Catalyst-Free Cyclization- and Curtius Rearrangement-Induced Functional Group Transformation: An Improved Synthetic Strategy of First-in-Class ATX Inhibitor Ziritaxestat (GLPG-1690)
Author:
Affiliation:
1. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
Funder
Ministry of Education of the People's Republic of China
National Natural Science Foundation of China
Shenyang Pharmaceutical University
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry,Physical and Theoretical Chemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.9b00511
Reference23 articles.
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2. 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
3. European Respiratory Society 2015 Annual Congress. Amsterdam, The Netherlands - September 26-30, 2015
4. Desroy, N.; Heckmann, B.; Brys, R.; Joncour, A.; Peixoto, C.; Bock, X.; Housseman, C. Compounds and Pharmaceutical Compositions Thereof for the Treatment of Inflammatory Disorders. US9,249,1412016.
5. Identification and development of 2-methylimidazo[1,2-a]pyridine-3-carboxamides as Mycobacterium tuberculosis pantothenate synthetase inhibitors
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