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公开(公告)号：US09636410B2
公开(公告)日：2017-05-02
申请号：US14130886
申请日：2012-07-06
申请人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
发明人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
CPC分类号： A61K39/39 , A61K9/1075 , A61K39/12 , A61K39/155 , A61K39/245 , A61K47/02 , A61K47/06 , A61K47/12 , A61K47/22 , A61K47/24 , A61K47/26 , A61K47/34 , A61K2039/5256 , A61K2039/53 , A61K2039/55555 , A61K2039/55566 , A61K2039/575 , C12N7/00 , C12N2710/16134 , C12N2710/16171 , C12N2710/16734 , C12N2710/16771 , C12N2760/18534 , C12N2760/18571 , C12N2770/36134 , C12N2770/36143 , C12N2840/203 , Y02A50/386 , Y02A50/388 , Y02A50/412
摘要： This invention generally relates to cationic oil-in-water emulsions that contain high concentrations of cationic lipids and have a defined oil:lipid ratio. The cationic lipid can interact with the negatively charged molecule thereby anchoring the molecule to the emulsion particles. The cationic emulsions described herein are useful for delivering negatively charged molecules, such as nucleic acid molecules to cells, and for formulating nucleic acid-based vaccines.
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公开(公告)号：US09655845B2
公开(公告)日：2017-05-23
申请号：US14130880
申请日：2012-07-06
申请人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
发明人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
IPC分类号： A61K9/107 , A61K31/713 , A61K39/155 , A61K39/12 , A61K9/00 , A61K39/00
CPC分类号： A61K9/107 , A61K9/0019 , A61K31/713 , A61K39/12 , A61K39/155 , A61K2039/53 , A61K2039/55566 , C12N2760/18534 , Y02A50/412
摘要： This invention generally relates to cationic oil-in-water emulsions that can be used to deliver nucleic acid molecules, such as an RNA molecule. The emulsion particles comprise an oil core and a cationic lipid. The emulsion particles have an average diameter of about 80 nm to about 180 nm, and the emulsion have an N/P ratio of at least 1.1:1.
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公开(公告)号：US09295646B2
公开(公告)日：2016-03-29
申请号：US13235454
申请日：2011-09-18
申请人： Luis Brito , Andrew Geall , Derek O'Hagan , Manmohan Singh
发明人： Luis Brito , Andrew Geall , Derek O'Hagan , Manmohan Singh
CPC分类号： A61K39/385 , A61K9/107 , A61K39/39 , A61K2039/53 , A61K2039/55566
摘要： This invention generally relates to cationic oil-in-water emulsions that can be used to deliver negatively charged molecules, such as an RNA molecule. The emulsion particles comprise an oil core and a cationic lipid. The cationic lipid can interact with the negatively charged molecule thereby anchoring the molecule to the emulsion particles. The cationic emulsions described herein are particularly suitable for delivering nucleic acid molecules (such as an RNA molecule encoding an antigen) to cells and formulating nucleic acid-based vaccines.
摘要翻译： 本发明一般涉及阳离子水包油乳液，其可用于递送带负电荷的分子，例如RNA分子。 乳剂颗粒包含油芯和阳离子脂质。 阳离子脂质可以与带负电荷的分子相互作用，从而将分子固定在乳液颗粒上。 本文所述的阳离子乳剂特别适用于将核酸分子（例如编码抗原的RNA分子）递送至细胞并配制基于核酸的疫苗。
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公开(公告)号：US20120156251A1
公开(公告)日：2012-06-21
申请号：US13235454
申请日：2011-09-18
申请人： Luis BRITO , Andrew Geall , Derek O'Hagan , Manmohan Singh
发明人： Luis BRITO , Andrew Geall , Derek O'Hagan , Manmohan Singh
CPC分类号： A61K39/385 , A61K9/107 , A61K39/39 , A61K2039/53 , A61K2039/55566
摘要： This invention generally relates to cationic oil-in-water emulsions that can be used to deliver negatively charged molecules, such as an RNA molecule. The emulsion particles comprise an oil core and a cationic lipid. The cationic lipid can interact with the negatively charged molecule thereby anchoring the molecule to the emulsion particles. The cationic emulsions described herein are particularly suitable for delivering nucleic acid molecules (such as an RNA molecule encoding an antigen) to cells and formulating nucleic acid-based vaccines.
摘要翻译： 本发明一般涉及阳离子水包油乳液，其可用于递送带负电荷的分子，例如RNA分子。 乳剂颗粒包含油芯和阳离子脂质。 阳离子脂质可以与带负电荷的分子相互作用，从而将分子固定在乳液颗粒上。 本文所述的阳离子乳剂特别适用于将核酸分子（例如编码抗原的RNA分子）递送至细胞并配制基于核酸的疫苗。
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公开(公告)号：US20140220083A1
公开(公告)日：2014-08-07
申请号：US14130886
申请日：2012-07-06
申请人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
发明人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
CPC分类号： A61K39/39 , A61K9/1075 , A61K39/12 , A61K39/155 , A61K39/245 , A61K47/02 , A61K47/06 , A61K47/12 , A61K47/22 , A61K47/24 , A61K47/26 , A61K47/34 , A61K2039/5256 , A61K2039/53 , A61K2039/55555 , A61K2039/55566 , A61K2039/575 , C12N7/00 , C12N2710/16134 , C12N2710/16171 , C12N2710/16734 , C12N2710/16771 , C12N2760/18534 , C12N2760/18571 , C12N2770/36134 , C12N2770/36143 , C12N2840/203 , Y02A50/386 , Y02A50/388 , Y02A50/412
摘要： This invention generally relates to cationic oil-in-water emulsions that contain high concentrations of cationic lipids and have a defined oil:lipid ratio. The cationic lipid can interact with the negatively charged molecule thereby anchoring the molecule to the emulsion particles. The cationic emulsions described herein are useful for delivering negatively charged molecules, such as nucleic acid molecules to cells, and for formulating nucleic acid-based vaccines.
摘要翻译： 本发明一般涉及含有高浓度阳离子脂质并具有确定的油脂比例的阳离子水包油乳剂。 阳离子脂质可以与带负电荷的分子相互作用，从而将分子固定在乳液颗粒上。 本文所述的阳离子乳液可用于将带负电荷的分子（例如核酸分子）递送至细胞，以及配制基于核酸的疫苗。
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公开(公告)号：US20140212498A1
公开(公告)日：2014-07-31
申请号：US14130880
申请日：2012-07-06
申请人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
发明人： Luis Brito , Michelle Chan , Andrew Geall , Derek O'Hagan , Manmohan Singh
IPC分类号： A61K9/107 , A61K31/713
CPC分类号： A61K9/107 , A61K9/0019 , A61K31/713 , A61K39/12 , A61K39/155 , A61K2039/53 , A61K2039/55566 , C12N2760/18534 , Y02A50/412
摘要： This invention generally relates to cationic oil-in-water emulsions that can be used to deliver nucleic acid molecules, such as an RNA molecule. The emulsion particles comprise an oil core and a cationic lipid. The emulsion particles have an average diameter of about 80 nm to about 180 nm, and the emulsion have an N/P ratio of at least 1.1:1.
摘要翻译： 本发明一般涉及可用于递送核酸分子（例如RNA分子）的阳离子水包油乳液。 乳剂颗粒包含油芯和阳离子脂质。 乳剂颗粒的平均直径为约80nm至约180nm，乳液的N / P比至少为1.1:1。
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7.发明申请公开(公告)号：US20130195968A1
公开(公告)日：2013-08-01
申请号：US13808089
申请日：2011-07-06
申请人： Andrew Geall , Christian Mandl , Derek O'Hagan , Manmohan Singh
发明人： Andrew Geall , Christian Mandl , Derek O'Hagan , Manmohan Singh
IPC分类号： A61K9/50
CPC分类号： A61K9/50 , A61K9/0019 , A61K9/127 , A61K39/00 , A61K39/12 , A61K39/155 , A61K39/245 , A61K2039/53 , A61K2039/55505 , A61K2039/55555 , A61K2039/55566 , C12N15/86 , C12N15/88 , C12N2710/16134 , C12N2760/18522 , C12N2760/18534 , C12N2770/36143
摘要： Nucleic acid immunisation is achieved by delivering a self-replicating RNA encapsulated within a small particle. The RNA encodes an immunogen of interest, and the particle may deliver this RNA by mimicking the delivery function of a natural RNA virus. Thus the invention provides a non-virion particle for in vivo delivery of RNA to a vertebrate cell, wherein the particle comprises a delivery material encapsulating a self-replicating RNA molecule which encodes an immunogen. These particles are useful as components in pharmaceutical compositions for immunising subjects against various diseases.
摘要翻译： 通过递送封装在小颗粒内的自我复制RNA来实现核酸免疫。 RNA编码感兴趣的免疫原，并且颗粒可以通过模拟天然RNA病毒的递送功能递送该RNA。 因此，本发明提供了用于体内将RNA递送至脊椎动物细胞的非病毒颗粒，其中所述颗粒包含封装编码免疫原的自复制RNA分子的递送材料。 这些颗粒可用作免疫针对各种疾病的受试者的药物组合物中的组分。
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公开(公告)号：US11291635B2
公开(公告)日：2022-04-05
申请号：US13808089
申请日：2011-07-06
申请人： Andrew Geall , Christian Mandi , Derek O'Hagan , Manmohan Singh
发明人： Andrew Geall , Christian Mandi , Derek O'Hagan , Manmohan Singh
IPC分类号： A61K9/50 , A61K39/155 , A61K39/245 , C12N15/86 , C12N15/88 , A61K39/12 , A61K9/127 , A61K9/00 , A61K39/00
摘要： Nucleic acid immunisation is achieved by delivering a self-replicating RNA encapsulated within a small particle. The RNA encodes an immunogen of interest, and the particle may deliver this RNA by mimicking the delivery function of a natural RNA virus. Thus the invention provides a non-virion particle for in vivo delivery of RNA to a vertebrate cell, wherein the particle comprises a delivery material encapsulating a self-replicating RNA molecule which encodes an immunogen. These particles are useful as components in pharmaceutical compositions for immunising subjects against various diseases.
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公开(公告)号：US20160317458A1
公开(公告)日：2016-11-03
申请号：US15104723
申请日：2014-12-17
申请人： Luis Brito , Delai Chen , Gabriel Grant Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
发明人： Luis Brito , Delai Chen , Gabriel Grant Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
IPC分类号： A61K9/51 , C07C219/06 , C07D211/62 , C07C229/12 , C07C323/52 , C07C235/08 , C07D211/06 , C07D295/13 , C07D211/22 , C07D207/16 , C07D319/06 , C07D207/12 , C07D211/46 , C07D233/64 , A61K9/127 , A61K38/22 , A61K38/18 , A61K39/12 , C12N7/00 , C12N15/113
CPC分类号： A61K9/5123 , A61K9/1272 , A61K31/7105 , A61K31/713 , A61K38/1816 , A61K38/2264 , A61K39/12 , A61K47/18 , A61K2039/53 , C07C219/06 , C07C219/16 , C07C229/12 , C07C235/08 , C07C323/52 , C07D207/12 , C07D207/16 , C07D211/06 , C07D211/22 , C07D211/46 , C07D211/62 , C07D233/60 , C07D233/64 , C07D295/088 , C07D295/13 , C07D319/06 , C12N7/00 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2320/32 , C12N2760/00034 , C12N2760/00071
摘要： This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
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公开(公告)号：US10059655B2
公开(公告)日：2018-08-28
申请号：US15104736
申请日：2014-12-17
申请人： Luis Brito , Delai Chen , Gabriel Grant Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
发明人： Luis Brito , Delai Chen , Gabriel Grant Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
IPC分类号： C07C229/12 , C07C229/38 , C07D205/04 , C07D265/30 , C07D207/12 , C07D207/16 , C07D211/22 , C07D295/088 , C07D211/46 , C07D211/60 , C07D211/62 , C07D295/15 , C07C271/20 , C07C219/04 , A61K47/18 , A61K9/127 , A61K9/51 , A61K31/7105 , A61K31/713 , A61K39/39 , C07C271/22 , C07D211/06 , C07D211/34 , C07D211/44
CPC分类号： C07C229/12 , A61K9/1272 , A61K9/5123 , A61K31/7105 , A61K31/713 , A61K39/12 , A61K39/39 , A61K47/18 , A61K2039/53 , A61K2039/55555 , C07C219/04 , C07C229/38 , C07C271/20 , C07C271/22 , C07D205/04 , C07D207/12 , C07D207/16 , C07D211/06 , C07D211/22 , C07D211/34 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/62 , C07D265/30 , C07D295/088 , C07D295/15 , C12N2760/18534
摘要： This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
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