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公开(公告)号：US20230355626A1
公开(公告)日：2023-11-09
申请号：US17802194
申请日：2021-03-03
发明人： Eric P. GILLIS , Christiana IWUAGWU
IPC分类号： A61K31/519 , C07D471/04 , A61K31/5365 , A61K31/537 , A61K31/513 , A61K31/675 , A61K31/4985 , A61K31/54 , A61K45/06 , A61P31/18
CPC分类号： A61K31/519 , C07D471/04 , A61K31/5365 , A61K31/537 , A61K31/513 , A61K31/675 , A61K31/4985 , A61K31/54 , A61K45/06 , 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：US11084845B2
公开(公告)日：2021-08-10
申请号：US16534208
申请日：2019-08-07
发明人： Jie Chen , Yan Chen , Ira B. Dicker , Richard A. Hartz , Nicholas A. Meanwell , Beata Nowicka-Sans , Alicia Regueiro-Ren , Sing-Yuen Sit , Ny Sin , Jacob Swidorski , Brian Lee Venables
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: These compounds are useful for the treatment of HIV and AIDS.
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3.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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4.发明授权公开(公告)号：US10351546B2
公开(公告)日：2019-07-16
申请号：US15749584
申请日：2016-08-10
发明人： Kyle J. Eastman , John F. Kadow , B. Narasimhulu Naidu , Kyle E. Parcella , Manoj Patel , Prasanna Sivaprakasam , Yong Tu
IPC分类号： A61K31/444 , C07D401/14 , C07D405/14 , C07D401/04 , C07D487/04 , A61P31/18 , A61K31/5365
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.
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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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公开(公告)号：US20190092754A1
公开(公告)日：2019-03-28
申请号：US16202653
申请日：2018-11-28
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 , C07D401/04 , A61K31/444 , 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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7.发明授权公开(公告)号：US10221156B2
公开(公告)日：2019-03-05
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
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：US20190031709A1
公开(公告)日：2019-01-31
申请号：US16071925
申请日：2017-02-02
发明人： Jie CHEN , Yan CHEN , Ira B. DICKER , Richard A. HARTZ , Nicholas A. MEANWELL , Beata NOWICKA-SANS , Alicia REGUEIRO-REN , Sing-Yuen SIT , Ny SIN , Jacob SWIDORSKI , Brian Lee VENABLES
CPC分类号： C07J53/002 , A61P31/18 , C07J63/008 , C12N9/506 , C12N2740/16222
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: These compounds are useful for the treatment of HIV and AIDS.
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9.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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10.发明授权公开(公告)号：US10106504B2
公开(公告)日：2018-10-23
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 , C07D405/14 , C07D405/04 , C07D487/04 , C07D491/052 , A61K31/5365 , A61K31/4433 , A61K31/4418 , A61P31/18 , A61K31/519 , A61K31/506 , C07D401/04 , C07D491/06 , A61K31/4741 , A61K31/4725
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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