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公开(公告)号:US20220249482A1
公开(公告)日:2022-08-11
申请号:US17675917
申请日:2022-02-18
Inventor: Kwangho Lee , Inji Shin , Gildon Choi , Chong Hak Chae , Hyeon Jeong Choe , Myoung Eun Jung , Byeong Uk Jeon , Byoung Chul Cho , Chae Won Park , Hwan Kim , Krishna Babu Duggirala
IPC: A61K31/506 , A61P35/00 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
Abstract: The present invention relates to a N2,N4-diphenylpyrimidin-2,4-diamine derivative, a method for preparing the same, and a pharmaceutical composition for the prevention or treatment of cancer, containing the same as an active ingredient. The derivative shows a relatively weak EGFR activity inhibitory effect on wild-type EGFR, a high inhibitory ability on EGFR mutation, and a high inhibitory ability on even FLT3 and FLT3 mutation, and thus, can be effectively used for the treatment of cancer with EGFR mutation or cancer with FLT3 or a mutation thereof, and the derivative shows a synergy effect at the time of combination administration, and thus can be effectively used for the treatment of combination administration.
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公开(公告)号:US11976059B2
公开(公告)日:2024-05-07
申请号:US17268869
申请日:2019-08-12
Inventor: Kwangho Lee , Gildon Choi , Seoyoung Lee , Jiwon Kim , Byoung Chul Cho , Chae Won Park , Jiyeon Yun
IPC: C07D401/14 , A61K45/06 , C07D403/06 , C07D403/14 , C07D471/04
CPC classification number: C07D403/06 , A61K45/06 , C07D401/14 , C07D403/14 , C07D471/04
Abstract: The present invention relates to an isoindolin-1-on derivative, a method for preparing same, and a pharmaceutical composition comprising same as an effective component for preventing or treating tumors, wherein the isoindolin-1-on derivative exhibits a high inhibitory effect on EGFR mutations, and thus can be beneficially used for the treatment of EGFR-mutated tumors, and the isoindolin-1-on derivative exhibits a significant synergistic effect when co-administered, and thus can be beneficially used in concomitant therapy.
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公开(公告)号:US20200179384A1
公开(公告)日:2020-06-11
申请号:US16622057
申请日:2018-12-06
Inventor: Kwangho Lee , Inji Shin , Gildon Choi , Chong Hak Chae , Hyeon Jeong Choe , Myoung Eun Jung , Byeong Uk Jeon , Byoung Chul Cho , Chae Won Park , Hwan Kim , Krishna Babu Duggirala
IPC: A61K31/506 , C07D413/12 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K45/06 , C07D401/12 , A61P35/00
Abstract: The present invention relates to a N2,N4-diphenylpyrimidin-2,4-diamine derivative, a method for preparing the same, and a pharmaceutical composition for the prevention or treatment of cancer, containing the same as an active ingredient. The derivative shows a relatively weak EGFR activity inhibitory effect on wild-type EGFR, a high inhibitory ability on EGFR mutation, and a high inhibitory ability on even FLT3 and FLT3 mutation, and thus, can be effectively used for the treatment of cancer with EGFR mutation or cancer with FLT3 or a mutation thereof, and the derivative shows a synergy effect at the time of combination administration, and thus can be effectively used for the treatment of combination administration.
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公开(公告)号:US20220281817A1
公开(公告)日:2022-09-08
申请号:US17637044
申请日:2020-11-19
Inventor: Kwangho Lee , Jiwon Kim , Byoung Chul Cho , Gildon Choi , Jiyeon Yun , Chae Won Park , Krishna Babu Duggirala , Chong Hak Chae , Seo Young Lee , A Reum Go
IPC: C07D209/14 , C07D209/18 , C07D401/12
Abstract: The present invention relates to a benzamide derivative, a preparation method therefor, and a pharmaceutical composition comprising same as an active ingredient for prevention or treatment of cancer. The benzamide derivative provided in an aspect of the present invention can be used for preventing or treating cancer by suppressing EGFR mutation, and exhibits a remarkable synergy effect on anticancer activity when administered in combination with an EGFR antagonist such as Cetuximab, thus finding advantageous uses as an anticancer agent.
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公开(公告)号:US11253516B2
公开(公告)日:2022-02-22
申请号:US16622057
申请日:2018-06-12
Inventor: Kwangho Lee , Inji Shin , Gildon Choi , Chong Hak Chae , Hyeon Jeong Choe , Myoung Eun Jung , Byeong Uk Jeon , Byoung Chul Cho , Chae Won Park , Hwan Kim , Krishna Babu Duggirala
IPC: A61K31/506 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D413/12 , C07D401/14 , C07D413/14 , C07D401/12
Abstract: The present invention relates to a N2,N4-diphenylpyrimidin-2,4-diamine derivative, a method for preparing the same, and a pharmaceutical composition for the prevention or treatment of cancer, containing the same as an active ingredient. The derivative shows a relatively weak EGFR activity inhibitory effect on wild-type EGFR, a high inhibitory ability on EGFR mutation, and a high inhibitory ability on even FLT3 and FLT3 mutation, and thus, can be effectively used for the treatment of cancer with EGFR mutation or cancer with FLT3 or a mutation thereof, and the derivative shows a synergy effect at the time of combination administration, and thus can be effectively used for the treatment of combination administration.
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公开(公告)号:US20210332029A1
公开(公告)日:2021-10-28
申请号:US17268869
申请日:2019-08-12
Inventor: Kwangho Lee , Gildon Choi , Seoyoung Lee , Jiwon Kim , Byoung Chul Cho , Chae Won Park , Jiyeon Yun
IPC: C07D403/06 , C07D471/04 , C07D403/14 , C07D401/14 , A61K45/06
Abstract: The present invention relates to an isoindolin-1-on derivative, a method for preparing same, and a pharmaceutical composition comprising same as an effective component for preventing or treating tumors, wherein the isoindolin-1-on derivative exhibits a high inhibitory effect on EGFR mutations, and thus can be beneficially used for the treatment of EGFR-mutated tumors, and the isoindolin-1-on derivative exhibits a significant synergistic effect when co-administered, and thus can be beneficially used in concomitant therapy.
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