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公开(公告)号：US10245275B2
公开(公告)日：2019-04-02
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
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：US10780102B2
公开(公告)日：2020-09-22
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：US09527882B2
公开(公告)日：2016-12-27
申请号：US14682179
申请日：2015-04-09
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： C07D279/12 , C07J63/00 , C07C309/65 , C07F5/04 , C07F5/02
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.
摘要翻译： 其中X选自C4-8环烷基，C4-8环烯基，C4-9螺环烷基，C4-9螺环烯基，C4-8氧杂环烷基，C4-8二氧杂环烷基，C6-8氧杂环烯基，C6-8二氧杂环烯基，C6环二烯基，C6氧杂环戊烯基， C6-9氧杂环烷基和C6-9氧杂环烯烯基环，使得X被A取代，其中A是-C 1-6烷基 - 卤素。 这些化合物可用于治疗艾滋病毒和艾滋病。
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