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Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Ghosh S, Hou X, Houle C, Karki K, Lazzaro JT, Mancuso JY, Marcek JM, Miller EL, Moen MA, O'Neil S, Sakurada I, Skaddan M, Parikh V, Smith DL, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Won A, Wright AS, Whritenour J, Zasadny K, Zaleska MM, Zhang L, Shaffer CL. Stepan AF, et al. Among authors: mancuso jy. J Med Chem. 2017 Sep 28;60(18):7764-7780. doi: 10.1021/acs.jmedchem.7b00604. Epub 2017 Sep 13. J Med Chem. 2017. PMID: 28817277
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL. Zhang L, et al. Among authors: mancuso jy. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
Clinical trial of an inhibitor of RAGE-Aβ interactions in Alzheimer disease.
Galasko D, Bell J, Mancuso JY, Kupiec JW, Sabbagh MN, van Dyck C, Thomas RG, Aisen PS; Alzheimer's Disease Cooperative Study. Galasko D, et al. Among authors: mancuso jy. Neurology. 2014 Apr 29;82(17):1536-42. doi: 10.1212/WNL.0000000000000364. Epub 2014 Apr 2. Neurology. 2014. PMID: 24696507 Free PMC article. Clinical Trial.
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of PF-06751979, a Potent and Selective Oral BACE1 Inhibitor: Results from Phase I Studies in Healthy Adults and Healthy Older Subjects.
Qiu R, Ahn JE, Alexander R, Brodney MA, He P, Leurent C, Mancuso J, Margolin RA, Tankisheva E, Chen D. Qiu R, et al. Among authors: mancuso j. J Alzheimers Dis. 2019;71(2):581-595. doi: 10.3233/JAD-190228. J Alzheimers Dis. 2019. PMID: 31424395 Free PMC article. Clinical Trial.
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of PF-06817024 in Healthy Participants, Participants with Chronic Rhinosinusitis with Nasal Polyps, and Participants with Atopic Dermatitis: A Phase 1, Randomized, Double-Blind, Placebo-Controlled Study.
Danto SI, Tsamandouras N, Reddy P, Gilbert S, Mancuso J, Page K, Peeva E, Vincent MS, Beebe JS. Danto SI, et al. Among authors: mancuso j. J Clin Pharmacol. 2024 May;64(5):529-543. doi: 10.1002/jcph.2360. Epub 2023 Oct 30. J Clin Pharmacol. 2024. PMID: 37772436 Clinical Trial.
294 results