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Page 1
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease.
Candito DA, Simov V, Gulati A, Kattar S, Chau RW, Lapointe BT, Methot JL, DeMong DE, Graham TH, Kurukulasuriya R, Keylor MH, Tong L, Morriello GJ, Acton JJ, Pio B, Liu W, Scott JD, Ardolino MJ, Martinot TA, Maddess ML, Yan X, Gunaydin H, Palte RL, McMinn SE, Nogle L, Yu H, Minnihan EC, Lesburg CA, Liu P, Su J, Hegde LG, Moy LY, Woodhouse JD, Faltus R, Xiong T, Ciaccio P, Piesvaux JA, Otte KM, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Neelamkavil S, Wood HB, Fuller PH, Ellis JM. Candito DA, et al. Among authors: yu h. J Med Chem. 2022 Dec 22;65(24):16801-16817. doi: 10.1021/acs.jmedchem.2c01605. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475697
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
Siu T, Brubaker J, Fuller P, Torres L, Zeng H, Close J, Mampreian DM, Shi F, Liu D, Fradera X, Johnson K, Bays N, Kadic E, He F, Goldenblatt P, Shaffer L, Patel SB, Lesburg CA, Alpert C, Dorosh L, Deshmukh SV, Yu H, Klappenbach J, Elwood F, Dinsmore CJ, Fernandez R, Moy L, Young JR. Siu T, et al. Among authors: yu h. J Med Chem. 2017 Dec 14;60(23):9676-9690. doi: 10.1021/acs.jmedchem.7b01135. Epub 2017 Dec 4. J Med Chem. 2017. PMID: 29156136
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Methot JL, Zhou H, McGowan MA, Anthony NJ, Christopher M, Garcia Y, Achab A, Lipford K, Trotter BW, Altman MD, Fradera X, Lesburg CA, Li C, Alves S, Chappell CP, Jain R, Mangado R, Pinheiro E, Williams SMG, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Lee HH, Yu H, Shah S, Katz JD. Methot JL, et al. Among authors: yu h. J Med Chem. 2021 Apr 22;64(8):5137-5156. doi: 10.1021/acs.jmedchem.1c00237. Epub 2021 Apr 2. J Med Chem. 2021. PMID: 33797901
Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD. Methot JL, et al. Among authors: yu h. J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22. J Med Chem. 2019. PMID: 30986068
Characterizing Pharmacokinetic-Pharmacodynamic Relationships and Efficacy of PI3Kδ Inhibitors in Respiratory Models of TH2 and TH1 Inflammation.
McLeod RL, Gil MA, Chen D, Cabal A, Katz J, Methot J, Woodhouse JD, Dorosh L, Geda P, Mehta K, Cicmil M, Baltus GA, Bass A, Houshyar H, Caniga M, Yu H, Gervais F, Alves S, Shah S. McLeod RL, et al. Among authors: yu h. J Pharmacol Exp Ther. 2019 May;369(2):223-233. doi: 10.1124/jpet.118.252551. Epub 2019 Feb 25. J Pharmacol Exp Ther. 2019. PMID: 30804001
Inhibition of spleen tyrosine kinase attenuates allergen-mediated airway constriction.
Moy LY, Jia Y, Caniga M, Lieber G, Gil M, Fernandez X, Sirkowski E, Miller R, Alexander JP, Lee HH, Shin JD, Ellis JM, Chen H, Wilhelm A, Yu H, Vincent S, Chapman RW, Kelly N, Hickey E, Abraham WM, Northrup A, Miller T, Houshyar H, Crackower MA. Moy LY, et al. Among authors: yu h. Am J Respir Cell Mol Biol. 2013 Dec;49(6):1085-92. doi: 10.1165/rcmb.2013-0200OC. Am J Respir Cell Mol Biol. 2013. PMID: 23889698
Design, synthesis, and evaluation of prodrugs of ertapenem.
Singh SB, Rindgen D, Bradley P, Cama L, Sun W, Hafey MJ, Suzuki T, Wang N, Wu H, Zhang B, Wang L, Ji C, Yu H, Soll R, Olsen DB, Meinke PT, Nicoll-Griffith DA. Singh SB, et al. Among authors: yu h. ACS Med Chem Lett. 2013 Jul 3;4(8):715-9. doi: 10.1021/ml400092n. eCollection 2013 Aug 8. ACS Med Chem Lett. 2013. PMID: 24900737 Free PMC article.
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