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公开(公告)号：US10780174B2
公开(公告)日：2020-09-22
申请号：US16063666
申请日：2016-12-22
IPC分类号： A61K31/573 , A61K31/337 , A61K31/58 , A61K31/495 , A61K31/519 , A61K31/436 , A61K47/54 , C07J5/00 , C07J41/00 , C07D475/08 , C07J31/00 , C07D305/14 , C07J43/00 , C07D487/04 , C07D295/185 , A61P29/00 , A61P35/00
摘要： This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.
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公开(公告)号：US20160095924A1
公开(公告)日：2016-04-07
申请号：US14838703
申请日：2015-08-28
发明人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Pieter R. Cullis , Marco A. Ciufolini , Barbara Low Shoud Mui
IPC分类号： A61K47/22 , A61K39/39 , A61K31/713 , C07D317/28
CPC分类号： A61K47/22 , A61K9/1271 , A61K31/713 , A61K39/39 , A61K2039/55511 , A61K2039/55555 , C07D317/28 , C07D319/06
摘要： The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
摘要翻译： 本发明提供优异的用于将治疗剂递送至细胞的组合物和方法。 特别地，这些包括提供核酸的有效包封的新型脂质和核酸 - 脂质颗粒，并将包封的核酸有效地递送到细胞体内。 本发明的组合物是高度有效的，从而允许在相对低的剂量下有效击倒特异性靶蛋白。 此外，与本领域已知的组合物和方法相比，本发明的组合物和方法毒性低，并提供更大的治疗指数。
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公开(公告)号：US20220304929A1
公开(公告)日：2022-09-29
申请号：US17634649
申请日：2020-08-11
发明人： Joshua Zaifman , Sam Chen , Yuen Yi Tam , Marco A. Ciufolini
IPC分类号： A61K9/127 , C07C69/732 , C07C69/675 , C07C219/06 , C07C309/67 , C07C309/68
摘要： Disclosed herein is a lipid having a net charge at physiological pH, and being covalently attached to a lipid moiety. The lipid moiety comprises a hydrocarbon structure having two or more linked hydrocarbon chains, optionally having cis or trans C═C, at least one of said chains being covalently attached to the head group optionally via the linker region. The hydrocarbon chains are bonded to one another at a branch point at an internal carbon of the chain attached to the linker region, which branch point comprises a functional group having an electronegative atom. The hydrocarbon chains each have between 1 and 40 carbon atoms, wherein the hydrocarbon structure in total comprises between 10 and 150 carbon atoms. Advantageously, the hydrocarbon structure may assume a generally flared shape for enhanced delivery of cargo molecules. Further provided are delivery vehicles comprising the lipids.
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公开(公告)号：US10653780B2
公开(公告)日：2020-05-19
申请号：US14838703
申请日：2015-08-28
发明人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Pieter R. Cullis , Marco A. Ciufolini , Barbara Low Shoud Mui
IPC分类号： C07D317/28 , C07D319/06 , A61K47/22 , A61K9/127 , A61K31/713 , A61K39/39 , A61K39/00
摘要： The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
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公开(公告)号：US20190151458A1
公开(公告)日：2019-05-23
申请号：US16063666
申请日：2016-12-22
IPC分类号： A61K47/54 , A61P35/00 , A61P29/00 , A61K31/573 , A61K31/337 , A61K31/58 , A61K31/495 , A61K31/519 , A61K31/436
摘要： This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.
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