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Page 1
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Guo L, et al. Among authors: hagmann wk. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994747 Free PMC article.
Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.
Esser CK, Bugianesi RL, Caldwell CG, Chapman KT, Durette PL, Girotra NN, Kopka IE, Lanza TJ, Levorse DA, MacCoss M, Owens KA, Ponpipom MM, Simeone JP, Harrison RK, Niedzwiecki L, Becker JW, Marcy AI, Axel MG, Christen AJ, McDonnell J, Moore VL, Olszewski JM, Saphos C, Visco DM, Hagmann WK, et al. Esser CK, et al. Among authors: hagmann wk. J Med Chem. 1997 Mar 14;40(6):1026-40. doi: 10.1021/jm960465t. J Med Chem. 1997. PMID: 9083493
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T Jr, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK. Lin LS, et al. Among authors: hagmann wk. Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4. doi: 10.1016/s0960-894x(01)00818-6. Bioorg Med Chem Lett. 2002. PMID: 11844683
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Fong TM, Shen CP, Lao J, Xiao JC, Shearman LP, Stribling DS, Rosko K, Strack A, Marsh DJ, Feng Y, Kumar S, Samuel K, Yin W, Van der Ploeg LH, Goulet MT, Hagmann WK. Lin LS, et al. Among authors: hagmann wk. J Med Chem. 2006 Dec 28;49(26):7584-7. doi: 10.1021/jm060996+. J Med Chem. 2006. PMID: 17181138
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Vachal P, Fletcher JM, Fong TM, Huang CC, Lao J, Xiao JC, Shen CP, Strack AM, Shearman L, Stribling S, Chen RZ, Frassetto A, Tong X, Wang J, Ball RG, Tsou NN, Hickey GJ, Thompson DF, Faidley TD, Nicolich S, Achanfuo-Yeboah J, Hora DF, Hale JJ, Hagmann WK. Vachal P, et al. Among authors: hagmann wk. J Med Chem. 2009 Apr 23;52(8):2550-8. doi: 10.1021/jm900063x. J Med Chem. 2009. PMID: 19320488
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Lin LS, Lanza T, Jewell JP, Liu P, Jones C, Kieczykowski GR, Treonze K, Si Q, Manior S, Koo G, Tong X, Wang J, Schuelke A, Pivnichny J, Wang R, Raab C, Vincent S, Davies P, Maccoss M, Mumford RA, Hagmann WK. Lin LS, et al. Among authors: hagmann wk. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: hagmann wk. ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900499 Free PMC article.
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
Li D, Wu Z, Yu Y, Ball RG, Guo L, Sherer E, He S, Hong Q, Lai Z, Qi H, Truong Q, Yang DX, Chicchi GG, Tsao KL, Trusca D, Trujillo M, Pachanski M, Eiermann GJ, Howard AD, Zhou YP, Zhang BB, Nargund RP, Hagmann WK. Li D, et al. Among authors: hagmann wk. ACS Med Chem Lett. 2014 Apr 24;5(6):690-5. doi: 10.1021/ml500079u. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944745 Free PMC article.
Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.
He S, Lai Z, Ye Z, Dobbelaar PH, Shah SK, Truong Q, Du W, Guo L, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Reibarkh M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang B, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: hagmann wk. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53. doi: 10.1021/ml500028c. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050159 Free PMC article.
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Shah SK, He S, Guo L, Truong Q, Qi H, Du W, Lai Z, Liu J, Jian T, Hong Q, Dobbelaar P, Ye Z, Sherer E, Feng Z, Yu Y, Wong F, Samuel K, Madiera M, Karanam BV, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Feng Y, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Pachanski M, Fernandez G, Nelson D, Bunting P, Morissette P, Volksdorf S, Kerr J, Zhang BB, Howard AD, Zhou YP, Pasternak A, Nargund RP, Hagmann WK. Shah SK, et al. Among authors: hagmann wk. ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. doi: 10.1021/ml500514w. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005524 Free PMC article.
86 results