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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：US20200016136A1
公开(公告)日：2020-01-16
申请号：US16465622
申请日：2018-01-02
发明人： Michael S. BOWSHER , Jeffrey DESKUS , Kyle J. EASTMAN , Eric P. GILLIS , David B. FRENNESSON , Christiana IWUAGWU , B. Narasimhulu NAIDU , Kyle E. PARCELLA , Kevin M. PEESE , Mark G. SAULNIER , Prasanna SIVAPRAKASAM
IPC分类号： A61K31/444 , C07D401/14 , C07D413/14 , C07D491/048 , C07D491/08 , A61K31/5377 , A61K31/506 , A61K31/519 , A61K31/497 , A61K31/5386 , A61K31/4995 , C07D471/08 , C07D417/14 , A61K31/541 , C07D491/147 , 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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3.发明申请公开(公告)号：US20180162831A1
公开(公告)日：2018-06-14
申请号：US15579977
申请日：2016-07-06
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61P31/18
CPC分类号： C07D401/04 , A61P31/18 , C07D401/14 , C07D405/14 , 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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4.发明申请公开(公告)号：US20210024503A1
公开(公告)日：2021-01-28
申请号：US17042413
申请日：2019-04-11
发明人： Makonen BELEMA , John A. BENDER , David B. FRENNESSON , Eric P. GILLIS , Christiana IWUAGWU , John F. KADOW , B. Narasimhulu NAIDU , Kyle E. PARCELLA , Kevin M. PEESE , Ramkumar RAJAMANI , Mark G. SAULNIER , Alan Xiangdong WANG , Manoj PATEL , Michael S. BOWSHER
IPC分类号： C07D403/14 , A61P31/18 , C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/052
摘要： Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:
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5.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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6.发明申请公开(公告)号：US20190010139A1
公开(公告)日：2019-01-10
申请号：US15748791
申请日：2016-08-03
发明人： John F. KADOW , B. Narasimhulu NAIDU , Jeffrey Lee ROMINE , Denis R. ST. LAURENT , Prasanna SIVAPRAKASAM
IPC分类号： C07D401/04 , A61P31/18 , C07D401/14 , C07D407/14 , C07D471/10 , C07D493/10
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 H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, (alkoxy)alkoxyalkyl, or (R6)alkyl; R2 is phenyl substituted with 1 R7 substituent and with 0-3 substituents selected from halo, alkyl, haloalkyl, alkoxy, and haloalkoxy; or R2 is selected from tetrahydroisoquinolinyl, ((Ar1)alkyl)tetrahydroisoquinolinyl, or ((N-alkoxycarbonyl) tetrahydroisoquinolinyl; R3 is selected from tetrahydroisoquinolinyl or decahydroisoquinolinyl and is substituted with 0-3 substituents selected from halo, alkyl, and haloalkyl; or R3 is a [5-7.3-7.0-2] fused or bridged bicyclic amine and is substituted with 0-3 alkyl substituents; or R3 is selected from azetidinyl, pyrrolidinyl, piperidinyl, or homopiperidinyl and contains a spirocyclic moiety wherein the spirocyclic moiety, including the carbon atom to which it is attached, forms C3-7 cycloalkane, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, N-alkylpyrrolidinyl, piperidinyl, N-alkylpiperidinyl, homopiperidinyl, or N-alkylpiperidinyl, and wherein the spirocyclic moiety is substituted with 0-3 halo or alkyl substituents; R4 is selected from alkyl or haloalkyl; R5 is selected from H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, (alkoxy)alkoxyalkyl, or (R6) alkyl; R6 is selected from (oxetanyl)oxy, ((oxetanyl)alkoxy)alkyl, (tetrahydropyranyloxy)alkyl, (tetrahydropyranyl)alkoxy)alkyl, or (R9)(R9)N; R7 is selected from (Ar1)alkoxy or ((Ar1)alkyl)HNCO; R8 is selected from hydrogen, alkyl, (cycloalkyl)alkyl, alkoxyalkyl, (tetrahydropyanyl)alkyl, tetrahydropyanyl, or alkoxyphenyl; R9 is selected from hydrogen or alkyl; or (R8)(R9)N taken together is selected from azetidinyl, pyrrolidinyl, piperidinyl, (spirocyclobutyl) piperidinyl, piperazinyl, or morpholinyl; and Ar1 is phenyl substituted with 0-3 substituents selected from halo, alkyl, haloalkyl, alkoxy, and haloalkoxy.
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![IMIDAZO[1,2-A]PYRIDINE DERIVATIVES FOR USE AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION](/abs-image/US/2018/08/09/US20180222901A1/abs.jpg.150x150.jpg)
7.发明申请公开(公告)号：US20180222901A1
公开(公告)日：2018-08-09
申请号：US15505955
申请日：2015-08-25
IPC分类号： C07D471/04 , C07D519/00 , A61P31/18
CPC分类号： C07D471/04 , A61P31/18 , C07D519/00
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, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
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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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9.发明申请公开(公告)号：US20180222864A1
公开(公告)日：2018-08-09
申请号：US15749133
申请日：2016-08-18
发明人： John F. KADOW , B. Narasimhulu NAIDU , Yong TU
IPC分类号： C07D213/55 , A61K31/5365 , C07D405/14 , A61K31/4433 , A61K31/4418 , C07D405/04 , A61K31/4725 , C07D487/04 , A61K31/519 , A61K31/506 , C07D401/04 , C07D491/06 , A61K31/4741 , A61P31/18
CPC分类号： C07D213/55 , A61K31/4418 , A61K31/4433 , A61K31/4725 , A61K31/4741 , A61K31/506 , A61K31/519 , A61K31/5365 , A61P31/18 , C07D401/04 , C07D405/04 , C07D405/14 , C07D487/04 , C07D491/052 , C07D491/06
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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10.发明申请公开(公告)号：US20180147196A1
公开(公告)日：2018-05-31
申请号：US15580742
申请日：2016-07-07
发明人： Kyle J. EASTMAN , John F. KADOW , B. Narasimhulu NAIDU , Kyle E. PARCELLA , Manoj PATEL , Yong TU
IPC分类号： A61K31/4545 , C07D401/04 , C07D401/14 , A61K31/5365 , A61P31/18
CPC分类号： A61K31/4545 , A61K31/5365 , A61P31/18 , C07D401/04 , C07D401/14
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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