Purecodon (Hong Kong) Biopharma Ltd.

Soochow University

Yinjia Gao

Zhenhua Sun

Yuping Liu

Ke Huang

Yingwen Li

Haibin Shi

Binxi Ge

Chaoxuan Jing

The present invention discloses HOresponsive crosslinking NIR molecular probe for tumor microenvironment and application therefor. The preparation method includes the following steps: the amide condensation of 2-propynylamine and Fmoc-Lys(Boc)-OH to obtain compound A01-01; removing protecting groups from compound A01-01, to obtain compound C1-2; reacting compound C1-2 and NHS-activated (3-carboxypropyl)triphenylphosphonium bromide, to obtain compound C1-3; removing protecting groups from compound C1-3, to obtain compound C1-4; reacting compound C1-4 with NHS-activated 3,5-dioxocyclohexane carboxylic acid, to obtain a compound C1-5; and reacting compound C1-5 with NIR dye, to obtain a HOresponsive crosslinking NIR molecular probe for tumor microenvironment. The probe itself uses HOin a tumor microenvironment for crosslinking on a tumor site, achieving the goal of a long-term retention, thereby improving a result of tumor imaging, and providing a novel strategy and means for improving long-term retention of a NIR molecular probe at a tumor site.

HO-responsive crosslinking near-infrared molecular probe for tumor microenvironment and use therefor

The present disclosure belongs to the technical field of gene therapy, and specifically relates to a series of lipid compounds as well as lipid vectors, nucleic acid lipid nanoparticle compositions, and pharmaceutical preparations containing the same. The compound having the structure of formula (I) provided by the present disclosure may be used in combination with other lipid compounds to prepare a lipid vector, which exhibits pH responsiveness, has high encapsulation efficiency for nucleic acid drugs, and greatly enhances the in-vivo delivery efficiency of nucleic acid drugs. Moreover, it is possible to select lipid compounds with different structures as lipid vectors to adjust the enrichment of nucleic acid drugs in different organs, thereby having good market application prospect.

Lipid compound as well as lipid vector, nucleic acid lipid nanoparticle composition, and pharmaceutical preparation comprising the same

The present invention belongs to the technical field of gene therapy, and particularly relates to a series of lipid compounds as well as a lipid carrier, nucleic acid lipid nanoparticle composition and pharmaceutical preparation containing the same. A compound having a structure of a formula (I) provided by the present invention can be used for preparing a lipid carrier together with other lipid compounds, and exhibits pH response, and the entrapment efficiency to a nucleic acid drug is high, which greatly improves in-vivo delivery efficiency of the nucleic acid drug; and furthermore, a lipid compound with a specific structure can be chosen as a lipid carrier based on an organ in which the nucleic acid drug needs to be enriched, having a good market application prospect.

Lipid compound as well as lipid carrier, nucleic acid lipid nanoparticle composition and pharmaceutical preparation containing same

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Suzhou, China

Yinjia Gao