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1. 发明申请

WO2006091769A1 NOVEL QUINOLINE DERIVATIVES AS POTASSIUM ION CHANNEL OPENERS 审中-公开
标题翻译：新型喹啉衍生物作为离子通道开放剂
公开(公告)号：WO2006091769A1
公开(公告)日：2006-08-31
申请号：PCT/US2006/006515
申请日：2006-02-23
申请人： JANSSEN PHARMACEUTICA N.V. , JAIN, Nareshkumar , XU, Jiayi , SUI, Zhihua
发明人： JAIN, Nareshkumar , XU, Jiayi , SUI, Zhihua
IPC分类号： C07D215/54 , A61K31/47 , A61P13/00 , A61P15/00 , A61P25/00
CPC分类号： C07D215/54
摘要： ABSTRACT The present invention is directed to novel quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels.
摘要翻译：摘要本发明涉及新颖的喹啉衍生物，含有它们的药物组合物及其用于治疗与离子通道如钾通道相关的疾病的用途。

2. 发明申请

WO2006091800A2 NOVEL PYRIDINE DERIVATIVES AS POTASSIUM ION CHANNEL OPENERS 审中-公开
标题翻译：新型吡啶衍生物作为钾离子通道开放剂
公开(公告)号：WO2006091800A2
公开(公告)日：2006-08-31
申请号：PCT/US2006/006566
申请日：2006-02-23
申请人： JANSSEN PHARMACEUTICA N.V. , JAIN, Nareshkumar , XU, Jiayi , SUI, Zhihua
发明人： JAIN, Nareshkumar , XU, Jiayi , SUI, Zhihua
IPC分类号： C07D213/30 , C07D491/04 , A61K31/44 , A61P9/00
CPC分类号： C07D213/48 , C07D213/30 , C07D213/50 , C07D213/57 , C07D215/54 , C07D491/04 , C07F7/1856
摘要： The present invention is directed to novel pyridine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels.
摘要翻译：本发明涉及新颖的吡啶衍生物，含有它们的药物组合物及其用于治疗与离子通道如钾通道有关的疾病的用途。

3. 发明申请

WO2006055694A1 NOVEL 2H-CHROMENE DERIVATIVES AS SELECTIVE ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：新的2H-色酮衍生物作为选择性雌激素受体调节剂
公开(公告)号：WO2006055694A1
公开(公告)日：2006-05-26
申请号：PCT/US2005/041648
申请日：2005-11-17
申请人： JANSSEN PHARMACEUTICA N.V. , JAIN, Nareshkumar F. , XU, Jiayi , SUI, Zhihua
发明人： JAIN, Nareshkumar F. , XU, Jiayi , SUI, Zhihua
IPC分类号： C07D311/60 , C07D311/78 , C07D311/80 , C07D493/04 , A61K31/352 , A61K31/35 , A61P5/28
CPC分类号： C07D493/04 , C07D311/18 , C07D311/60 , C07D311/78 , C07F7/1856
摘要： The present invention is directed to novel 2H-chromene derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more estrogen receptors and processes for their preparation.
摘要翻译：本发明涉及新的2H-色烯衍生物，含有它们的药物组合物，其用于治疗由一种或多种雌激素受体介导的病症及其制备方法。

4. 发明申请

WO2015160636A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2015160636A1
公开(公告)日：2015-10-22
申请号：PCT/US2015/025229
申请日：2015-04-10
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
发明人： SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC分类号： C07D413/14 , C07D261/20 , C07D207/02
CPC分类号： C07D413/14 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K45/06 , C07D413/04 , C07D417/14 , C07D471/04 , C07D498/04 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：在其许多实施方案中，本发明提供了一类新的由式（I）表示的苯甲酰胺化合物或其药学上可接受的盐或溶剂合物，或包含一种或多种所述化合物或药学上可接受的盐或其溶剂化物，以及使用所述化合物或其药学上可接受的盐或溶剂合物治疗或预防血栓形成，栓塞，高凝血性或纤维变性的方法。

5. 发明申请

WO2014099584A1 NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT 审中-公开
标题翻译：新的2-吡啶甲酰胺衍生物，包含这些化合物的组合物和处理方法
公开(公告)号：WO2014099584A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/074584
申请日：2013-12-12
申请人： MERCK SHARP & DOHME CORP. , LIN, Songnian , PARMEE, Emma, R. , XU, Jiayi
发明人： PARMEE, Emma, R. , XU, Jiayi
IPC分类号： C07D401/14
CPC分类号： C07D417/12 , A61K31/4439 , A61K31/444 , A61K31/675 , C07D401/12 , C07D417/14 , C07F9/65583
摘要： Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment.
摘要翻译：公开了新的式I吡啶-2-甲酰胺衍生物及其药学上可接受的盐，用于治疗或预防2型糖尿病和类似病症。这些化合物作为葡萄糖激酶活化剂是有效的。还包括药物组合物和治疗方法。本发明涉及作为葡糖激酶活化剂有效的新型吡啶-2-甲酰胺衍生物及其盐。此外，它涉及含有这些化合物的组合物和治疗方法。

6. 发明申请

WO2017074832A1 FACTOR XIa INHIBITORS 审中-公开
标题翻译：因子XIa抑制剂
公开(公告)号：WO2017074832A1
公开(公告)日：2017-05-04
申请号：PCT/US2016/058362
申请日：2016-10-24
申请人： MERCK SHARP & DOHME CORP. , XU, Jiayi , ALI, Amjad , ZHOU, Wei , GAO, Ying-Duo , EDMONDSON, Scott, D. , MERTZ, Eric , NEELAMKAVIL, Santhosh, F. , LIU, Weiguo , SUN, Wanying , SHEN, Dong-Ming , HARPER, Bart , ZHU, Cheng , BARA, Thomas , LIM, Yeon-Hee , YANG, Meng
发明人： XU, Jiayi , ALI, Amjad , ZHOU, Wei , GAO, Ying-Duo , EDMONDSON, Scott, D. , MERTZ, Eric , NEELAMKAVIL, Santhosh, F. , LIU, Weiguo , SUN, Wanying , SHEN, Dong-Ming , HARPER, Bart , ZHU, Cheng , BARA, Thomas , LIM, Yeon-Hee , YANG, Meng
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , C07D213/02 , C07D213/04 , C07D401/06
CPC分类号： C07D513/08 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/14 , C07D471/08 , C07D487/04 , C07D487/08
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）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，高凝状态或纤维化改变的方法。这些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。

7. 发明申请

WO2016109221A1 BTK INHIBITORS 审中-公开
标题翻译： BTK抑制剂
公开(公告)号：WO2016109221A1
公开(公告)日：2016-07-07
申请号：PCT/US2015/066229
申请日：2015-12-17
申请人： MERCK SHARP & DOHME CORP. , LIU, Jian , KOZLOWSKI, Joseph, A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
发明人： LIU, Jian , KOZLOWSKI, Joseph, A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , WANG, Dahai , WU, Hao , YANG, Chundao
IPC分类号： A61K31/5377 , A61K31/55 , C07D487/04 , A61K31/541
CPC分类号： A61K45/06 , C07D519/00
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
摘要翻译：本发明提供了布鲁顿的式I的酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐，式I或包含这些化合物的药物组合物及其在治疗中的用途。特别地，本发明涉及式I的Btk抑制剂化合物在治疗Btk介导的病症中的用途。

8. 发明申请

WO2016106625A1 BTK INHIBITORS 审中-公开
标题翻译： BTK抑制剂
公开(公告)号：WO2016106625A1
公开(公告)日：2016-07-07
申请号：PCT/CN2014/095766
申请日：2014-12-31
申请人： MERCK SHARP & DOHME CORP. , LIU, Jian , KOZLOWSKI, Joseph A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
发明人： LIU, Jian , KOZLOWSKI, Joseph A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
IPC分类号： C07D487/04 , C07D471/04 , C07D519/06 , A61K31/4985 , A61K31/5365 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/437 , A61P19/02 , A61P11/00 , A61P21/04 , A61P25/00 , A61P3/10 , A61P7/02
CPC分类号： A61K45/06 , C07D519/00
摘要： Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders is provided.
摘要翻译：提供了根据式I的Bruton的酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐，包含这些化合物的药物组合物及其在治疗中的用途。特别地，提供了使用Btk抑制剂式I化合物治疗Btk介导的病症。

9. 发明申请

WO2015160634A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2015160634A1
公开(公告)日：2015-10-22
申请号：PCT/US2015/025219
申请日：2015-04-10
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
发明人： SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC分类号： C07D413/14 , C07D261/20 , C07D207/02
CPC分类号： A61K31/439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/52 , C07D261/20 , C07D413/04 , C07D413/14 , C07D498/04 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：在其许多实施方案中，本发明提供了由式（I）表示的新一类苯甲酰胺化合物或其药学上可接受的盐或溶剂化物，或包含一种或多种所述化合物或其药学上可接受的盐或溶剂化物的药物组合物，以及使用所述化合物或其药学上可接受的盐或溶剂合物用于治疗或预防血栓形成，栓塞，高凝状态或纤维变性。

10. 发明申请

WO2014120346A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2014120346A1
公开(公告)日：2014-08-07
申请号：PCT/US2013/075233
申请日：2013-12-16
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , XU, Jiayi , CHEN, Yi-heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , NAGASUE, Hiroshi , OGAWA, Kouki
发明人： SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , XU, Jiayi , CHEN, Yi-heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , NAGASUE, Hiroshi , OGAWA, Kouki
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present invention provides a compound of Formula (I) (structurally represented) wherein R1 is H or C1-6 alkyl, R2 is H or C1-6 alkyl or CH20H, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or-CH20H, and when R2, R3, and R4 are H, then R1 is C 1-6 alkyl; A is 1 ) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and 0, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with -CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or 0, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
摘要翻译：本发明提供式（I）（结构上表示）的化合物，其中R 1是H或C 1-6烷基，R 2是H或C 1-6烷基或CH 2 OH，R 3是H或C 1-6烷基，R 4是H或 C 1 -C 6烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基，并且当R 1，R 2和R 4为H时，R 3为C 1-6烷基，并且当R 1，R 3和 R 4是H，R 2是C 1-6烷基或-CH 2 OH，当R 2，R 3和R 4是H时，R 1是C 1-6烷基; A是1）具有1-3个独立地选自N，S和0的杂原子的9-10元双环杂环，其中9-10元双环杂环是未取代的或被R5取代，未被取代或被R6取代，未被取代或被NH 2取代，或2）未被取代或被未取代或被R 6取代的R 5取代的未取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 和B为1）具有1或2个独立地选自N，S或0的杂原子的5或6元单环杂环，其未被取代或在碳或氮原子上被取代或未取代或在碳或氮上取代的R7取代具有R 8的未取代或取代的碳原子或氮原子上的取代基，或2）具有1,2或3个氮原子的8或9元稠合双环杂环，其未被取代或在碳原子或氮原子上被取代， R7，并且在碳或氮原子上未被取代或取代为R8; 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的方法。

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