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Page 1
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
Bogen SL, Pan W, Gibeau CR, Lahue BR, Ma Y, Nair LG, Seigel E, Shipps GW Jr, Tian Y, Wang Y, Lin Y, Liu M, Liu S, Mirza A, Wang X, Lipari P, Seidel-Dugan C, Hicklin DJ, Bishop WR, Rindgen D, Nomeir A, Prosise W, Reichert P, Scapin G, Strickland C, Doll RJ. Bogen SL, et al. Among authors: rindgen d. ACS Med Chem Lett. 2016 Jan 20;7(3):324-9. doi: 10.1021/acsmedchemlett.5b00472. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985323 Free PMC article.
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Yu T, Zhang Y, Kerekes AD, Tagat JR, Doll RJ, Xiao Y, Esposite S, Hruza A, Belanger DB, Voss M, Rainka MP, Basso A, Liu M, Liang L, Sui N, Prelusky D, Rindgen D, Zhang L. Yu T, et al. Among authors: rindgen d. Bioorg Med Chem Lett. 2018 May 1;28(8):1397-1403. doi: 10.1016/j.bmcl.2018.02.037. Epub 2018 Feb 23. Bioorg Med Chem Lett. 2018. PMID: 29545102
Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.
Huang X, Brubaker J, Zhou W, Biju PJ, Xiao L, Shao N, Huang Y, Dong L, Liu Z, Bitar R, Buevich A, Jung J, Peterson SL, Butcher JW, Close J, Martinez M, MacCoss RN, Zhang H, Crawford S, McCormick KD, Aslanian R, Nargund R, Correll C, Gervais F, Qiu H, Yang X, Garlisi C, Rindgen D, Maloney KM, Siliphaivanh P, Palani A. Huang X, et al. Among authors: rindgen d. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684. doi: 10.1021/acsmedchemlett.8b00145. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034600 Free PMC article.
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.
Ho GD, Yang SW, Smotryski J, Bercovici A, Nechuta T, Smith EM, McElroy W, Tan Z, Tulshian D, McKittrick B, Greenlee WJ, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R. Ho GD, et al. Among authors: rindgen d. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1019-22. doi: 10.1016/j.bmcl.2011.11.127. Epub 2011 Dec 9. Bioorg Med Chem Lett. 2012. PMID: 22222034
Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J. Mandal M, et al. Among authors: rindgen d. J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28322556
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Xiao D, Zhu X, Yu Y, Shao N, Wu J, McCormick KD, Dhondi P, Qin J, Mazzola R, Tang H, Rao A, Siliphaivanh P, Qiu H, Yang X, Rivelli M, Garlisi CG, Eckel S, Mukhopadhyay G, Correll C, Rindgen D, Aslanian R, Palani A. Xiao D, et al. Among authors: rindgen d. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1615-20. doi: 10.1016/j.bmcl.2014.01.043. Epub 2014 Feb 2. Bioorg Med Chem Lett. 2014. PMID: 24556380
Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.
Ho GD, Tulshian D, Bercovici A, Tan Z, Hanisak J, Brumfield S, Matasi J, Heap CR, Earley WG, Courneya B, Herr RJ, Zhou X, Bridal T, Rindgen D, Sorota S, Yang SW. Ho GD, et al. Among authors: rindgen d. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4110-3. doi: 10.1016/j.bmcl.2014.07.060. Epub 2014 Jul 29. Bioorg Med Chem Lett. 2014. PMID: 25113934
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Ho GD, Michael Seganish W, Bercovici A, Tulshian D, Greenlee WJ, Van Rijn R, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R. Ho GD, et al. Among authors: rindgen d. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2585-9. doi: 10.1016/j.bmcl.2012.01.113. Epub 2012 Feb 9. Bioorg Med Chem Lett. 2012. PMID: 22377514
33 results