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Page 1
Neuroactive Steroid N-Methyl-d-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity.
La DS, Salituro FG, Martinez Botella G, Griffin AM, Bai Z, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lewis MC, Quirk MC, Robichaud AJ. La DS, et al. Among authors: hoffmann ec. J Med Chem. 2019 Aug 22;62(16):7526-7542. doi: 10.1021/acs.jmedchem.9b00591. Epub 2019 Aug 13. J Med Chem. 2019. PMID: 31390523
SAGE-718: A First-in-Class N-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.
Hill MD, Blanco MJ, Salituro FG, Bai Z, Beckley JT, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lanzetta D, Lewis M, Quirk MC, Robichaud AJ. Hill MD, et al. Among authors: hoffmann ec. J Med Chem. 2022 Jul 14;65(13):9063-9075. doi: 10.1021/acs.jmedchem.2c00313. Epub 2022 Jul 2. J Med Chem. 2022. PMID: 35785990
Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.
Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Blanco MJ, Belfort GM, Dai J, Loya CM, Ackley MA, Althaus AL, Grossman SJ, Hoffmann E, Doherty JJ, Robichaud AJ. Martinez Botella G, et al. J Med Chem. 2017 Sep 28;60(18):7810-7819. doi: 10.1021/acs.jmedchem.7b00846. Epub 2017 Aug 17. J Med Chem. 2017. PMID: 28753313
Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator.
Althaus AL, Ackley MA, Belfort GM, Gee SM, Dai J, Nguyen DP, Kazdoba TM, Modgil A, Davies PA, Moss SJ, Salituro FG, Hoffmann E, Hammond RS, Robichaud AJ, Quirk MC, Doherty JJ. Althaus AL, et al. Neuropharmacology. 2020 Dec 15;181:108333. doi: 10.1016/j.neuropharm.2020.108333. Epub 2020 Sep 22. Neuropharmacology. 2020. PMID: 32976892 Free PMC article.
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.
Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Shen K, Belfort GM, Loya CM, Ackley MA, Grossman SJ, Hoffmann E, Jia S, Wang J, Doherty JJ, Robichaud AJ. Martinez Botella G, et al. J Med Chem. 2015 Apr 23;58(8):3500-11. doi: 10.1021/acs.jmedchem.5b00032. Epub 2015 Apr 14. J Med Chem. 2015. PMID: 25799373
Brexanolone as adjunctive therapy in super-refractory status epilepticus.
Rosenthal ES, Claassen J, Wainwright MS, Husain AM, Vaitkevicius H, Raines S, Hoffmann E, Colquhoun H, Doherty JJ, Kanes SJ. Rosenthal ES, et al. Ann Neurol. 2017 Sep;82(3):342-352. doi: 10.1002/ana.25008. Epub 2017 Sep 11. Ann Neurol. 2017. PMID: 28779545 Free PMC article. Clinical Trial.
Brexanolone (SAGE-547 injection) in post-partum depression: a randomised controlled trial.
Kanes S, Colquhoun H, Gunduz-Bruce H, Raines S, Arnold R, Schacterle A, Doherty J, Epperson CN, Deligiannidis KM, Riesenberg R, Hoffmann E, Rubinow D, Jonas J, Paul S, Meltzer-Brody S. Kanes S, et al. Lancet. 2017 Jul 29;390(10093):480-489. doi: 10.1016/S0140-6736(17)31264-3. Epub 2017 Jun 12. Lancet. 2017. PMID: 28619476 Clinical Trial.
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.
Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, Davies AM, Peng B, Su M, Zhang HJ, Hoffmann E, Rivard C, Green I, Howard T, Pollard H, Read J, Alimzhanov M, Bebernitz G, Bell K, Ye M, Huszar D, Zinda M. Ioannidis S, et al. J Med Chem. 2011 Jan 13;54(1):262-76. doi: 10.1021/jm1011319. Epub 2010 Dec 7. J Med Chem. 2011. PMID: 21138246
13 results