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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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2.
公开(公告)号:US20230013022A1
公开(公告)日:2023-01-19
申请号:US17731766
申请日:2022-04-28
发明人: Anthony Nicholas , Casi M. Schienebeck , Erik W. Bush , Tao Pei , Zhao Xu , Zhen Li , Rui Zhu
IPC分类号: C12N15/113 , A61K47/68
摘要: Described are RNAi agents, compositions that include RNAi agents, and methods for inhibition of a beta-ENaC (SCNN1B) gene. The beta-ENaC RNAi agents and RNAi agent conjugates disclosed herein inhibit the expression of a beta-ENaC gene. Pharmaceutical compositions that include one or more beta-ENaC RNAi agents, optionally with one or more additional therapeutics, are also described. Delivery of the described beta-ENaC RNAi agents to epithelial cells, such as pulmonary epithelial cells, in vivo, provides for inhibition of beta-ENaC gene expression and a reduction in ENaC activity, which can provide a therapeutic benefit to subjects, including human subjects, for the treatment of various diseases including chronic obstructive pulmonary disease (COPD).
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3.
公开(公告)号:US20230265437A1
公开(公告)日:2023-08-24
申请号:US18048577
申请日:2022-10-21
发明人: Anthony Nicholas , Tao Pei , Erik W. Bush , Tingting Yuan
IPC分类号: C12N15/113 , A61P11/00
CPC分类号: C12N15/1137 , A61P11/00 , C12N2310/14 , C12N2310/11 , C12N2310/32
摘要: Described are RNAi agents, compositions that include RNAi agents, and methods for inhibition of a matrix metallopeptidase 7 (MMP7) gene. The MMP7 RNAi agents and RNAi agent conjugates disclosed herein inhibit the expression of an MMP7 gene. Pharmaceutical compositions that include one or more MMP7 RNAi agents, optionally with one or more additional therapeutics, are also described. Delivery of the described MMP7 RNAi agents to pulmonary cells, in vivo, provides for inhibition of MMP7 gene expression, which can provide a therapeutic benefit to subjects, including human subjects, for the treatment of various diseases including pulmonary inflammation diseases such as idiopathic pulmonary fibrosis (IPF).
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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:US20230002767A1
公开(公告)日:2023-01-05
申请号:US17824841
申请日:2022-05-25
IPC分类号: C12N15/113 , A61P11/12
摘要: Described are RNAi agents, compositions that include RNAi agents, and methods for inhibition of a Mucin 5AC (MUC5AC) gene. The MUC5AC RNAi agents and RNAi agent conjugates disclosed herein inhibit the expression of an MUC5AC gene. Pharmaceutical compositions that include one or more MUC5AC RNAi agents, optionally with one or more additional therapeutics, are also described. Delivery of the described MUC5AC RNAi agents to pulmonary epithelial cells, in vivo, provides for inhibition of MUC5AC gene expression and a reduction in MUC5AC production, which can provide a therapeutic benefit to subjects, including human subjects, for the treatment of various diseases including mucoobstructive lung disease such as severe asthma and various cancers.
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公开(公告)号:US20220396791A1
公开(公告)日:2022-12-15
申请号:US17715444
申请日:2022-04-07
IPC分类号: C12N15/113 , A61K9/00 , A61P11/00
摘要: Described are RNAi agents, compositions that include RNAi agents, and methods for inhibition of a Receptor for Advanced Glycation End-products (AGER or RAGE) gene. The RAGE RNAi agents and RNAi agent conjugates disclosed herein inhibit the expression of an AGER gene. Pharmaceutical compositions that include one or more RAGE RNAi agents, optionally with one or more additional therapeutics, are also described. Delivery of the described RAGE RNAi agents to pulmonary cells, in vivo, provides for inhibition of AGER gene expression and a reduction in membrane RAGE activity, which can provide a therapeutic benefit to subjects, including human subjects, for the treatment of various diseases including pulmonary inflammation diseases such as severe asthma.
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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: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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公开(公告)号:US20190248832A1
公开(公告)日:2019-08-15
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: C07K5/062 , C12N15/113 , A61K47/64 , A61K47/60 , A61K31/713
CPC分类号: C07K5/06026 , A61K31/713 , A61K47/60 , A61K47/64 , C07K16/28 , C12N15/1138 , C12N2310/14 , C12N2310/3513 , C12N2320/32
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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