公开(公告)号：WO2011052923A2

公开(公告)日：2011-05-05

申请号：PCT/KR2010/007205

申请日：2010-10-20

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  SIM, Tae Bo ,  HAM, Young Jin ,  YOO, Kyung Ho ,  OH, Chang Hyun ,  HAH, Jung Mi ,  CHOI, Hwan Geun ,  KIM, Hwan ,  JUN, Eun Jin

Inventor： SIM, Tae Bo ,  HAM, Young Jin ,  YOO, Kyung Ho ,  OH, Chang Hyun ,  HAH, Jung Mi ,  CHOI, Hwan Geun ,  KIM, Hwan ,  JUN, Eun Jin

IPC: C07D403/04 ,  C07D209/04 ,  A61K31/40 ,  A61P35/00

CPC classification number: C07D403/04 ,  A61K31/404 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

Abstract: Disclosed are a 1,6-substituted indole compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of cancers caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel indole compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.

Abstract translation: 公开了具有蛋白激酶抑制活性的1,6-取代的吲哚化合物，药学上可接受的盐，以及用于预防和治疗由包含该化合物作为有效成分的异常细胞生长引起的癌症的药物组合物。 由于新型吲哚化合物对参与生长因子信号转导的各种蛋白激酶具有优异的抑制活性，因此可用作预防或治疗由异常细胞生长引起的癌症的药剂。

公开(公告)号：WO2011049274A1

公开(公告)日：2011-04-28

申请号：PCT/KR2010/000589

申请日：2010-02-01

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  HAH, Jung-Mi ,  YOO, Kyung Ho ,  SIM, Tae-Bo ,  OH, Chang Hyun ,  LEE, Jung Hun ,  YU, Hana ,  KIM, Hwan

Inventor： HAH, Jung-Mi ,  YOO, Kyung Ho ,  SIM, Tae-Bo ,  OH, Chang Hyun ,  LEE, Jung Hun ,  YU, Hana ,  KIM, Hwan

IPC: C07D401/04 ,  C07D401/02 ,  A61K31/415 ,  A61P35/00

CPC classification number: C07D403/14 ,  A61K31/415 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to novel imidazole derivatives or pharmaceutically acceptable salts thereof, preparation methods thereof and pharmaceutical compositions for prevention and treatment of melanoma containing the same as active ingredients. The novel imidazole derivatives or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory effects on various protein kinases, which cause melanoma, such as B-RAF, C-RAF, Aurora-A, BTK, Flt3, Ret, KDR/VEGFR2, P38α/MAPK14, RAF1, FMS, and the like, so they can be used for the prevention and treatment of melanoma.

Abstract translation: 本发明涉及新颖的咪唑衍生物或其药学上可接受的盐，其制备方法和用于预防和治疗含有与活性成分相同的黑素瘤的药物组合物。 根据本发明的新型咪唑衍生物或其药学上可接受的盐对各种蛋白激酶具有优异的抑制作用，其引起黑素瘤，例如B-RAF，C-RAF，Aurora-A，BTK，Flt3，Ret，KDR / VEGFR2 ，P38a / MAPK14，RAF1，FMS等，因此可用于预防和治疗黑素瘤。

公开(公告)号：WO2010064875A2

公开(公告)日：2010-06-10

申请号：PCT/KR2009/007247

申请日：2009-12-04

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY ,  KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY ,  SIM, Tae Bo ,  SON, Jung Beom ,  KIM, Hwan ,  PARK, Dong Sik ,  CHOI, Hwan Geun ,  HAM, Young Jin ,  HAH, Jung Mi ,  YOO, Kyung Ho ,  OH, Chang Hyun ,  LEE, So Ha ,  HA, Jae Du ,  CHO, Sung Yun ,  KWON, Byoung-Mog ,  HAN, Dong Cho

Inventor： SIM, Tae Bo ,  SON, Jung Beom ,  KIM, Hwan ,  PARK, Dong Sik ,  CHOI, Hwan Geun ,  HAM, Young Jin ,  HAH, Jung Mi ,  YOO, Kyung Ho ,  OH, Chang Hyun ,  LEE, So Ha ,  HA, Jae Du ,  CHO, Sung Yun ,  KWON, Byoung-Mog ,  HAN, Dong Cho

IPC: C07D231/56

CPC classification number: C07D413/14 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.

Abstract translation: 公开了由以下化学式1表示的新型吲唑衍生物或其药学上可接受的盐，水合物或溶剂化物，以及用于预防或治疗增殖性疾病的药物组合物，其含有作为活性成分的药物组合物。 新型吲唑衍生物对b-raf，KDR，Fms，Tie2，SAPK2a，Ret等蛋白激酶具有强效抑制作用，可诱导异常细胞增殖引起的疾病，可用于预防或治疗由异常细胞引起的疾病 增殖。

公开(公告)号：WO2010032901A1

公开(公告)日：2010-03-25

申请号：PCT/KR2008/006688

申请日：2008-11-13

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  OH, Chang Hyun ,  CHO, Jung Hyuck

Inventor： OH, Chang Hyun ,  CHO, Jung Hyuck

IPC: C07D403/06

CPC classification number: C07D413/10

Abstract: Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant en- terococci (VRE), the pharmaceutical composition is useful as an antibiotic.

Abstract translation: 提供了具有由化学式1表示的二氟苯基部分的新型恶唑烷酮衍生物，其药学上可接受的盐，其制备方法和包含其作为活性成分的药物组合物。 展示了抗革兰氏阳性菌（包括嗜血杆菌流感和凝固酶阴性葡萄球菌）和抗万古霉素耐药细菌（VRE）的抑制活性，药物组合物可用作抗生素。

公开(公告)号：EP3483166A1

公开(公告)日：2019-05-15

申请号：EP17824476.0

申请日：2017-07-03

Applicant: Korea Institute of Science and Technology

Inventor： MAHMOUD, Gamal El-din ,  CHOI, Hong Seok ,  YOO, Kyung Ho ,  HAN, Dong Keun ,  OH, Chang Hyun ,  MOHAMMED, Abdel-Maksoud ,  MOHAMMED, I. El-Gamal

IPC: C07D498/04 ,  C07D513/04 ,  C07D417/14 ,  A61K31/424 ,  A61K31/429 ,  A61K31/433 ,  A61K31/506

Abstract: Provided is a pharmaceutical composition for preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated.

公开(公告)号：EP3845539A1

公开(公告)日：2021-07-07

申请号：EP20153435.1

申请日：2020-01-23

Applicant: Korea Institute of Science and Technology

Inventor： MAHMOUD, Gamal El-din ,  CHOI, Hong Seok ,  YOO, Kyung Ho ,  HAN, Dong Keun ,  OH, Chang Hyun ,  MOHAMMED, Abdel-Maksoud ,  MOHAMMED, El-Gamal I. ,  AMMAR, Usama M.

IPC: C07D498/04 ,  C07D513/04 ,  A61P35/00 ,  A61K31/424 ,  A61K31/429

Abstract: Provided is a pharmaceutical composition for use in preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated.