公开(公告)号：US20220024918A1

公开(公告)日：2022-01-27

申请号：US17368712

申请日：2021-07-06

Applicant: YUHAN CORPORATION

Inventor： Tae Dong HAN ,  Hee Jae TAK ,  Eun Kyung KIM ,  Dong Hoon KIM ,  Su Bin CHOI ,  Sol PARK ,  Hyun Ho CHOI ,  Tae Wang KIM ,  Mi Kyeong JU ,  Na Ry HA

IPC: C07D471/04 ,  C07D519/00

Abstract: The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit 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：US20200223827A1

公开(公告)日：2020-07-16

申请号：US16712660

申请日：2019-12-12

Applicant: YUHAN CORPORATION

Inventor： 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: C07D403/10 ,  C07D249/12 ,  C07D403/04 ,  C07D401/04 ,  C07D405/10 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

Abstract: 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：US20230021395A1

公开(公告)日：2023-01-26

申请号：US17697655

申请日：2022-03-17

Applicant: Yuhan Corporation

Inventor： 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: C07D403/04 ,  C07C303/22 ,  C07C309/04

Abstract: The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-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：US20210147368A1

公开(公告)日：2021-05-20

申请号：US17104557

申请日：2020-11-25

Applicant: YUHAN CORPORATION

Inventor： 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: C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D409/10 ,  C07D405/10 ,  C07D407/14 ,  C07D401/10 ,  C07D403/10 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D413/10 ,  C07D417/10 ,  C07D249/12 ,  C07D403/14

Abstract: 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：US20210139461A1

公开(公告)日：2021-05-13

申请号：US16605944

申请日：2018-04-18

Applicant: Yuhan Corporation

Inventor： 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: C07D403/04 ,  C07C309/04 ,  C07C303/22

Abstract: 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：US20200223844A1

公开(公告)日：2020-07-16

申请号：US16712673

申请日：2019-12-12

Applicant: YUHAN CORPORATION

Inventor： Tae Dong HAN ,  Hee Jae TAK ,  Eun Kyung KIM ,  Dong Hoon KIM ,  Su Bin CHOI ,  Sol PARK ,  Hyun Ho CHOI ,  Tae Wang KIM ,  Mi Kyeong JU ,  Na Ry HA

IPC: C07D471/04 ,  C07D519/00

Abstract: The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit 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：US20240417392A1

公开(公告)日：2024-12-19

申请号：US18422735

申请日：2024-01-25

Applicant: YUHAN CORPORATION

Inventor： 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: C07D403/10 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

Abstract: 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：US20240279203A1

公开(公告)日：2024-08-22

申请号：US18618379

申请日：2024-03-27

Applicant: Yuhan Corporation

Inventor： 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: C07D403/04 ,  C07C303/22 ,  C07C309/04

CPC classification number: C07D403/04 ,  C07C303/22 ,  C07C309/04 ,  C07B2200/13

Abstract: The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-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：US20230044255A1

公开(公告)日：2023-02-09

申请号：US17368738

申请日：2021-07-06

Applicant: YUHAN CORPORATION

Inventor： 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: C07D403/10 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

Abstract: 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：US20210317110A1

公开(公告)日：2021-10-14

申请号：US17208887

申请日：2021-03-22

Applicant: YUHAN CORPORATION

Inventor： 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: C07D409/04 ,  C07D409/14 ,  C07D498/04 ,  C07D413/14 ,  C07D471/04 ,  C07D405/14

Abstract: 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).