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1. 发明申请

WO2017008205A1 SUBSTITUTED AMINOQUINAZOLINE COMPOUNDS AS A2A ANTAGONIST 审中-公开
标题翻译：取代的氨基喹啉化合物作为A2A拮抗剂
公开(公告)号：WO2017008205A1
公开(公告)日：2017-01-19
申请号：PCT/CN2015/083777
申请日：2015-07-10
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , HUANG, Xianhai , KUANG, Rongze , LIM, Yeon-Hee , WU, Heping , ANAND, Rajan , YU, Younong , METZGER, Edward , LO, Michael Man-Chu , TING, Pauline , STAMFORD, Andrew W. , TEMPEST, Paul
发明人： ALI, Amjad , HUANG, Xianhai , KUANG, Rongze , LIM, Yeon-Hee , WU, Heping , ANAND, Rajan , YU, Younong , METZGER, Edward , LO, Michael Man-Chu , TING, Pauline , STAMFORD, Andrew W. , TEMPEST, Paul
IPC分类号： C07D487/04 , A61K31/519 , A61P25/16 , A61P25/00
CPC分类号： C07D487/04
摘要： Provide the compound of generic formula I: The compound can be useful as A2A-receptor antagonist. Use the compound for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. Pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are also provided.
摘要翻译：提供通式I化合物：该化合物可用作A2A受体拮抗剂。使用该化合物制备用于治疗和/或预防与抑制受体有关的疾病（其包括中枢神经系统疾病如帕金森病）的药物。还提供了包含有效量的式（I）化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物。

2. 发明申请

WO2017107087A1 6, 7-DIHYDRO-5H-PYRROLO [3, 4-B] PYRIDIN-5-ONEALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR 审中-公开
标题翻译： M4肉毒碱乙酰胆碱受体的6,7-二氢-5H-吡咯并[3,4-B]吡啶-5-酮体调节剂
公开(公告)号：WO2017107087A1
公开(公告)日：2017-06-29
申请号：PCT/CN2015/098382
申请日：2015-12-23
申请人： MERCK SHARP & DOHME CORP. , MSD R&D (CHINA) CO., LTD. , BAO, Jianming , GAO, Xiaolei , KNOWLES, Sandra Lee , LI, Chunsing , LO, Michael Man-Chu , MAZZOLA, Robert D., Jr. , ONEDEYKA, Debra L. , STAMFORD, Andrew W. , ZHANG, Fengqi
发明人： BAO, Jianming , GAO, Xiaolei , KNOWLES, Sandra Lee , LI, Chunsing , LO, Michael Man-Chu , MAZZOLA, Robert D., Jr. , ONEDEYKA, Debra L. , STAMFORD, Andrew W. , ZHANG, Fengqi
IPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D405/14 , C07D471/04 , A61K31/352 , A61K31/424 , A61P29/00 , A61P9/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention is directed to 6, 7-dihydro-5H-pyrrolo [3, 4-b] pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
摘要翻译：本发明涉及作为M4毒蕈碱乙酰胆碱受体的变构调节剂的6,7-二氢-5H-吡咯并[3,4-b]吡啶-5-酮化合物。本发明还涉及本文所述化合物在潜在治疗或预防其中涉及M4毒蕈碱乙酰胆碱受体的神经病学和精神病学障碍和疾病中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在地预防或治疗其中涉及M4毒蕈碱乙酰胆碱受体的疾病中的用途。

3. 发明申请

WO2017113288A1 FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：融合三环杂环化合物作为HIV整合酶抑制剂
公开(公告)号：WO2017113288A1
公开(公告)日：2017-07-06
申请号：PCT/CN2015/100106
申请日：2015-12-31
申请人： MERCK SHARP & DOHME CORP. , YU, Tao , WADDELL, Sherman T. , GRAHAM, Thomas H. , MCCAULEY, John A. , STAMFORD, Andrew W. , CAI, Jiaqiang , QI, Zhiqi
发明人： YU, Tao , WADDELL, Sherman T. , GRAHAM, Thomas H. , MCCAULEY, John A. , STAMFORD, Andrew W. , CAI, Jiaqiang , QI, Zhiqi
IPC分类号： C07D471/16 , C07D487/16 , A61K31/5025 , A61P31/18
CPC分类号： C07D471/16 , A61K31/427 , A61K31/4402 , A61K31/4985 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/5365 , A61K31/635 , A61K31/683
摘要： The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I) :and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.
摘要翻译：本发明涉及式（I）的稠合三环杂环化合物及其药学上可接受的盐，其中R 1，R 2和 R 3如本文所定义。本发明还涉及包含至少一种稠合三环杂环化合物的组合物，以及使用稠合三环杂环化合物治疗或预防受试者HIV感染的方法。

4. 发明申请

WO2016187788A1 FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS USEFUL FOR TREATING HIV INFECTION 审中-公开
标题翻译：用于治疗艾滋病毒感染的FUSED TRICYCLIC HETEROCYCLIC COMPOUNDE有用
公开(公告)号：WO2016187788A1
公开(公告)日：2016-12-01
申请号：PCT/CN2015/079730
申请日：2015-05-25
申请人： MERCK SHARP & DOHME CORP. , YU, Tao , GRAHAM, Thomas H. , WADDELL, Sherman T. , MCCAULEY, John A. , STAMFORD, Andrew W. , SANDERS, John M. , HU, Lihong , CAI, Jiaqiang , ZHAO, Lianyun
发明人： YU, Tao , GRAHAM, Thomas H. , WADDELL, Sherman T. , MCCAULEY, John A. , STAMFORD, Andrew W. , SANDERS, John M. , HU, Lihong , CAI, Jiaqiang , ZHAO, Lianyun
IPC分类号： C07D487/14 , C07D471/14 , C07D491/147 , A61K31/437 , A61K31/4355 , A61P31/18
CPC分类号： C07D491/147 , A61K31/427 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61P31/18 , C07D471/14 , A61K2300/00
摘要： Fused tricyclic heterocycle derivatives of formula (I) and pharmaceutically acceptable salts thereof, compositions comprising at least one fused tricyclic heterocycle derivative, and methods of using the fused tricyclic heterocycle derivatives for treating or preventing HIV infection in a subject are provided.
摘要翻译：提供式（I）的稠合三环杂环衍生物及其药学上可接受的盐，包含至少一种稠合三环杂环衍生物的组合物，以及使用稠合三环杂环衍生物治疗或预防受试者中HIV感染的方法。

5. 发明申请

WO2016058144A1 PREPARATION AND USE OF CYCLIC SULFONAMIDE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：循环磺酰胺衍生物作为PAR-1受体拮抗剂的制备和使用
公开(公告)号：WO2016058144A1
公开(公告)日：2016-04-21
申请号：PCT/CN2014/088655
申请日：2014-10-15
申请人： MERCK SHARP & DOHME CORP. , STAMFORD, Andrew W. , CAI, Senlin , DUAN, Xiaobang , CAO, Jianhua , YANG, Zhi-Qiang , MALETIC, Milana
发明人： STAMFORD, Andrew W. , CAI, Senlin , DUAN, Xiaobang , CAO, Jianhua , YANG, Zhi-Qiang , MALETIC, Milana
IPC分类号： C07D417/06 , C07D417/14 , A61K31/4439 , A61K31/444 , A61P7/00
CPC分类号： A61K31/4439 , A61K31/444 , C07D417/06 , C07D417/14
摘要： Cyclic sulfonamide derivatives of Formula (I) or a pharmaceutically acceptable salt thereof are disclosed.
摘要翻译：公开了式（I）的环磺酰胺衍生物或其药学上可接受的盐。

6. 发明申请

WO2012139425A1 5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS,COMPOSITIONS,AND THEIR USE 审中-公开
标题翻译： 5代替IMINOTHIAZINES及其单和二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：WO2012139425A1
公开(公告)日：2012-10-18
申请号：PCT/CN2012/000497
申请日：2012-04-12
申请人： SCHERING CORPORATION , WU, Wen-Lian , BURNETT, Duane A. , STAMFORD, Andrew W. , CUMMING, Jared N. , BENNETT, Chad Edward , GILBERT, Eric J. , PENG, Xuanjia , SCOTT, Jack D. , YU, Younong
发明人： WU, Wen-Lian , BURNETT, Duane A. , STAMFORD, Andrew W. , CUMMING, Jared N. , BENNETT, Chad Edward , GILBERT, Eric J. , PENG, Xuanjia , SCOTT, Jack D. , YU, Younong
IPC分类号： C07D279/12 , C07D417/12 , C07D417/14 , C07D417/04 , A61K31/54 , A61K31/541 , A61P25/28 , A61P25/16
CPC分类号： C07D279/12 , A61K31/54 , A61K31/541 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoismers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be 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 uses, including Alzheimer's disease, are also disclosed.
摘要翻译：本发明公开了某些亚氨基噻嗪化合物及其一氧化二氮和二氧化物，包括式（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中式如本文所定义。本发明的化合物可用作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，及其制备和用途的方法，包括阿尔茨海默氏病。

7. 发明授权

EP2697210B1 5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： 5-取代IMINOTHIAZINE及其单和二氧化AS BACE抑制剂，THEREOF组合物及其
公开(公告)号：EP2697210B1
公开(公告)日：2017-03-01
申请号：EP12771100.0
申请日：2012-04-12
申请人： Merck Sharp & Dohme Corp.
发明人： WU, Wen-Lian , BURNETT, Duane A. , STAMFORD, Andrew W. , CUMMING, Jared N. , BENNETT, Chad Edward , GILBERT, Eric J. , PENG, Xuanjia , SCOTT, Jack D. , YU, Younong
IPC分类号： C07D279/12 , C07D417/12 , C07D417/14 , C07D417/04 , A61K31/54 , A61K31/541 , A61P25/28 , A61P25/16
CPC分类号： C07D279/12 , A61K31/54 , A61K31/541 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04

8. 发明授权

EP3194396B1 DIAZINE-FUSED AMIDINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权转让
公开(公告)号：EP3194396B1
公开(公告)日：2019-04-17
申请号：EP15841974.7
申请日：2015-09-14
申请人： Merck Sharp & Dohme Corp.
发明人： LIU, Kun , HE, Shuwen , CUMMING, Jared N. , STAMFORD, Andrew W.
IPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , A61P25/00

9. 发明公开

EP2697210A1 5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： 5-取代IMINOTHIAZINE及其单和二氧化AS BACE抑制剂，THEREOF组合物及其
公开(公告)号：EP2697210A1
公开(公告)日：2014-02-19
申请号：EP12771100.0
申请日：2012-04-12
申请人： Merck Sharp & Dohme Corp.
发明人： WU, Wen-Lian , BURNETT, Duane A. , STAMFORD, Andrew W. , CUMMING, Jared N. , BENNETT, Chad Edward , GILBERT, Eric J. , PENG, Xuanjia , SCOTT, Jack D. , YU, Younong
IPC分类号： C07D279/12 , C07D417/12 , C07D417/14 , C07D417/04 , A61K31/54 , A61K31/541 , A61P25/28 , A61P25/16
CPC分类号： C07D279/12 , A61K31/54 , A61K31/541 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoismers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be 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 uses, including Alzheimer's disease, are also disclosed.

10. 发明公开

EP3194396A1 DIAZINE-FUSED AMIDINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权转让
标题翻译： DIAZINE-FUSED脒化合物作为BACE缓蚀剂，组合物及其使用
公开(公告)号：EP3194396A1
公开(公告)日：2017-07-26
申请号：EP15841974.7
申请日：2015-09-14
申请人： Merck Sharp & Dohme Corp.
发明人： LIU, Kun , HE, Shuwen , CUMMING, Jared N. , STAMFORD, Andrew W.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K45/06 , A61P25/00
摘要： In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, and p 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，本发明提供了某些C-6螺环碳亚胺基噻二嗪化合物，包括式（I）化合物或其互变异构体，以及所述化合物和所述互变异构体的药学上可接受的盐，其中R1A，R1B，R2，RA，环A ，RA，m，L1，RL，环C，RC和p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有关的各种病症。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他活性剂组合）的药物组合物，以及它们的制备和使用方法，包括用于可能治疗阿尔茨海默氏病。

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