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公开(公告)号：US20240197633A1
公开(公告)日：2024-06-20
申请号：US18284740
申请日：2022-04-07
发明人： Wengui WENG , Chao LIU , Ailan WANG , Minggui LIN , Qiaoyan LIU
IPC分类号： A61K9/127
CPC分类号： A61K9/1271
摘要： A novel PEGylated lipid and preparation methods thereof, a cationic liposome containing the PEGylated lipid, a pharmaceutical composition containing the liposome, a formulation and application thereof. The PEGylated lipid can be used for modifying a liposome, and it can be further modified and coupled with a targeting group, and then used for modifying a liposome to obtain a liposome with the targeting group. Due to the presence of a long-chain PEG and the targeting group on the lipid, the modified liposome can avoid being removed by the reticuloendothelial system in a human body and realize a targeting function. Therefore, when the modified liposome delivers an active drug to cells or a patient, especially when delivering a nucleic acid or anti-tumor drug, the liposome can realize long circulation in vivo and improve the transport efficiency of drug, and has a targeting unction so the therapeutic effect of a drug is improved.
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公开(公告)号：US20240180951A1
公开(公告)日：2024-06-06
申请号：US18284762
申请日：2022-04-07
发明人： Wengui WENG , Chao LIU , Ailan WANG , Congming LIN , Linlin WANG
IPC分类号： A61K31/7105 , A61K9/127 , A61K9/51 , A61K31/713
CPC分类号： A61K31/7105 , A61K9/1272 , A61K9/5192 , A61K31/713
摘要： A novel PEGylated lipid and preparation methods thereof, a cationic liposome containing the lipid, a pharmaceutical composition containing the liposome, a formulation and application thereof. The PEGylated lipid can be used for modifying a liposome, and can be further modified and coupled with a targeting group and then used for modifying a liposome to obtain a liposome having the targeting group. Due to the presence of a long-chain PEG and the targeting group on the lipid, the modified liposome can avoid being removed by the reticuloendothelial system in a human body and realize a targeting function. Therefore, when the modified liposome delivers an active drug to cells or a patient, especially when delivering a nucleic acid or anti-tumor drug, the liposome can realize long circulation in vivo and improve the transport efficiency of drug, and has a targeting function, so the therapeutic effect of a drug is improved.
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公开(公告)号：US20240342088A1
公开(公告)日：2024-10-17
申请号：US18269728
申请日：2022-04-01
发明人： Wengui WENG , Chao LIU , Ailan WANG , Sheng LIN
IPC分类号： A61K9/127 , A61K9/51 , A61K45/06 , C07C219/06 , C07C229/16 , C07C229/26 , C07C271/16 , C07C271/18 , C07D207/452 , C07D233/60 , C12N15/113
CPC分类号： A61K9/1272 , A61K9/5123 , A61K45/06 , C07C219/06 , C07C229/16 , C07C229/26 , C07C271/16 , C07C271/18 , C07D207/452 , C07D233/60 , C12N15/113 , C12N2310/14
摘要： A novel cationic lipid has a structure as represented by general formula (1) and specifically relates to a nitrogen-branched cationic lipid, and a liposome containing the cationic lipid, and a nucleic-acid pharmaceutical composition containing the liposome, a preparation method and application thereof, wherein, the definition of each symbol in the formula (1) is as defined herein. The cationic liposome containing the cationic lipid as represented by formula (1) can improve the loading rate and transport efficiency of nucleic-acid drugs. The formulation of the cationic liposome nucleic-acid pharmaceutical composition has good cell compatibility and higher gene transfection capability, and can improve the treatment and/or prevention effects of nucleic-acid drugs.
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公开(公告)号：US20240335384A1
公开(公告)日：2024-10-10
申请号：US18700022
申请日：2022-10-13
发明人： Sheng LIN , Minggui LIN , Ailan WANG , Linlin WANG , Wengui WENG , Chao LIU , Jinchun YUAN , Qian LIN
IPC分类号： A61K9/127 , A61K45/00 , A61K47/18 , C07C217/08 , C07C219/06 , C07C229/10 , C07C229/26 , C07C235/10
CPC分类号： A61K9/1272 , A61K45/00 , A61K47/18 , C07C217/08 , C07C219/06 , C07C229/10 , C07C229/26 , C07C235/10
摘要： A novel cationic lipid having a structure as represented by general formula (1), which specifically relates to a nitrogen-containing cationic lipid, and also relates to a liposome containing the cationic lipid, a liposome pharmaceutical composition containing said cationic lipid, preparation and application thereof. A cationic liposome containing the cationic lipid represented by formula (1), can improve the loading rate and transport rate of drugs, particularly nucleic acid drugs. The terminus of the novel cationic lipid can contain a fluorescent group or a targeting group, so that the cationic liposome pharmaceutical composition containing the cationic lipid can have fluorescent or targeting function. A formulation of cationic liposome pharmaceutical composition containing nucleic acid exhibiting a very good gene complexing ability and high gene transfection ability, thereby further improves the gene therapeutic and/or gene diagnostic effect of the drug, and provides more selectable cationic lipids in the field of drug delivery.
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