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公开(公告)号：US20220331321A1
公开(公告)日：2022-10-20
申请号：US17633655
申请日：2020-07-21
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research , MSD R & D (China) Co. LTD.
发明人： John A. McCauley , Alan F. Cowman , Manuel de Lera Ruiz , Paola Favuzza , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , David B. Olsen , Brad Sleebs , Jennifer K. Thompson , Tony Triglia , Dongmei Zhan , Cailing Zhang , Lianyun Zhao
IPC分类号： A61K31/513 , C07D405/14 , C07D493/10 , C07D491/052 , C07D409/14 , C07D239/22 , C07D405/12 , C07D409/04 , A61P33/06 , A61K45/06
摘要： Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
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2.发明授权公开(公告)号：US11339156B2
公开(公告)日：2022-05-24
申请号：US16621953
申请日：2018-06-22
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Timothy J. Henderson , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Meng Na , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang , Takao Suzuki
IPC分类号： C07D471/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D417/14
摘要： The present invention is directed to pyrazol-4-yl-pyridine 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.
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3.发明申请公开(公告)号：US20210380580A1
公开(公告)日：2021-12-09
申请号：US16621953
申请日：2018-06-22
发明人： John J. ACTON, III , Jianming BAO , Qiaolin DENG , Melissa EGBERTSON , Ronald FERGUSON, II , Xiaolei GAO , Scott Timothy HARRISON , Timothy J. HENDERSON , Sandra L. KNOWLES , Chunsing LI , Michael Man-Chu LO , Robert D. MAZZOLA, Jr. , Meng NA , Michael T. RUDD , Oleg B. Selyutin , David M. TELLERS , Ling TONG , Fengqi ZHANG , Takao SUZUKI
IPC分类号： C07D471/04 , C07D401/14 , C07D417/14 , C07D413/14 , C07D487/04 , C07D405/14
摘要： The present invention is directed to pyrazol-4-yl-pyridine 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.
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4.发明授权公开(公告)号：US11149036B2
公开(公告)日：2021-10-19
申请号：US16621959
申请日：2018-06-22
申请人： John J. Acton, III , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd. , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/048 , C07D498/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine 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.
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5.发明授权公开(公告)号：US10933056B2
公开(公告)日：2021-03-02
申请号：US16674546
申请日：2019-11-05
发明人： John J. Acton, III , Jianming Bao , Melissa Egbertson , Xiaolei Gao , Scott T. Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Jenny Miu-Chun Wai
IPC分类号： C07D401/14 , C07D405/14 , C07D471/04 , A61K31/4439 , A61P25/28 , A61P25/18 , A61P25/16 , A61K31/437
摘要： The present invention is directed to pyrazol-4-yl-pyridine 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.
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公开(公告)号：US10202401B2
公开(公告)日：2019-02-12
申请号：US15807992
申请日：2017-11-09
发明人： Hongming Li , Jingjun Yin , Kevin M. Belyk , Kevin R. Campos , Qinghao Chen , Alan M. Hyde , Tetsuji Itoh , Artis Klapars , Matthew Thomas Tudge , Edward Cleator , Aaron M. Dumas , Louis-Charles Campeau , Yonggang Chen , Ji Qi , Wensong Xiao
IPC分类号： C07D265/14 , C07D498/04 , C07C251/24 , C07F9/6509 , C07F17/02 , C07D413/14 , C07D239/74 , C07D413/04 , C07D417/04 , C07D265/36
摘要： The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.
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公开(公告)号：US10160762B2
公开(公告)日：2018-12-25
申请号：US15574411
申请日：2016-05-24
发明人： Dong-Ming Shen , Michael P. Dwyer , Christopher J. Sinz , Deping Wang , Shawn J. Stachel , Daniel V. Paone , Ashley Forster , Richard Berger , Yili Chen , Yimin Qian , Shimin Xu , Chunmei Hu , William D. Shipe , Jianmin Fu , Zhigang Guo , Haitang Li , Yingjian Bo
IPC分类号： C07D487/04 , A61K31/519 , A61P25/14 , A61P25/28 , A61P25/18 , A61P25/00 , A61P25/16
摘要： The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.
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公开(公告)号：US10138255B2
公开(公告)日：2018-11-27
申请号：US15124635
申请日：2015-03-06
发明人： Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC分类号： A61K31/554 , C07D513/08 , A61K45/06
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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公开(公告)号：US20170233412A1
公开(公告)日：2017-08-17
申请号：US15514536
申请日：2015-09-23
发明人： JIAQIANG CAI , ALEJANDRO CRESPO , XIAOXING DU , BYRON GABRIEL DUBOIS , DEODIALSINGH GUIADEEN , SHANKARAN KOTHANDARAMAN , PING LIU , RONGQIANG LIU , WEIGUO QUAN , CHRISTOPHER SINZ , LIPING WANG
IPC分类号： C07D513/06 , C07D471/06 , C07D498/16 , C07D498/06
CPC分类号： C07D513/06 , C07D471/04 , C07D471/06 , C07D498/04 , C07D498/06 , C07D498/16 , C07D513/04
摘要： The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
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10.发明授权公开(公告)号：US11319298B2
公开(公告)日：2022-05-03
申请号：US16471679
申请日：2017-12-18
发明人： Jianming Bao , Ronald Ferguson , Xiaolei Gao , Scott Harrison , Sandra L. Knowles , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Jeffrey W. Shubert
IPC分类号： C07D401/02 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D491/107 , C07D498/08 , C07D513/04
摘要： The present invention is directed to heteroarylpiperidine ether 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.
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