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Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: cai j. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
Discovery of novel BTK inhibitors with carboxylic acids.
Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Gao X, et al. Among authors: cai j. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 28254166
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA. Boga SB, et al. Among authors: cai j. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18. Bioorg Med Chem Lett. 2017. PMID: 28720503
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Cai J, Baugh M, Black D, Long C, Jonathan Bennett D, Dempster M, Fradera X, Gillespie J, Andrews F, Boucharens S, Bruin J, Cameron KS, Cumming I, Hamilton W, Jones PS, Kaptein A, Kinghorn E, Maidment M, Martin I, Mitchell A, Rankovic Z, Robinson J, Scullion P, Uitdehaag JC, Vink P, Westwood P, van Zeeland M, van Berkom L, Bastiani M, Meulemans T. Cai J, et al. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4350-4. doi: 10.1016/j.bmcl.2010.06.072. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20598883
Imidazopyridyl compounds as aldosterone synthase inhibitors.
Whitehead BR, Lo MM, Ali A, Park MK, Hoyt SB, Xiong Y, Cai J, Carswell E, Cooke A, MacLean J, Ratcliffe P, Robinson J, Bennett DJ, Clemas JA, Wisniewski T, Struthers M, Cully D, MacNeil DJ. Whitehead BR, et al. Among authors: cai j. Bioorg Med Chem Lett. 2017 Jan 15;27(2):143-146. doi: 10.1016/j.bmcl.2016.12.003. Epub 2016 Dec 2. Bioorg Med Chem Lett. 2017. PMID: 27979595
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T. Cai J, et al. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. doi: 10.1016/j.bmcl.2010.10.012. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2010. PMID: 21030256
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia.
Liu P, Wang L, DuBois BG, Colandrea VJ, Liu R, Cai J, Du X, Quan W, Morris W, Bai J, Bishwokarma B, Cheng M, Piesvaux J, Ray K, Alpert C, Chiu CS, Zielstorff M, Metzger JM, Yang L, Leung D, Alleyne C, Vincent SH, Pucci V, Li X, Crespo A, Stickens D, Hale JJ, Ujjainwalla F, Sinz CJ. Liu P, et al. Among authors: cai j. ACS Med Chem Lett. 2018 Nov 13;9(12):1193-1198. doi: 10.1021/acsmedchemlett.8b00274. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613325 Free PMC article.
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Finlay W, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Arbuckle W, Anderson M, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Jones P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Rankovic Z, et al. Among authors: cai j. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6237-41. doi: 10.1016/j.bmcl.2010.08.101. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20843687
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