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Pyridone derivative crystal form and preparation method and application therefor

Grant US12583867B2 Kind: B2 Mar 24, 2026

Assignee

Jiangxi Caishi Pharmaceutical Technology Co., Ltd.

Inventors

Qing Shao, Libin Gan, Li Chen

Abstract

Crystals of (((R)-12′-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-6′,8′-dioxo-6′,8′,12′,12a′-tetrahydro-1′H,4′H-spiro[cyclopropane-1,3′-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin]-7′-yl)oxy)methyl methyl carbonate, i.e. compound of formula (1) or a solvate thereof and a preparation method therefor. The crystals include crystal form A, crystal form B, crystal form C, crystal form D, crystal form E, crystal form F, and single crystal. The crystal of the compound of formula (1) or a solvate thereof can be individually used for clinical treatment or in combination with other anti-influenza drugs such as neuraminidase inhibitors, nucleoside drugs, or PB2 inhibitors, are capable of clinically curing influenza patients quickly, and have very good activity and good bioavailability compared to existing pyridone derivatives. In addition, the stability, hygroscopicity, and storability of the crystals meet the requirements for pharmaceutical use.

CPC Classifications

C07D 498/14 C07D 498/20 C07B 2200/13 A61K 31/5383 A61K 31/55 A61P 31/16

Filing Date

2019-11-05

Application No.

17595013

Claims

33