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81.
公开(公告)号:US20220380344A1
公开(公告)日:2022-12-01
申请号:US17873966
申请日:2022-07-26
申请人: YUHAN CORPORATION
发明人: Ja-Heouk KHOO , Doo-Byung LEE , Jun-Sup LEE , Hyun JU , Woo-Seob SHIN
IPC分类号: C07D403/04 , C07D239/47
摘要: The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
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公开(公告)号:US11492335B2
公开(公告)日:2022-11-08
申请号:US17104557
申请日:2020-11-25
申请人: YUHAN CORPORATION
发明人: Tae Dong Han , Hee Jae Tak , Eun Kyung Kim , Su Bin Choi , Dong Hoon Kim , Sol Park , Eun Hye Jung , Hyun Ho Choi , Tae Wang Kim , Mi Kyeong Ju , Na Ry Ha
IPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D409/10 , C07D413/14 , C07D417/04 , C07D417/14 , C07D249/08 , C07D401/04 , C07D405/10 , C07D407/14 , C07D401/10 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D249/12
摘要: The present technology provides aryl or heteroaryl triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The aryl or heteroaryl triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
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公开(公告)号:US11453656B2
公开(公告)日:2022-09-27
申请号:US16605944
申请日:2018-04-18
申请人: Yuhan Corporation
发明人: Sang Ho Oh , Jong Gyun Kim , Se-Woong Oh , Tae Dong Han , Soo Yong Chung , Seong Ran Lee , Kyeong Bae Kim , Young Sung Lee , Woo Seob Shin , Hyun Ju , Jeong Ki Kang , Su Min Park , Dong Kyun Kim
IPC分类号: C07C309/04 , C07C303/22 , C07C403/04 , C07D403/04
摘要: The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yppyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same.
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公开(公告)号:US11332436B2
公开(公告)日:2022-05-17
申请号:US17254718
申请日:2019-07-01
申请人: YUHAN CORPORATION
发明人: Woo Seob Shin , Cheol Hee Lim
IPC分类号: C07C271/14 , C07C269/06
摘要: The present technology provides a process for selectively preparing an (E)-(2-(chloromethyl)-3-fluoroallyl)carbamate compound by refluxing an (E/Z)-(2-(chloromethyl)-3-fluoroallyl)carbamate compound in an organic solvent, followed by crystallization by cooling.
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公开(公告)号:US11286253B2
公开(公告)日:2022-03-29
申请号:US17115037
申请日:2020-12-08
申请人: Yuhan Corporation
发明人: Sang-Ho Oh , Ja-Heouk Khoo , Jong-Chul Lim , Seong-Ran Lee , Hyun Ju , Woo-Seob Shin , Dae-Gyu Park , Su-Min Park , Yoon-Ah Hwang
IPC分类号: C07D413/14
摘要: The present invention provides an improved process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. Additional, the present invention provides novel intermediates useful for said process and processes for preparing the same.
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公开(公告)号:US11198684B2
公开(公告)日:2021-12-14
申请号:US16633756
申请日:2018-07-25
申请人: Yuhan Corporation
发明人: Sang-Ho Oh , Ja-Heouk Khoo , Jong-Chul Lim , Doo-Byung Lee , Jung-Ae Lee , Jun-Sup Lee , Hyun Ju , Woo-Seob Shin , Sang-Seol Jeon
IPC分类号: C07D265/30 , C07D295/135 , C07D403/04 , C07D413/14
摘要: The present invention provides intermediates useful for the synthesis of an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors; and processes for preparing the same. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.
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87.
公开(公告)号:US20210317110A1
公开(公告)日:2021-10-14
申请号:US17208887
申请日:2021-03-22
申请人: YUHAN CORPORATION
发明人: Tae Dong HAN , Hee Jae TAK , Eun Kyung KIM , Su Bin CHOI , Sol PARK , Dong Hoon KIM , So Young KIM , Hyun Ho CHOI , Tae Wang KIM , Mi Kyeong JU , Na Ry HA , Eui Chul LEE
IPC分类号: C07D409/04 , C07D409/14 , C07D498/04 , C07D413/14 , C07D471/04 , C07D405/14
摘要: The present technology provides triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g. for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
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88.
公开(公告)号:US20210206746A1
公开(公告)日:2021-07-08
申请号:US17056557
申请日:2019-05-16
申请人: YUHAN CORPORATION
发明人: Ja-Heouk KHOO , Doo-Byung LEE , Jun-Sup LEE , Hyun JU , Woo-Seob SHIN
IPC分类号: C07D403/04 , C07D239/47
摘要: Provided are a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist, crystalline forms of a hydrochloride of the diaminopyrimidine derivative, and processes for preparing the same.
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公开(公告)号:US10889578B2
公开(公告)日:2021-01-12
申请号:US16633684
申请日:2018-07-25
申请人: Yuhan Corporation
发明人: Sang-Ho Oh , Ja-Heouk Khoo , Jong-Chul Lim , Seong-Ran Lee , Hyun Ju , Woo-Seob Shin , Dae-Gyu Park , Su-Min Park , Yoon-Ah Hwang
IPC分类号: C07D413/14
摘要: The present invention provides an improved process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.
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公开(公告)号:US20200024318A1
公开(公告)日:2020-01-23
申请号:US15768865
申请日:2016-10-28
申请人: YUHAN CORPORATION
发明人: Jun Hwan KIM , Seyoung LIM , Minji SEO , Hyun Ho CHOI , Dohoon KIM , Mi Kyeong JU , Ju-Young PARK , Seul Gi KIM , Sangmyoun LIM , Jong Gyun KIM , Su Youn NAM
IPC分类号: C07K14/50 , C07K14/605 , C07K14/575 , A61P3/04 , A61P3/06 , A61P3/10 , A61P1/16
摘要: The present invention provides a dual function protein prepared by linking a biologically active protein and an FGF mutant protein to an Fc region of an immunoglobulin, which has improved pharmacological efficacy, in vivo duration and protein stability. A dual function protein according to the present invention exhibits improved pharmacological efficacy, in vivo duration and protein stability, and a pharmaceutical composition containing the dual function protein as an active ingredient may be effectively used as a therapeutic agent for diabetes, obesity, dyslipidemia, metabolic syndrome, non-alcoholic fatty liver diseases, non-alcoholic steatohepatitis or cardiovascular diseases.
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