公开(公告)号：US11028090B2

公开(公告)日：2021-06-08

申请号：US16480908

申请日：2018-01-25

Applicant: Dong Wha Pharm. Co., Ltd. ,  Korea Research Institute of Chemical Technology

Inventor： Kwangho Lee ,  Gildon Choi ,  Imran Ali ,  Joo Yun Lee ,  Jin Soo Lee ,  Whui Jung Park ,  Yong Tae Kim ,  Seung Hwan Kim ,  Jung Hwan Kim ,  Jae-Kyung Lim

IPC: C07D487/04 ,  A61P35/00 ,  C07D519/00

Abstract: Provided are a novel [1,2,4]triazolo[4,3-a]quinoxaline derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating bromodomain extra-terminal (BET) protein-related diseases including cancer and autoimmune diseases, containing the same as an active ingredient.

公开(公告)号：US10647686B2

公开(公告)日：2020-05-12

申请号：US16347480

申请日：2017-11-01

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Kwangho Lee ,  Gildon Choi ,  Na Ri Lee ,  Sang Jun Park ,  Myoung Eun Jung ,  Seong Jin Kim ,  Kyung-Min Yang ,  Jihee Lee

IPC: A61K31/505 ,  C07D239/48 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  C07D405/12

Abstract: The present invention relates to compounds represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is chloro or methyl; R2 is hydrogen or chloro; R3 is hydrogen, fluoro, chloro, bromo, methyl, ethyl, isopropyl, pentyl, hexyl, octyl, methoxy, phenoxy, (4-nitrophenyl)sulfonyl, piperidin-4-yl, or piperazin-1-yl; R4 is hydrogen, chloro, methyl or trifluoromethyl, phenoxy, (4-nitrophenyl)sulfonyl or piperidin-4-yl; or R3 and R4, together with the carbons to which they are attached, form a fused ring selected form the group consisting of: n is 1 or 2. These compounds according to the present invention remarkably inhibits activity of DRAK that inhibits signal systems of TGF-β, which is known to suppress cancer growth, and thus the novel pyrimidine compounds can be used as a pharmaceutical composition for preventing or treating cancer and can be used as a pharmaceutical composition for preventing or treating inflammatory disease.

公开(公告)号：US20200039984A1

公开(公告)日：2020-02-06

申请号：US16480908

申请日：2018-01-25

Applicant: Dong Wha Pharm. Co., Ltd. ,  Korea Research Institute of Chemical Technology

Inventor： Kwangho Lee ,  Gildon Choi ,  Imran Ali ,  Joo Yun Lee ,  Jin Soo Lee ,  Whui Jung Park ,  Yong Tae Kim ,  Seung Hwan Kim ,  Jung Hwan Kim ,  Jae-Kyung Lim

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00

Abstract: Provided are a novel [1,2,4]triazolo[4,3-a]quinoxaline derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating bromodomain extra-terminal (BET) protein-related diseases including cancer and autoimmune diseases, containing the same as an active ingredient.

公开(公告)号：US10053458B2

公开(公告)日：2018-08-21

申请号：US15319151

申请日：2015-05-21

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Chang Soo Yun ,  Hyoung Rae Kim ,  Sung Yun Cho ,  Hee Jung Jung ,  Kwangho Lee ,  Chong Hak Chae ,  Chong Ock Lee ,  Chi Hoon Park ,  Pilho Kim ,  Jong Yeon Hwang ,  Jae Du Ha ,  Sun Joo Ahn

IPC: C07D471/04 ,  C07D405/14 ,  C07D401/14 ,  C07D403/12 ,  C07D401/12

CPC classification number: C07D471/04 ,  A61K31/506 ,  C07D209/04 ,  C07D239/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

Abstract: The present invention relates to a pyrimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for prevention or treatment of cancer comprising the same as an effective ingredient. A compound according to the present invention has the good effect of inhibiting anaplastic lymphoma kinase (ALK) activity, whereby a therapeutic effect on cancer cells having an anaplastic lymphoma kinase (ALK) fusion protein such as EML4-ALK, NPM-ALK, etc. can be enhanced and it is expected that a recurrence of cancer will be effectively inhibited. As such, the compound can be effectively used in a pharmaceutical composition for prevention or treatment of cancer.

公开(公告)号：US20200179384A1

公开(公告)日：2020-06-11

申请号：US16622057

申请日：2018-12-06

Applicant: Korea Research Institute of Chemical Technology

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.