Abstract: Disclosed are an ATX inhibitor, a preparation method therefor, and the use thereof, which belong to the technical field of pharmaceutical chemistry. In particular, the ATX inhibitor is a compound having the structure of formula I?, or a pharmaceutically acceptable salt, an ester, an isomer, a solvate, a prodrug or an isotope marker thereof. Compared with the existing ATX inhibitor GLPG-1690, the ATX inhibitor has higher inhibitory activity, also has excellent efficacy, in vitro/in vivo pharmacokinetic properties and safety, and has broad clinical application prospects.

Abstract: The present disclosure provides an elastase inhibitor prodrug and use thereof, being a compound of formula I or a pharmaceutically acceptable salt, ester, isomer or solvate thereof, prodrugs or isotopically labeled compound. Compared with the compound 52 (control example) in WO 2018/175173 A1, the compound disclosed herein has the advantages of high pulmonary exposure and long half-life. The prodrugs of the present disclosure significantly increase the concentration and residence time of the active compound (control example) in the lungs with significant improvements in pharmacokinetics in vivo compared to the control example.

Abstract: The present disclosure provides the synthesis and application of respiratory syncytial virus inhibitor, being a compound of formula I or a pharmaceutically acceptable salt, ester, isomer, solvate, prodrug or isotope label thereof. Compared with the existing inhibitors, the compounds of formula I have the advantages of superior activity and higher exposure in vivo.