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：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：US20140161880A1

公开(公告)日：2014-06-12

申请号：US14234219

申请日：2012-07-20

申请人： Jeong-Hoon Woo ,  Woon-Sook Na ,  Yang-Soo Jeong ,  Chang-Keun Hyun ,  Yoong-Sik Park

发明人： Jeong-Hoon Woo ,  Woon-Sook Na ,  Yang-Soo Jeong ,  Chang-Keun Hyun ,  Yoong-Sik Park

IPC分类号： A61K9/24 ,  A61K9/20 ,  A61K31/197

CPC分类号： A61K9/209 ,  A61K9/0065 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2095 ,  A61K31/197

摘要： Provided is a sustained release tablet having two-phase release-controlling system, which consists of a first release-controlling phase comprising pregabalin or its salt and hydroxypropyl methylcellulose; and a second release-controlling phase comprising polyethylene oxide as a swelling polymer, the first release-controlling phase being homogeneously dispersed in the second release-controlling phase.

摘要翻译： 提供了一种具有两相释放控制系统的缓释片剂，其由包含普瑞巴林或其盐和羟丙基甲基纤维素的第一释放控制相组成; 以及包含聚环氧乙烷作为溶胀聚合物的第二释放控制阶段，第一释放控制阶段均匀分散在第二释放控制阶段。

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：US08461146B2

公开(公告)日：2013-06-11

申请号：US12993418

申请日：2009-05-19

申请人： Hyun Uk Seol ,  Young Sung Lee ,  Young Hun Kim ,  Kyeong Bae Kim ,  Jeong Min Seo ,  Kyoung Kyu Ahn

发明人： Hyun Uk Seol ,  Young Sung Lee ,  Young Hun Kim ,  Kyeong Bae Kim ,  Jeong Min Seo ,  Kyoung Kyu Ahn

IPC分类号： A61K31/55 ,  A61K31/137 ,  A61K31/138 ,  A61P15/00

CPC分类号： A61K45/06 ,  A61K31/135 ,  A61K31/138 ,  A61K31/55 ,  A61K2300/00

摘要： The present invention provides an oral pharmaceutical composition for the treatment of premature ejaculation, and the composition provides the effective and excellent treatment of premature ejaculation as well as reduced side effects like nausea, vomiting, drowsiness, sedation effect, awakening effect, and weight-loss etc.

摘要翻译： 本发明提供了一种用于治疗早泄的口服药物组合物，并且该组合物提供了有效和优异的早泄治疗以及减少的副作用，如恶心，呕吐，嗜睡，镇静作用，觉醒作用和体重减轻 等等

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。

公开(公告)号：US20110071138A1

公开(公告)日：2011-03-24

申请号：US12993418

申请日：2009-05-19

申请人： Hyun Uk Seol ,  Young Sung Lee ,  Young Hun Kim ,  Kyeong Bae Kim ,  Jeong Min Seo ,  Kyoung Kyu Ahn

发明人： Hyun Uk Seol ,  Young Sung Lee ,  Young Hun Kim ,  Kyeong Bae Kim ,  Jeong Min Seo ,  Kyoung Kyu Ahn

IPC分类号： A61K31/55 ,  A61P15/00

CPC分类号： A61K45/06 ,  A61K31/135 ,  A61K31/138 ,  A61K31/55 ,  A61K2300/00

摘要： The present invention provides an oral pharmaceutical composition for the treatment of premature ejaculation, and the composition provides the effective and excellent treatment of premature ejaculation as well as reduced side effects like nausea, vomiting, drowsiness, sedation effect, awakening effect, and weight-loss etc.

摘要翻译： 本发明提供了一种用于治疗早泄的口服药物组合物，并且该组合物提供了有效和优异的早泄治疗以及减少的副作用，如恶心，呕吐，嗜睡，镇静作用，觉醒作用和体重减轻 等等

公开(公告)号：US20080312408A1

公开(公告)日：2008-12-18

申请号：US12160704

申请日：2006-01-13

申请人： Bok-Luel Lee ,  Ji-Won Park ,  Byung-Rok Je ,  Nam-Chul Ha

发明人： Bok-Luel Lee ,  Ji-Won Park ,  Byung-Rok Je ,  Nam-Chul Ha

IPC分类号： C07K9/00 ,  C07H21/04 ,  C07K1/22

CPC分类号： C07K1/22 ,  C07K9/001 ,  C07K14/43504

摘要： Provided is a method of separating a peptidoglycan-recognition protein from the hemolymph of Tenebrio molitor larvae, the method including: (a) preparing an affinity chromatography column by packing a column with a resin bound with at least one synthetic peptidoglycan; (b) applying the hemolymph of Tenebrio molitor larvae to the affinity chromatography column; (c) applying a mobile phase to the affinity chromatography column to obtain a peptidoglycan-recognition protein-containing solution eluted from the affinity chromatography column; and (d) purifying a peptidoglycan-recognition protein from the eluted solution.

摘要翻译： 本发明提供了一种将聚乙烯吡咯烷酮识别蛋白与泰乐菌幼虫血淋巴分离的方法，该方法包括：（a）通过用至少一种合成肽聚糖结合的树脂填充柱制备亲和色谱柱; （b）将Tenebrio molitor幼虫的血淋巴应用于亲和层析柱; （c）将流动相施加到亲和色谱柱上，以获得从亲和色谱柱洗脱的含有聚肽聚糖识别蛋白的溶液; 和（d）从洗脱液中纯化肽聚糖识别蛋白。