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Synthesis of immune agonist target compound and application thereof

A technology of agonists, compounds, applied in the interdisciplinary field of medicinal chemistry and immunology

Active Publication Date: 2018-08-10
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the experimental results show that TKI antagonizes the activation of immune cells by TLR7 agonists and inhibits the production of immune activation cytokines (Scientific Reports, 2016Dec 21; 6:39598.doi: 10.1038 / srep39598)

Method used

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  • Synthesis of immune agonist target compound and application thereof
  • Synthesis of immune agonist target compound and application thereof
  • Synthesis of immune agonist target compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0118] The synthesis of compounds related to the present invention is exemplified as follows, and the exemplification method can inspire those skilled in the art to realize the synthesis of novel compounds in the present invention, but can not be limited to the synthesis method in the exemplification:

[0119] SZU-112

[0120]

[0121] 1g of SZU-101, 311mg of NHS and 518mg of EDC were dissolved in 12mL of anhydrous DMF, reacted at room temperature for 2h under nitrogen protection, and monitored the reaction by TLC. After the reaction, the reaction solution was poured into water to precipitate a precipitate, which was filtered and dried to obtain the crude product of SZU-009T, which was directly carried out to the next reaction.

[0122] Dissolve 500mg of SZU-009T and 339mg of Fmoc-D-lysine in 10mL of anhydrous DMF, and stir at room temperature for 1h. After the reaction is complete, add water to precipitate a solid, and filter it with suction. Chloroform:methanol=3:1 colu...

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Abstract

The invention relates to series micromolecular immune agonist target coupling target medicines. A novel target compound medicine with immune activation function has the effect of improving the immunity activating effect of a target medicine and the effect of resisting tumor and other diseases in vivo and in vitro, and the target medicine is endowed with two functions and is also called bifunctional target medicine. The improvement effect is under the coordination effect of two functions of antitumor factor (such as IFN-gamma) and pathogenic target site resistance; the compound is a novel efficient target medicine integrating two functions.

Description

technical field [0001] The invention relates to a series of homologue small molecule immune stimulants and uses thereof, which belong to the interdisciplinary field of medicinal chemistry and immunology. technical background [0002] Toll-like receptor (TLR) is the first line of defense of the organism defense system (Kaisho, T. & Akira, S. Toll-like receptor function and signaling. J. Allergy Clin. Immunol. 117, 979-987 (2006); Miyake, K.Innate immune sensing of pathogens and danger signals by cell surface Toll-like receptors.Semin.Immunol.19,3–10(2007)); wherein the natural ligand for activation of TLR7 is ssRNA, which has a role in the defense of ssRNA series virus attack Important role (Blasius, A.L. & Beutler, B. Intracellular toll-like receptors. Immunity 32, 305–315 (2010)); In addition, TLR7 can be activated by artificially synthesized small molecular compounds to induce immune regulation of the body, in antiviral and antitumor aspects Has an important role (Huju Ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K39/395A61P35/00A61P37/04A61P31/18A61P31/20
CPCA61K39/3955A61K47/545A61P35/00A61P37/04A61P31/18A61P31/20A61K47/6803C07K16/2827A61K2039/505A61P31/12A61P37/02A61K31/522A61K47/64A61K47/6849A61K47/55A61K47/549C07D473/18A61K31/52A61K47/54
Inventor 靳广毅王竹林唐黎
Owner SHENZHEN UNIV
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