公开(公告)号：US10155767B2

公开(公告)日：2018-12-18

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

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：US08871950B1

公开(公告)日：2014-10-28

申请号：US14065793

申请日：2013-10-29

Applicant: Korea Institute of Science and Technology

Inventor： Tae Bo Sim ,  Ho Jong Yoon ,  Eun Joo Roh

IPC: C07D203/10 ,  C07C229/08 ,  C07C227/02

CPC classification number: C07C227/02 ,  C07B2200/07 ,  C07C213/08 ,  C07C217/28 ,  C07C229/22 ,  C07D203/10

Abstract: The present invention relates to a method for preparing (+)-polyoxamic acid and a novel intermediate compound synthesized during preparation thereof.The preparation method according to the present invention allows preparation of (+)-polyoxamic acid with high optical purity in high yield. In particular, the preparation method is useful for mass production because the process is simple.

Abstract translation: 本发明涉及一种制备（+） - 聚氧杂恶唑酸的方法及其制备过程中合成的新型中间体化合物。 根据本发明的制备方法允许以高产率制备具有高光学纯度的（+） - 多异羟肟酸。 特别是，由于该方法简单，所以制备方法对于批量生产是有用的。

公开(公告)号：US10442796B2

公开(公告)日：2019-10-15

申请号：US15998791

申请日：2018-08-16

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION

Inventor： Tae Bo Sim ,  Woo Young Hur ,  Chi Man Song ,  Ho Jong Yoon ,  Seung Hye Choi ,  Han Na Cho ,  Hwan Geun Choi ,  Nam Doo Kim ,  Jung Beom Son ,  Eun Hwa Ko ,  Hyun Kyoung Kim ,  Joong Heui Cho ,  Seock Yong Kang ,  So Young Kim ,  Yi Kyung Ko ,  Seung Yeon Lee ,  Suk Kyoon Yoon ,  Jae Hyun Bae

IPC: C07D409/12 ,  A61P35/02 ,  A61K31/381 ,  A61K31/4436 ,  C07D333/10 ,  C07D409/14

Abstract: The present invention relates to a novel 2,3,5-substituted thiophene compound having inhibitory activity against kinases, an anticancer agent including the compound as an active ingredient, and a method for preparing the compound.

公开(公告)号：US10130631B2

公开(公告)日：2018-11-20

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 ,  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：US09586936B2

公开(公告)日：2017-03-07

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: A61K31/506 ,  C07D403/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04

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：US20190047993A1

公开(公告)日：2019-02-14

申请号：US15998791

申请日：2018-08-16

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION

Inventor： Tae Bo Sim ,  Woo Young Hur ,  Chi Man Song ,  Ho Jong Yoon ,  Seung Hye Choi ,  Han Na Cho ,  Hwan Geun Choi ,  Nam Doo Kim ,  Jung Beom Son ,  Eun Hwa Ko ,  Hyun Kyoung Kim ,  Joong Heui Cho ,  Seock Yong Kang ,  So Young Kim ,  Yi Kyung Ko ,  Seung Yeon Lee ,  Suk Kyoon Yoon ,  Jae Hyun Bae

IPC: C07D409/12 ,  A61P35/02 ,  C07D409/14

CPC classification number: C07D409/12 ,  A61K31/381 ,  A61K31/4436 ,  A61P35/02 ,  C07D333/10 ,  C07D409/14 ,  Y02P20/55

Abstract: The present invention relates to a novel 2,3,5-substituted thiophene compound having inhibitory activity against kinases, an anticancer agent including the compound as an active ingredient, and a method for preparing the compound.

公开(公告)号：US10059717B2

公开(公告)日：2018-08-28

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 ,  C07D403/14 ,  C07D401/14 ,  A61K31/4985 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D487/04 ,  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：US10040803B2

公开(公告)日：2018-08-07

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: C07D495/02 ,  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：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。