Invention Grant
- Patent Title: Crystal form of deuterated AZD9291, preparation method therefor, and use thereof
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Application No.: US16615771Application Date: 2018-05-22
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Publication No.: US10882845B2Publication Date: 2021-01-05
- Inventor: Yusheng Wu , Yang Geng , Apeng Liang , Chengshan Niu
- Applicant: TYK MEDICINES INC.
- Applicant Address: CN Zhejiang
- Assignee: TYK MEDICINES INC.
- Current Assignee: TYK MEDICINES INC.
- Current Assignee Address: CN Zhejiang
- Agency: Novick, Kim & Lee, PLLC
- Agent Bin Lu
- Priority: CN201710374457 20170524
- International Application: PCT/CN2018/087902 WO 20180522
- International Announcement: WO2018/214886 WO 20181129
- Main IPC: C07D401/04
- IPC: C07D401/04 ; A61P35/04 ; C07D403/04 ; C07C309/04

Abstract:
A crystal form of a deuterated AZD9291 has an X-ray powder diffraction measured using Cu-Kα rays with diffraction peaks at 7.1±0.2, 8.5±0.2, 9.4±0.2, 10.3±0.2, 15.1±0.2, 16.3±0.2, 18.7±0.2, 22.0±0.2, 25.6±0.2, and 26.0±0.2. The crystal form of the deuterated AZD9291 is used in the preparation of medicaments for the treatment of cancer. The crystal form of the deuterated AZD9291 provided by the present invention has stable physical and chemical properties and good metabolic stability, and blood concentrations in vivo and concentrations in the brain thereof are significantly improved, achieving an improved therapeutic effect.
Public/Granted literature
- US20200157080A1 CRYSTAL FORM OF DEUTERATED AZD9291, PREPARATION METHOD THEREFOR, AND USE THEREOF Public/Granted day:2020-05-21
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