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The Discovery of ( S)-1-(6-(3-((4-(1-(Cyclopropanecarbonyl)piperidin-4-yl)-2-methylphenyl)amino)-2,3-dihydro-1 H-inden-4-yl)pyridin-2-yl)-5-methyl-1 H-pyrazole-4-carboxylic Acid, a Soluble Guanylate Cyclase Activator Specifically Designed for Topical Ocular Delivery as a Therapy for Glaucoma.
Ehara T, Adams CM, Bevan D, Ji N, Meredith EL, Belanger DB, Powers J, Kato M, Solovay C, Liu D, Capparelli M, Bolduc P, Grob JE, Daniels MH, Ferrara L, Yang L, Li B, Towler CS, Stacy RC, Prasanna G, Mogi M. Ehara T, et al. Among authors: bolduc p. J Med Chem. 2018 Mar 22;61(6):2552-2570. doi: 10.1021/acs.jmedchem.8b00007. Epub 2018 Mar 2. J Med Chem. 2018. PMID: 29498522
A small-molecule inhibitor of C5 complement protein.
Jendza K, Kato M, Salcius M, Srinivas H, De Erkenez A, Nguyen A, McLaughlin D, Be C, Wiesmann C, Murphy J, Bolduc P, Mogi M, Duca J, Namil A, Capparelli M, Darsigny V, Meredith E, Tichkule R, Ferrara L, Heyder J, Liu F, Horton PA, Romanowski MJ, Schirle M, Mainolfi N, Anderson K, Michaud GA. Jendza K, et al. Among authors: bolduc p. Nat Chem Biol. 2019 Jul;15(7):666-668. doi: 10.1038/s41589-019-0303-9. Epub 2019 Jun 17. Nat Chem Biol. 2019. PMID: 31209353
The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
Evans R, Bolduc PN, Pfaffenbach M, Gao F, May-Dracka T, Fang T, Hopkins BT, Chodaparambil JV, Henry KL, Li P, Metrick C, Nelson A, Trapa P, Thomas A, Burkly L, Peterson EA. Evans R, et al. Among authors: bolduc pn. J Med Chem. 2024 Mar 28;67(6):4676-4690. doi: 10.1021/acs.jmedchem.3c02226. Epub 2024 Mar 11. J Med Chem. 2024. PMID: 38467640
Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation.
Pfaffenbach M, Bolduc PN, Xin Z, Gao F, Evans R, Fang T, Chodaparambil JV, Henry KL, Li P, Mathieu S, Metrick C, Vera Rebollar JA, Gu RF, Mccarl CA, Silbereis J, Peterson EA. Pfaffenbach M, et al. Among authors: bolduc pn. J Med Chem. 2024 May 23;67(10):8383-8395. doi: 10.1021/acs.jmedchem.4c00560. Epub 2024 May 2. J Med Chem. 2024. PMID: 38695469
Synthesis of N-Substituted 3-Amino-2-pyridones.
Bolduc PN, Pfaffenbach M, Blasczak VD, Mathieu SR, Peterson EA. Bolduc PN, et al. Org Lett. 2022 Aug 26;24(33):6133-6136. doi: 10.1021/acs.orglett.2c02189. Epub 2022 Aug 12. Org Lett. 2022. PMID: 35960821
Overcoming Limitations in Decarboxylative Arylation via Ag-Ni Electrocatalysis.
Palkowitz MD, Laudadio G, Kolb S, Choi J, Oderinde MS, Ewing TE, Bolduc PN, Chen T, Zhang H, Cheng PTW, Zhang B, Mandler MD, Blasczak VD, Richter JM, Collins MR, Schioldager RL, Bravo M, Dhar TGM, Vokits B, Zhu Y, Echeverria PG, Poss MA, Shaw SA, Clementson S, Petersen NN, Mykhailiuk PK, Baran PS. Palkowitz MD, et al. Among authors: bolduc pn. J Am Chem Soc. 2022 Sep 28;144(38):17709-17720. doi: 10.1021/jacs.2c08006. Epub 2022 Sep 15. J Am Chem Soc. 2022. PMID: 36106767 Free PMC article.
Synthesis of Unnatural Amino Acids via Ni/Ag Electrocatalytic Cross-Coupling.
Laudadio G, Neigenfind P, Chebolu R, Blasczak VD, Maddirala SJ, Palkowitz MD, Bolduc PN, Nicastri MC, Puthukanoori RK, Paraselli BR, Baran PS. Laudadio G, et al. Among authors: bolduc pn. Org Lett. 2024 Mar 22;26(11):2276-2281. doi: 10.1021/acs.orglett.4c00474. Epub 2024 Mar 11. Org Lett. 2024. PMID: 38467055
Nickel-Electrocatalytic Decarboxylative Arylation to Access Quaternary Centers.
Laudadio G, Neigenfind P, Péter Á, Rubel CZ, Emmanuel MA, Oderinde MS, Ewing TE, Palkowitz MD, Sloane JL, Gillman KW, Ridge D, Mandler MD, Bolduc PN, Nicastri MC, Zhang B, Clementson S, Petersen NN, Martín-Gago P, Mykhailiuk P, Engle KM, Baran PS. Laudadio G, et al. Among authors: bolduc pn. Angew Chem Int Ed Engl. 2024 Feb 19;63(8):e202314617. doi: 10.1002/anie.202314617. Epub 2024 Jan 18. Angew Chem Int Ed Engl. 2024. PMID: 38181042
45 results