公开(公告)号：US20210155607A1

公开(公告)日：2021-05-27

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： C07D403/04 ,  C07D295/135

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：US20200165236A1

公开(公告)日：2020-05-28

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.

公开(公告)号：US20200207750A1

公开(公告)日：2020-07-02

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：US20230021395A1

公开(公告)日：2023-01-26

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

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.

公开(公告)号：US20210139461A1

公开(公告)日：2021-05-13

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

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：US20240279203A1

公开(公告)日：2024-08-22

申请号：US18618379

申请日：2024-03-27

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.

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：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.