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2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.
Dubowchik GM, Michne JA, Zuev D, Schwartz W, Scola PM, James CA, Ruediger EH, Pin SS, Burris KD, Balanda LA, Gao Q, Wu D, Fung L, Fiedler T, Browman KE, Taber MT, Zhang J. Dubowchik GM, et al. Among authors: pin ss. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3997-4000. doi: 10.1016/j.bmcl.2003.08.055. Bioorg Med Chem Lett. 2003. PMID: 14592493
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure.
Degnan AP, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Denton R, Han X, Macci R, Mathias NR, Moench P, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Macor JE, Dubowchik GM. Degnan AP, et al. Among authors: pin ss. J Med Chem. 2008 Aug 28;51(16):4858-61. doi: 10.1021/jm800546t. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665579
Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R).
Vrudhula VM, Dasgupta B, Pin SS, Burris KD, Balanda LA, Fung LK, Fiedler T, Browman KE, Taber MT, Zhang J, Macor JE, Dubowchik GM. Vrudhula VM, et al. Among authors: pin ss. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1905-9. doi: 10.1016/j.bmcl.2010.01.127. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20185312
30 results