期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 5, 页码 582-586出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00157
关键词
DP2 receptor antagonist; severe asthma; clinical candidate
Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-ypacetic acid (compound 11, NVP-QAW039, fevipiprant), which exhibits improved potency on human eosinophils and Th2 cells, together with a longer receptor residence time, and is currently in clinical trials for severe asthma.
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