公开(公告)号：US20130331377A1

公开(公告)日：2013-12-12

申请号：US14001475

申请日：2012-02-24

Applicant: 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

Inventor： 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: C07D417/04 ,  C07D413/14 ,  C07D403/04 ,  C07D401/04 ,  C07D413/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: 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：US20070129414A1

公开(公告)日：2007-06-07

申请号：US10574795

申请日：2004-10-15

Applicant: Tai Au Lee ,  Sang Sun Park ,  Doo Byung Lee ,  Sang Jung Kim

Inventor： Tai Au Lee ,  Sang Sun Park ,  Doo Byung Lee ,  Sang Jung Kim

IPC: A61K31/4178 ,  C07D403/02

CPC classification number: C07D403/06

Abstract: 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or its salt is prepared in high yield by reacting a compound of formula 2 with a compound of formula 3 and a compound of formula 4 in the presence of an acid, an alkylsilylhalide compound or an acylhalide compound, in an solvent, and thus, such an inventive process can be favorably applied to a large-scale mass production thereof.

Abstract translation: -1,2,3,9-四氢-9-甲基-3 - [（2-甲基-1H-咪唑-1-基）甲基] -4H-咔唑-4-酮或其盐通过使 在酸，烷基甲硅烷基卤化合物或酰卤化合物的存在下，在溶剂中，式2化合物与式3化合物和式4化合物反应，因此，本发明方法可有利地应用于大 - 大规模生产。

公开(公告)号：US07220861B2

公开(公告)日：2007-05-22

申请号：US10537945

申请日：2003-12-19

Applicant: Tai Au Lee ,  Nam Jin Park ,  Ja Heouk Khoo ,  Seong Ho Song ,  Ju Young An

Inventor： Tai Au Lee ,  Nam Jin Park ,  Ja Heouk Khoo ,  Seong Ho Song ,  Ju Young An

IPC: C07D215/56 ,  C07D498/06

CPC classification number: C07D471/04

Abstract: Provided is a process for preparing quinolonecarboxylate derivatives under a mild condition in high yield, so as to be favorably applied to a large-scale mass production thereof.

Abstract translation: 本发明提供了一种以高产率在温和条件下制备喹诺酮羧酸酯衍生物的方法，从而有利地用于大规模批量生产。

公开(公告)号：US06689913B2

公开(公告)日：2004-02-10

申请号：US10330927

申请日：2002-12-27

Applicant: Tai-Au Lee ,  Kyu-Jung Wang ,  Hong-Bae Kim ,  Kyoung-Chan Kwon ,  Chang-Hoe Ku

Inventor： Tai-Au Lee ,  Kyu-Jung Wang ,  Hong-Bae Kim ,  Kyoung-Chan Kwon ,  Chang-Hoe Ku

IPC: C07C20900

CPC classification number: C07C209/28 ,  C07C211/30

Abstract: Provided is a process for preparing terbinafine or its HCl salt comprising: reacting a furan derivative with a base to form a second compound; performing a reductive alkylation of the second compound obtained in the step with N-methyl-1-naphthalenemethylamine or its HCl salt to form a third compound; and purifying the third compound.

Abstract translation: 提供了一种制备特比萘芬或其HCl盐的方法，包括：使呋喃衍生物与碱反应形成第二化合物; 用N-甲基-1-萘甲胺或其HCl盐进行步骤中获得的第二化合物的还原烷基化，形成第三化合物; 并纯化第三化合物。

公开(公告)号：US20130338179A1

公开(公告)日：2013-12-19

申请号：US14001489

申请日：2012-02-24

Applicant: 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

Inventor： 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: C07D403/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: 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：US07521565B2

公开(公告)日：2009-04-21

申请号：US10574795

申请日：2004-10-15

Applicant: Tai Au Lee ,  Sang Sun Park ,  Doo Byung Lee ,  Sang Jung Kim

Inventor： Tai Au Lee ,  Sang Sun Park ,  Doo Byung Lee ,  Sang Jung Kim

IPC: C07D403/06

CPC classification number: C07D403/06

Abstract: 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or its salt is prepared in high yield by reacting a compound of formula 2 with a compound of formula 3 and a compound of formula 4 in the presence of an acid, an alkylsilylhalide compound or an acylhalide compound, in an solvent, and thus, such an inventive process can be favorably applied to a large-scale mass production thereof.

Abstract translation: -1,2,3,9-四氢-9-甲基-3 - [（2-甲基-1H-咪唑-1-基）甲基] -4H-咔唑-4-酮或其盐通过使 在酸，烷基甲硅烷基卤化合物或酰卤化合物的存在下，在溶剂中，式2化合物与式3化合物和式4化合物反应，因此，本发明方法可有利地应用于大量 - 大规模生产。

公开(公告)号：US09850227B2

公开(公告)日：2017-12-26

申请号：US14001475

申请日：2012-02-24

Applicant: 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

Inventor： 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: A01N43/00 ,  A01N43/46 ,  A61K31/55 ,  C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: 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：US06706888B2

公开(公告)日：2004-03-16

申请号：US10359057

申请日：2003-02-06

Applicant: Jeong-Seok Chae ,  Tai-Au Lee ,  Sang-Seon Park ,  Doo-Byung Lee ,  Beom-Joo Maeng

Inventor： Jeong-Seok Chae ,  Tai-Au Lee ,  Sang-Seon Park ,  Doo-Byung Lee ,  Beom-Joo Maeng

IPC: C07D23354

CPC classification number: C07D233/64

Abstract: The present invention provides a process for preparing an imidazole derivative or its salt which comprises reacting a tetrahydrofuran or tetrahydropyran derivative with formamidine or its salt in the presence of a base.

Abstract translation: 本发明提供了制备咪唑衍生物或其盐的方法，其包括在碱的存在下使四氢呋喃或四氢吡喃衍生物与甲脒或其盐反应。

公开(公告)号：US09890138B2

公开(公告)日：2018-02-13

申请号：US14001489

申请日：2012-02-24

Applicant: 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

Inventor： 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: C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: 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：US20150274700A2

公开(公告)日：2015-10-01

申请号：US14001489

申请日：2012-02-24

Applicant: 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

Inventor： 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: C07D403/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: 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.

Abstract translation: 本发明提供二氨基嘧啶衍生物或其药学上可接受的盐，其制备方法，包含该二胺化合物的药物组合物及其用途。 二氨基嘧啶衍生物或其药学上可接受的盐用作5-HT 4受体激动剂，因此可用于预防或治疗胃肠道运动功能障碍，胃肠道疾病之一，例如胃食管反流病（GERD），便秘，易怒 肠综合征（IBS），消化不良，术后肠梗阻，胃排空迟缓，胃轻瘫，肠假性梗阻，药物诱导的延迟转移或糖尿病胃失调。