- Patent Title: Isoxazole derivative as mutant isocitrate dehydrogenase 1 inhibitor
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Application No.: US15516362Application Date: 2015-10-01
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Publication No.: US10040791B2Publication Date: 2018-08-07
- Inventor: Shoichi Saito , Masao Itoh , Tetsunori Fujisawa , Hironao Saito , Yohei Kiyotsuka , Hideaki Watanabe , Hironori Matsunaga , Yoshiko Kagoshima , Tetsuya Suzuki , Yoko Ogawara , Kazuo Kitabayashi
- Applicant: Daiichi Sankyo Company, Limited , National Cancer Center
- Applicant Address: JP Chuo-ku JP Chuo-ko
- Assignee: Daiichi Sankyo Company, Limited,National Cancer Center
- Current Assignee: Daiichi Sankyo Company, Limited,National Cancer Center
- Current Assignee Address: JP Chuo-ku JP Chuo-ko
- Agency: Christensen O'Connor Johnson Kindness PLLC
- Priority: JP2014-203475 20141001; JP2015-116774 20150609
- International Application: PCT/JP2015/077916 WO 20151001
- International Announcement: WO2016/052697 WO 20160407
- Main IPC: A61K31/437
- IPC: A61K31/437 ; A61K31/454 ; A61K31/5377 ; A61K31/422 ; A61K31/4439 ; A61K31/496 ; C07D413/06 ; C07D413/14 ; C07D471/04

Abstract:
It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.
Public/Granted literature
- US20170313696A1 ISOXAZOLE DERIVATIVE AS MUTANT ISOCITRATE DEHYDROGENASE 1 INHIBITOR Public/Granted day:2017-11-02
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