Novel Imidazo[1,2-a]pyridine Derivatives with Potent Autotaxin/ENPP2 Inhibitor Activity

Novel Imidazo[1,2-a]pyridine Derivatives with Potent Autotaxin/ENPP2 Inhibitor Activity Descriptor: 2-[[2-ethyl-8-methyl-6-[4-[2-(3-oxidanylazetidin-1-yl)-2-oxidanylidene-ethyl]piperazin-1-yl]imidazo[1,2-a]pyridin-3-yl]-methyl-amino]-4-(4-fluorophenyl)-1,3-thiazole-5-carbonitrile, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... Authors: Fleury, D, Mueller, I, Lamers, M, Triballeau, N, Mollat, P, Vercheval, L. Deposit date: 2016-11-25 Release date: 2017-08-30 Last modified: 2024-11-13 Method: X-RAY DIFFRACTION (2.43 Å) Cite: Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis. J. Med. Chem., 60, 2017

具有强效自分泌运动因子（Autotaxin/ENPP2）抑制活性的新型咪唑并[1,2-a]吡啶衍生物
描述项：2-[[2-乙基-8-甲基-6-[4-[2-(3-羟基氮杂环丁烷-1-基)-2-氧代乙基]哌嗪-1-基]咪唑并[1,2-a]吡啶-3-基]-甲氨基]-4-(4-氟苯基)-1,3-噻唑-5-甲腈、2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖、钙离子……
作者：Fleury D、Mueller I、Lamers M、Triballeau N、Mollat P、Vercheval L
入库日期：2016-11-25
发布日期：2017-08-30
最后修改日期：2024-11-13
实验方法：X射线衍射（分辨率2.43埃）
引用文献：《发现2-[[2-乙基-6-[4-[2-(3-羟基氮杂环丁烷-1-基)-2-氧代乙基]哌嗪-1-基]-8-甲基咪唑并[1,2-a]吡啶-3-基]甲氨基]-4-(4-氟苯基)噻唑-5-甲腈（GLPG1690）：一款首创（First-in-Class）自分泌运动因子抑制剂，目前正处于特发性肺纤维化治疗的临床评估阶段》，《药物化学杂志》（J. Med. Chem.），60卷，2017年