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1. 发明申请

WO2005021539A1 BENZIMIDAZOLONE COMPOUNDS HAVING 5-HT4 RECEPTOR AGONISTIC ACTIVITY 审中-公开
标题翻译：具有5-HT4受体激活活性的苯并咪唑化合物
公开(公告)号：WO2005021539A1
公开(公告)日：2005-03-10
申请号：PCT/IB2004/002741
申请日：2004-08-20
申请人： PFIZER JAPAN, INC. , PFIZER INC. , IGUCHI, Satoru , KATSU, Yasuhiro , SONE, Hiroki , UCHIDA, Chikara , KOJIMA, Takashi
发明人： IGUCHI, Satoru , KATSU, Yasuhiro , SONE, Hiroki , UCHIDA, Chikara , KOJIMA, Takashi
IPC分类号： C07D405/14
CPC分类号： C07D413/14 , C04B35/632 , C07D401/12 , C07D405/06 , C07D405/14
摘要： This invention provides a compound of the formula (I) or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT 4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，以及含有这些化合物的组合物，以及这些化合物在制备胃食管反流疾病，胃肠道疾病，胃动力障碍，非溃疡性消化不良的药物中的用途，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病和呼吸暂停综合征。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

2. 发明申请

WO2005123718A2 BENZIMIDAZOLONE CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：苯并咪唑羧酸羧酸衍生物
公开(公告)号：WO2005123718A2
公开(公告)日：2005-12-29
申请号：PCT/IB2005/001825
申请日：2005-06-01
申请人： PFIZER JAPAN INC. , PFIZER INC., , ANDO, Koji , IGUCHI, Satoru , MURASE, Noriaki , MURATA, Yoshinori , NUMATA, Toyoharu , SONE, Hiroki , UCHIDA, Chikara , UEKI, Tatsuo
发明人： ANDO, Koji , IGUCHI, Satoru , MURASE, Noriaki , MURATA, Yoshinori , NUMATA, Toyoharu , SONE, Hiroki , UCHIDA, Chikara , UEKI, Tatsuo
IPC分类号： C07D403/00
CPC分类号： C07D401/12 , C07D211/26 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14
摘要： This invention relates to compounds of the formula (I): wherein R 1 , R 2 , R 3 , A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT 4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
摘要翻译：本发明涉及式（I）的化合物：其中R 1，R 2，R 3，A和m各自如本文所述，或其药学上可接受的盐或溶剂合物，以及含有这些化合物的组合物以及这些化合物在治疗由5-HT4受体活性介导的病症（例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征 IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病如心脏衰竭和心律失常，糖尿病和呼吸暂停综合征。

3. 发明申请

WO2006090279A1 OXYINDOLE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS 审中-公开
标题翻译：氧化衍生物作为5HT4受体激动剂
公开(公告)号：WO2006090279A1
公开(公告)日：2006-08-31
申请号：PCT/IB2006/000519
申请日：2006-02-10
申请人： PFIZER JAPAN INC. , PFIZER INC. , KAWAMURA, Kiyoshi , SONE, Hiroki , UCHIDA, Chikara
发明人： KAWAMURA, Kiyoshi , SONE, Hiroki , UCHIDA, Chikara
IPC分类号： C07D405/14 , C07D401/14 , C07D401/12 , A61K31/454 , A61P1/04
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R 1 , R 2 , R 3 , R4 and R 5 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT 4 agonisitic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：A，R 1，R 2，R 3，其中R 4和R 5各自如本文所述或其药学上可接受的盐，以及含有这些化合物的组合物以及这些化合物在治疗病症介导中的用途通过5-HT 4激动剂活性，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病或呼吸暂停综合征。

4. 发明申请

WO2013063068A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2013063068A1
公开(公告)日：2013-05-02
申请号：PCT/US2012/061625
申请日：2012-10-24
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD , ALBANY MOLECULAR RESEARCH, INC. , CHACKALAMANNIL, Samuel , OHKOUCHI, Munetaka , VOSS, Matthew , SONE, Hiroki
发明人： CHACKALAMANNIL, Samuel , OHKOUCHI, Munetaka , VOSS, Matthew , SONE, Hiroki
IPC分类号： A61K31/4412
CPC分类号： C07D401/12 , A61K31/4375 , A61K31/4439 , A61K31/4725 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：本发明提供本文所述的式（I）化合物或其药学上可接受的盐。本发明还提供包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。

5. 发明申请

WO2015164308A1 FACTOR XIa INHIBITORS 审中-公开
标题翻译：因子XIA抑制剂
公开(公告)号：WO2015164308A1
公开(公告)日：2015-10-29
申请号：PCT/US2015/026774
申请日：2015-04-21
申请人： MERCK SHARP & DOHME CORP. , LIM, Yeon-Hee , GUO, Zhuyan , ALI, Amjad , EDMONDSON, Scott, D. , LIU, Weiguo , GALLO-ETIENNE, Gioconda, V. , WU, Heping , GAO, Ying-Duo , STAMFORD, Andrew, M. , YU, Younong , KEVIN, Nancy, J. , ANAND, Rajan , SHA, Deyou , NEELAMKAVIL, Santhosh, F. , HUSSAIN, Zahid , KUMAR, Puneet , MONINGKA, Remond , DUFFY, Joseph, L. , XU, Jiayi , JIANG, Yu , SONE, Hiroki , CHAKRABARTI, Anjan
发明人： LIM, Yeon-Hee , GUO, Zhuyan , ALI, Amjad , EDMONDSON, Scott, D. , LIU, Weiguo , GALLO-ETIENNE, Gioconda, V. , WU, Heping , GAO, Ying-Duo , STAMFORD, Andrew, M. , YU, Younong , KEVIN, Nancy, J. , ANAND, Rajan , SHA, Deyou , NEELAMKAVIL, Santhosh, F. , HUSSAIN, Zahid , KUMAR, Puneet , MONINGKA, Remond , DUFFY, Joseph, L. , XU, Jiayi , JIANG, Yu , SONE, Hiroki , CHAKRABARTI, Anjan
IPC分类号： C07D471/10 , A61K31/438 , C07D498/20
CPC分类号： C07D498/20 , C07D471/10 , C07D487/10 , C07D498/10 , C07F9/6561
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
摘要翻译：本发明提供式（I）的化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。

6. 发明申请

WO2010062265A1 THERAPEUTIC MACROLIDE COMPOUNDS AND THEIR USE 审中-公开
标题翻译：治疗性大鼠化合物及其用途
公开(公告)号：WO2010062265A1
公开(公告)日：2010-06-03
申请号：PCT/SG2009/000446
申请日：2009-11-24
申请人： MERLION PHARMACEUTICALS PTE LTD , BOYCE, Rustum S. , SIHOMBING, Muhammad Sofian Asi , SONE, Hiroki
发明人： BOYCE, Rustum S. , SIHOMBING, Muhammad Sofian Asi , SONE, Hiroki
IPC分类号： C07D407/06 , A61K31/4427 , A61K31/551 , C07D413/14 , A61K31/365 , A61K31/4523 , A61K31/553 , A61K31/404 , A61K31/496 , A61P35/00 , A61K31/422 , A61K31/5377 , C07D407/14
CPC分类号： C07D407/06 , C07D403/14 , C07D405/14 , C07D413/14
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as "MC compounds"), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
摘要翻译：本发明一般涉及治疗化合物的领域，更具体地涉及某些大环内酯类化合物（为方便起见，本文统称为“MC化合物”），其尤其可用于治疗癌症。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以治疗增殖性疾病如癌症，以及治疗由调节介导的疾病和病症（例如抑制）细胞增殖，任选与另一种试剂组合。

7. 发明申请

WO2002085862A1 IMIDAZOLIDINE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：咪唑啉衍生物作为化合物受体调节剂
公开(公告)号：WO2002085862A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/012650
申请日：2002-04-19
申请人： MILLENNIUM PHARMACEUTICALS, INC. , KYOWA HAKKO KOGYO CO., LTD. , OHSHIMA, Etsuo , SONE, Hiroki , KOTERA, Osamu , KOMATSU, Rie , LAROSA, Gregory, J. , LULY, Jay, R.
发明人： OHSHIMA, Etsuo , SONE, Hiroki , KOTERA, Osamu , KOMATSU, Rie , LAROSA, Gregory, J. , LULY, Jay, R.
IPC分类号： C07D233/26
CPC分类号： C07D233/26
摘要： Disclosed are novel compounds and a method of treating inflammatory diseases. The method comprises administering to an individual in need an effective amount of an imidazolidine compound represented by Structural Formula (I): and physiologically or pharmaceutically acceptable salts thereof.
摘要翻译：公开了新型化合物和治疗炎性疾病的方法。该方法包括向需要的个体施用有效量的由结构式（I）表示的咪唑烷化合物及其生理学或药学上可接受的盐。

8. 发明申请

WO2002085861A1 IMIDAZOLIDINE COMPOUNDS AND THEIR USE AS CXCR3 ANTAGONISTS 审中-公开
标题翻译：咪唑啉化合物及其作为CXCR3拮抗剂的用途
公开(公告)号：WO2002085861A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/012647
申请日：2002-04-19
申请人： MILLENNIUM PHARMACEUTICALS, INC. , KYOWA HAKKO KOGYO CO., LTD. , OHSHIMA, Etsuo , SONE, Hiroki , KOTERA, Osamu , KOMATSU, Rie , LAROSA, Gregory, J. , LULY, Jay, R.
发明人： OHSHIMA, Etsuo , SONE, Hiroki , KOTERA, Osamu , KOMATSU, Rie , LAROSA, Gregory, J. , LULY, Jay, R.
IPC分类号： C07D233/26
CPC分类号： C07D405/12 , C07D233/26 , C07D409/12
摘要： Disclosed are novel compounds and a method of treating inflammatory diseases. The method comprises administering to an individual in need an effective amount of an imidazolidine compound represented by Structural Formula (1): and physiologically of pharmaceutically acceptable salts thereof.
摘要翻译：公开了新型化合物和治疗炎性疾病的方法。该方法包括向需要的个体施用有效量的由结构式（1）表示的咪唑烷化合物：及其生理学上可药用的盐。

9. 发明申请

WO2003087063A1 IMIDAZOLIDINE COMPOUNDS AS CHEMOKINE RECEPTOR MODULATORS 审中-公开
标题翻译：咪唑啉化合物作为化学受体调节剂
公开(公告)号：WO2003087063A1
公开(公告)日：2003-10-23
申请号：PCT/US2003/011618
申请日：2003-04-14
申请人： KYOWA HAKKO KOGYO CO., LTD. , MILLENIUM PHARMACEUTICALS, INC. , OHSHIMA, Etsuo , SONE, Hiroki , KOTERA, Osamu , LULY, Jay, R. , LAROSA, Gregory, J.
发明人： OHSHIMA, Etsuo , SONE, Hiroki , KOTERA, Osamu , LULY, Jay, R. , LAROSA, Gregory, J.
IPC分类号： C07D233/26
CPC分类号： C07D401/12 , C07D233/26 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Disclosed are novel compounds and a method of treating inflammatory diseases. The method comprises administering to an individual in need an effective amount of an imidazolidine compound represented by Structural Formula (I), or quaternary ammonium salt thereof, or a solvate thereof, or a physiologically or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了新型化合物和治疗炎性疾病的方法。该方法包括向需要的个体施用有效量的由结构式（I）表示的咪唑烷化合物或其季铵盐，或其溶剂合物或其生理学或药学上可接受的盐。

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