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Page 1
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG. Augeri DJ, et al. Among authors: cap m. J Med Chem. 2005 Jul 28;48(15):5025-37. doi: 10.1021/jm050261p. J Med Chem. 2005. PMID: 16033281
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG. Magnin DR, et al. Among authors: cap m. J Med Chem. 2004 May 6;47(10):2587-98. doi: 10.1021/jm049924d. J Med Chem. 2004. PMID: 15115400
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R, Cheng L, Sleph P, Sun W, Tieman A, Wetterau JR, Doweyko A, Chandrasena G, Chang SY, Humphreys WG, Sasseville VG, Biller SA, Ryono DE, Selan F, Hariharan N, Cheng PT. Devasthale PV, et al. Among authors: cap m. J Med Chem. 2005 Mar 24;48(6):2248-50. doi: 10.1021/jm0496436. J Med Chem. 2005. PMID: 15771468
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG. Devasthale P, et al. Among authors: cap m. J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9. J Med Chem. 2013. PMID: 23964740
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1H-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Shi Y, Wang Y, Meng W, Brigance RP, Ryono DE, Bolton S, Zhang H, Chen S, Smirk R, Tao S, Tino JA, Williams KN, Sulsky R, Nielsen L, Ellsworth B, Wong MKY, Sun JH, Leith LW, Sun D, Wu DR, Gupta A, Rampulla R, Mathur A, Chen BC, Wang A, Fuentes-Catanio HG, Kunselman L, Cap M, Zalaznick J, Ma X, Liu H, Taylor JR, Zebo R, Jones B, Kalinowski S, Swartz J, Staal A, O'Malley K, Kopcho L, Muckelbauer JK, Krystek SR Jr, Spronk SA, Marcinkeviciene J, Everlof G, Chen XQ, Xu C, Li YX, Langish RA, Yang Y, Wang Q, Behnia K, Fura A, Janovitz EB, Pannacciulli N, Griffen S, Zinker BA, Krupinski J, Kirby M, Whaley J, Zahler R, Barrish JC, Robl JA, Cheng PTW. Shi Y, et al. Among authors: cap m. J Med Chem. 2022 Mar 10;65(5):4291-4317. doi: 10.1021/acs.jmedchem.1c02110. Epub 2022 Feb 18. J Med Chem. 2022. PMID: 35179904
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.
Wang W, Devasthale P, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Li YX, Zahler R, Kirby MS, Hamann LG. Wang W, et al. Among authors: cap m. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6646-51. doi: 10.1016/j.bmcl.2011.09.074. Epub 2011 Sep 24. Bioorg Med Chem Lett. 2011. PMID: 21996520
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
Gavai AV, Sher PM, Mikkilineni AB, Poss KM, McCann PJ, Girotra RN, Fisher LG, Wu G, Bednarz MS, Mathur A, Wang TC, Sun CQ, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Harper TW, Ciosek CP Jr, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Washburn WN. Gavai AV, et al. Among authors: cap m. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3041-4. doi: 10.1016/s0960-894x(01)00629-1. Bioorg Med Chem Lett. 2001. PMID: 11714606
BMS-201620: a selective beta 3 agonist.
Washburn WN, Sun CQ, Bisacchi G, Wu G, Cheng PT, Sher PM, Ryono D, Gavai AV, Poss K, Girotra RN, McCann PJ, Mikkilineni AB, Dejneka TC, Wang TC, Merchant Z, Morella M, Arbeeny CM, Harper TW, Slusarchyk DA, Skwish S, Russell AD, Allen GT, Tesfamariam B, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Young D, Dickinson KE, Seymour AA. Washburn WN, et al. Among authors: cap m. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3525-9. doi: 10.1016/j.bmcl.2004.04.074. Bioorg Med Chem Lett. 2004. PMID: 15177466
An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits.
Wetterau JR, Gregg RE, Harrity TW, Arbeeny C, Cap M, Connolly F, Chu CH, George RJ, Gordon DA, Jamil H, Jolibois KG, Kunselman LK, Lan SJ, Maccagnan TJ, Ricci B, Yan M, Young D, Chen Y, Fryszman OM, Logan JV, Musial CL, Poss MA, Robl JA, Simpkins LM, Slusarchyk WA, Sulsky R, Taunk P, Magnin DR, Tino JA, Lawrence RM, Dickson JK Jr, Biller SA. Wetterau JR, et al. Among authors: cap m. Science. 1998 Oct 23;282(5389):751-4. doi: 10.1126/science.282.5389.751. Science. 1998. PMID: 9784135
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
Washburn WN, Sher PM, Poss KM, Girotra RN, McCann PJ, Gavai AV, Mikkilineni AB, Mathur A, Cheng P, Dejneka TC, Sun CQ, Wang TC, Harper TW, Russell AD, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Ciosek CP Jr, Ryono D, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Gregg RE. Washburn WN, et al. Among authors: cap m. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3035-9. doi: 10.1016/s0960-894x(01)00628-x. Bioorg Med Chem Lett. 2001. PMID: 11714605
84 results