公开(公告)号：US20230027716A1

公开(公告)日：2023-01-26

申请号：US17770630

申请日：2020-10-22

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Seong Shick RYU ,  Yun Ju NAM ,  Woo Young HUR

IPC: C07D403/12 ,  C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  A61P35/00

Abstract: The present invention relates to: a compound selected from among a novel pyridinyltriazine derivative having protein kinase inhibitory activity, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof; a method for preparing the compound; and a pharmaceutical composition which is for preventing, alleviating, or treating cancer and comprises the compound. A novel compound according to the present invention exhibits excellent inhibitory effects against FGFR, which is a major trigger of bladder cancer, endometrial cancer, etc., point mutations thereof, and various protein kinases other than FGFR involved in signal transduction, and is thus effective as an agent for preventing and treating abnormal cell growth diseases caused by such protein kinases.

公开(公告)号：US20210061810A1

公开(公告)日：2021-03-04

申请号：US17002748

申请日：2020-08-25

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Seo Jung HAN ,  Tae Bo SIM ,  Do Hee OH ,  Jae Eun CHEONG ,  Dong Keon HWANG

IPC: C07D487/04 ,  A61P35/00

Abstract: Disclosed are a compound selected from novel pyrimido[4,5-d]pyrimidin-2-one derivative compounds having excellent anti-proliferative activity against cancer cells, pharmaceutically acceptable salts thereof, hydrates thereof and stereoisomers thereof, a method for preparing the compound, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative diseases containing the compound as an active ingredient, and an anticancer composition against cancer cells, containing the compound as an active ingredient. The compounds of this invention exhibit most excellent selective inhibitory activity agaist LCK and anti-proliferative activity against cancer cells, thus being useful for inhibiting cancer cells, and for preventing or treating cancer metastasis and proliferative diseases.

公开(公告)号：US20180050036A1

公开(公告)日：2018-02-22

申请号：US15677742

申请日：2017-08-15

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Ho Jong YOON ,  Woo Young HUR ,  Yun Ju NAM ,  Hwan Geun CHOI

IPC: A61K31/506

CPC classification number: A61K31/506 ,  A61K31/519 ,  A61K31/5377

Abstract: The present invention relates to a therapeutic agent for chronic myelogenous leukemia with reduced drug-resistance and side-effects containing a 1,6-disubstituted indole compound.

公开(公告)号：US20140155635A1

公开(公告)日：2014-06-05

申请号：US14066053

申请日：2013-10-29

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Ho Jong Yoon ,  Ji Nyeo Kim

IPC: C07D313/00 ,  C07D493/08 ,  C07D317/30 ,  C07D407/10 ,  C07D319/08 ,  C07D317/32

CPC classification number: C07D313/00 ,  C07D317/20 ,  C07D317/22 ,  C07D317/30 ,  C07D317/32 ,  C07D319/08 ,  C07D407/10 ,  C07D493/08

Abstract: Disclosed are a novel resorcyclic acid lactone compound with inhibitory activity against protein kinases, a pharmaceutically acceptable salt thereof, a method for the synthesis thereof, and a pharmaceutical composition for the treatment and prevention of various cancer diseases comprising the same as an active ingredient. The novel resorcyclic acid lactone compound is useful as a therapeutic for cancer diseases, especially blood cancer, inter alia, acute myeloid leukemia (AML).

Abstract translation: 本发明公开了一种对蛋白激酶具有抑制活性的新型重链内酯化合物，其药学上可接受的盐，其合成方法以及用于治疗和预防包含其的活性成分的各种癌症疾病的药物组合物。 新型的再环内酯化合物可用作癌症疾病，特别是血液癌，尤其是急性骨髓性白血病（AML）的治疗剂。