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BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.
Sanderson MP, Apgar J, Garin-Chesa P, Hofmann MH, Kessler D, Quant J, Savchenko A, Schaaf O, Treu M, Tye H, Zahn SK, Zoephel A, Haaksma E, Adolf GR, Kraut N. Sanderson MP, et al. Among authors: tye h. Mol Cancer Ther. 2015 Dec;14(12):2762-72. doi: 10.1158/1535-7163.MCT-15-0539. Epub 2015 Oct 5. Mol Cancer Ther. 2015. PMID: 26438154
Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).
Takahashi H, Riether D, Bartolozzi A, Bosanac T, Berger V, Binetti R, Broadwater J, Chen Z, Crux R, De Lombaert S, Dave R, Dines JA, Fadra-Khan T, Flegg A, Garrigou M, Hao MH, Huber J, Hutzler JM, Kerr S, Kotey A, Liu W, Lo HY, Loke PL, Mahaney PE, Morwick TM, Napier S, Olague A, Pack E, Padyana AK, Thomson DS, Tye H, Wu L, Zindell RM, Abeywardane A, Simpson T. Takahashi H, et al. Among authors: tye h. J Med Chem. 2015 Feb 26;58(4):1669-90. doi: 10.1021/jm501185j. Epub 2015 Feb 11. J Med Chem. 2015. PMID: 25671290
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
Moss N, Choi Y, Cogan D, Flegg A, Kahrs A, Loke P, Meyn O, Nagaraja R, Napier S, Parker A, Thomas Peterson J, Ramsden P, Sarko C, Skow D, Tomlinson J, Tye H, Whitaker M. Moss N, et al. Among authors: tye h. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2206-10. doi: 10.1016/j.bmcl.2009.02.126. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19307114
DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: synthesis and antibacterial activity.
East SP, White CB, Barker O, Barker S, Bennett J, Brown D, Boyd EA, Brennan C, Chowdhury C, Collins I, Convers-Reignier E, Dymock BW, Fletcher R, Haydon DJ, Gardiner M, Hatcher S, Ingram P, Lancett P, Mortenson P, Papadopoulos K, Smee C, Thomaides-Brears HB, Tye H, Workman J, Czaplewski LG. East SP, et al. Among authors: tye h. Bioorg Med Chem Lett. 2009 Feb 1;19(3):894-9. doi: 10.1016/j.bmcl.2008.11.102. Epub 2008 Dec 3. Bioorg Med Chem Lett. 2009. PMID: 19095445
31 results