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Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB 3rd, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC. Carter PH, et al. Among authors: brown gd. ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. doi: 10.1021/ml500505q. eCollection 2015 Apr 9. ACS Med Chem Lett. 2015. PMID: 25893046 Free PMC article.
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Yang MG, et al. Among authors: brown gd. ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891130 Free PMC article.
Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Yang MG, Xiao Z, Zhao R, Tebben AJ, Wang B, Cherney RJ, Batt DG, Brown GD, Cvijic ME, Duncia JV, Gallela MA, Gardner DS, Khandelwal P, Malley MF, Pang J, Rose AV, Santella JB 3rd, Sarjeant AA, Xu S, Mathur A, Mandlekar S, Vuppugalla R, Zhao Q, Carter PH. Yang MG, et al. Among authors: brown gd. ACS Med Chem Lett. 2021 May 25;12(6):969-975. doi: 10.1021/acsmedchemlett.1c00082. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141082 Free PMC article.
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.
Cherney RJ, Anjanappa P, Selvakumar K, Batt DG, Brown GD, Rose AV, Vuppugalla R, Chen J, Pang J, Xu S, Yarde M, Tebben AJ, Paidi VR, Cvijic ME, Mathur A, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Cherney RJ, et al. Among authors: brown gd. ACS Med Chem Lett. 2021 Oct 15;12(11):1753-1758. doi: 10.1021/acsmedchemlett.1c00373. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795864 Free PMC article.
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST. Duan JJ, et al. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24. Bioorg Med Chem Lett. 2014. PMID: 25453808
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.
Voss ME, Carter PH, Tebben AJ, Scherle PA, Brown GD, Thompson LA, Xu M, Lo YC, Yang G, Liu RQ, Strzemienski P, Everlof JG, Trzaskos JM, Decicco CP. Voss ME, et al. Among authors: brown gd. Bioorg Med Chem Lett. 2003 Feb 10;13(3):533-8. doi: 10.1016/s0960-894x(02)00941-1. Bioorg Med Chem Lett. 2003. PMID: 12565966
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Morales-Ramos AI, Mecom JS, Kiesow TJ, Graybill TL, Brown GD, Aiyar NV, Davenport EA, Kallal LA, Knapp-Reed BA, Li P, Londregan AT, Morrow DM, Senadhi S, Thalji RK, Zhao S, Burns-Kurtis CL, Marino JP Jr. Morales-Ramos AI, et al. Among authors: brown gd. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6222-6. doi: 10.1016/j.bmcl.2008.09.102. Epub 2008 Oct 2. Bioorg Med Chem Lett. 2008. PMID: 18926700
563 results