公开(公告)号：US10889578B2

公开(公告)日：2021-01-12

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：US20200223808A1

公开(公告)日：2020-07-16

申请号：US16721020

申请日：2019-12-19

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： 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

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：US20200024318A1

公开(公告)日：2020-01-23

申请号：US15768865

申请日：2016-10-28

申请人： YUHAN CORPORATION

发明人： Jun Hwan KIM ,  Seyoung LIM ,  Minji SEO ,  Hyun Ho CHOI ,  Dohoon KIM ,  Mi Kyeong JU ,  Ju-Young PARK ,  Seul Gi KIM ,  Sangmyoun LIM ,  Jong Gyun KIM ,  Su Youn NAM

IPC分类号： C07K14/50 ,  C07K14/605 ,  C07K14/575 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

摘要： The present invention provides a dual function protein prepared by linking a biologically active protein and an FGF mutant protein to an Fc region of an immunoglobulin, which has improved pharmacological efficacy, in vivo duration and protein stability. A dual function protein according to the present invention exhibits improved pharmacological efficacy, in vivo duration and protein stability, and a pharmaceutical composition containing the dual function protein as an active ingredient may be effectively used as a therapeutic agent for diabetes, obesity, dyslipidemia, metabolic syndrome, non-alcoholic fatty liver diseases, non-alcoholic steatohepatitis or cardiovascular diseases.

公开(公告)号：US20190322655A1

公开(公告)日：2019-10-24

申请号：US16359985

申请日：2019-03-20

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 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04

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).

公开(公告)号：US20190308944A1

公开(公告)日：2019-10-10

申请号：US16359984

申请日：2019-03-20

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

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：US20180111918A1

公开(公告)日：2018-04-26

申请号：US15848760

申请日：2017-12-20

申请人： YUHAN CORPORATION

发明人： Hyun-Joo LEE ,  Dong-Hoon KIM ,  Tae-Kyun KIM ,  Young-Ae YOON ,  Jae-Young SIM ,  Myung-Hun CHA ,  Eun-Jung JUNG ,  Kyoung-Kyu AHN ,  Tai-Au LEE

IPC分类号： C07D403/04 ,  C07D413/14 ,  C07D413/04 ,  C07D417/04 ,  C07D401/04

CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.

公开(公告)号：US20170152241A9

公开(公告)日：2017-06-01

申请号：US14893517

申请日：2014-05-23

申请人： YUHAN CORPORATION

发明人： Jae Young SIM ,  Myung Hun CHA ,  Tae Kyun KIM ,  Young Ae YOON ,  Dong Hoon KIM

IPC分类号： C07D403/04 ,  C07D409/14 ,  C07D401/04

CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D409/14

摘要： The present invention provides: a bicyclic derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof; a preparation method therefor, a pharmaceutical composition comprising the same; and a use therefor. According to the present invention, the bicyclic compound derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof acts as a 5-HT4 receptor agonist, and thus can be usefully applied to the prevention or treatment of dysfunction in gastrointestinal motility, for example, gastrointestinal diseases such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, diabetic gastric atony and the like.

公开(公告)号：US09593098B2

公开(公告)日：2017-03-14

申请号：US14881930

申请日：2015-10-13

申请人： Yuhan Corporation

发明人： Byung-Chul Suh ,  Paresh Devidas Salgaonkar ,  Jaekyoo Lee ,  Jong Sung Koh ,  Ho-Juhn Song ,  In Yong Lee ,  Jaesang Lee ,  Dong Sik Jung ,  Jung-Ho Kim ,  Se-Won Kim

IPC分类号： A61K31/506 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14

CPC分类号： C07D403/04 ,  A61K31/506 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14

摘要： The present invention provides a new group of protein kinase inhibitors, aminopyrimidine derivatives, and pharmaceutically acceptable salts thereof that are useful for treating cell proliferative disease and disorder such as cancer and immune disease. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefore. The invention also provides useful intermediates generated during the syntheses of the aminopyrimidine derivatives.

摘要翻译： 本发明提供了一组可用于治疗细胞增殖性疾病和病症如癌症和免疫疾病的蛋白激酶抑制剂，氨基嘧啶衍生物及其药学上可接受的盐。 本发明提供了合成和施用蛋白激酶抑制剂化合物的方法。 本发明还提供了包含至少一种蛋白激酶抑制剂化合物以及药学上可接受的载体，稀释剂或赋形剂的药物制剂。 本发明还提供了在合成氨基嘧啶衍生物期间产生的有用的中间体。

公开(公告)号：US08633223B2

公开(公告)日：2014-01-21

申请号：US13726937

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： A61K31/445 ,  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 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.

摘要翻译： 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

申请人： YUHAN CORPORATION

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

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

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 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.

摘要翻译： 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。