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Page 1
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.
Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Jones SA, Kaldor I, Liu Y, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F III, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB. Akwabi-Ameyaw A, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43. doi: 10.1016/j.bmcl.2008.06.073. Epub 2008 Jun 28. Bioorg Med Chem Lett. 2008. PMID: 18621523
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.
Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Parks DJ, Todd D, Williams SP, Wisely GB. Bass JY, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2969-73. doi: 10.1016/j.bmcl.2009.04.047. Epub 2009 Apr 18. Bioorg Med Chem Lett. 2009. PMID: 19410460
FXR agonist activity of conformationally constrained analogs of GW 4064.
Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Bruce Wisely G. Akwabi-Ameyaw A, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4733-9. doi: 10.1016/j.bmcl.2009.06.062. Epub 2009 Jun 21. Bioorg Med Chem Lett. 2009. PMID: 19586769
Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.
Katamreddy SR, Carpenter AJ, Ammala CE, Boros EE, Brashear RL, Briscoe CP, Bullard SR, Caldwell RD, Conlee CR, Croom DK, Hart SM, Heyer DO, Johnson PR, Kashatus JA, Minick DJ, Peckham GE, Ross SA, Roller SG, Samano VA, Sauls HR, Tadepalli SM, Thompson JB, Xu Y, Way JM. Katamreddy SR, et al. Among authors: caldwell rd. J Med Chem. 2012 Dec 27;55(24):10972-94. doi: 10.1021/jm301404a. Epub 2012 Dec 12. J Med Chem. 2012. PMID: 23214471
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists.
Xiao Y, Karra S, Goutopoulos A, Morse NT, Zhang S, Dhanabal M, Tian H, Seenisamy J, Jayadevan J, Caldwell R, Potnick J, Bleich M, Chekler E, Sherer B, Sriraman V. Xiao Y, et al. Bioorg Med Chem Lett. 2019 Jul 1;29(13):1660-1664. doi: 10.1016/j.bmcl.2019.04.033. Epub 2019 Apr 24. Bioorg Med Chem Lett. 2019. PMID: 31031055
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B. Qiu H, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2018 Sep 15;28(17):2939-2944. doi: 10.1016/j.bmcl.2018.07.008. Epub 2018 Jul 5. Bioorg Med Chem Lett. 2018. PMID: 30122225
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Qiu H, Ali Z, Bender A, Caldwell R, Chen YY, Fang Z, Gardberg A, Glaser N, Goettsche A, Goutopoulos A, Grenningloh R, Hanschke B, Head J, Johnson T, Jones C, Jones R, Kulkarni S, Maurer C, Morandi F, Neagu C, Poetzsch S, Potnick J, Schmidt R, Roe K, Viacava Follis A, Wing C, Zhu X, Sherer B. Qiu H, et al. Bioorg Med Chem. 2021 Jun 15;40:116163. doi: 10.1016/j.bmc.2021.116163. Epub 2021 Apr 20. Bioorg Med Chem. 2021. PMID: 33932711
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Caldwell RD, et al. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. J Med Chem. 2019. PMID: 31368705
Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.
Qiu H, Liu-Bujalski L, Caldwell RD, Viacava Follis A, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones CCV, Jones R, Mochalkin I, Morandi F, Neagu C, Potnick J, Sherer B. Qiu H, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3307-3311. doi: 10.1016/j.bmcl.2018.09.018. Epub 2018 Sep 15. Bioorg Med Chem Lett. 2018. PMID: 30243592
30 results