公开(公告)号：US20130116439A1

公开(公告)日：2013-05-09

申请号：US13726932

申请日：2012-12-26

Applicant: YUHAN CORPORATION

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

IPC: C07D401/04

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 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.

Abstract translation: 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：US09663495B2

公开(公告)日：2017-05-30

申请号：US14786837

申请日：2014-04-22

Applicant: YUHAN CORPORATION

Inventor： Tae-Dong Han ,  Eun-Hye Jung ,  Chung-Ho Yi ,  Byoung-Moon Lee ,  Yoo-Hoi Park ,  Dong-Hoon Lee ,  Jong-Ho Kang ,  Na-Yeon Yang ,  Do-Hoon Kim ,  Kwan-Hoon Hyun ,  Kaap-Joo Park ,  Chun-Ho Lee ,  Su-Youn Nam

IPC: C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07C403/10 ,  C07C403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D413/14 ,  C07D249/12 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14

CPC classification number: C07D401/14 ,  C07D249/12 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14

Abstract: Provided is a triazolone derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The triazolone derivative or its pharmaceutically acceptable salt can effectively activate GPR119; and therefore be usefully applied for preventing or treating diabetes mellitus.

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。

公开(公告)号：US09376420B2

公开(公告)日：2016-06-28

申请号：US14438299

申请日：2013-10-23

Applicant: YUHAN CORPORATION

Inventor： Chan-Sun Park ,  Young-Hwan Kim ,  Gyu-Jin Lee ,  Youn Hur ,  Eun-Hye Jung ,  Hee-Jae Tak ,  Seung-Yub Shin ,  Ho-Jin Lee ,  Chun-Ho Lee ,  Koo-Yeon Lee

IPC: C07D403/04 ,  C07D231/06 ,  C07D401/10 ,  C07D403/10 ,  C07D401/06

CPC classification number: C07D403/10 ,  C07D231/06 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04

Abstract: The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis.

Abstract translation: 本发明提供了4,5-二氢-1H-吡唑衍生物或其药学上可接受的盐，其制备方法和包含其的药物组合物。 4,5-二氢-1H-吡唑衍生物或其药学上可接受的盐有效地增加LXR转录活性，因此可用于预防或治疗胆固醇代谢功能障碍，例如胆固醇胆结石，高脂血症或冠状动脉粥样硬化。

公开(公告)号：US20150291563A1

公开(公告)日：2015-10-15

申请号：US14438299

申请日：2013-10-23

Applicant: YUHAN CORPORATION

Inventor： Chan-Sun Park ,  Young-Hwan Kim ,  Gyu-Jin Lee ,  Youn Hur ,  Eun-Hye Jung ,  Hee-Jae Tak ,  Seung-Yub Shin ,  Ho-Jin Lee ,  Chun-Ho Lee ,  Koo-Yeon Lee

IPC: C07D403/10 ,  C07D401/10 ,  C07D231/06 ,  C07D403/04

CPC classification number: C07D403/10 ,  C07D231/06 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04

Abstract: The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis.

Abstract translation: 本发明提供了4,5-二氢-1H-吡唑衍生物或其药学上可接受的盐，其制备方法和包含其的药物组合物。 4,5-二氢-1H-吡唑衍生物或其药学上可接受的盐有效地增加LXR转录活性，因此可用于预防或治疗胆固醇代谢功能障碍，例如胆固醇胆结石，高脂血症或冠状动脉粥样硬化。

公开(公告)号：US08487106B2

公开(公告)日：2013-07-16

申请号：US13726932

申请日：2012-12-26

Applicant: Yuhan Corporation

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

IPC: 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 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.

Abstract translation: 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。