公开(公告)号：US20230090406A1

公开(公告)日：2023-03-23

申请号：US17822445

申请日：2022-08-26

申请人： YUHAN CORPORATION ,  JANSSEN BIOTECH, INC.

发明人： Hyunjoo LEE ,  Su Bin CHOI ,  Misong KIM ,  Young Ae YOON ,  Kwan Hoon HYUN ,  Jae Young SIM

IPC分类号： C07D401/14 ,  C07D413/14

摘要： Provided are 6-membered heteroaryl-containing aminopyridine compounds and pharmaceutically acceptable compositions thereof which exhibit inhibition activity against certain mutated forms of EGFR.

公开(公告)号：US20230044255A1

公开(公告)日：2023-02-09

申请号：US17368738

申请日：2021-07-06

申请人： YUHAN CORPORATION

发明人： Tae Dong HAN ,  Hee Jae TAK ,  Eun Kyung KIM ,  Eui Chul LEE ,  Sol PARK ,  Hyok Jun CHO ,  Cheol Hee LIM ,  So Young KIM ,  Hyun Ho CHOI ,  Da Na JEONG ,  Na Yeon YANG ,  Na Ry HA

IPC分类号： C07D403/10 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

摘要： The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

公开(公告)号：US20230002379A1

公开(公告)日：2023-01-05

申请号：US17755843

申请日：2020-11-12

申请人： YUHAN CORPORATION ,  GREEN CROSS CORPORATION

发明人： Dong-Hoon KIM ,  Jae-Eun JOO ,  Eui-Chul LEE ,  Tae-Dong HAN ,  Seung-Yub SHIN ,  Sool-Ki KWON ,  Ji-Hye KIM

IPC分类号： C07D471/08

摘要： Provided are a compound having a 2,3-dihydro-1H-indene or 2,3-dihydrobenzofuran moiety or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same and a use thereof, where the compound having a 2,3-dihydro-1H-indene or 2,3-dihydrobenzofuran moiety or pharmaceutically acceptable salt thereof has an inhibitory activity against glucosylceramide synthase (GCS), and therefore can be usefully applied for preventing or treating various diseases associated with GCS, such as Gaucher disease, Fabry disease, Tay-Sachs disease, Parkinson's disease, etc.

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.

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).

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.

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.

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.

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.

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).