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Page 1
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
Loughran HM, Schirripa KM, Roecker AJ, Breslin MJ, Tong L, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Newman JA, Drolet RE, Cosden M, Jinn S, Flick RB, Liu X, Minnick C, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Loughran HM, et al. Among authors: fillgrove kl. ACS Med Chem Lett. 2023 Dec 21;15(1):123-131. doi: 10.1021/acsmedchemlett.3c00436. eCollection 2024 Jan 11. ACS Med Chem Lett. 2023. PMID: 38229758
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Roecker AJ, et al. Among authors: fillgrove kl. ACS Med Chem Lett. 2023 Jan 12;14(2):146-155. doi: 10.1021/acsmedchemlett.2c00441. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793422 Free PMC article.
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, Sur SM, Hartman GD. Brnardic EJ, et al. Among authors: fillgrove kl. Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31. Bioorg Med Chem Lett. 2010. PMID: 20409708
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.
Rudd MT, Manley PJ, Hanney B, Meng Z, Shu Y, de Leon P, Frie JL, Han Y, Wai JM, Yang ZQ, Perkins JJ, Hurzy DM, Manikowski JJ, Zhu H, Bungard CJ, Converso A, Meissner RS, Cosden ML, Hayashi I, Ma L, O'Brien J, Uebele VN, Schachter JB, Bhandari N, Ward GJ, Fillgrove KL, Lu B, Liang Y, Dubost DC, Puri V, Eddins DM, Vardigan JD, Drolet RE, Kern JT, Uslaner JM. Rudd MT, et al. Among authors: fillgrove kl. ACS Med Chem Lett. 2023 Jul 12;14(8):1088-1094. doi: 10.1021/acsmedchemlett.3c00210. eCollection 2023 Aug 10. ACS Med Chem Lett. 2023. PMID: 37583812 Free PMC article.
Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.
Garbaccio RM, Brnardic EJ, Fraley ME, Hartman GD, Hutson PH, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Small JH, Tang C, Kuo Y, Jacobson MA. Garbaccio RM, et al. Among authors: fillgrove kl. ACS Med Chem Lett. 2010 Jul 12;1(8):406-10. doi: 10.1021/ml100115a. eCollection 2010 Nov 11. ACS Med Chem Lett. 2010. PMID: 24900224 Free PMC article.
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA. Pero JE, et al. Among authors: fillgrove kl. ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985321 Free PMC article.
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA. Layton ME, et al. Among authors: fillgrove kl. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26810316
In Vitro Evaluation of the Drug Interaction Potential of Doravirine.
Bleasby K, Fillgrove KL, Houle R, Lu B, Palamanda J, Newton DJ, Lin M, Chan GH, Sanchez RI. Bleasby K, et al. Among authors: fillgrove kl. Antimicrob Agents Chemother. 2019 Mar 27;63(4):e02492-18. doi: 10.1128/AAC.02492-18. Print 2019 Apr. Antimicrob Agents Chemother. 2019. PMID: 30745395 Free PMC article.
Identification of second-generation P2X3 antagonists for treatment of pain.
Ginnetti AT, Paone DV, Stauffer SR, Potteiger CM, Shaw AW, Deng J, Mulhearn JJ, Nguyen DN, Segerdell C, Anquandah J, Calamari A, Cheng G, Leitl MD, Liang A, Moore E, Panigel J, Urban M, Wang J, Fillgrove K, Tang C, Cook S, Kane S, Salvatore CA, Graham SL, Burgey CS. Ginnetti AT, et al. Bioorg Med Chem Lett. 2018 May 1;28(8):1392-1396. doi: 10.1016/j.bmcl.2018.02.039. Epub 2018 Feb 21. Bioorg Med Chem Lett. 2018. PMID: 29548573
30 results