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公开(公告)号：EP4461316A1
公开(公告)日：2024-11-13
申请号：EP22922990.1
申请日：2022-02-10
发明人： LIU, Zhijia , CHEN, Yongming , HE, Zepeng , LE, Zhicheng
IPC分类号： A61K47/18 , A61K47/22 , A61K48/00 , C07D295/13 , C07C237/22 , C07C231/06
摘要： A cationic lipid analogue, a composition and a use thereof. An aldehyde, an amine, a carboxylic acid and an isonitrile are adopted as raw materials to synthesize a cationic lipid analogue via the Ugi reaction. The synthesized cationic lipid analogue, together with a sterol, an auxiliary lipid and a polyethylene glycol lipid derivative, further forms a nanoparticle-like lipid composition, which can be used for drug delivery, including the delivery of small molecule drugs, nucleic acid drugs such as mRNA, DNA, siRNA, etc., protein/peptide drugs, and gene editing complexes such as mRNA/sgRNA, Cas9/sgRNA, etc. The nanoparticle-like lipid composition achieves mRNA expressions in different organs of animals through different administration methods, and thus can meet the application requirements of mRNA nucleic acid therapies, nucleic acid vaccines, gene editing, etc.
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公开(公告)号：EP4309674A1
公开(公告)日：2024-01-24
申请号：EP21925480.2
申请日：2021-12-07
发明人： LIU, Zhijia , LE, Zhicheng , HE, Zepeng , CHEN, Yongming
摘要： The present disclosure discloses an ionizable cationic lipid analogue material and use thereof as a drug delivery carrier. In the present disclosure, a series of cationic lipid analogue materials are reasonably designed, and a preparation method of the cationic lipid analogue materials involves mild reaction conditions, a simple process, and excellent stability. The cationic lipid analogue materials have excellent biocompatibility, and can allow an efficient and safe intracellular delivery of a biomacromolecular drug. The cationic lipid analogue materials can also be used as delivery carriers for other types of drugs.
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