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Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.
Hughes RO, Rogier DJ, Devraj R, Zheng C, Cao G, Feng H, Xia M, Anand R, Xing L, Glenn J, Zhang K, Covington M, Morton PA, Hutzler JM, Davis JW 2nd, Scherle P, Baribaud F, Bahinski A, Mo ZL, Newton R, Metcalf B, Xue CB. Hughes RO, et al. Among authors: hutzler jm. Bioorg Med Chem Lett. 2011 May 1;21(9):2626-30. doi: 10.1016/j.bmcl.2011.01.034. Epub 2011 Jan 15. Bioorg Med Chem Lett. 2011. PMID: 21315584
Discovery and optimization of oxadiazole-based FLAP inhibitors.
Bartolozzi A, Abeywardane A, Bosanac T, Broadwater JA, Chen Z, Hutzler JM, Huber JD, Nemoto P, Olague A, Riether D, Simpson T, Takahashi H, Wu L, Zhang Y, Zindell RM. Bartolozzi A, et al. Among authors: hutzler jm. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4652-4659. doi: 10.1016/j.bmcl.2017.09.007. Epub 2017 Sep 8. Bioorg Med Chem Lett. 2017. PMID: 28927794
Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).
Takahashi H, Riether D, Bartolozzi A, Bosanac T, Berger V, Binetti R, Broadwater J, Chen Z, Crux R, De Lombaert S, Dave R, Dines JA, Fadra-Khan T, Flegg A, Garrigou M, Hao MH, Huber J, Hutzler JM, Kerr S, Kotey A, Liu W, Lo HY, Loke PL, Mahaney PE, Morwick TM, Napier S, Olague A, Pack E, Padyana AK, Thomson DS, Tye H, Wu L, Zindell RM, Abeywardane A, Simpson T. Takahashi H, et al. Among authors: hutzler jm. J Med Chem. 2015 Feb 26;58(4):1669-90. doi: 10.1021/jm501185j. Epub 2015 Feb 11. J Med Chem. 2015. PMID: 25671290
34 results