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1. 发明申请

WO2019000237A1 3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR 审中-公开
公开(公告)号：WO2019000237A1
公开(公告)日：2019-01-03
申请号：PCT/CN2017/090385
申请日：2017-06-27
申请人： MERCK SHARP & DOHME CORP. , MSD R & D (CHINA) CO., LTD. , ACTON, John J., III , BAO, Jianming , DENG, Qiaolin , EGBERTSON, Melissa , FERGUSON, Ronald , GAO, Xiaolei , HARRISON, Scott T. , HENDERSON, Timothy J. , KNOWLES, Sandra L. , LO, Michael Man-Chu , MAZZOLA, Robert D., Jr , SELYUTIN, Oleg , ZHANG, Fengqi , NA, Meng , SUZUKI, Takao
发明人： ACTON, John J., III , BAO, Jianming , DENG, Qiaolin , EGBERTSON, Melissa , FERGUSON, Ronald , GAO, Xiaolei , HARRISON, Scott T. , HENDERSON, Timothy J. , KNOWLES, Sandra L. , LO, Michael Man-Chu , MAZZOLA, Robert D., Jr , SELYUTIN, Oleg , ZHANG, Fengqi , NA, Meng , SUZUKI, Takao
IPC分类号： C07D231/10 , C07D231/02 , C07D401/14 , A61K31/455 , A61P25/00
摘要： Provided are pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. Provided is also use 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. Provided are also compositions comprising these compounds. Provided is also use of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

2. 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。

3. 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。

4. 发明申请

WO2014105664A1 PIPERAZINE-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 审中-公开
标题翻译：哌嗪取代[1,2,4]三唑[1,5-C]喹唑啉-5-胺化合物与A2A拮抗剂性质
公开(公告)号：WO2014105664A1
公开(公告)日：2014-07-03
申请号：PCT/US2013/076775
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 , BERLIN, Michael , TING, Pauline , ZHOU, Gang , YU, Tao , BOYCE, Christopher , KELLY, Joseph Michael , TAGAT, Jayaram, R. , ZHENG, Junying , HUANG, Xianhai , ZHOU, Wei , KIM, Jae-Hun , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda, V. , WON, Walter , WU, Heping , ANAND, Rajan
发明人： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , BERLIN, Michael , TING, Pauline , ZHOU, Gang , YU, Tao , BOYCE, Christopher , KELLY, Joseph Michael , TAGAT, Jayaram, R. , ZHENG, Junying , HUANG, Xianhai , ZHOU, Wei , KIM, Jae-Hun , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda, V. , WON, Walter , WU, Heping , ANAND, Rajan
IPC分类号： A61K31/4985 , A61K31/519
CPC分类号： C07D487/04 , C07D487/08 , C07D487/18 , C07D513/04
摘要： Disclosed are compounds of Formula A: (structurally represented) where "RG1", "RG2a", "RG4", "RG5", "MG1", "n" and "m" 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A化合物（结构上表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”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。

5. 发明申请

WO2011043914A1 DIURETICS 审中-公开
标题翻译：利尿剂
公开(公告)号：WO2011043914A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/049425
申请日：2010-09-20
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
发明人： ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
IPC分类号： A61K31/535
CPC分类号： C07D491/04
摘要： A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，以及使用该化合物治疗高血压的方法。

6. 发明申请

WO2009106471A2 NEW ANGIOTENSIN II RECEPTOR BLOCKER DERIVATIVES 审中-公开
标题翻译：新型血管紧张素II受体阻断剂衍生物
公开(公告)号：WO2009106471A2
公开(公告)日：2009-09-03
申请号：PCT/EP2009051943
申请日：2009-02-19
申请人： NICOX SA , MERCK & CO INC , ALMIRANTE NICOLETTA , NICOTRA ALESSIA , MANDELLI VALENTINO , BIONDI STEFANO , STEFANINI SILVIA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU
发明人： ALMIRANTE NICOLETTA , NICOTRA ALESSIA , MANDELLI VALENTINO , BIONDI STEFANO , STEFANINI SILVIA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU
IPC分类号： C07D403/10 , A61P9/00 , C07D403/14 , C07D405/14
CPC分类号： C07D403/10 , C07D403/14 , C07D405/14
摘要： New angiotensin II receptor blocker nitroderivatives of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: and their use for treating cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.
摘要翻译：通式（I）的新型血管紧张素II受体阻断剂硝基衍生物及其药学上可接受的盐或立体异构体及其用于治疗心血管，肾和慢性肝脏疾病，炎症过程和代谢综合征的用途。

7. 发明申请

WO2008076247A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2008076247A2
公开(公告)日：2008-06-26
申请号：PCT/US2007/025233
申请日：2007-12-11
申请人： MERCK & CO., INC. , NICOX S.A. , SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARUGUND, Ravi, P. , ALI, Amjad , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STORONI, Laura , STEFANINI, Silvia
发明人： SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARUGUND, Ravi, P. , ALI, Amjad , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STORONI, Laura , STEFANINI, Silvia
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R is an angiotensin receptor antagonist active group, Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 .; Y 1 is C(R 1 R 2 ); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and -0C(0)C 1-4 alkyl; Y 2 is O or CH 2 ; Y 3 is C(O) or CH 2 ; Y 4 is O or CH 2 ; Y5 is -(CH2) 1-2 -(X) 0- l -(CH 2 ) 0-l - or is absent; X is -O- or - CR 3 R 4 -; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y 1 -Y 2 -Y 3， SUP> -Y ^{4 -Y ^{5 .; Y 1是C（R 1 R 2）2）。 R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-C（O）C 1-4烷基; Y 2是O或CH 2; Y 3是C（O）或CH 2 O 2; Y 4是O或CH 2; Y 5是 - （CH 2）n 1-2 - （X）0-1 - （CH 2）2 - SUB> - 或不存在; X是-O-或-CR 3 R 4 - 。和R 3和R 4独立地选自氢和C 1 -C 4烷基 ; 或其药学上可接受的盐或水合物，其可用于治疗高血压。}}

8. 发明申请

WO2008076246A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2008076246A2
公开(公告)日：2008-06-26
申请号：PCT/US2007/025232
申请日：2007-12-11
申请人： MERCK & CO., INC. , NICOX S.A. , SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARGUND, Ravi, P. , ALI, Amjad , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STORONI, Laura , STEFANINI, Silvia
发明人： SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARGUND, Ravi, P. , ALI, Amjad , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STORONI, Laura , STEFANINI, Silvia
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R is an angiotensin receptor antagonist active group, Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 .; Y 1 is C(R 1 R 2 ); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and -0C(0)C 1- 4 alkyl; Y 2 is O or CH 2 ; Y 3 is C(O) or CH 2 ; Y 4 is O or CH 2 ; Y5 is -(CH2) 1-2 -(X) 0- l -(CH 2 ) 0-l - or is absent; X is -O- or - CR 3 R 4 -; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y 1 -Y 2 -Y 3， SUP> -Y ^{4 -Y ^{5 .; Y 1是C（R 1 R 2）2）。 R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-C（O）C 1 -}}

9. 发明申请

WO2008076245A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2008076245A2
公开(公告)日：2008-06-26
申请号：PCT/US2007/025231
申请日：2007-12-11
申请人： MERCK & CO., INC. , SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARGUND, Ravi, P. , ALI, Amjad
发明人： SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARGUND, Ravi, P. , ALI, Amjad
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 -; Y 1 is C(O) or C(R 1 R 2 ); Y 2 is O, C(O), P(O)(OH) or CH 2 , provided that when Y 1 is C(O), Y 2 is not C(O); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and -OC(O)C 1-4 alkyl; Y 3 is O, C(O) or CH 2 , provided that when Y 2 is C(O), then Y 3 is not C(O), and further provided that when Y 2 is O, then Y 3 is not O; Y 4 is O or CH 2 or is absent, provided that when Y 3 is O, then Y 4 is not O; Y5 is -(CH 2 ) 1-2 -(X) 0- l -(CH 2 ) 0-l - or is absent; X is -O- or -CR 3 R 4 -; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中Y为-Y 1 -Y 2 -Y 3 -Y 4 - / SUP> -Y ^{5 - ; Y 1是C（O）或C（R 1 R 2）2）。 Y 2是O，C（O），P（O）（OH）或CH 2，条件是当Y 1是C（ O），Y 2不是C（O）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-OC（O）C 1-4烷基; Y 3是O，C（O）或CH 2，条件是当Y 2是C（O）时，则Y 3不是C（O），并且进一步地，当Y 2为O时，Y 3不为O; Y 4是O或CH 2或不存在，条件是当Y 3为O时，则Y 4为O，不是O Y 5是 - （CH 2）2 - （X）0-1 - （CH 2）2 - 0-1 - 或不存在; X是-O-或-CR 3 R 4 - 。和R 3和R 4独立地选自氢和C 1 -C 4烷基 ; 或其药学上可接受的盐，其可用于治疗高血压。}

10. 发明申请

WO2022020550A1 ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY 审中-公开
公开(公告)号：WO2022020550A1
公开(公告)日：2022-01-27
申请号：PCT/US2021/042702
申请日：2021-07-22
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , BOYCE, Christopher, W. , CUMMING, Jared, N. , DEMONG, Duane , GRAHAM, Thomas, H. , GUDIPATI, Subrahmanyam , HOOVER, Andrew, J. , HUANG, Xianhai , KUANG, Rongze , KIM, Jae-Hun , KELLY, Joseph, M. , LIM, Yeon-Hee , LO, Michael, Man-Chu , MORENO, Jesus , SU, Jing , WU, Heping , XIAO, Dong , YU, Younong , ZHU, Xiaohong
发明人： ALI, Amjad , BOYCE, Christopher, W. , CUMMING, Jared, N. , DEMONG, Duane , GRAHAM, Thomas, H. , GUDIPATI, Subrahmanyam , HOOVER, Andrew, J. , HUANG, Xianhai , KUANG, Rongze , KIM, Jae-Hun , KELLY, Joseph, M. , LIM, Yeon-Hee , LO, Michael, Man-Chu , MORENO, Jesus , SU, Jing , WU, Heping , XIAO, Dong , YU, Younong , ZHU, Xiaohong
IPC分类号： A61K31/519 , C07D487/04 , C07D487/08 , C07D513/04
摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

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