公开(公告)号：US11981659B2

公开(公告)日：2024-05-14

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

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：US11453656B2

公开(公告)日：2022-09-27

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: C07C309/04 ,  C07C303/22 ,  C07C403/04 ,  C07D403/04

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：US11286253B2

公开(公告)日：2022-03-29

申请号：US17115037

申请日：2020-12-08

Applicant: Yuhan Corporation

Inventor： 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: C07D413/14

Abstract: 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

Applicant: Yuhan Corporation

Inventor： 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: C07D265/30 ,  C07D295/135 ,  C07D403/04 ,  C07D413/14

Abstract: 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：US10889578B2

公开(公告)日：2021-01-12

申请号：US16633684

申请日：2018-07-25

Applicant: Yuhan Corporation

Inventor： 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: C07D413/14

Abstract: 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.

公开(公告)号：US08633223B2

公开(公告)日：2014-01-21

申请号：US13726937

申请日：2012-12-26

Applicant: Yuhan Corporation

Inventor： Chun-Ho Lee ,  Ja-Heouk Khoo ,  Kyoung-Chan Kwon ,  Hyun Ju

IPC: A61K31/445 ,  C07D401/04 ,  C07D413/14

CPC classification number: C07D401/04 ,  C07C67/31 ,  C07C67/46 ,  C07C69/612

Abstract: The present invention relates to a process for preparing 2-methyl-2′-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present invention, pharmaceutically useful 2-methyl-2′-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.

Abstract translation: 本发明涉及以更简化的方式制备显示抗组胺活性的2-甲基-2'-苯基丙酸衍生物的方法，中间体化合物及其制备方法。 根据本发明，可以以工业规模高产率和纯度制备药学上可用的2-甲基-2'-苯基丙酸衍生物。

公开(公告)号：US20130116466A1

公开(公告)日：2013-05-09

申请号：US13726937

申请日：2012-12-26

Applicant: YUHAN CORPORATION

Inventor： Chun-Ho Lee ,  Ja-Heouk Khoo ,  Kyoung-Chan Kwon ,  Hyun Ju

IPC: C07C67/31 ,  C07C67/46 ,  C07C69/612

CPC classification number: C07D401/04 ,  C07C67/31 ,  C07C67/46 ,  C07C69/612

Abstract: The present invention relates to a process for preparing 2-methyl-2″-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present invention, pharmaceutically useful 2-methyl-2″-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.

Abstract translation: 本发明涉及以更简化的方式制备显示抗组胺活性的2-甲基-2'-苯基丙酸衍生物的方法，中间体化合物及其制备方法。 根据本发明，可以以工业规模高产率和纯度制备药学上可用的2-甲基-2'-苯基丙酸衍生物。