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公开(公告)号：US20190016703A1
公开(公告)日：2019-01-17
申请号：US16066150
申请日：2016-12-29
发明人： Nathanael S. GRAY , James BRADNER , Pasi JANNE , Jaebong JANG , Hwan Geun CHOI , Eunhwa KO , Joong-Heui CHO
IPC分类号： C07D401/14 , A61P35/00 , A61K47/54 , A61K47/18 , A61K47/08
摘要： The present invention provides bifunctional compounds which act as protein degradation inducing moieties for a HER family protein, such as Her3. The present invention also provides methods for the targeted degradation of a HER family protein through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to the HER family protein which can be utilized in the treatment of disorders modulated by a HER family protein.
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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：US20220106307A1
公开(公告)日：2022-04-07
申请号：US17398478
申请日：2021-08-10
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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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：US20180290975A1
公开(公告)日：2018-10-11
申请号：US15580088
申请日：2016-06-30
发明人： Nathanael S. GRAY , Michael ECK , Pasi JANNE , Hwan Geun CHOI , Jaebong JANG , Kwok-Kin WONG
IPC分类号： C07D209/46 , C07D417/12 , C07D401/12 , C07D413/12 , C07D417/14 , C07D403/12 , C07D513/04 , C07D487/04 , C07D277/46 , C07D413/14 , C07D403/14 , C07D471/04
CPC分类号： C07D209/46 , A61P35/00 , C07D277/46 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The disclosure relates to a compound having Formula (I′): and in particular, Compound I-126: which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US20170362204A1
公开(公告)日：2017-12-21
申请号：US15536486
申请日：2015-12-23
发明人： Nathanael S. GRAY , Pasi JANNE , Hwan Geun CHOI , Jaebong JANG
IPC分类号： C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04
CPC分类号： C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US20190194169A1
公开(公告)日：2019-06-27
申请号：US16290153
申请日：2019-03-01
发明人： Nathanael S. GRAY , Pasi JANNE , Hwan Geun CHOI , Jaebong JANG
IPC分类号： C07D403/04 , C07D487/04 , C07D471/04 , C07D403/14
CPC分类号： C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US20180244676A1
公开(公告)日：2018-08-30
申请号：US15547913
申请日：2016-02-12
发明人： Nathanael S. GRAY , John HATCHER , Hwan Geun CHOI
IPC分类号： C07D487/04 , C07D473/18 , A61P25/28
CPC分类号： C07D487/04 , A61P25/28 , C07D473/18
摘要： Compounds having the formula I, II, or III: are provided. Compounds of the present disclosure are useful for the treatment of neurodegenerative diseases, such as Parkinson's Disease.
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公开(公告)号：US20210094913A1
公开(公告)日：2021-04-01
申请号：US17035164
申请日：2020-09-28
发明人： Nathanael S. GRAY , Michael ECK , Pasi JANNE , Hwan Geun CHOI , Jaebong JANG , Kwok-Kin WONG
IPC分类号： C07D209/46 , C07D401/12 , C07D417/12 , C07D417/14 , C07D403/12 , C07D413/14 , C07D403/14 , C07D413/12 , C07D471/04 , C07D487/04 , C07D277/46 , C07D513/04 , A61P35/00
摘要： The disclosure relates to a compound having Formula (I′): and in particular, Compound I-126: which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US20200002279A1
公开(公告)日：2020-01-02
申请号：US16440803
申请日：2019-06-13
发明人： Nathanael S. GRAY , Michael ECK , Pasi JANNE , Hwan Geun CHOI , Jaebong JANG , Kwok-Kin WONG
IPC分类号： C07D209/46 , A61P35/00 , C07D277/46 , C07D401/12 , C07D403/12 , C07D403/14 , C07D513/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D413/12
摘要： The disclosure relates to a compound having Formula (I′): and in particular, Compound I-126: which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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