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1. 发明申请

WO2014101373A1 HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS FOR TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDER 审中-公开
标题翻译： [1,2,4]三唑并[1,5-C]喹唑啉-5-胺化合物用于治疗中枢神经系统疾病
公开(公告)号：WO2014101373A1
公开(公告)日：2014-07-03
申请号：PCT/CN2013/076853
申请日：2013-06-06
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda V. , WON, Walter , WU, Heping
发明人： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda V. , WON, Walter , WU, Heping
IPC分类号： C07D519/00 , A61K31/519 , A61P25/16
CPC分类号： C07D519/00 , C07D487/04
摘要： Disclosed are compounds of heterobicyclo-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine herein, which have specific binding on an A 2A -receptor and are useful for quantifying in vivo receptor-site occupancy of various compounds which have an affinity for binding to an A 2A -receptor.
摘要翻译：公开了本文中具有与A2A受体的特异性结合的异二环取代的[1,2,4]三唑并[1,5-c]喹唑啉-5-胺的化合物，并且可用于定量体内受体位点占有率具有与A2A受体结合的亲和力的各种化合物。

2. 发明申请

WO2014105666A1 HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 审中-公开
标题翻译：取代[1,2,4]三唑并[1,5-C]喹唑啉-5-胺化合物与A2A拮抗剂性质
公开(公告)号：WO2014105666A1
公开(公告)日：2014-07-03
申请号：PCT/US2013/076781
申请日：2013-12-20
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy, J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda, V. , WON, Walter , WU, Heping
发明人： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy, J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda, V. , WON, Walter , WU, Heping
IPC分类号： A61K31/4985 , A61K31/519 , C07D487/04 , A61P25/16
CPC分类号： C07D519/00 , C07D487/04
摘要： Disclosed are compounds of Formula Gl (structurally represented): where "RG3" "Rd1" to "Rd4", "n", "m", "p", "W", "X", "Y", and "Z" are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
摘要翻译：公开了式（式III）化合物：其中“RG3”“Rd1”至“Rd4”，“n”，“m”，“p”，“W”，“X”，“Y” “在本文中定义为哪些化合物是A2A受体的拮抗剂。本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

3. 发明申请

WO2014101120A1 HETEROBICYCLO-SUBSTITUTED-7-METHOXY-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 审中-公开
标题翻译：具有A2A拮抗剂性质的偶氮二环取代-7-甲氧基 - [1,2,4]三唑[1,5-C]喹唑啉-5-胺化合物
公开(公告)号：WO2014101120A1
公开(公告)日：2014-07-03
申请号：PCT/CN2012/087865
申请日：2012-12-28
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael , LIM, Yeon Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda , WON, Walter , WU, Heping
发明人： ALI, Amjad , LO, Michael , LIM, Yeon Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda , WON, Walter , WU, Heping
IPC分类号： C07D487/04 , A61K31/519 , A61P25/16 , A61P25/00
CPC分类号： C07D519/00 , C07D487/04
摘要： Disclosed are compounds of Formulae A defined herein, which have specific binding on an A 2A -receptor and are useful for quantifying in vivo receptor-site occupancy of various compounds which have an affinity for binding to an A 2A receptor.
摘要翻译：公开了本文定义的式A化合物，其具有对A2A受体的特异性结合，并且可用于定量对与AβA受体结合的亲和力的各种化合物的体内受体位置占有。

4. 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。

5. 发明申请

WO2017011214A1 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：WO2017011214A1
公开(公告)日：2017-01-19
申请号：PCT/US2016/040926
申请日：2016-07-05
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： A61K31/535
CPC分类号： C07D487/04
摘要： The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A 2A -receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A 2A -receptor is involved. The invention further involves use of the compounds as an A 2A -receptor antagonist and/or inhibitor 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. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
摘要翻译：本发明涉及被认为可用作A2A受体拮抗剂的通式（I）的化合物或其药学上可接受的盐。本发明进一步涉及治疗患有（优选人）的患有A2A受体涉及的疾病或病症的方法。本发明还涉及使用化合物作为A2A受体拮抗剂和/或抑制剂来制备用于治疗和/或预防与抑制受体有关的疾病的药物，所述疾病包括中枢神经系统疾病如帕金森病。本发明还涉及包含有效量的式（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，以及本发明的化合物和药物组合物在治疗中的用途的这种疾病。

6. 发明申请

WO2015027431A1 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2,2-DIFLUORODIOXOLO A2A受体拮抗剂
公开(公告)号：WO2015027431A1
公开(公告)日：2015-03-05
申请号：PCT/CN2013/082560
申请日：2013-08-29
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , GALLO, Gioconda V. , HENDERSON, Timothy J. , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , METZGER, Edward , RUIZ, Manuel de Lera , STAMFORD, Andrew , TEMPEST, Paul , WHITEHEAD, Brent , WU, Heping
发明人： ALI, Amjad , GALLO, Gioconda V. , HENDERSON, Timothy J. , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , METZGER, Edward , RUIZ, Manuel de Lera , STAMFORD, Andrew , TEMPEST, Paul , WHITEHEAD, Brent , WU, Heping
IPC分类号： C07D487/14 , C07D487/04 , A61K31/517 , A61K31/505 , A61K31/41 , A61K31/52 , A61K31/55 , A61K31/53
CPC分类号： C07D519/00 , C07D491/147
摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A 2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A 2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A 2A receptors are involved.
摘要翻译：本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。

7. 发明申请

WO2015031221A1 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2,2-DIFLUORODIOXOLO A2A受体拮抗剂
公开(公告)号：WO2015031221A1
公开(公告)日：2015-03-05
申请号：PCT/US2014/052442
申请日：2014-08-25
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , GALLO, Gioconda, V. , HENDERSON, Timothy, J. , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , METZGER, Edward , RUIZ, Manuel de Lera , STAMFORD, Andrew , TEMPEST, Paul , WHITEHEAD, Brent , WU, Heping
发明人： ALI, Amjad , GALLO, Gioconda, V. , HENDERSON, Timothy, J. , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , METZGER, Edward , RUIZ, Manuel de Lera , STAMFORD, Andrew , TEMPEST, Paul , WHITEHEAD, Brent , WU, Heping
IPC分类号： A01N43/58 , A01N43/60
CPC分类号： C07D519/00 , C07D491/147
摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A 2A receptor. The present invention is also directed to uses of the 2,2- difluorodioxolo compounds described herein in the potential treatment or prevention of 5 neurological disorders and diseases in which A 2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A 2A receptors are involved.
摘要翻译：本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。本发明还涉及本文所述的2,2-二氟二氧代己基化合物在潜在的治疗或预防涉及A2A受体的5种神经障碍和疾病中的用途。本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。

8. 发明申请

WO2012058203A1 DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：二氮杂环戊烷杂环衍生物
公开(公告)号：WO2012058203A1
公开(公告)日：2012-05-03
申请号：PCT/US2011/057641
申请日：2011-10-25
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , BAKER, Robert, K. , GUO, Zhiqiang , WHITEHEAD, Brent , HENDERSON, Timothy, J. , METZGER, Edward , YAN, Lin , SHAH, Shrenik, K. , DELLUREFICIO, James , WANG, Jun
发明人： ALI, Amjad , LO, Michael Man-Chu , BAKER, Robert, K. , GUO, Zhiqiang , WHITEHEAD, Brent , HENDERSON, Timothy, J. , METZGER, Edward , YAN, Lin , SHAH, Shrenik, K. , DELLUREFICIO, James , WANG, Jun
IPC分类号： A01N33/26 , A61K31/655
CPC分类号： C07D211/44 , A61K31/655 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/273 , C07D307/20 , C07D309/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D413/10 , C07D417/04
摘要： A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
摘要翻译：具有以下结构的化合物：用于治疗高血压，肺动脉高压（PAH），充血性心力衰竭，由过度保水引起的病症，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松症或肾病。

9. 发明申请

WO2011100384A1 DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES 审中-公开
标题翻译：二氮杂环戊烷衍生物
公开(公告)号：WO2011100384A1
公开(公告)日：2011-08-18
申请号：PCT/US2011/024275
申请日：2011-02-10
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YAN, Lin
发明人： ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YAN, Lin
IPC分类号： A01N51/00
CPC分类号： C07C291/00 , C07C291/08 , C07C2601/08 , C07D249/04
摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen, -OH, -O-C 1 - 6 alkyl, =O, or halogen;R 2 is hydrogen, C(O)OR 8 , C 6 H 5 C(O)OR 8 , (CH 2 ) 1-2 OH, CR 9 R 10 OH, C(O)O(CH 2 ) 0-2 aryl, C(O)NR 9 R 10 , C(O)SO 2 NR 9 R 10 , C 6 H 5 OR 9 , W-C(O)OR 8 , W-OR 9 , Y, or P(O)(OR 9 )(ORlO); R 3 is hydrogen or -C 1-6 alkyl; R 4 is hydrogen, -OH or -C(O)OR 9 ; R 5 is hydrogen or deuterium; R 6 and R 7 are independently-C 1-6 alkyl, fluoro-substituted -C 1-6 alkyl, deutero-substituted -C 1-6 alkyl or -(CH 2 ) 1-2 R 11 , wherein any carbon atom of the fluoro-substituted -C 1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted -C 1-6 alkyl is mono- or di-substituted with fluoro; R 8 , in each instance in which it occurs, is independently hydrogen, -C 1-6 alkyl, or -(CH 2 ) 2 N + (CH 3 ) 3 ; R 9 and R 10 , in each instance in which they occur, are independently -C 1-6 alkyl; R 11 is -OH, -O-C 1-6 alkyl, -0CD3, -OC(O)OC 1-6 alkyl, -NH 2 , -C 6 H 5 , -N 3 , or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R 6 or R 7 ; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构或其药学上可接受的盐的化合物，其中R 1是氢，-OH，-O-C 1-6烷基，= O或卤素; R 2是氢，C（O）OR 8，C 6 H 5 C（O）OR 8，（O）OR 2，C（O）O（CH 2）0-2芳基，C（O）NR 9 R 10，C（O）SO 2 NR 9 R 10，C 6 H 5 OR 9，WC（O）OR 8，W-OR 9，Y或P （O）（OR 9）（ORlO）; R3是氢或-C 1-6烷基; R4是氢，-OH或-C（O）OR9; R5是氢或氘; R 6和R 7独立地是C 1-6烷基，氟取代的C 1-6烷基，取代的C 1-6烷基或 - （CH 2）1-2 R 11，其中氟取代的-C 1-6的任何碳原子烷基被氟单取代或二取代，并且取代的C 1-6烷基的任何碳原子被氟单取代或二取代; 在其每次发生的情况下，R 8独立地为氢，-C 1-6烷基或 - （CH 2）2 N +（CH 3）3; 在其各自出现的情况下，R 9和R 10独立地为-C 1-6烷基; R 11是-OH，-O-C 1-6烷基，-CD 3，-OC（O）OC 1-6烷基，-NH 2，-C 6 H 5，-N 3或W; W是具有1,2或3个氮原子的未取代的5-或6-元杂芳基环，或具有1,2或3个氮原子的取代的5-或6-元杂芳基环，其被单取代或二取代在任何具有R6或R7的碳原子上; Y是具有1,2,3或4个杂原子的5或6元杂环，其为N，O或S或其立体异构体，或其药学上可接受的盐，或其立体异构体的药学上可接受的盐，以及使用用于治疗高血压的化合物。

10. 发明申请

WO2014055595A1 INDOLINE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITIORS RELATED APPLICATIONS 审中-公开
标题翻译：吲哚酚化合物作为醛固酮合成酶抑制剂相关应用
公开(公告)号：WO2014055595A1
公开(公告)日：2014-04-10
申请号：PCT/US2013/062975
申请日：2013-10-02
申请人： MERCK SHARP & DOHME CORP. , ELEXOPHARM GMBH , ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YIN, Lina , HARTMANN, Rolf , HU, Qingzhong , HEIM, Ralf , ZIMMER, Christina
发明人： ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YIN, Lina , HARTMANN, Rolf , HU, Qingzhong , HEIM, Ralf , ZIMMER, Christina
IPC分类号： A61K31/4439 , A61K31/4164
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D409/14 , A61K2300/00
摘要： This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatmen amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
摘要翻译：本发明涉及结构式I的吲哚类化合物或其药学上可接受的盐，其中变量在本文中定义。本发明化合物选择性地抑制醛固酮合酶。本发明还提供包含式I化合物或其盐的药物组合物，以及可能涉及治疗改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

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