公开(公告)号：US20180065969A1

公开(公告)日：2018-03-08

申请号：US15672987

申请日：2017-08-09

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Han Na CHO ,  Eun Hye JU ,  Woo Young HUR ,  Ho Jong YOON ,  Chi Man SONG

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention provides a therapeutic agent of acute myeloid leukemia containing a 1,3,7-trisubstituted 3,4-dihydropyrimido[4,5-d]pyrimidine-2(1H)-one compound as an active ingredient, which has proliferation inhibitory activity for a human acute myeloid leukemia cell line OCI-AML3 having a NRAS mutant gene while having low inhibitory activity for wild type NRAS and has activity of inhibiting GCK and ACK1 protein kinases at the same time.

公开(公告)号：US20140148606A1

公开(公告)日：2014-05-29

申请号：US14066020

申请日：2013-10-29

Applicant: Korea Institute of Science and Technology

Inventor： Tae Bo SIM ,  Hwan KIM

IPC: C07C251/20

CPC classification number: A61K31/136

Abstract: Disclosed is a methyl violet derivative having inhibitory activity against allosteric focal adhesion kinase (FAK) and is useful as an agent for preventing or treating cancer.

Abstract translation: 公开了对变构性粘着斑激酶（FAK）具有抑制活性的甲基紫衍生物，可用作预防或治疗癌症的药剂。

公开(公告)号：US20230263792A1

公开(公告)日：2023-08-24

申请号：US18006584

申请日：2021-07-30

Applicant: PHAROS IBIO CO., LTD ,  KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Seung Hye CHOI ,  Han Na CHO ,  Woo Young HUR ,  Chi Man SONG ,  Ky Youb NAM ,  Jeong Hyeok YOON

IPC: A61K31/4535 ,  A61P35/02 ,  A61P29/00

CPC classification number: A61K31/4535 ,  A61P35/02 ,  A61P29/00

Abstract: The present invention relates to the use of a 2,3,5-substituted thiophene compound for the prevention, amelioration or treatment of mastocytosis. The 2,3,5-substituted thiophene compound has excellent inhibitory activity against the growth of mastocytosis cells and against an inflammatory response caused by mastocytosis, and thus may be effectively used for the prevention, amelioration or treatment of mastocytosis.

公开(公告)号：US20180065970A1

公开(公告)日：2018-03-08

申请号：US15674023

申请日：2017-08-10

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Woo Young HUR ,  Ho Jong YOON ,  Chi Man SONG ,  Eun Hye JU ,  Han na CHO ,  Hwan Geun CHOI

IPC: C07D487/04 ,  C07D401/14 ,  C07D403/14

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14

Abstract: The present invention provides a pharmaceutical composition, as an effective ingredient, a urea compound having a protein kinase inhibitory activity and containing a 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one skeleton, and a pharmaceutically acceptable salt thereof.

公开(公告)号：US20160145240A1

公开(公告)日：2016-05-26

申请号：US14947204

申请日：2015-11-20

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Ho Jong YOON ,  Ji Hye YOON ,  Woo Young HUR ,  Eun Joo ROH ,  Yeon Ui KWAK

IPC: C07D403/04 ,  C07D471/04 ,  C07D487/04 ,  C07D401/14

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04

Abstract: A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an active ingredient.

Abstract translation: 杂芳基胺化合物包括蛋白激酶抑制活性，其药学上可接受的盐和用于预防和治疗由异常细胞生长引起的疾病的药物组合物，其含有该化合物作为活性成分。

公开(公告)号：US20190315726A1

公开(公告)日：2019-10-17

申请号：US16362571

申请日：2019-03-22

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： So Ha LEE ,  Kyung Ho YOO ,  Eun Joo ROH ,  Tae Bo SIM ,  Tae Young KIM ,  Jae Ho KIM

IPC: C07D405/14 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D239/48 ,  A61P35/00 ,  A61P25/28 ,  A61P37/02 ,  A61P29/00

Abstract: Disclosed are a novel pyrimidine derivative compound, a pharmaceutically acceptable salt thereof, a method for preparing the compound and a pharmaceutical use of the compound as an anticancer agent or a therapeutic agent for degenerative brain diseases. Specifically, the novel pyrimidine derivative compound has excellent inhibitory activities against kinase enzymes such as ARK5/NUAK1, ACK1, FLT3, JAK1, JAK2 and JAK2 (V617F) and thus is useful for treating and preventing leukemia, ovarian cancer, breast cancer, non-small cell carcinoma, colorectal cancer, glioma, and brain protein abnormalities such as Alzheimer's disease, progressive supranuclear palsy and frontotemporal dementia, that is, degenerative diseases caused by Tau deposition.

公开(公告)号：US20190135765A1

公开(公告)日：2019-05-09

申请号：US16090072

申请日：2017-03-30

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY

Inventor： Tae Bo SIM ,  Woo Young HUR ,  Ho Jong YOON ,  Chi Man SONG ,  In Jae SHUN ,  Byeong Yun LIM ,  HanNa CHO ,  Seung Hye CHOI ,  Gu KONG ,  Jeong Yeon LEE

IPC: C07D239/42 ,  A61P35/00 ,  C07D405/12 ,  C07D409/12 ,  C07D403/12

Abstract: The present invention relates to a novel pyrimidine-4-carboxylic acid derivative having an anticancer activity, and the compound of the present invention is useful as a drug for treating and preventing tumor diseases.

公开(公告)号：US20180148459A1

公开(公告)日：2018-05-31

申请号：US15821962

申请日：2017-11-24

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Ho Jong YOON ,  In Jae SHIN ,  Yun Ju NAM ,  Hwan Geun CHOI

IPC: C07D495/04 ,  A61P35/00

CPC classification number: C07D495/04 ,  A61P35/00

Abstract: The present invention relates to a novel 4-((2-acrylamidophenyl)amino)thieno[3,2-d]pyrimidine-7-carboxamide compound, an anticancer agent containing the compound as an active ingredient and an intermediate compound for preparing the compound.

公开(公告)号：US20230270733A1

公开(公告)日：2023-08-31

申请号：US18006582

申请日：2021-07-30

Applicant: PHAROS IBIO CO., LTD. ,  KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Seung Hye CHOI ,  Han Na CHO ,  Nam Kyoung KIM ,  Woo Young HUR ,  Chi Man SONG ,  Ky Youb NAM ,  Jeong Hyeok YOON

IPC: A61K31/4535 ,  A23L33/10 ,  A61P35/00

CPC classification number: A61K31/4535 ,  A23L33/10 ,  A61P35/00

Abstract: The present invention relates to the use of a 2,3,5-substituted thiophene compound for the prevention, amelioration or treatment of gastrointestinal stromal tumor. The 2,3,5-substituted thiophene compound exhibits high inhibitory activity against the growth of gastrointestinal stromal tumor, and thus may be effectively used for the prevention, amelioration or treatment of gastrointestinal stromal tumor.

公开(公告)号：US20230120564A1

公开(公告)日：2023-04-20

申请号：US17794314

申请日：2020-07-14

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Tae Bo SIM ,  Chan Sun PARK ,  Seung Hye CHOI ,  Han Na CHO ,  Sandip SENGUPTA ,  In Jae SHIN ,  Woo Young HUR ,  Jayprakash Narayan KUMAR

IPC: C07D471/04

Abstract: The present invention relates to a pyrido[[3,4-d]pyrimidine derivative compound showing excellent anti-proliferative efficacy against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating, or treating cancer metastasis and proliferative diseases containing the same as an active ingredient, and an anticancer composition for cancer cells. The compound exhibits excellent inhibitory activity and anti-proliferative efficacy against cancer cells, and thus the compound is useful not only for inhibiting cancer cells, but also for preventing cancer metastasis and proliferative diseases or for treating cancer.