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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：US20160296527A1
公开(公告)日：2016-10-13
申请号：US15104782
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 , Helen Juteau , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Christian Nadeau , Daniel Simard , Satyanarayana Tummanapalli , Vouy Linh Truong , Karine M. Villeneuve , Peter D. Williams
IPC分类号： A61K31/5377 , C07D413/14 , C07D471/04 , C07D487/04 , A61K45/06 , C07D413/04
CPC分类号： A61K31/5377 , A61K45/06 , C07D265/30 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention is directed to 5-heteroarylmorpholine 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.
摘要翻译： 本发明涉及5-杂芳基吗啉衍生物及其用于抑制HIV蛋白酶，HIV复制的抑制，HIV预防感染，HIV感染治疗以及预防，治疗和延迟的用途 艾滋病的发病或进展。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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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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公开(公告)号：US20200069691A1
公开(公告)日：2020-03-05
申请号：US16461899
申请日：2017-12-19
发明人： Brian McKittrick , John P. Caldwell , John McCauley , Henry Vaccaro , Tin-Yau Chan , Hyunjin Kim , Elizabeth Smith , Liwu Hong , Tanweer Khan , Shihong Ying , Hongwu Wang , Peter D. Williams , Jae-Hun Kim , M. Brad Nolt , Maryann Caplen
IPC分类号： A61K31/519 , A61K45/06 , C07D487/04 , A61K31/4985 , C07D519/00 , C07D413/14 , A61K31/496 , C07D498/04 , C07D403/14 , C07D413/10 , C07D498/14 , A61K31/5383 , A61K31/4178 , A61K31/4188 , A61K31/424 , A61K31/4355 , A61K31/429 , C07D513/04 , A61P31/18
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：US09737545B2
公开(公告)日：2017-08-22
申请号：US15104782
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 , Helen Juteau , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Christian Nadeau , Daniel Simard , Satyanarayana Tummanapalli , Vouy Linh Truong , Karine M. Villeneuve , Peter D. Williams
IPC分类号： A61K31/5377 , C07D417/04 , A61K45/06 , C07D487/04 , C07D471/04 , C07D413/04 , C07D265/30 , C07D413/14
CPC分类号： A61K31/5377 , A61K45/06 , C07D265/30 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention is directed to 5-heteroarylmorpholine 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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公开(公告)号：US20160311786A1
公开(公告)日：2016-10-27
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： C07D265/30 , A61K45/06 , C07D413/12 , A61K31/5377 , C07D471/04 , C07D417/14 , C07D487/04 , C07D417/12 , C07D513/04 , A61K31/5375 , C07D413/14
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.
摘要翻译： 本发明涉及2,5,6-取代的吗啉衍生物及其在抑制HIV蛋白酶，HIV复制抑制，HIV感染预防，HIV感染治疗和预防治疗中的应用 ，并延迟艾滋病的发病或进展。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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