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公开(公告)号：US20200046743A1
公开(公告)日：2020-02-13
申请号：US16659786
申请日：2019-10-22
发明人： Yasutsugu UEDA , Timothy P. CONNOLLY , John F. KADOW , Nicholas A. MEANWELL , Tao WANG , Chung-Pin H. CHEN , Kap-Sun YEUNG , Zhongxing ZHANG , David Kenneth LEAHY , Shawn K. PACK , Nachimuthu SOUNDARARAJAN , Pierre SIRARD , Kathia LEVESQUE , Dominique THORAVAL
IPC分类号： A61K31/675 , C07C215/10 , A61K31/519 , A61K45/06 , C07F9/06 , C07F9/6561 , C07F9/6558 , C07F9/655 , C07F9/572 , C07D471/04 , A61K31/497
摘要： This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
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公开(公告)号：US20190151336A1
公开(公告)日：2019-05-23
申请号：US16253393
申请日：2019-01-22
发明人： Sing-Yuen SIT , Yan CHEN , Jie CHEN , Jacob SWIDORSKI , Brian Lee VENABLES , Ny SIN , Nicholas A. MEANWELL , Alicia REGUEIRO-REN , Richard A. HARTZ , Li XU , Zheng LIU
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.
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公开(公告)号：US20170340650A1
公开(公告)日：2017-11-30
申请号：US15678381
申请日：2017-08-16
发明人： Sing-Yuen Sit , Yan Chen , Jie Chen , Jacob Swidorski , Brian Lee Venables , Ny Sin , Nicholas A. Meanwell , Alicia Regueiro-Ren , Richard A. Hartz , Li Xu , Zheng Liu
IPC分类号： A61K31/58 , C07F5/04 , C07C309/65 , A61K45/06 , C07J63/00 , C07F5/02 , C07C2601/16
CPC分类号： A61K31/58 , A61K45/06 , C07C309/65 , C07C2601/16 , C07F5/025 , C07F5/04 , C07J63/008
摘要： Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.
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公开(公告)号：US20220106341A1
公开(公告)日：2022-04-07
申请号：US17421851
申请日：2020-01-15
IPC分类号： C07F9/6561 , C07D471/04
摘要： A method for the preparation of a compound of Formula IV wherein P1 is H or a suitable protecting group, comprising preparation of a compound of Formula I wherein P2 is H or a suitable protecting group and R1 is H or C1-6alkyl.
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公开(公告)号：US10221208B2
公开(公告)日：2019-03-05
申请号：US15563635
申请日：2016-04-14
发明人： Adrian Ortiz , Maxime Soumeillant , Scott A. Savage , Neil A. Strotman , Martin D. Eastgate , Matthew W. Haley , Jeanne Ho , Jeffrey A. Nye , Zhongmin Xu , Susanne Kiau , Tamas Benkovics , Yichen Tan
IPC分类号： C07D295/155 , C07J63/00 , A61P31/18 , A61K31/58 , A61K45/06
摘要： A method for producing HIV maturation inhibitor compound is set forth using betulin as starting material, and utilizing Lossen rearrangement techniques.
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公开(公告)号：US20180072691A1
公开(公告)日：2018-03-15
申请号：US15563635
申请日：2016-04-14
发明人： Adrian ORTIZ , Maxime SOUMEILLANT , Scott A. SAVAGE , Neil A. STROTMAN , Martin D. EASTGATE , Matthew W. HALEY , Jeanne HO , Jeffrey A. NYE , Zhongmin XU , Susanne KIAU , Tamas BENKOVICS , Yichen TAN
IPC分类号： C07D295/155 , C07J63/00
CPC分类号： C07J63/008 , A61K31/58 , A61K45/06 , A61P31/18 , C07D295/155
摘要： A method for producing HIV maturation inhibitor compound is set forth using betulin as starting material, and utilizing Lossen rearrangement techniques.
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公开(公告)号：US09908882B2
公开(公告)日：2018-03-06
申请号：US15529537
申请日：2015-12-17
IPC分类号： C07D401/00 , C07D471/04 , C07D401/14 , C07D249/08 , C07F9/6561 , C07F5/02 , C07C17/02
CPC分类号： C07D471/04 , C07C17/02 , C07D249/08 , C07D401/14 , C07F5/022 , C07F9/6561 , Y02P20/582
摘要： A process for preparing halogenated azaindole compounds makes use of stable reagents including a brominating reagent, a boroxine and a sulfonic anhydride to enhance the selectivity and yield of the final product. In addition, the process is associated with various other advantages, including the ability to recycle reagents, cost reduction, and improved manufacturability.
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公开(公告)号：US20180000849A1
公开(公告)日：2018-01-04
申请号：US15704100
申请日：2017-09-14
发明人： Yasutsugu UEDA , Timothy P. CONNOLLY , John F. KADOW , Nicholas A. MEANWELL , Tao WANG , Chung-Pin H. CHEN , Kap-Sun YEUNG , Zhongxing ZHANG , David Kenneth LEAHY , Shawn K. PACK , Nachimuthu SOUNDARARAJAN , Pierre SIRARD , Kathia LEVESQUE , Dominique THORAVAL
IPC分类号： A61K31/675 , C07F9/6558 , C07F9/655 , C07F9/572 , C07F9/06 , C07D471/04 , A61K45/06 , C07F9/6561 , A61K31/497
CPC分类号： A61K31/675 , A61K31/497 , A61K31/519 , A61K45/06 , C07C215/10 , C07D471/04 , C07F9/062 , C07F9/5728 , C07F9/65515 , C07F9/65586 , C07F9/6561
摘要： This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
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公开(公告)号：US20160361328A1
公开(公告)日：2016-12-15
申请号：US15249827
申请日：2016-08-29
发明人： Yasutsugu UEDA , Timothy P. CONNOLLY , John F. KADOW , Nicholas A. MEANWELL , Tao WANG , Chung-Pin H. CHEN , Kap-Sun YEUNG , Zhongxing ZHANG , David Kenneth LEAHY , Shawn K. PACK , Nachimuthu SOUNDARARAJAN , Pierre SIRARD , Kathia LEVESQUE , Dominique THORAVAL
IPC分类号： A61K31/675 , A61K45/06
CPC分类号： A61K31/675 , A61K31/497 , A61K31/519 , A61K45/06 , C07C215/10 , C07D471/04 , C07F9/062 , C07F9/5728 , C07F9/65515 , C07F9/65586 , C07F9/6561
摘要： This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
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