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.

公开(公告)号：US10369149B2

公开(公告)日：2019-08-06

申请号：US15567224

申请日：2015-12-30

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

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

IPC: A61K31/506 ,  C07D239/30 ,  C07D239/48 ,  A23L33/10 ,  A61P35/00 ,  C07B43/04 ,  C07C13/48

Abstract: The present invention relates to a 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.

公开(公告)号：US10100019B2

公开(公告)日：2018-10-16

申请号：US15565897

申请日：2016-04-06

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

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

IPC: C07D239/48 ,  A61K31/505 ,  A61P35/00 ,  A23L33/10 ,  A23L33/00 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.