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公开(公告)号:US20210395248A1
公开(公告)日:2021-12-23
申请号:US17287736
申请日:2019-11-04
IPC分类号: C07D471/04 , C07D519/00 , A61P31/18
摘要: Compounds of Formula I, and pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:
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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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3.
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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4.
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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公开(公告)号:US20220389007A1
公开(公告)日:2022-12-08
申请号:US17763133
申请日:2020-09-29
发明人: Michael S. BOWSHER , Eric P. GILLIS , Christiana IWUAGWU , B Narasimhulu NAIDU , Kyle E. PARCELLA , Manoj PATEL
IPC分类号: C07D471/04 , C07D277/08 , A61P31/18
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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公开(公告)号:US20210403465A1
公开(公告)日:2021-12-30
申请号:US17285680
申请日:2019-10-28
IPC分类号: C07D417/14 , C07D403/14 , C07D405/14 , C07D401/14
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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7.
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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公开(公告)号:US20220089598A1
公开(公告)日:2022-03-24
申请号:US17272377
申请日:2019-09-12
IPC分类号: C07D487/04
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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公开(公告)号:US20210393633A1
公开(公告)日:2021-12-23
申请号:US17284855
申请日:2019-10-22
IPC分类号: A61K31/517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D401/14 , A61K31/5377 , A61P31/18
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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公开(公告)号:US20210379071A1
公开(公告)日:2021-12-09
申请号:US17288085
申请日:2019-11-04
发明人: Michael S. BOWSHER , Eric P. GILLIS , Christiana IWUAGWU , B. Narasimhulu NAIDU , Kyle E. PARCELLA , Manoj PATEL , Kevin M. PEESE
IPC分类号: A61K31/517 , A61K45/06 , C07D403/14 , C07D471/04 , A61P31/18 , A61K31/519
摘要: Compounds and pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth.
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