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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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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：US09840478B2
公开(公告)日：2017-12-12
申请号：US14908421
申请日：2014-07-29
发明人： Peter D. Williams , John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Kartik M. Keertikar , H. Marie Loughran , Jessie J. Manikowski , Gregori J. Morriello , Dong-Ming Shen , Edward C. Sherer , Jurgen Schultz , Sherman T. Waddell , Catherine M. Wiscount , Nicolas Zorn , Xin-Jie Chu , Satyanarayana Tummanapalli , Vijayasaradhi Sivalenka , Bin Hu , Tao Ji , Bin Zhong
IPC分类号： C07D241/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to piperazine derivatives, 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：US20170073354A1
公开(公告)日：2017-03-16
申请号：US15124635
申请日：2015-03-06
申请人： Jurgen SCHULZ , Peter D. WILLIAMS , John A. MCCAULEY , Christopher J. BUNGARD , David Jonathan BENNETT , Sherman T. WADDELL , Gregori J. MORRIELLO , Lehua CHANG , Michael P. DWYER , Katharine M. HOLLOWAY , Alejandro CRESPO , Xin-Jie CHU , Catherine WISCOUNT , Marie H. LOUGHRAN , Jesse J. MANIKOWSKI , Kartik M. KEERTIKAR , Bin HU , Bin ZHONG , Tao JI , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd.
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： C07D513/08 , A61K31/554 , A61K45/06
CPC分类号： C07D513/08 , A61K31/554 , 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.
摘要翻译： 本发明涉及含有该化合物的式I药物组合物的化合物及其在抑制HIV蛋白酶，抑制HIV复制，预防HIV感染，HIV感染治疗和预防， 治疗和延迟艾滋病的发病或进展。
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公开(公告)号：US20160159752A1
公开(公告)日：2016-06-09
申请号：US14908421
申请日：2014-07-29
发明人： Peter D. Williams , John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Kartik M. Keertikar , H. Marie Loughran , Jessie J. Manikowski , Gregori J. Morriello , Dong-Ming Shen , Edward C. Sherer , Jurgen Schultz , Sherman T. Waddell , Catherine M. Wiscount , Nicolas Zorn , Xin-Jie Chu , Satyanarayana Tummanapalli , Vijayasaradhi Sivalenka , Bin Hu , Tao Ji , Bin Zhong
IPC分类号： C07D241/04 , C07D401/12 , C07D417/14 , C07D405/14 , C07D413/14 , C07D401/06 , C07D405/12
CPC分类号： C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to piperazine derivatives, 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.
摘要翻译： 本发明涉及哌嗪衍生物，包含它们的药物组合物及其在抑制HIV蛋白酶，HIV复制抑制，HIV预防感染，HIV感染治疗和预防治疗中的用途 ，并延迟艾滋病的发病或进展。
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公开(公告)号：US20230139282A1
公开(公告)日：2023-05-04
申请号：US17795349
申请日：2021-02-02
申请人： Manuel DE LERA RUIZ , Paola FAVUZZA , Zhuyan GUO , Bin HU , Michael J. KELLY, III , Zhiyu LEI , John A. MCCAULEY , David B. OLSEN , Brad SLEEBS , Tony TRIGLIA , Dongmei ZHAN , Lianyun ZHAO , Merck Sharp & Dohme LLC , The Walter and Eliza Hall Institute of Medical Research , MSD R&D (China) Co., Ltd.
发明人： Manuel de Lera Ruiz , Paola Favuzza , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , John A. McCauley , David B. Olsen , Brad Sleebs , Tony Triglia , Dongmei Zhan , Lianyun Zhao
IPC分类号： A61K31/513 , A61K45/06 , C07D405/12 , C07D233/88 , C07D405/14 , C07D417/14 , C07D491/18 , A61P33/06 , A61K31/529 , A61K31/5377 , C07D401/06
摘要： Provided are 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. Also provided are uses of the compounds of Formula (I), as defined herein, 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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公开(公告)号：US20230013692A1
公开(公告)日：2023-01-19
申请号：US17776040
申请日：2020-11-16
申请人： Merck Sharp & Dohme LLC , MSD R&D (China) Co. Ltd. , The Walter and Eliza Hall Institute of Medical Research
发明人： John A. McCauley , Manuel de Lera Ruiz , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , David B. Olsen , Brad Sleebs , Dongmei Zhan , Lianyun Zhao
IPC分类号： C07D239/22 , C07D401/06 , C07D405/14 , A61P33/06
摘要： The present invention provides 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. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of 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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公开(公告)号：US20190315769A1
公开(公告)日：2019-10-17
申请号：US16447271
申请日：2019-06-20
发明人： Thomas H. Graham , Tao Yu , Yonglian Zhang , John A. McCauley
IPC分类号： C07D498/22 , A61P31/18 , C07D498/16 , C07D487/16 , A61K31/553 , A61K31/4188 , A61K31/407 , A61K31/5365 , A61K31/4985 , C07D471/22
摘要： The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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公开(公告)号：US20180325926A1
公开(公告)日：2018-11-15
申请号：US15775871
申请日：2016-11-11
发明人： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley , Andrew Stamford , Wengsheng Liu , Jay A. Grobler , Libo Xu
IPC分类号： A61K31/675 , A61P31/18
CPC分类号： A61K31/675 , A61K31/426 , A61K31/513 , A61K31/52 , A61K2300/00 , A61P31/18 , C07D491/20 , C07F9/6561
摘要： The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R16 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US09834526B2
公开(公告)日：2017-12-05
申请号：US15104510
申请日：2014-12-17
发明人： John A. McCauley , Christian Beaulieu , David Jonathan Bennett , Christopher J. Bungard , Sheldon Crane , Thomas J. Greshock , Katharine M. Holloway , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Satyanarayana Tummanapalli , Vouy Linh Truong , Peter D. Williams
IPC分类号： A61K31/535 , C07D265/28 , C07D265/30 , A61K45/06 , A61K31/5375 , A61K31/5377 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to 2,5,6-substituted morpholine derivatives 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. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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