- 专利标题: Solid forms of stemospironine and its salts
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申请号: US16646694申请日: 2018-09-07
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公开(公告)号: US11414427B2公开(公告)日: 2022-08-16
- 发明人: Yang Ye , Sheng Yao , Hui-Yin Li , Qun Li
- 申请人: Yang Ye , Sheng Yao , Hui-Yin Li , Qun Li
- 申请人地址: CN Shanghai; CN Shanghai; US DE Hockessen; US DE Newark
- 专利权人: Yang Ye,Sheng Yao,Hui-Yin Li,Qun Li
- 当前专利权人: Yang Ye,Sheng Yao,Hui-Yin Li,Qun Li
- 当前专利权人地址: CN Shanghai; CN Shanghai; US DE Hockessen; US DE Newark
- 代理机构: Wenderoth, Lind & Ponack, L.L.P.
- 国际申请: PCT/US2018/049851 WO 20180907
- 国际公布: WO2019/055294 WO 20190321
- 主分类号: C07D491/20
- IPC分类号: C07D491/20 ; C07C59/255 ; C07C309/04 ; C07C309/05 ; C07C309/19
摘要:
Disclosed are stemospironine salts of Formula 1: wherein HX represents HCl, HBr, L-tartaric acid, D-tartaric acid, sulfuric acid, (+)-(1S)-10-camphorsulfonic acid, ethanesulfonic acid and ethane-1,2-disulfonic acid. This invention also provides crystalline polymorph forms of the compound of Formula 1 wherein HX is HCl, stemospironine hydrochloride. This invention also provides a new crystalline form of the compound of Formula 2, stemospironine free base: Also disclosed are compositions containing one or more compounds of Formula 1, methods for controlling cough comprising administering a therapeutically effective amount of a compound of Formula 1, and methods for preparing compounds of Formula 1. Also disclosed is a method for preparing crystalline stemospironine hydrochloride polymorph Form II from stemospironine hydrochloride polymorph Form I.
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