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Page 1
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Himmelbauer MK, Bajrami B, Basile R, Capacci A, Chen T, Choi CK, Gilfillan R, Gonzalez-Lopez de Turiso F, Gu C, Hoemberger M, Johnson DS, Jones JH, Kadakia E, Kirkland M, Lin EY, Liu Y, Ma B, Magee T, Mantena S, Marx IE, Metrick CM, Mingueneau M, Murugan P, Muste CA, Nadella P, Nevalainen M, Parker Harp CR, Pattaropong V, Pietrasiewicz A, Prince RJ, Purgett TJ, Santoro JC, Schulz J, Sciabola S, Tang H, Vandeveer HG, Wang T, Yousaf Z, Helal CJ, Hopkins BT. Himmelbauer MK, et al. Among authors: metrick cm. J Med Chem. 2024 May 23;67(10):8122-8140. doi: 10.1021/acs.jmedchem.4c00220. Epub 2024 May 7. J Med Chem. 2024. PMID: 38712838 Free PMC article.
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: metrick c. 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
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: metrick c. 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 structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Vandeveer GH, Arduini RM, Baker DP, Barry K, Bohnert T, Bowden-Verhoek JK, Conlon P, Cullen PF, Guan B, Jenkins TJ, Liao SY, Lin L, Liu YT, Marcotte D, Mertsching E, Metrick CM, Negrou E, Powell N, Scott D, Silvian LF, Hopkins BT. Vandeveer GH, et al. Among authors: metrick cm. Bioorg Med Chem Lett. 2023 Jan 15;80:129108. doi: 10.1016/j.bmcl.2022.129108. Epub 2022 Dec 17. Bioorg Med Chem Lett. 2023. PMID: 36538993
Corrigendum to "Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors" [Bioorg. Med. Chem. Lett. 60 (2022) 128549].
Ma B, Metrick CM, Gu C, Hoemberger M, Bajrami B, Bame E, Huang J, Mingueneau M, Murugan P, Nevalainen M, Santoro JC, Tang H, Wang T, Hopkins BT. Ma B, et al. Among authors: metrick cm. Bioorg Med Chem Lett. 2022 Sep 15;72:128856. doi: 10.1016/j.bmcl.2022.128856. Epub 2022 Jun 18. Bioorg Med Chem Lett. 2022. PMID: 35728998 No abstract available.
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.
May-Dracka TL, Gao F, Hopkins BT, Hronowski X, Chen T, Chodaparambil JV, Metrick CM, Cullivan M, Enyedy I, Kaliszczak M, Kankel MW, Marx I, Michell-Robinson MA, Murugan P, Kumar PR, Rooney M, Schuman E, Sen A, Wang T, Ye T, Peterson EA. May-Dracka TL, et al. Among authors: metrick cm. ACS Med Chem Lett. 2022 Mar 3;13(4):665-673. doi: 10.1021/acsmedchemlett.1c00682. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450377 Free PMC article.
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Hopkins BT, Bame E, Bajrami B, Black C, Bohnert T, Boiselle C, Burdette D, Burns JC, Delva L, Donaldson D, Grater R, Gu C, Hoemberger M, Johnson J, Kapadnis S, King K, Lulla M, Ma B, Marx I, Magee T, Meissner R, Metrick CM, Mingueneau M, Murugan P, Otipoby KL, Polack E, Poreci U, Prince R, Roach AM, Rowbottom C, Santoro JC, Schroeder P, Tang H, Tien E, Zhang F, Lyssikatos J. Hopkins BT, et al. Among authors: metrick cm. J Med Chem. 2022 Jan 27;65(2):1206-1224. doi: 10.1021/acs.jmedchem.1c00926. Epub 2021 Nov 4. J Med Chem. 2022. PMID: 34734694
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Ma B, Bohnert T, Otipoby KL, Tien E, Arefayene M, Bai J, Bajrami B, Bame E, Chan TR, Humora M, MacPhee JM, Marcotte D, Mehta D, Metrick CM, Moniz G, Polack E, Poreci U, Prefontaine A, Sheikh S, Schroeder P, Smirnakis K, Zhang L, Zheng F, Hopkins BT. Ma B, et al. Among authors: metrick cm. J Med Chem. 2020 Nov 12;63(21):12526-12541. doi: 10.1021/acs.jmedchem.0c00702. Epub 2020 Aug 6. J Med Chem. 2020. PMID: 32696648
16 results