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公开(公告)号：US11180529B2
公开(公告)日：2021-11-23
申请号：US16399073
申请日：2019-04-30
发明人： Aaron Almeida , Zhen Li , Erik W. Bush , Tao Pei , Agnieszka Glebocka , Anthony Nicholas , Jeffrey Carlson , Matthew Fowler-Watters
IPC分类号： A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K38/08 , C07K5/062 , C12N15/113 , A61K47/60 , A61K47/64 , C07K16/28 , C07K7/06 , A61K31/713
摘要： Integrin ligands having serum stability and affinity for αvβ6 integrins are described. Compositions comprising αvβ6 integrin ligands having serum stability and having affinity for αvβ6 integrins and methods of using them are also described.
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公开(公告)号：US12065458B2
公开(公告)日：2024-08-20
申请号：US16970130
申请日：2019-02-15
发明人： Zhen Li , Erich Altenhofer , Jeffrey Carlson , Matthew Fowler-Watters , Bo Chen
IPC分类号： C07F9/06 , A61K47/54 , C07C205/59 , C07C235/34 , C07D403/14 , C12N15/113
CPC分类号： C07F9/06 , A61K47/545 , C07C205/59 , C07C235/34 , C07D403/14 , C12N15/113 , C12N2310/14 , C12N2310/351
摘要： Described are improved linking agents that are useful for facilitating the attachment of targeting groups, pharmacokinetic (PK) enhancers or modifiers, or other delivery agents to oligonucleotides. The described linking agents may exhibit improved reaction yields, stability, and biological activity, particularly when used in connection with oligonucleotide-based compounds, such as RNA interference (RNAi) agents.
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公开(公告)号：US20240076270A1
公开(公告)日：2024-03-07
申请号：US18160114
申请日：2023-01-26
发明人： Zhen Li , Xiaokai Li , Erik W. Bush , Rui Zhu , Dongxu Shu , Jonathan Benson , Patrick Shao , Matthew Fowler-Watters
IPC分类号： C07D213/74 , A61K47/54 , A61K47/56 , A61K47/60 , C07D409/12 , C07D413/12 , C12N15/11 , C12N15/113
CPC分类号： C07D213/74 , A61K47/545 , A61K47/56 , A61K47/60 , C07D409/12 , C07D413/12 , C12N15/111 , C12N15/1138 , C12N2310/3513
摘要： Synthetic αvβ6 integrin ligands of Formula I having serum stability and affinity for integrin αvβ6, which is a receptor expressed in a variety of cell types, are described. The described ligands are useful for delivering cargo molecules, such as RNAi agents or other oligonucleotide-based compounds, to cells that express integrin αvβ6, and thereby facilitating the uptake of the cargo molecules into these cells. Compositions that include αvβ6 integrin ligands and methods of use are also described.
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公开(公告)号：US11597701B2
公开(公告)日：2023-03-07
申请号：US16759610
申请日：2018-10-31
发明人： Zhen Li , Xiaokai Li , Erik W. Bush , Rui Zhu , Dongxu Shu , Jonathan Benson , Patrick Shao , Matthew Fowler-Watters
IPC分类号： C07H21/04 , C07D213/74 , C07D409/12 , C07D413/12 , A61K47/54 , A61K47/56 , A61K47/60 , C12N15/11 , C12N15/113
摘要： Synthetic αvβ6 integrin ligands of Formula I having serum stability and affinity for integrin αvβ6, which is a receptor expressed in a variety of cell types, are described. The described ligands are useful for delivering cargo molecules, such as RNAi agents or other oligonucleotide-based compounds, to cells that express integrin αvβ6, and thereby facilitating the uptake of the cargo molecules into these cells. Compositions that include αvβ6 integrin ligands and methods of use are also described.
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公开(公告)号：US20220402947A1
公开(公告)日：2022-12-22
申请号：US16970130
申请日：2019-02-15
发明人： Zhen Li , Erich Altenhofer , Jeffrey Carlson , Matthew Fowler-Watters , Bo Chen
IPC分类号： C07F9/06 , A61K47/54 , C07C235/34 , C07C205/59 , C07D403/14 , C12N15/113
摘要： Described are improved linking agents that are useful for facilitating the attachment of targeting groups, pharmacokinetic (PK) enhancers or modifiers, or other delivery agents to oligonucleotides. The described linking agents may exhibit improved reaction yields, stability, and biological activity, particularly when used in connection with oligonucleotide-based compounds, such as RNA interference (RNAi) agents.
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公开(公告)号：US20210069337A1
公开(公告)日：2021-03-11
申请号：US17078331
申请日：2020-10-23
发明人： Zhen Li , Jeffrey Carlson , Anthony Nicholas , Xiaokai Li , Dongxu Shu , Matthew Fowler-Watters
IPC分类号： A61K47/54 , C07D401/12 , C07D471/04 , C07D403/12 , C12N15/113 , A61K47/60
摘要： Compounds having affinity for integrins, the synthesis of these compounds, and the use of these compounds as ligands to facilitate the delivery of cargo molecules to cells expressing integrins are described. The described integrin targeting ligands have serum stability and affinity for αvβ3 integrin and/or αvβ5 integrin, and are suitable for conjugation to cargo molecules, such as such as oligonucleotide-based therapeutic agents (e.g., RNAi agents), to facilitate delivery of the cargo molecules to cells and tissues, such as tumor cells, that express integrin αvβ3, integrin αvβ5, or both integrin αvβ3 and integrin αvβ5. Compositions that include integrin targeting ligands and methods of use are also described.
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公开(公告)号：US20220204976A1
公开(公告)日：2022-06-30
申请号：US17420460
申请日：2020-01-08
发明人： Zhen Li , Dongxu Shu , Anthony Nicholas , Rui Zhu , Jeffrey Carlson , So Wong , Xiaokai Li , Erich Altenhofer , Matthew Fowler-Watters , Bo Chen
IPC分类号： C12N15/113 , A61P35/00
摘要： The present disclosure relates to RNAi agents, for example, double stranded RNAi agents, able to inhibit HIF-2 alpha (EPAS1) gene expression. Also disclosed are pharmaceutical compositions that include HIF-2 alpha RNAi agents and methods of use thereof. The HIF-2 alpha RNAi agents disclosed herein may be linked or conjugated to targeting ligands (such as compounds that have affinity for integrins, including alpha-v-beta-3 and alpha-v-beta-5 integrins) and pharmacokinetic (PK) enhancers, to facilitate the delivery to cells and tissues, including to clear cell renal cell carcinoma (ccRCC) cells and tumors. Delivery of compositions comprising the HIF-2 alpha RNAi agents in vivo provides for inhibition of HIF-2 alpha gene expression. The HIF-2 alpha RNAi agents can be used in methods of treatment of various diseases and disorders, including ccRCC.
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公开(公告)号：US20220024975A1
公开(公告)日：2022-01-27
申请号：US17501486
申请日：2021-10-14
发明人： Aaron Almeida , Zhen Li , Erik W. Bush , Tao Pei , Agnieszka Glebocka , Anthony Nicholas , Jeffrey Carlson , Matthew Fowler-Watters
IPC分类号： C07K5/062 , C12N15/113 , A61K47/60 , A61K47/64 , C07K16/28 , C07K7/06 , A61K38/08 , A61K31/713
摘要： Integrin ligands having serum stability and affinity for αvβ6 integrins are described. Compositions comprising αvβ6 integrin ligands having serum stability and having affinity for αvβ6 integrins and methods of using them are also described.
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公开(公告)号：US20210093725A1
公开(公告)日：2021-04-01
申请号：US17050042
申请日：2019-04-26
发明人： Zhen Li , Jeffrey Carlson , Anthony Nicholas , Xiaokai Li , Dongxu Shu , Matthew Fowler-Watters
IPC分类号： A61K47/54 , C12N15/113 , A61K47/60 , A61P35/00
摘要： Compounds having affinity for integrins, the synthesis of these compounds, and the use of these compounds as ligands to facilitate the delivery of cargo molecules to cells expressing integrins are described. The described integrin targeting ligands have serum stability and affinity for αvβ3 integrin and/or αvβ5 integrin, and are suitable for conjugation to cargo molecules, such as such as oligonucleotide-based therapeutic agents (e.g., RNAi agents), to facilitate delivery of the cargo molecules to cells and tissues, such as tumor cells, that express integrin αvβ3, integrin αvβ5, or both integrin αvβ3 and integrin αvβ5. Compositions that include integrin targeting ligands and methods of use are also described.
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公开(公告)号：US20200369613A1
公开(公告)日：2020-11-26
申请号：US16759610
申请日：2018-10-31
发明人： Zhen Li , Xiaokai Li , Erik W. Bush , Rui Zhu , Dongxu Shu , Jonathan Benson , Patrick Shao , Matthew Fowler-Watters
IPC分类号： C07D213/74 , C07D413/12 , C07D409/12
摘要： Synthetic avβ6 integrin ligands of Formula I having serum stability and affinity for integrin avβ6, which is a receptor expressed in a variety of cell types, are described. The described ligands are useful for delivering cargo molecules, such as RNAi agents or other oligonucleotide-based compounds, to cells that express integrin avβ6, and thereby facilitating the uptake of the cargo molecules into these cells. Compositions that include avB6 integrin ligands and methods of use are also described.
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