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1. 发明申请

WO2021202254A1 FACTOR XI ACTIVATION INHIBITORS 审中-公开
公开(公告)号：WO2021202254A1
公开(公告)日：2021-10-07
申请号：PCT/US2021/024267
申请日：2021-03-26
申请人： MERCK SHARP & DOHME CORP. , HICKS, Jacqueline, D. , ALI, Amjad , DEBENHAM, John, S. , DONOFRIO, Anthony , FU, Wenlang , GAO, Ying-Duo , HRUZA, Alan, W. , LIM, Yeon-Hee , LOMBARDO, Matthew, J. , NIZNER, Peter , SO, Sung-Sau , TAN, Zheng , TATOSIAN, Daniel, A. , XIAO, Dong , YANG, Dexi , YU, Yang
发明人： HICKS, Jacqueline, D. , ALI, Amjad , DEBENHAM, John, S. , DONOFRIO, Anthony , FU, Wenlang , GAO, Ying-Duo , HRUZA, Alan, W. , LIM, Yeon-Hee , LOMBARDO, Matthew, J. , NIZNER, Peter , SO, Sung-Sau , TAN, Zheng , TATOSIAN, Daniel, A. , XIAO, Dong , YANG, Dexi , YU, Yang
IPC分类号： A61K31/444 , A61K31/4709 , A61K31/4725
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 XI activation inhibitors.

2. 发明申请

WO2017205193A1 SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS GPR120 AGONISTS 审中-公开
标题翻译：用作GPR120激动剂的取代的四氢异喹啉化合物
公开(公告)号：WO2017205193A1
公开(公告)日：2017-11-30
申请号：PCT/US2017/033451
申请日：2017-05-19
申请人： MERCK SHARP & DOHME CORP. , ADAMS, Gregory, L. , COX, Jason, M. , DEBENHAM, John, S. , EDMONDSON, Scott , GILBERT, Eric, J. , GUO, Yan , JIANG, Yu , JOSIEN, Hubert , KIM, Hyunjin, M. , LAN, Ping , MIAO, Shouwu , PLUMMER, Christopher, W. , RAJAGOPALAN, Murali , SHAH, Unmesh , SUN, Zhongxiang , TRUONG, Quang, T. , UJJAINWALLA, Feroze , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , SUZUKI, Takao , WANG, Nengxue
发明人： ADAMS, Gregory, L. , COX, Jason, M. , DEBENHAM, John, S. , EDMONDSON, Scott , GILBERT, Eric, J. , GUO, Yan , JIANG, Yu , JOSIEN, Hubert , KIM, Hyunjin, M. , LAN, Ping , MIAO, Shouwu , PLUMMER, Christopher, W. , RAJAGOPALAN, Murali , SHAH, Unmesh , SUN, Zhongxiang , TRUONG, Quang, T. , UJJAINWALLA, Feroze , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , SUZUKI, Takao , WANG, Nengxue
IPC分类号： A61K31/472 , A61K31/4725 , A61P3/10 , C07D217/02
摘要： The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：本发明涉及用于治疗或预防糖尿病，高脂血症，肥胖症，NASH，炎症相关病症和相关疾病的式（I）代表的化合物及其药学上可接受的盐，和条件。该化合物可用作G蛋白偶联受体GPR120的激动剂。药物组合物和治疗方法也包括在内。

3. 发明申请

WO2015112465A1 ISOQUINOLINE DERIVATIVES AS MGAT2 INHIBITORS 审中-公开
标题翻译：异喹啉衍生物作为MGAT2抑制剂
公开(公告)号：WO2015112465A1
公开(公告)日：2015-07-30
申请号：PCT/US2015/011939
申请日：2015-01-20
申请人： MERCK SHARP & DOHME CORP. , BERGER, Richard , BLIZZARD, Timothy, A. , CAMPBELL, Brian, T. , CHEN, Helen, Y. , DEBENHAM, John, S. , DEWNANI, Sunita, V. , DUBOIS, Byron , GUDE, Candido , GUO, Zhiqiang , HARPER, Bart , HU, Zhiyong , LIN, Songnian , LIU, Ping , WANG, Ming , UJJAINWALLA, Feroze , XU, Jiayi , XU, Libo , ZHANG, Rui
发明人： BERGER, Richard , BLIZZARD, Timothy, A. , CAMPBELL, Brian, T. , CHEN, Helen, Y. , DEBENHAM, John, S. , DEWNANI, Sunita, V. , DUBOIS, Byron , GUDE, Candido , GUO, Zhiqiang , HARPER, Bart , HU, Zhiyong , LIN, Songnian , LIU, Ping , WANG, Ming , UJJAINWALLA, Feroze , XU, Jiayi , XU, Libo , ZHANG, Rui
IPC分类号： C07D471/04
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/14 , C07D471/04
摘要： The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
摘要翻译：式I化合物作为MGAT2抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

4. 发明申请

WO2004012671A2 SUBSTITUTED FURO [2,3-B] PYRIDINE DERIVATIVES 审中-公开
标题翻译：取代的FURO [2,3-B]吡啶衍生物
公开(公告)号：WO2004012671A2
公开(公告)日：2004-02-12
申请号：PCT/US2003/024280
申请日：2003-08-01
申请人： MERCK & CO., INC. , TOUPENCE, Richard, B. , DEBENHAM, John, S. , GOULET, Mark, T. , MADSEN-DUGGAN, Christina, B. , WALSH, Thomas, F. , SHAH, Shrenik, K.
发明人： TOUPENCE, Richard, B. , DEBENHAM, John, S. , GOULET, Mark, T. , MADSEN-DUGGAN, Christina, B. , WALSH, Thomas, F. , SHAH, Shrenik, K.
IPC分类号： A61K
CPC分类号： C07D491/04 , C07D453/06
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

5. 发明申请

WO2020123272A1 PYRAZOLOPYRIMIDINE PDE9 INHIBITORS 审中-公开
公开(公告)号：WO2020123272A1
公开(公告)日：2020-06-18
申请号：PCT/US2019/064827
申请日：2019-12-06
申请人： MERCK SHARP & DOHME CORP. , ARASAPPAN, Ashok , COX, Jason, M. , DEBENHAM, John, S. , FENG, Zhe , GUO, Zhuyan , MENG, Dongfang
发明人： ARASAPPAN, Ashok , COX, Jason, M. , DEBENHAM, John, S. , FENG, Zhe , GUO, Zhuyan , MENG, Dongfang
IPC分类号： C07D487/04
摘要： The present invention is directed to amino and alkyl pyrazolopyrimidine compounds which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

6. 发明申请

WO2018039094A1 PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS 审中-公开
标题翻译：吡啶-1-氧化物衍生物及其作为因子XIA抑制剂的用途
公开(公告)号：WO2018039094A1
公开(公告)日：2018-03-01
申请号：PCT/US2017/047718
申请日：2017-08-21
申请人： MERCK SHARP & DOHME CORP. , SHEN, Dong-Ming , KUANG, Rongze , KUMAR, Puneet , DUFFY, Joseph, L. , ZHU, Cheng , ALI, Amjad , YANG, Meng , DEBENHAM, John, S.
发明人： SHEN, Dong-Ming , KUANG, Rongze , KUMAR, Puneet , DUFFY, Joseph, L. , ZHU, Cheng , ALI, Amjad , YANG, Meng , DEBENHAM, John, S.
IPC分类号： C07D213/89 , A61K31/4425 , A61P7/02
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

WO2017201683A1 SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS GPR120 AGONISTS 审中-公开
标题翻译：用作GPR120激动剂的取代的四氢异喹啉化合物
公开(公告)号：WO2017201683A1
公开(公告)日：2017-11-30
申请号：PCT/CN2016/083265
申请日：2016-05-25
申请人： MERCK SHARP & DOHME CORP. , ADAMS, Gregory L. , COX, Jason M. , DEBENHAM, John S. , EDMONDSON, Scott , GILBERT, Eric , GUO, Yan , JIANG, Yu , JOSIEN, Hubert , KIM, Hyunjin M. , LAN, Ping , MIAO, Shouwu , PLUMMER, Christopher W. , RAJAGOPALAN, Murali , SHAH, Unmesh , SUN, Zhongxiang , SUZUKI, Takao , TRUONG, Quang T. , UJJAINWALLA, Feroze , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , WANG, Nengxue
发明人： ADAMS, Gregory L. , COX, Jason M. , DEBENHAM, John S. , EDMONDSON, Scott , GILBERT, Eric , GUO, Yan , JIANG, Yu , JOSIEN, Hubert , KIM, Hyunjin M. , LAN, Ping , MIAO, Shouwu , PLUMMER, Christopher W. , RAJAGOPALAN, Murali , SHAH, Unmesh , SUN, Zhongxiang , SUZUKI, Takao , TRUONG, Quang T. , UJJAINWALLA, Feroze , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , WANG, Nengxue
IPC分类号： C07D217/16 , C07D401/04 , C07D401/12 , C07D403/04 , C07D413/04 , C07D417/12 , C07D417/14 , A61K31/4725 , A61P3/04 , A61P3/10 , A61P3/00
摘要： Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts thereof. The compounds are agonists of the G-protein coupled receptor GPR120 and are useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions.
摘要翻译：公开了由式（I）表示的化合物及其药学上可接受的盐。这些化合物是G蛋白偶联受体GPR120的激动剂，可用于治疗或预防糖尿病，高脂血症，肥胖症，NASH，炎症相关病症和相关疾病和病症。

8. 发明申请

WO2014176216A1 THIAZOLE-SUBSTITUTED AMINOPYRIMIDINES AS SPLEEN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：噻唑替代氨基嘧啶作为分离型酪氨酸激酶抑制剂
公开(公告)号：WO2014176216A1
公开(公告)日：2014-10-30
申请号：PCT/US2014/034917
申请日：2014-04-22
申请人： MERCK SHARP & DOHME CORP. , ARRINGTON, Kenneth, L. , DUBOIS, Byron , DEBENHAM, John, S. , LIU, Ping , NORTHRUP, Alan, B. , SZEWCZYK, Jason, W. , WANG, Liping , WANG, Ming
发明人： ARRINGTON, Kenneth, L. , DUBOIS, Byron , DEBENHAM, John, S. , LIU, Ping , NORTHRUP, Alan, B. , SZEWCZYK, Jason, W. , WANG, Liping , WANG, Ming
IPC分类号： A61K31/497 , A61P29/00 , C07D417/14
CPC分类号： C07D417/14 , A61K31/427 , A61K31/506 , A61K31/5377 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译：本发明提供了式（I）（I）的某些噻唑取代的氨基嘧啶化合物或其药学上可接受的盐，其中R1，R2，R3，R5，R6和下标r，s和t如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。

9. 发明申请

WO2008121257A1 SUBSTITUTED PYRIDO[2,3-D]PYRIMIDINE DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID-1受体调节剂的取代的吡咯并[2,3-D]吡啶衍生物
公开(公告)号：WO2008121257A1
公开(公告)日：2008-10-09
申请号：PCT/US2008/003848
申请日：2008-03-24
申请人： MERCK & CO., INC. , DEBENHAM, John, S. , MADSEN-DUGGAN, Christina, B. , WALSH, Thomas, F.
发明人： DEBENHAM, John, S. , MADSEN-DUGGAN, Christina, B. , WALSH, Thomas, F.
IPC分类号： A01N43/90 , A61K31/519
CPC分类号： C07D471/04
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，阿尔茨海默病，偏头痛，神经病，包括多发性硬化症和神经 - 巴利综合征的神经炎症性疾病以及病毒性炎症后遗症的中枢作用药物脑炎，脑血管意外和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻，肝硬化，非酒精性脂肪性肝病（NAFLD ），非酒精性脂肪性肝炎（NASH），以及促进觉醒。

10. 发明申请

WO2004012671A3 SUBSTITUTED FURO [2,3-B] PYRIDINE DERIVATIVES 审中-公开
标题翻译：取代的FURO [2,3-B]吡啶衍生物
公开(公告)号：WO2004012671A3
公开(公告)日：2005-06-09
申请号：PCT/US0324280
申请日：2003-08-01
申请人： MERCK & CO INC , TOUPENCE RICHARD B , DEBENHAM JOHN S , GOULET MARK T , MADSEN-DUGGAN CHRISTINA B , WALSH THOMAS F , SHAH SHRENIK K
发明人： TOUPENCE RICHARD B , DEBENHAM JOHN S , GOULET MARK T , MADSEN-DUGGAN CHRISTINA B , WALSH THOMAS F , SHAH SHRENIK K
IPC分类号： C07D491/048 , A61K31/00 , A61K31/4355 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4741 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D453/06 , C07D491/02 , C07D491/04 , C07D519/00 , A61K31/44 , C07D409/02
CPC分类号： C07D491/04 , C07D453/06
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

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