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1. 发明申请

WO2017003895A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译：作为PDE2抑制剂的双相杂环化合物
公开(公告)号：WO2017003895A1
公开(公告)日：2017-01-05
申请号：PCT/US2016/039479
申请日：2016-06-27
申请人： MERCK SHARP & DOHME CORP. , STACHEL, Shawn, J. , SINZ, Christopher, J. , CHEN, Yili , WILSON, Jonathan, E. , DWYER, Michael, P. , PAONE, Daniel, V. , XU, Shimin
发明人： STACHEL, Shawn, J. , SINZ, Christopher, J. , CHEN, Yili , WILSON, Jonathan, E. , DWYER, Michael, P. , PAONE, Daniel, V. , XU, Shimin
IPC分类号： C07D487/04 , A61K31/53 , C07D231/56 , C07D253/06 , C07D253/065 , C07D253/075
CPC分类号： C07D487/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28
摘要： The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及式（I）和（II）的二氢吡唑并嘧啶酮化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂。本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症等神经和精神疾病以及与纹状体功能不全或基底神经节功能障碍相关的疾病的用途。

2. 发明申请

WO2016179059A1 HETEROARYL-PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译：异噻唑啉酮化合物作为PDE2抑制剂
公开(公告)号：WO2016179059A1
公开(公告)日：2016-11-10
申请号：PCT/US2016/030342
申请日：2016-05-02
申请人： MERCK SHARP & DOHME CORP. , SHEN, Dong-Ming , WILSON, Jonathan, E. , MCCRACKEN, Troy
发明人： SHEN, Dong-Ming , WILSON, Jonathan, E. , MCCRACKEN, Troy
IPC分类号： A61K31/513 , C07D403/04 , C07D239/36
CPC分类号： C07D417/04 , C07D239/36 , C07D401/04 , C07D403/04 , C07D413/04
摘要： The present invention is directed to substituted pyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及式（I）的取代嘧啶酮化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂。本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症以及与纹状体功能不全或基底神经节功能障碍相关的神经和精神疾病的用途。

3. 发明申请

WO2016145614A1 TRIAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译：三唑并嘧啶酮化合物作为PDE2抑制剂
公开(公告)号：WO2016145614A1
公开(公告)日：2016-09-22
申请号：PCT/CN2015/074396
申请日：2015-03-17
申请人： MERCK SHARP & DOHME CORP. , SHEN, Dong-Ming , SINZ, Christopher J. , CRESPO, Alexander , WILSON, Jonathan E. , MCCRACKEN, Troy , XU, Shimin , LI, Haitang
发明人： SHEN, Dong-Ming , SINZ, Christopher J. , CRESPO, Alexander , WILSON, Jonathan E. , MCCRACKEN, Troy , XU, Shimin , LI, Haitang
IPC分类号： C07D239/36 , C07D249/06 , C07D249/08 , A61K31/4192 , A61K31/4196 , A61K31/505 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24
CPC分类号： C07D498/04 , A61P25/00 , C07D403/04 , C07D471/04 , C07D487/04
摘要： The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂的式I的嘧啶甲酰胺化合物。本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症等神经和精神疾病以及与纹状体功能不全或基底神经节功能障碍相关的疾病的用途。

4. 发明申请

WO2009064949A1 IMPLANT DELIVERY SYSTEM AND METHOD 审中-公开
标题翻译：植物输送系统和方法
公开(公告)号：WO2009064949A1
公开(公告)日：2009-05-22
申请号：PCT/US2008/083497
申请日：2008-11-14
申请人： CARDIOSOLUTIONS, INC. , MAURER, Christopher W. , WILSON, Jonathan E.
发明人： MAURER, Christopher W. , WILSON, Jonathan E.
IPC分类号： A61F2/24
CPC分类号： A61F2/2442 , A61F2/246 , A61F2/2466
摘要： An implant delivery system may comprise a catheter including at least one lumen, a guide wire configured to be received in the lumen, and an implant. The guide wire may comprise a clamping mechanism disposed about a distal end of the guide wire. The clamping mechanism may include a first and at least a second jaw wherein at least one of the jaws is configured to pivot between a closed position wherein the jaws define at least one internal cavity between the jaws configured to receive at least a portion of the implant and an open position configured to release the implant. The implant may be configured to be received in the lumen and may comprise a driver configured to be releasably received in the cavity of the clamping mechanism.
摘要翻译：植入物递送系统可以包括导管，其包括至少一个内腔，被配置为容纳在内腔中的导丝和植入物。引导线可以包括围绕导丝的远端设置的夹紧机构。夹紧机构可以包括第一和至少第二钳口，其中至少一个钳口构造成在闭合位置之间枢转，其中钳口限定钳口之间的至少一个内部空腔，构造成接收植入物的至少一部分以及构造成释放植入物的打开位置。植入物可以构造成容纳在内腔中，并且可以包括构造成可释放地容纳在夹紧机构的空腔中的驱动器。

5. 发明申请

WO2016149058A1 TRIAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译：三唑基嘧啶酮化合物作为PDE2抑制剂
公开(公告)号：WO2016149058A1
公开(公告)日：2016-09-22
申请号：PCT/US2016/021902
申请日：2016-03-11
申请人： MERCK SHARP & DOHME CORP. , SHEN, Dong-Ming , SINZ, Christopher, J. , CRESPO, Alexander , WILSON, Jonathan, E. , MCCRACKEN, Troy , XU, Shimin , LI, Haitang
发明人： SHEN, Dong-Ming , SINZ, Christopher, J. , CRESPO, Alexander , WILSON, Jonathan, E. , MCCRACKEN, Troy , XU, Shimin , LI, Haitang
IPC分类号： A61K31/513 , C07D401/04 , C07D401/14
CPC分类号： C07D498/04 , A61P25/00 , C07D403/04 , C07D471/04 , C07D487/04
摘要： The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及式I的嘧啶羧酰胺化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂。本发明还涉及这类化合物用于治疗神经和精神疾病如精神分裂症，精神病，帕金森氏病，帕金森病痴呆（PDD）或亨廷顿病的用途，以及与纹状体功能减退或基底节功能障碍相关的那些化合物。 / p>

6. 发明申请

WO2014099788A1 C5-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS 审中-公开
标题翻译： C5-SPIRO三嗪基二氧化物作为BACE抑制剂
公开(公告)号：WO2014099788A1
公开(公告)日：2014-06-26
申请号：PCT/US2013075400
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , CUMMING JARED N , SCOTT JACK D , STAMFORD ANDREW W , ISERLOH ULRICH , NEELAMKAVIL SANTHOSH FRANCIS , SHAO PENGCHENG PATRICK , WILSON JONATHAN E
发明人： CUMMING JARED N , SCOTT JACK D , STAMFORD ANDREW W , ISERLOH ULRICH , NEELAMKAVIL SANTHOSH FRANCIS , SHAO PENGCHENG PATRICK , WILSON JONATHAN E
IPC分类号： A61K31/519 , A61K31/497
CPC分类号： C07D285/24 , C07D285/20 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
摘要翻译：在其许多实施方案中，本发明提供某些C5-螺亚氨基二嗪二氧化物化合物，包括式（I）化合物：（结构表示）或其互变异构体及所述化合物的药学上可接受的盐，其中R1，R2，R3，X，Y ，s，环A，RA，m，-L1-和RL如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物，

7. 发明申请

WO2017000276A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译：双环杂环化合物作为PDE2抑制剂
公开(公告)号：WO2017000276A1
公开(公告)日：2017-01-05
申请号：PCT/CN2015/083059
申请日：2015-07-01
申请人： MERCK SHARP & DOHME CORP. , SATCHEL, Shawn J. , SINZ, Christopher J. , CHEN, Yili , WILSON, Jonathan E. , DWYER, Michael , PAONE, Daniel V. , XU, Shimin
发明人： SATCHEL, Shawn J. , SINZ, Christopher J. , CHEN, Yili , WILSON, Jonathan E. , DWYER, Michael , PAONE, Daniel V. , XU, Shimin
IPC分类号： C07D487/04 , C07D487/02 , C07D487/00 , A61K31/519 , A61K31/537 , C07D487/10 , A61K31/5395 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24
CPC分类号： C07D487/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28
摘要： The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及式（I）和（II）的二氢吡唑并嘧啶酮化合物，其可用作治疗剂以治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病。本发明还涉及这类化合物用于治疗神经和精神疾病如精神分裂症，精神病，帕金森氏病，帕金森病痴呆（PDD）或亨廷顿病的用途，以及与纹状体功能减退或基底节功能障碍相关的那些化合物。 / p>

8. 发明申请

WO2013028382A1 BENZOPIPERAZINE DERIVATIVES AS CETP INHIBITORS 审中-公开
标题翻译：苯并吡嗪衍生物作为CETP抑制剂
公开(公告)号：WO2013028382A1
公开(公告)日：2013-02-28
申请号：PCT/US2012/050520
申请日：2012-08-13
申请人： MERCK SHARP & DOHME CORP. , ANAND, Rajan , COLANDREA, Vincent, J. , REITER, Maud , VACHAL, Petr , ZWICKER, Aaron , WILSON, Jonathan, E. , ZHANG, Fengqi , ZHAO, Kake
发明人： ANAND, Rajan , COLANDREA, Vincent, J. , REITER, Maud , VACHAL, Petr , ZWICKER, Aaron , WILSON, Jonathan, E. , ZHANG, Fengqi , ZHAO, Kake
IPC分类号： C07D243/00 , C07D498/00 , C07D487/00
CPC分类号： C07D409/06 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D241/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06
摘要： Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
摘要翻译：具有式Ia结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

9. 发明申请

WO2003024349A1 FLUID-ASSISTED MEDICAL DEVICES, SYSTEMS AND METHODS 审中-公开
标题翻译：流体辅助医疗设备，系统和方法
公开(公告)号：WO2003024349A1
公开(公告)日：2003-03-27
申请号：PCT/US2002/028488
申请日：2002-09-05
申请人： TISSUELINK MEDICAL, INC. , MCCLURKEN, Michael, E. , LIPSON, David , LUZZI, Robert , OYOLA, Arnold, E. , WILSON, Jonathan, E. , MAURER, Christopher, W. , GREELEY, Roger, D.
发明人： MCCLURKEN, Michael, E. , LIPSON, David , LUZZI, Robert , OYOLA, Arnold, E. , WILSON, Jonathan, E. , MAURER, Christopher, W. , GREELEY, Roger, D.
IPC分类号： A61B18/18
CPC分类号： A61B18/148 , A61B17/32 , A61B18/1206 , A61B18/1442 , A61B2018/00011 , A61B2018/00029 , A61B2018/00035 , A61B2018/00065 , A61B2018/00404 , A61B2018/00589 , A61B2018/00595 , A61B2018/00601 , A61B2018/0063 , A61B2018/00702 , A61B2018/00744 , A61B2018/00779 , A61B2018/00791 , A61B2018/00809 , A61B2018/00875 , A61B2018/126 , A61B2018/1412 , A61B2018/1417 , A61B2018/1422 , A61B2018/1455 , A61B2018/1861 , A61B2218/002
摘要： Surgical devices, systems and methods for treating tissue are provided. Also provided are systems for treating tissue and methods of treating tissue. An exemplary surgical device comprises a handle (20a) having a proximal end and a distal end; a shaft extending distally beyond the distal end of the handle, the shaft having a proximal end and a distal end; an electrode tip (45), at least a portion of the electrode tip extending distally beyond the distal end of the shaft, the electrode tip extending distally beyond the distal end of the shaft comprising a spherical end surface portion (25) and a cylindrical side surface portion, the spherical end surface portion located distal to the cylindrical side surface portion and comprising at least a portion of the distal end surface of the surgical device; and a fluid passage directed to provide a fluid towards the cylindrical side portion of the electrode tip.
摘要翻译：提供了用于治疗组织的手术装置，系统和方法。还提供了用于治疗组织的系统和处理组织的方法。示例性手术装置包括具有近端和远端的手柄（20a）远离手柄远端延伸的轴，该轴具有近端和远端; 电极尖端（45），所述电极末端的至少一部分向远侧延伸超出所述轴的远端，所述电极末端向远侧延伸超过所述轴的远端，包括球形端面部分（25）和圆柱形侧面表面部分，所述球形端表面部分位于所述圆柱形侧表面部分的远侧并且包括所述外科装置的远端表面的至少一部分; 以及用于朝向电极末端的圆柱形侧部提供流体的流体通道。

10. 发明申请

WO2016154081A1 PYRAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS 审中-公开
标题翻译： PYRAZOLYL PYRIMIDINONE化合物作为PDE2抑制剂
公开(公告)号：WO2016154081A1
公开(公告)日：2016-09-29
申请号：PCT/US2016/023344
申请日：2016-03-21
申请人： MERCK SHARP & DOHME CORP. , SHEN, Dong-Ming , YANG, Meng , CRESPO, Alexander , WILSON, Jonathan, E. , MCCRACKEN, Troy , WANG, Deping , PARKER, Dann , GUO, Zack Zhiqiang
发明人： SHEN, Dong-Ming , YANG, Meng , CRESPO, Alexander , WILSON, Jonathan, E. , MCCRACKEN, Troy , WANG, Deping , PARKER, Dann , GUO, Zack Zhiqiang
IPC分类号： A01N43/90 , A61K31/535
CPC分类号： C07D403/04 , C07D401/14 , C07D405/14
摘要： The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂的式I的嘧啶甲酰胺化合物。本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症等神经和精神疾病以及与纹状体功能不全或基底神经节功能障碍相关的疾病的用途。

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