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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: devraj r. 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 of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B. Xue CB, et al. Among authors: devraj r. ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8. ACS Med Chem Lett. 2011. PMID: 24900280 Free PMC article.
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.
Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Among authors: devraj rv. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21640588
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Messing D, Yang J, Mao MK, Yalamanchili G, Vonder Embse R, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Among authors: devraj rv. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71. doi: 10.1016/j.bmcl.2011.04.121. Epub 2011 May 11. Bioorg Med Chem Lett. 2011. PMID: 21641211
89 results