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公开(公告)号：US20180230129A1
公开(公告)日：2018-08-16
申请号：US15749176
申请日：2016-08-10
发明人： Kyle J. EASTMAN , John F. KADOW , Kyle E. PARCELLA , B. Narasimhulu NAIDU , Tao WANG , Zhiwei YIN , Zhongxing ZHANG
IPC分类号： C07D401/14 , A61P31/18
CPC分类号： C07D401/14 , A61K31/444 , A61K31/5365 , A61K2300/00 , A61P31/18 , C07D401/04
摘要： Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. In the compounds of formula (I), R1 is selected from hydrogen, alkyl, or cycloalkyl; R2 is selected from tetrahydroisoquinolinyl and is substituted with 1 R6 substituent and also with 0-3 halo or alkyl substituents; R3 is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, homopiperidinyl, homopiperazinyl, or homomorpholinyl, and is substituted with 0-3 substituents selected from cyano, halo, alkyl, haloalkyl, alkoxy, and haloalkoxy; R4 is selected from alkyl or haloalkyl; R5 is alkyl; R6 is selected from Ar1, (Ar1)alkyl, (chromanyl)alkyl, cyanocycloalkyl or (dihydrobenzodioxinyl)alkyl; and Ar1 is phenyl substituted with 0-5 substituents selected from cyano, halo, alkyl, cycloalkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, (hydroxy)alkoxy, (alkoxy)alkoxy, phenoxy, benzyloxy, carboxy, phenyl, and cyanocycloalkyl.
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2.发明申请公开(公告)号：US20190152957A1
公开(公告)日：2019-05-23
申请号：US16096716
申请日：2017-05-09
发明人： John F. KADOW , B. Narasimhulu NAIDU , Tao WANG , Zhongxing ZHANG
IPC分类号： C07D405/14 , C07D401/14 , C07D417/14 , C07D413/14 , A61P31/18 , A61K31/5365 , A61K31/4725 , A61K31/506 , A61K31/501
摘要： Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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公开(公告)号：US20180230134A1
公开(公告)日：2018-08-16
申请号：US15749189
申请日：2016-08-10
发明人： John F. KADOW , B. Narasimhutu NAIDU , Tao WANG , Zhiwei YIN , Zhongxing ZHANG
IPC分类号： C07D403/14 , A61P31/18
CPC分类号： C07D403/14 , A61K31/5365 , A61K2300/00 , A61P31/18 , C07D401/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/147 , C07D495/04 , C07D513/14
摘要： Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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![5-(N-[6,5]-FUSED BICYCLIC ARYL TETRAHYDROISOQUINOLIN-6-YL) PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION](/abs-image/US/2018/08/09/US20180222890A1/abs.jpg.150x150.jpg)
公开(公告)号：US20180222890A1
公开(公告)日：2018-08-09
申请号：US15749144
申请日：2016-08-10
发明人： John F. KADOW , B. Narasimhulu NAIDU , Tao WANG , Zhiwei YIN , Zhongxing ZHANG
IPC分类号： C07D403/14 , A61P31/18
摘要： Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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5.发明申请PYRAZOLOPYRIMIDINE MACROCYCLES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION 有权作为人免疫缺陷病毒复制的抑制剂的吡唑并嘧啶大环化合物公开(公告)号：US20170057977A1
公开(公告)日：2017-03-02
申请号：US15119431
申请日：2015-02-13
发明人： John F. KADOW , B. Narasimhulu NAIDU , Manoj PATEL , Kevin PEESE , Tao WANG , Zhiwei YIN , Zhongxing ZHANG
IPC分类号： C07D498/16 , A61K31/519 , C07D498/22 , A61K45/06
CPC分类号： C07D498/16 , A61K31/519 , A61K45/06 , C07D498/22
摘要： The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
摘要翻译： 本公开一般涉及式I化合物，包括用于治疗人类免疫缺陷病毒（HIV）感染的组合物和方法。 本公开提供了HIV整合酶的新型抑制剂，含有这些化合物的药物组合物，以及使用这些化合物治疗HIV感染的方法。
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6.发明申请公开(公告)号：US20190127351A1
公开(公告)日：2019-05-02
申请号：US16094536
申请日：2017-05-09
发明人： John F. KADOW , B. Narasimhulu NAIDU , Manoj PATEL , Michael A. WALKER , Tao WANG , Zhiwei YIN , Zhongxing ZHANG , Zhizhen Barbara ZHENG
IPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , A61K31/5365 , A61K31/4725 , A61K31/4709 , A61K31/4545 , C07D409/14 , C07D413/14 , C07D411/14 , A61P31/18
CPC分类号： C07D401/14 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/5365 , A61P31/18 , C07D401/04 , C07D405/14 , C07D407/14 , C07D409/14 , C07D411/14 , C07D413/14 , C07D417/14
摘要： Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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7.发明申请公开(公告)号：US20180170904A1
公开(公告)日：2018-06-21
申请号：US15579993
申请日：2016-07-07
发明人： John F. KADOW , B. Narasimhulu NAIDU , Manoj PATEL , Jeffrey Lee ROMINE , Denis R. ST. LAURENT , Tao WANG , Zhongxing ZHANG
IPC分类号： C07D401/04 , C07D417/14 , C07D413/14 , A61P31/18
CPC分类号： C07D401/04 , A61P31/18 , C07D401/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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8.发明申请公开(公告)号：US20200325127A1
公开(公告)日：2020-10-15
申请号：US16094567
申请日：2017-05-09
发明人： John F. KADOW , B Narasimhulu NAIDU , Tao WANG , Zhiwei YIN , Zhongxing ZHANG
IPC分类号： C07D413/14 , C07D401/14 , C07D417/14 , C07D513/04 , C07D471/04
摘要： Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
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