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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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5.发明授权公开(公告)号：US10752587B2
公开(公告)日：2020-08-25
申请号：US15780289
申请日：2016-11-29
IPC分类号： C07D211/16 , C07D401/14 , C07D409/14 , C07D401/06 , C07D487/08 , C07D413/14 , C07D451/02 , C07D417/14 , C07D211/46 , C07D211/10 , C07D211/54 , C07D211/44
摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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公开(公告)号：US10961215B2
公开(公告)日：2021-03-30
申请号：US16341602
申请日：2017-10-09
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu
IPC分类号： C07D401/04 , C07D211/26 , C07D405/14
摘要： In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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7.发明申请公开(公告)号：US20200247754A1
公开(公告)日：2020-08-06
申请号：US16341595
申请日：2017-10-09
申请人： Michael T. RUDD , Zhaoyang MENG , Jenny WAI , David Jonathan BENNETT , Edward J. BRNARDIC , Nigel J. LIVERTON , Shawn J. STACHEL , Yongxin HAN , Paul TEMPEST , Jiuxiang ZHU , Xuewang XU , Bin ZHU , Merck Sharp & Dohme Corp.
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号： C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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8.发明申请公开(公告)号：US20200039951A1
公开(公告)日：2020-02-06
申请号：US16341602
申请日：2017-10-09
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu
IPC分类号： C07D401/04 , C07D405/14 , C07D211/26
摘要： In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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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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10.发明申请公开(公告)号：US20210179607A1
公开(公告)日：2021-06-17
申请号：US16758717
申请日：2018-10-29
发明人： Yongqi Deng , Abdelghani Achab , Bridget A. Becker , David Jonathan Bennett , Indu Bharathan , Xavier Fradera , Craig Gibeau , Yongxin Han , Derun Li , Kun Liu , Qinglin Pu , Sulagna Sanyal , David Sloman , Wensheng Yu , Hongjun Zhang
IPC分类号： C07D471/04 , C07D215/14 , A61K45/06
摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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