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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: lanza t. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
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: lanza tj jr. J Med Chem. 2006 Dec 28;49(26):7584-7. doi: 10.1021/jm060996+. J Med Chem. 2006. PMID: 17181138
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, Guthikonda R, Truong Q, Chang LL, Quaker G, Colandrea VJ, Tong X, Wang J, Xu S, Fong TM, Shen CP, Lao J, Chen J, Shearman LP, Stribling DS, Rosko K, Strack A, Ha S, Van der Ploeg L, Goulet MT, Hagmann WK. Armstrong HE, et al. Among authors: lanza tj jr. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. doi: 10.1016/j.bmcl.2007.01.087. Epub 2007 Feb 2. Bioorg Med Chem Lett. 2007. PMID: 17293109
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.
Lin LS, Lanza T Jr, McCauley E, Van Riper G, Kidambi U, Cao J, Egger LA, Mumford RA, Schmidt JA, MacCoss M, Hagmann WK. Lin LS, et al. Among authors: lanza t jr. Bioorg Med Chem Lett. 2002 Jan 21;12(2):133-6. doi: 10.1016/s0960-894x(01)00705-3. Bioorg Med Chem Lett. 2002. PMID: 11755338
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: lanza t jr. 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
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Li B, de Laszlo SE, Kamenecka TM, Kopka IE, Durette PL, Lanza T Jr, MacCoss M, Tong S, Mumford RA, McCauley ED, Van Riper G, Schmidt JA, Hagmann WK. Li B, et al. Among authors: lanza t jr. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2141-4. doi: 10.1016/s0960-894x(02)00366-9. Bioorg Med Chem Lett. 2002. PMID: 12127523
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.
Kamenecka TM, Lanza T Jr, de Laszlo SE, Li B, McCauley ED, Van Riper G, Egger LA, Kidambi U, Mumford RA, Tong S, MacCoss M, Schmidt JA, Hagmann WK. Kamenecka TM, et al. Among authors: lanza t jr. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2205-8. doi: 10.1016/s0960-894x(02)00356-6. Bioorg Med Chem Lett. 2002. PMID: 12127538
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Kopka IE, Lin LS, Mumford RA, Lanza T Jr, Magriotis PA, Young D, DeLaszlo SE, MacCoss M, Mills SG, Van Riper G, McCauley E, Lyons K, Vincent S, Egger LA, Kidambi U, Stearns R, Colletti A, Teffera Y, Tong S, Owens K, Levorse D, Schmidt JA, Hagmann WK. Kopka IE, et al. Among authors: lanza t jr. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2415-8. doi: 10.1016/s0960-894x(02)00460-2. Bioorg Med Chem Lett. 2002. PMID: 12161146
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka IE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA. Hagmann WK, et al. Among authors: lanza t. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2709-13. doi: 10.1016/s0960-894x(01)00544-3. Bioorg Med Chem Lett. 2001. PMID: 11591507
85 results