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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.
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公开(公告)号：US20200239474A1
公开(公告)日：2020-07-30
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
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.
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公开(公告)号：US20190047993A1
公开(公告)日：2019-02-14
申请号：US15998791
申请日：2018-08-16
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.
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公开(公告)号：US20230365530A1
公开(公告)日：2023-11-16
申请号：US18246178
申请日：2021-09-16
申请人： THE ASEAN FOUNDATION , DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION , UNIVERSITY OF ULSAN FOUNDATION FOR INDUSTRY COOPERATION
发明人： Jung Jin HWANG , Sang Eun PARK , Dong Eun KIM , Ji-Ye HONG , Choung-Soo KIM , Woo Chan SON , Shinae KIM , Sugyeong KWON , Kyungjin JUNG , Nayeon KIM , Jina KIM , Kyung-Hee KIM , Jung Wook CHIN , Sung Jin CHO , Sehan LEE , Eunju CHA , Jeongmin JOO , Ji Sun HWANG , Jeong-Eun PARK , Ji Hoon YU , Eunmi HONG , Young-Hoon PARK , Ju-Hee LEE
IPC分类号： C07D401/14 , A61K45/06 , A61P35/00 , C07D401/12 , C07D239/95
CPC分类号： C07D401/14 , A61K45/06 , A61P35/00 , C07D401/12 , C07D239/95
摘要： A compound, a stereoisomer thereof, a hydrate thereof, or a pharmaceutically acceptable salt thereof, provided as one aspect of the present invention, exhibits a high inhibitory ability on euchromatic histone-lysine N-methyltransferase 2 (EHMT2), and thus, the compound can be usefully used for the treatment of cancer.
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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.
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公开(公告)号：US20230010508A1
公开(公告)日：2023-01-12
申请号：US17773325
申请日：2020-10-29
发明人： Ji-Hoon Yu , Chun Young lm , SoYoung Kim , Ye Ri Han , Doohyun Lee , Hui-Jeon Jeon , Sang-Hyun Min , Bae Jun Oh , Sang-Wook Park , Dong-Kyu Choi , Young-Kyu Kim , Sung Hwan Kim , Yuri Lee , Seungyeon Lee , Nam Hui Kim , Sang Bum Kim , Ju-Sik Min
摘要： The present invention relates to a compound comprising an EZH2 inhibitor and an E3 ligase binder, and a pharmaceutical composition for preventing or treating EZH2-associated disease and a pharmaceutical composition for selective protein degradation containing the same as an active ingredient. Since the compound of the present invention can selectively degrade EZH2, it can be effectively used for the treatment of EZH2-related diseases and cancers, particularly, cancers in which EZH2 is overexpressed, and can be usefully used for the selective degradation of EZH2.
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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.
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18.发明授权公开(公告)号：US10934303B2
公开(公告)日：2021-03-02
申请号：US16313351
申请日：2016-09-13
申请人： Daegu-Gyeongbuk Medical Innovation Foundation , KYUNGPOOK NATIONAL UNIVERSITY HOSPITAL , Kyungpook National University Industry-Academic Cooperation Foundation
发明人： Sung Yeoun Hwang , Sung Jin Cho , Jina Kim , Jungwook Chin , Hayoung Hwang , In-Kyu Lee , Yong-Hyun Jeon , Jaetae Lee , Jae-Han Jeon , Sang Wook Kim
IPC分类号： C07D203/08 , C07D205/04 , C07D207/06 , C07D211/06 , C07D241/04 , C07D265/30 , C07D487/10 , C07D265/28 , A61K31/396 , A61K31/397 , A61K31/535 , A61K31/496 , C07D209/52 , C07D209/54 , C07D249/06 , C07D295/08 , C07D401/04 , C07D405/06 , C07D487/04 , A61P27/02 , A61P35/00
摘要： The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.
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公开(公告)号：US20200207756A1
公开(公告)日：2020-07-02
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 pyrrolopyridine 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.
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公开(公告)号：US20190315738A1
公开(公告)日：2019-10-17
申请号：US16311654
申请日：2017-06-20
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.
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