日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct M(4) Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust In Vivo Efficacy

VU6025733 (AG06827) 的发现:一种高选择性、口服生物利用度高、结构独特的 M(4) 毒蕈碱乙酰胆碱受体正向变构调节剂 (PAM),具有强大的体内疗效

Gregro, Alison R; Park, Charlotte; Long, Madeline F; Baker, Logan A; Bollinger, Katrina A; Ringuette, Anna E; Peng, Li; Luscombe, Vincent B; Billard, Natasha B; Rodriguez, Alice L; Niswender, Colleen M; Peng, Weimin; Dickerson, Jonathan W; Rook, Jerri M; O'Neill, Jordan; Chang, Sichen; Boonen, Harrie C M; Jensen, Thomas; Thomsen, Morten S; Bridges, Thomas M; Boutaud, Olivier; Conn, P Jeffrey; Engers, Darren W; Lindsley, Craig W; Temple, Kayla J

Application of Deuterium in an M(1) Positive Allosteric Modulator Back-Up Program: The Discovery of VU6045422

氘在M(1)正变构调节剂备用方案中的应用:VU6045422的发现

Engers, Julie L; Li, Jinming; Han, Changho; Long, Madeline F; Gregro, Alison R; Presley, Christopher C; Dickerson, Jonathan W; Peng, Weimin; Cho, Hyekyung P; Rodriguez, Alice L; Xiang, Zixiu; Boutaud, Olivier; O'Carroll, Colin; Dey, P Markus; Burstein, Ethan S; Niswender, Colleen M; Rook, Jerri M; Conn, P Jeffrey; Engers, Darren W; Lindsley, Craig W

Discovery of structurally distinct tricyclic M(4) positive allosteric modulator (PAM) chemotypes - Part 2

发现结构不同的三环M(4)正变构调节剂(PAM)化学类型——第二部分

Long, Madeline F; Capstick, Rory A; Spearing, Paul K; Engers, Julie L; Gregro, Alison R; Bollinger, Sean R; Chang, Sichen; Luscombe, Vincent B; Rodriguez, Alice L; Cho, Hyekyung P; Niswender, Colleen M; Bridges, Thomas M; Conn, P Jeffrey; Lindsley, Craig W; Engers, Darren W; Temple, Kayla J

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M(4) PAMs

受醛氧化酶 (AO) 代谢启发的 SAR 研究:新型中枢神经系统穿透性三环 M(4) PAM 的发现

Chopko, Trevor C; Han, Changho; Gregro, Alison R; Engers, Darren W; Felts, Andrew S; Poslusney, Mike S; Bollinger, Katrina A; Morrison, Ryan D; Bubser, Michael; Lamsal, Atin; Luscombe, Vincent B; Cho, Hyekyung P; Schnetz-Boutaud, Nathalie C; Rodriguez, Alice L; Chang, Sichen; Daniels, J Scott; Stec, Donald F; Niswender, Colleen M; Jones, Carrie K; Wood, Michael R; Wood, Michael W; Duggan, Mark E; Brandon, Nicholas J; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W; Melancon, Bruce J

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

基于5,6-二甲基-4-(哌啶-1-基)噻吩并[2,3-d]嘧啶核心结构,发现并优化了一系列新型高中枢神经系统渗透性的M4 PAMs。

Wood, Michael R; Noetzel, Meredith J; Engers, Julie L; Bollinger, Katrina A; Melancon, Bruce J; Tarr, James C; Han, Changho; West, Mary; Gregro, Alison R; Lamsal, Atin; Chang, Sichen; Ajmera, Sonia; Smith, Emery; Chase, Peter; Hodder, Peter S; Bubser, Michael; Jones, Carrie K; Hopkins, Corey R; Emmitte, Kyle A; Niswender, Colleen M; Wood, Michael W; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W