公开(公告)号：US11623925B2

公开(公告)日：2023-04-11

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：US20220281861A1

公开(公告)日：2022-09-08

申请号：US17704718

申请日：2022-03-25

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. Additional, the present invention provides novel intermediates useful for said process and processes for preparing the same.

公开(公告)号：US11434224B2

公开(公告)日：2022-09-06

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.

公开(公告)号：US20130116439A1

公开(公告)日：2013-05-09

申请号：US13726932

申请日：2012-12-26

申请人： YUHAN CORPORATION

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

IPC分类号： C07D401/04

CPC分类号： C07D401/04 ,  C07C67/31 ,  C07C67/46 ,  C07C69/612

摘要： 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 therefore. According to the present invention, pharmaceutically useful 2-methyl-2′-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.

摘要翻译： 本发明涉及以更简化的方式制备显示出抗组胺活性的2-甲基-2'-苯基丙酸衍生物的方法，因此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：US20230312545A1

公开(公告)日：2023-10-05

申请号：US18328267

申请日：2023-06-02

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

CPC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. Additionally, the present invention provides novel intermediates useful for said process and processes for preparing the same.

公开(公告)号：US20210269427A1

公开(公告)日：2021-09-02

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：US10858353B2

公开(公告)日：2020-12-08

申请号：US16633695

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： C07D413/14 ,  C07D265/32 ,  C07D403/10

摘要： The present invention provides a novel 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：US11708362B2

公开(公告)日：2023-07-25

申请号：US17704718

申请日：2022-03-25

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

CPC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：US08487106B2

公开(公告)日：2013-07-16

申请号：US13726932

申请日：2012-12-26

申请人： Yuhan Corporation

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

IPC分类号： C07D401/04 ,  C07D413/14

CPC分类号： C07D401/04 ,  C07C67/31 ,  C07C67/46 ,  C07C69/612

摘要： 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 therefore. According to the present invention, pharmaceutically useful 2-methyl-2′-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.

摘要翻译： 本发明涉及以更简化的方式制备显示出抗组胺活性的2-甲基-2'-苯基丙酸衍生物的方法，因此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：US11981659B2

公开(公告)日：2024-05-14

申请号：US17697655

申请日：2022-03-17

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

CPC分类号： C07D403/04 ,  C07C303/22 ,  C07C309/04 ,  C07B2200/13

摘要： 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.