, Mischke B, Munie GE, Swearingen C, Villamil CI. Becker DP, et al. Among authors: hockerman sl. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2719-22. doi: 10.1016/s0960-894x(01)00556-x. Bioorg Med Chem Lett. 2001. PMID: 11591509
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Kolodziej SA, Hockerman SL, Boehm TL, Carroll JN, DeCrescenzo GA, McDonald JJ, Mischke DA, Munie GE, Fletcher TR, Rico JG, Stehle NW, Swearingen C, Becker DP. Kolodziej SA, et al. Among authors: hockerman sl. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3557-60. doi: 10.1016/j.bmcl.2010.04.130. Epub 2010 May 23. Bioorg Med Chem Lett. 2010. PMID: 20529684
MMP-13 selective isonipecotamide alpha-sulfone hydroxamates.
Kolodziej SA, Hockerman SL, DeCrescenzo GA, McDonald JJ, Mischke DA, Munie GE, Fletcher TR, Stehle N, Swearingen C, Becker DP. Kolodziej SA, et al. Among authors: hockerman sl. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3561-4. doi: 10.1016/j.bmcl.2010.04.111. Epub 2010 Apr 28. Bioorg Med Chem Lett. 2010. PMID: 20529685
Selective inhibition of the p38α MAPK-MK2 axis inhibits inflammatory cues including inflammasome priming signals.
Wang C, Hockerman S, Jacobsen EJ, Alippe Y, Selness SR, Hope HR, Hirsch JL, Mnich SJ, Saabye MJ, Hood WF, Bonar SL, Abu-Amer Y, Haimovich A, Hoffman HM, Monahan JB, Mbalaviele G. Wang C, et al. Among authors: hockerman s. J Exp Med. 2018 May 7;215(5):1315-1325. doi: 10.1084/jem.20172063. Epub 2018 Mar 16. J Exp Med. 2018. PMID: 29549113 Free PMC article.