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Nanoparticle containing 5-methylpyrimidine-2, 4 (1H, 3H)-diketone derivative and preparation method and application thereof

A technology of derivatives and nanoparticles, applied in medical preparations containing active ingredients, medical preparations with non-active ingredients, pharmaceutical formulas, etc.

Pending Publication Date: 2022-06-10
SHENZHEN LONGUIDE BIOPHARMA CORP
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

Compared with viral vectors, liposome nanoparticles have the advantages of low production cost, clear chemical structure, convenient quality control, targeted drug delivery through targeted modification, and unlimited loading capacity in theory. Plastid lipid materials are non-degradable and highly toxic, so it is difficult to meet the clinical needs of repeated administration. In addition, there are problems such as poor transfection effect in vivo, nucleic acid is metabolized or cleared in serum, and poor bioavailability.

Method used

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  • Nanoparticle containing 5-methylpyrimidine-2, 4 (1H, 3H)-diketone derivative and preparation method and application thereof
  • Nanoparticle containing 5-methylpyrimidine-2, 4 (1H, 3H)-diketone derivative and preparation method and application thereof
  • Nanoparticle containing 5-methylpyrimidine-2, 4 (1H, 3H)-diketone derivative and preparation method and application thereof

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Embodiment Construction

[0015] In order to solve the above problems, the present invention provides the following technical solutions.

[0016] In a first aspect, the present invention provides a nanoparticle.

[0017] A kind of nanoparticle, it comprises: as shown in formula I compound and auxiliary material,

[0018]

[0019] Wherein, m is selected from an integer of 0-5; n is selected from an integer of 5-20. In some embodiments, m is 0, 1, 2, 3, 4 or 5, n is 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20.

[0020] In some embodiments, the compound represented by the formula I is a compound represented by NBD002,

[0021]

[0022] The compound of formula I can be synthesized by Michael addition reaction.

[0023] The auxiliary material includes at least one selected from: PEG derivatives, lipids, lipidoids, alcohols or inorganic salts. In some embodiments, the auxiliary material includes at least one selected from the group consisting of PEG derivatives, lipids and lipidoid...

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Abstract

The invention relates to nanoparticles as well as a preparation method and application thereof, and belongs to the field of biological medicines. The nanoparticle comprises a 5-methylpyrimidine-2, 4 (1H, 3H)-diketone derivative and an auxiliary material. The nanoparticles can entrap nucleic acid, and have the advantages of low toxicity, high entrapment efficiency, good transfection effect and good bioavailability. The preparation method is simple to operate, low in cost, environment-friendly and beneficial to industrial production.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a nanoparticle and its preparation method and application. Background technique [0002] Gene transfection is a technology that transfers or transports nucleic acids with biological functions into cells and enables the nucleic acids to maintain their biological functions in cells. Gene carrier refers to a tool for introducing exogenous therapeutic genes into biological cells. At present, the gene vectors with industrial transformation potential in the world are mainly viral vectors and non-viral vectors. [0003] Viral vectors are a gene delivery tool that utilizes the ability of viruses to transmit their genomes into other cells for infection. Currently, there are lentiviruses, adenoviruses, retrovirus vectors, and adeno-associated virus vectors with good application prospects. However, due to their inherent physical and chemical properties and biological activities, viral vectors h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/00A61K9/14A61K47/22A61K47/54A61K31/7105C07D239/54
CPCA61K39/00A61K9/145A61K47/22A61K9/146A61K47/545A61K31/7105C07D239/54A61K2039/5156A61K2039/53
Inventor 张龙贵刘晨梁梅桂王宇恒
Owner SHENZHEN LONGUIDE BIOPHARMA CORP
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