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：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.

公开(公告)号：US11192878B2

公开(公告)日：2021-12-07

申请号：US16609805

申请日：2018-05-11

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Jong Yeon Hwang ,  Jae Du Ha ,  Sung Yun Cho ,  Pil Ho Kim ,  Chang Soo Yun ,  Chi Hoon Park ,  Chong Ock Lee ,  Sang Un Choi ,  Joo Youn Lee ,  Sunjoo Ahn

IPC: C07D401/04 ,  A61P35/00 ,  C07D401/14

Abstract: The present disclosure relates to a novel piperidine-2,6-dione derivative and a use thereof and, more specifically, to a piperidine-2,6-dione derivative compound having a structure of a thalidomide analog. A compound of chemical formula 1 according to the present disclosure specifically binds with CRBN protein, and is involved in functions thereof. Therefore, the compound of the present disclosure can be favorably used in the prevention or treatment of leprosy, chronic graft versus host disease, an inflammatory disease, or cancer, which are caused by actions of CRBN protein.

公开(公告)号：US11084824B2

公开(公告)日：2021-08-10

申请号：US16612592

申请日：2018-05-14

Applicant: Korea Research Institute of Chemical Technology

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

IPC: A61K31/519 ,  A61P25/16 ,  A61P35/00 ,  A61P37/00 ,  C07D487/04 ,  A23L33/10

Abstract: The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.

公开(公告)号：US20180111905A1

公开(公告)日：2018-04-26

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 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  A23L33/00 ,  A23L33/10

CPC classification number: C07D239/48 ,  A23L33/10 ,  A23L33/30 ,  A23L33/40 ,  A23V2002/00 ,  A61K31/505 ,  A61P35/00 ,  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.

公开(公告)号：US09499537B2

公开(公告)日：2016-11-22

申请号：US14278955

申请日：2014-05-15

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Jong Chan Son ,  Bong Jin Kim ,  Jae Hak Kim ,  Ill Young Lee ,  Chang Soo Yun ,  Sang Ho Lee ,  Chong Kgo Lee

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).

Abstract translation: 本发明涉及由化学式I表示的吡咯并吡啶衍生物及其外消旋物或其立体异构体或其药学上可接受的盐，涉及包含其作为活性成分的抗病毒组合物。 化学式I的化合物对野生型和抗性HIV-1具有优异的抗病毒活性和选择性，因此可用作获得性免疫缺陷综合征（AIDS）的治疗剂。