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1.发明授权N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or pharmaceutically acceptable salt thereof, and composition containing same as active ingredient for preventing or treating cancer 有权N2，N4-双（4-（哌嗪-1-基）苯基）吡啶嘧啶-2,4-二胺衍生物或其药学上可接受的盐，以及含有作为预防或治疗癌症的活性成分的组合物公开(公告)号：US09199944B2
公开(公告)日：2015-12-01
申请号：US14617079
申请日：2015-02-09
Inventor： Kwangho Lee , Hyoung Rae Kim , Chi Hoon Park , Chong Ock Lee , Jong Kook Lee , Hee Jung Jung , Sung Yun Cho , Chong Hak Chae , Sang Un Choi , Jae Du Ha
IPC: A61K31/506 , C07D239/48 , C07D403/12 , C07D403/14
CPC classification number: C07D239/48 , A61K31/506 , C07D403/12 , C07D403/14
Abstract: Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.
Abstract translation: 本文公开了一种新的N 2，N 4 - 双（4-（哌嗪-1-基）苯基）嘧啶-2,4-二胺衍生物或其药学上可接受的盐和用于预防或治疗含有其的癌症的药物组合物 作为活性成分。 本发明的化合物对于间变性淋巴瘤激酶（ALK）和活化的cdc42相关激酶（ACK1）的活性具有优异的抑制作用，因此可以改善对具有间变性淋巴瘤激酶融合蛋白的癌细胞的治疗效果，例如 EML4-ALK和NPM-ALK，并且还有效地预防癌症的复发因此可用作用于预防和治疗癌症的药物组合物。
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公开(公告)号：US20240246948A1
公开(公告)日：2024-07-25
申请号：US18561855
申请日：2022-05-13
Inventor： Seockyong Kang , Daseul Yoon , Hyejeong Kim , Som Yi Park , Dongkyu Kim , Ji-Yeon Park , Yeji Byeon , Hye-Im Jo , Seung Hee Jung , Seong-Il Choi , Seung Chul Lee , Kwangho Lee
IPC: C07D413/14 , A61K31/454 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D401/12 , C07D401/14 , C07D403/14 , C07D487/08
CPC classification number: C07D413/14 , A61K31/454 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D401/12 , C07D401/14 , C07D403/14 , C07D487/08
Abstract: The present invention relates to a benzamide derivative, a method for preparing same, and a pharmaceutical composition for the prevention or treatment of cancer, containing same as an active ingredient. The benzamide derivative according to an aspect of the present invention can be used in the prevention or treatment of cancer by suppressing EGFR mutation, and, when administered in combination with an EGFR antagonist such as cetuximab, exhibits a significantly synergistic effect on anticancer activity, and thus can be effectively used as an anticancer agent.
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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：US11365215B2
公开(公告)日：2022-06-21
申请号：US15921596
申请日：2018-03-14
Applicant: Research & Business Foundation Sungkyunkwan University , Korea Research Institute of Chemical Technology
Inventor： Kwangho Lee , Sang Dal Rhee , Gildon Choi , Imran Ali , Chong Hak Chae , Moon Kook Jeon , Seok Hee Park , Youn Sook Lee
IPC: A61K47/54 , C07K5/117 , C07K5/103 , C07K5/107 , C07K5/097 , C07D207/04 , A61P1/00 , C07D403/06 , A61K38/00
Abstract: Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.
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5.发明申请PYRROLIDINE CARBOXAMIDO DERIVATIVES AND METHODS FOR PREPARING AND USING THE SAME 审中-公开吡咯烷羧酰胺衍生物及其制备和使用方法公开(公告)号：US20170008924A1
公开(公告)日：2017-01-12
申请号：US15205853
申请日：2016-07-08
Applicant: Research & Business Foundation Sungkyunkwan University , Korea Research Institute of Chemical Technology
Inventor： Kwangho Lee , Sang Dal Rhee , Gildon Choi , Imran Ali , Chong Hak Chae , Moon Kook Jeon , Seok Hee Park , Youn Sook Lee
CPC classification number: C07K5/1024 , A61K38/00 , A61K47/542 , C07D207/04 , C07D403/06 , C07K5/0823 , C07K5/1008 , C07K5/1016
Abstract: Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.
Abstract translation: 提供能够预防，改善和/或治疗炎症性疾病，包括炎症性肠病的吡咯烷甲酰胺衍生物，其光学异构体及其盐及其制备和使用方法。
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Patent Agency Ranking
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：US20180208625A1
公开(公告)日：2018-07-26
申请号：US15921596
申请日：2018-03-14
Applicant: Research & Business Foundation Sungkyunkwan University , Korea Research Institute of Chemical Technology
Inventor： Kwangho Lee , Sang Dal Rhee , Gildon Choi , Imran Ali , Chong Hak Chae , Moon Kook Jeon , Seok Hee Park , Youn Sook Lee
CPC classification number: C07K5/1024 , A61K38/00 , A61K47/542 , C07D207/04 , C07D403/06 , C07K5/0823 , C07K5/1008 , C07K5/1016
Abstract: Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.
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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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