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公开(公告)号：EP3148542B1
公开(公告)日：2019-02-27
申请号：EP15800524.9
申请日：2015-05-22
发明人： LIU, Weiguo , EDMONDSON, Scott D. , GUO, Zhuyan , MERTZ, Eric , OGAWA, Anthony K. , SO, Sung-Sau , SUN, Wanying , BROCKUNIER, Linda L. , ALI, Amjad , KUANG, Rongze , WU, Heping
IPC分类号： C07D401/10 , C07D213/89 , C07D401/14 , C07D401/12 , C07D413/10 , C07D417/10 , A61K31/4427 , A61P7/02
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2.发明授权HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS SUITABLE FOR TREATMENT OR PREVENTION OF CENTRAL NERVOUS SYSTEM DISORDERS 有权适用于治疗或预防中枢神经系统疾病的杂环基取代的[1,2,4]三唑并[1,5-C]喹唑啉-5-胺化合物
公开(公告)号：EP2945632B1
公开(公告)日：2018-03-07
申请号：EP13866588.0
申请日：2013-12-20
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 , DENG, Qiaolin
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61P25/16
CPC分类号： C07D519/00 , C07D487/04
摘要： 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.
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公开(公告)号：EP3148542A1
公开(公告)日：2017-04-05
申请号：EP15800524.9
申请日：2015-05-22
发明人： LIU, Weiguo , EDMONDSON, Scott D. , GUO, Zhuyan , MERTZ, Eric , OGAWA, Anthony K. , SO, Sung-Sau , SUN, Wanying , BROCKUNIER, Linda L. , ALI, Amjad , KUANG, Rongze , WU, Heping
IPC分类号： A61K31/44 , A61K31/4192 , A61K31/167
CPC分类号： C07D417/10 , C07D213/89 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10
摘要： The present invention provides a compound of Formula I(The chemical formula should be inserted here.) 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： 本发明提供了式I化合物（化学式应插入此处）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。
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4.发明公开PIPERAZINE-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 有权哌嗪[1,2,4]三唑[1,5-C]喹唑啉-5-氨基 - 维生素M11A-ANTAGONISTISCHEN EIGENSCHAFTEN
公开(公告)号：EP2938344A1
公开(公告)日：2015-11-04
申请号：EP13867977.4
申请日：2013-12-20
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 , DENG, Qiaolin
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。
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公开(公告)号：EP3283464A1
公开(公告)日：2018-02-21
申请号：EP16780505.0
申请日：2016-04-11
发明人： MERTZ, Eric , EDMONDSON, Scott D. , SO, Sung-Sau , SUN, Wanying , LIU, Weiguo , NEELAMKAVIL, Santhosh F. , GAO, Ying-Duo , HRUZA, Alan , ZANG, Yi , ALI, Amjad , MAL, Rudrajit , HE, Jiafang , KUANG, Rongze , WU, Heping , OGAWA, Anthony K. , NOLTING, Andrew F.
IPC分类号： C07D233/68 , A61K31/426 , A61K31/4178 , A61P9/00 , C07D241/00
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14
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.
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公开(公告)号：EP3038466A1
公开(公告)日：2016-07-06
申请号：EP14840648.1
申请日：2014-08-25
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
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A 2A受体的拮抗剂的2,2-二氟间二氧杂环戊烯化合物。 本发明还涉及本文所述的2,2-二氟二氧代环戊烯化合物在潜在治疗或预防其中涉及A 2A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，并涉及这些药物组合物在预防或治疗涉及A 2A受体的疾病中的用途。
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公开(公告)号：EP2137179B1
公开(公告)日：2015-09-02
申请号：EP08726734.0
申请日：2008-03-12
发明人： TING, Pauline, C. , ASLANIAN, Robert, G. , CAO, Jianhua , KIM, David, Won-Shik , KUANG, Rongze , ZHOU, Gang , HERR, Robert, Jason , ZYCH, Andrew, John , YANG, Jinhai , WU, Heping , ZORN, Nicolas
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22 , A61K31/501 , A61P31/00
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
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公开(公告)号：EP3331532A1
公开(公告)日：2018-06-13
申请号：EP16824890.4
申请日：2016-07-05
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 , C07D491/153
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 A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-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.
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公开(公告)号：EP3180317A1
公开(公告)日：2017-06-21
申请号：EP15826790.6
申请日：2015-07-23
发明人： LIU, Weiguo , EDMONDSON, Scott D. , GUO, Zhuyan , SO, Sung-Sau , OGAWA, Anthony K. , KUANG, Rongze , WU, Heping , ALI, Amjad , GAO, Ying-Duo , JIANG, Yu , LI, Chunsing , YU, Tingting , PANDYA, Bhuamik , LIPPA, Blaise , ZHANG, Xin , BABER, Jon Christian , ROMERO, Jan Antoinette C. , ZHANG, Jing
IPC分类号： C07D233/54 , C07D257/06 , C07D263/30 , C07D249/06 , C07D285/04 , C07D271/10 , A61K31/4164 , A61K31/4192 , A61K31/422 , A61K31/433 , A61P7/02
CPC分类号： C07D409/14 , A61P7/02 , C07D401/06 , C07D401/14 , C07D413/14 , C07D417/14
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）的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，高凝状态或纤维变化的方法。 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。
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公开(公告)号：EP3134408A1
公开(公告)日：2017-03-01
申请号：EP15783339.3
申请日：2015-04-21
发明人： LIM, Yeon-Hee , GUO, Zhuyan , ALI, Amjad , EDMONDSON, Scott D. , LIU, Weiguo , GALLO-ETIENNE, Gioconda V. , WU, Heping , GAO, Ying-Duo , STAMFORD, Andrew M. , YU, Younong , KEVIN, Nancy J. , ANAND, Rajan , SHA, Deyou , NEELAMKAVIL, Santhosh F. , HUSSAIN, Zahid , KUMAR, Puneet , MONINGKA, Remond , DUFFY, Joseph L. , XU, Jiayi , JIANG, Yu , SONE, Hiroki , CHAKRABARTI, Anjan
IPC分类号： C07D471/10 , A61K31/438 , C07D498/20
CPC分类号： C07D498/20 , C07D471/10 , C07D487/10 , C07D498/10 , C07F9/6561
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.
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