公开(公告)号：US10442796B2

公开(公告)日：2019-10-15

申请号：US15998791

申请日：2018-08-16

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

发明人： 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分类号： C07D409/12 ,  A61P35/02 ,  A61K31/381 ,  A61K31/4436 ,  C07D333/10 ,  C07D409/14

摘要： 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：US20190047993A1

公开(公告)日：2019-02-14

申请号：US15998791

申请日：2018-08-16

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

发明人： 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分类号： C07D409/12 ,  A61P35/02 ,  C07D409/14

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

摘要： 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：US20230248740A1

公开(公告)日：2023-08-10

申请号：US17953867

申请日：2022-09-27

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION ,  NATIONAL CANCER CENTER ,  SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

发明人： Hwan Geun Choi ,  Jong Bae Park ,  Eunhwa Ko ,  Jung Beom Son ,  Nam Doo Kim ,  Seung Hoon Lee ,  Do-Hyun Nam

IPC分类号： A61K31/5513 ,  A61P35/04 ,  A61K31/415 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/506 ,  A61K31/5377 ,  C07K16/22

CPC分类号： A61K31/5513 ,  A61K31/415 ,  A61K31/437 ,  A61K31/506 ,  A61K31/4365 ,  A61K31/5377 ,  A61P35/04 ,  C07K16/22

摘要： Disclosed is a pharmaceutical composition for the prevention or treatment of brain cancer, containing a compound capable of penetrating the blood-brain barrier as an active ingredient, the pharmaceutical composition for the prevention or treatment of brain cancer is capable of efficiently penetrating the blood-brain barrier of the brain to thereby effectively inhibit LRRK2 protein expression, and is thus useful in the prevention or treatment of brain cancer.

公开(公告)号：US20230295153A1

公开(公告)日：2023-09-21

申请号：US17801757

申请日：2021-02-26

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION ,  IMMUNOFORGE CO.,LTD.

发明人： Doohyun Lee ,  Seungyeon Lee ,  Ye Ri Han ,  Chun Young Im ,  So Young Kim ,  Nam Hui Kim ,  Hwan Geun Choi ,  Eunhwa Ko ,  Heegyum Moon ,  Sun Joo Lee ,  Sang Bum Kim ,  Hyo-Ji Kim ,  Sion Lee ,  Sung-Min Ahn ,  Kiho Chang ,  Eunkyu Lee ,  Hyun Jin Kwon ,  Myeong-Sook Jeong ,  Ji Young Kim

IPC分类号： C07D471/04 ,  A61P35/00

CPC分类号： C07D471/04 ,  A61P35/00

摘要： The present invention relates to a 3-((8-((1H-pyrazol-4-yl)amino)imidazo[1,2-a]pyridin-3-yl)ethynyl)-N-phenylbenzamide derivative, a method for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating cancer. The derivative can significantly inhibit the proliferation of cancer cells by inhibiting kinases, particularly Bcr-Abl kinase or Bcr-Abl (T315I) kinase. Therefore, the derivative can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer.

公开(公告)号：US11208412B2

公开(公告)日：2021-12-28

申请号：US16488194

申请日：2018-02-22

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION ,  NATIONAL CANCER CENTER ,  SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

发明人： Hwan Geun Choi ,  Jong Bae Park ,  Eunhwa Ko ,  Jung Beom Son ,  Joong-heui Cho ,  Yi Kyung Ko ,  Jin-Hee Park ,  So Young Kim ,  Seock Yong Kang ,  Seungyeon Lee ,  Nam Doo Kim ,  Yunho Lee ,  Sun-Hwa Lee ,  Dayea Kim ,  Sun Joo Lee ,  Jae Hyun Bae ,  Eunmi Hong ,  Tae-ho Jang ,  Sang Bum Kim ,  Seung Hoon Lee ,  Do-Hyun Nam

IPC分类号： C07D487/04 ,  A61P35/00 ,  A61P29/00 ,  A61P25/28 ,  A61K31/519

摘要： The present invention relates to a novel pyrrolo-pyrimidine derivative compound, a preparation method therefor, and a pharmaceutical composition comprising the same compound as an effective ingredient for preventing or treating a protein kinase-related disease. The compound represented by Chemical Formula 1 according to the present invention, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an effective ingredient has outstanding inhibitory activity against LRRK2 kinase and against phosphorylation in the NIH-3T3 cell line, which is an LRRK2-expressing cell line, and NCC01 and 448T cell lines, which are both derived from patients with brain tumors. Verified to have inhibitory activity against various protein kinases in addition to LRRK2, the compound can find effective applications in the treatment or prevention of protein kinase-related diseases.

公开(公告)号：US20210267997A1

公开(公告)日：2021-09-02

申请号：US16488706

申请日：2018-02-23

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION ,  NATIONAL CANCER CENTER ,  SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

发明人： Hwan Geun Choi ,  Jong Bae Park ,  Eunhwa Ko ,  Jung Beom Son ,  Nam Doo Kim ,  Seung Hoon Lee ,  Do-Hyun Nam

IPC分类号： A61K31/5513 ,  A61K31/506 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/4365 ,  A61K31/415 ,  C07K16/22 ,  A61P35/04

摘要： Disclosed is a pharmaceutical composition for the prevention or treatment of brain cancer, containing a compound capable of penetrating the blood-brain barrier as an active ingredient, the pharmaceutical composition for the prevention or treatment of brain cancer is capable of efficiently penetrating the blood-brain barrier of the brain to thereby effectively inhibit LRRK2 protein expression, and is thus useful in the prevention or treatment of brain cancer.

公开(公告)号：US20230181596A1

公开(公告)日：2023-06-15

申请号：US17953819

申请日：2022-09-27

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION ,  NATIONAL CANCER CENTER ,  SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

发明人： Hwan Geun Choi ,  Jong Bae Park ,  Eunhwa Ko ,  Jung Beom Son ,  Nam Doo Kim ,  Seung Hoon Lee ,  Do-Hyun Nam

IPC分类号： A61K31/5513 ,  A61P35/04 ,  A61K31/415 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/506 ,  A61K31/5377 ,  C07K16/22

CPC分类号： A61K31/5513 ,  A61P35/04 ,  A61K31/415 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/506 ,  A61K31/5377 ,  C07K16/22

摘要： Disclosed is a pharmaceutical composition for the prevention or treatment of brain cancer, containing a compound capable of penetrating the blood-brain barrier as an active ingredient, the pharmaceutical composition for the prevention or treatment of brain cancer is capable of efficiently penetrating the blood-brain barrier of the brain to thereby effectively inhibit LRRK2 protein expression, and is thus useful in the prevention or treatment of brain cancer.

公开(公告)号：US11117892B2

公开(公告)日：2021-09-14

申请号：US16495455

申请日：2018-03-23

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION ,  KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY ,  DAEGU GYEONGBUK INSTITUTE OF SCIENCE AND TECHNOLOGY

发明人： Hwan Geun Choi ,  Eunhwa Ko ,  Joong-heui Cho ,  Jung Beom Son ,  Yi Kyung Ko ,  Jin-Hee Park ,  So Young Kim ,  Seock Yong Kang ,  Seungyeon Lee ,  Hee Yoon Ryu ,  Nam Doo Kim ,  Sang Bum Kim ,  Sun-Hwa Lee ,  Dayea Kim ,  Sun Joo Lee ,  Sungchan Cho ,  Kyu-Sun Lee ,  Kweon Yu ,  Miri Choi ,  Ja Wook Koo ,  Hyang-Sook Hoe

IPC分类号： C07D471/04 ,  A61P25/28

摘要： The present invention relates to a pyrrolo-pyridine derivative compound, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for the prevention or treatment of protein kinase-related diseases. A compound represented by chemical formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, according to the present invention, has excellent inhibitory activity against various protein kinases including DYRK1A, and therefore, the pharmaceutical composition containing the same as an active ingredient can be favorably used in the treatment or prevention of protein kinase-related diseases. Particularly, the pharmaceutical composition can be effectively used in the prevention, treatment, or alleviation of Alzheimer's disease, dementia, or Alzheimer's dementia.

公开(公告)号：US20190315738A1

公开(公告)日：2019-10-17

申请号：US16311654

申请日：2017-06-20

申请人： DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION

发明人： Hwan Geun Choi ,  Jung Beom Son ,  Shinae Kim ,  Seungyeon Lee ,  Eunhwa Ko ,  Joongheui Cho ,  Seock Yong Kang ,  So Young Kim ,  Jin-Hee Park ,  Yi Kyung Ko ,  Hee Yoon Ryu ,  Nam Doo Kim ,  Hyunkyoung Kim ,  Younho Lee ,  Sun-Hwa Lee ,  Dayea Kim ,  Sun Joo Lee ,  Seongho Hong ,  Sang Hyun Min ,  Sungwoo Lee ,  Dong Kyu Choi ,  Jae Hyun Bae ,  Eunmi Hong ,  Tae-ho Jang ,  Jaeyoung Song ,  Sangbum Kim ,  Suk Kyoon Yoon

IPC分类号： C07D471/04 ,  C07D519/00 ,  A23L29/00

摘要： The present invention relates to a novel imidazopyridine derivative, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating cancer. The novel imidazopyridine derivative according to the present invention, a stereoisomer thereof and a pharmaceutically acceptable salt thereof can effectively inhibit cancer-related kinases, are excellent in inhibiting proliferation of cancer cells in a cancer cell line, and effectively inhibit proliferation of cancer cells (cancer cell apoptosis) in a cancer cell heterograft model, and thus can be useful as a pharmaceutical composition containing the same as an active ingredient for preventing or treating cancer.Also, the novel imidazopyridine derivative according to the present invention, the stereoisomer thereof, and the pharmaceutically acceptable salt thereof can effectively inhibit Src and Fyn, thereby being useful as a pharmaceutical composition for preventing or treating the Src and Fyn related diseases, and in particular, have been confirmed to be useful in diabetic nephropathy in animal model experiments. Therefore, the compound of the present invention can be effective as a pharmaceutical composition containing the same as an active ingredient for preventing or treating diabetic nephropathy.

公开(公告)号：US20130079343A1

公开(公告)日：2013-03-28

申请号：US13684507

申请日：2012-11-24

申请人： Korea Institute of Science and Technology

发明人： Tae Bo Sim ,  Young Jin Ham ,  Hwan Geun Choi

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D401/14 ,  C07D401/04

CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient.Since the novel indole compound exhibits superior inhibitory activity for 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.

摘要翻译： 公开了对蛋白激酶具有抑制活性的1,3,6-取代的吲哚化合物，其药学上可接受的物质，以及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，包括该化合物作为活性成分。 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。