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Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13.
ACS Med Chem Lett. 2020.
PMID: 32071676
Free PMC article.
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.
Simov V, Deshmukh SV, Dinsmore CJ, Elwood F, Fernandez RB, Garcia Y, Gibeau C, Gunaydin H, Jung J, Katz JD, Kraybill B, Lapointe B, Patel SB, Siu T, Su H, Young JR.
Simov V, et al.
Bioorg Med Chem Lett. 2016 Apr 1;26(7):1803-8. doi: 10.1016/j.bmcl.2016.02.035. Epub 2016 Feb 19.
Bioorg Med Chem Lett. 2016.
PMID: 26927423
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Strategy for Extending Half-life in Drug Design and Its Significance.
Gunaydin H, Altman MD, Ellis JM, Fuller P, Johnson SA, Lahue B, Lapointe B.
Gunaydin H, et al.
ACS Med Chem Lett. 2018 Apr 2;9(6):528-533. doi: 10.1021/acsmedchemlett.8b00018. eCollection 2018 Jun 14.
ACS Med Chem Lett. 2018.
PMID: 29937977
Free PMC article.
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Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Gulati A, Yeung CS, Lapointe B, Kattar SD, Gunaydin H, Scott JD, Childers KK, Methot JL, Simov V, Kurukulasuriya R, Pio B, Morriello GJ, Liu P, Tang H, Neelamkavil S, Wood HB, Rada VL, Ardolino MJ, Yan XC, Palte R, Otte K, Faltus R, Woodhouse J, Hegde LG, Ciaccio P, Minnihan EC, DiMauro EF, Fell MJ, Fuller PH, Ellis JM.
Gulati A, et al.
RSC Med Chem. 2021 Jun 4;12(7):1164-1173. doi: 10.1039/d1md00097g. eCollection 2021 Jul 21.
RSC Med Chem. 2021.
PMID: 34355182
Free PMC article.
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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: lapointe bt.
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
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Preparation of a stable trifluoroborate salt for the synthesis of 1-aryl-2,2-difluoro-enolethers and/or 2,2-difluoro-1-aryl-ketones via palladium-mediated cross-coupling.
Katz JD, Lapointe BT, Dinsmore CJ.
Katz JD, et al. Among authors: lapointe bt.
J Org Chem. 2009 Nov 20;74(22):8866-9. doi: 10.1021/jo901789b.
J Org Chem. 2009.
PMID: 19845317
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