IMMUNE RECEPTOR MODIFIER CONJUGATE AND PREPARATION METHOD AND USE THEREOF, COUPLING PRECURSOR FOR PREPARING SAME, AND COMPOUND FOR SYNTHESIZING COUPLING PRECURSOR

摘要

Disclosed is an immune receptor modifier conjugate, obtained from the reaction between a coupling precursor and a biotic ligand, the coupling precursor being a 9-position aminomethyl benzyl purine biotic coupling precursor, and the biotic ligand being selected from one or more of polypeptide, protein, glycoprotein, polysaccharide, polynucleotide, inactivated cells and inactivated microbes. The immune receptor modifier couplet can be used for immunomodulation, antibody preparation, anti-virus, diabetes, tumor immunomodulation, and tumor bio-immunotherapy. The conjugate compounds or salts thereof can be prepared into various therapeutic drugs, and can be prepared into a compound drug together with other drugs, or pharmaceutically acceptable carrier composites or conjugates. Also disclosed are compounds for synthesizing the coupling precursor and salts thereof.

主权项

1. An immune receptor modifier conjugate, characterized in that the conjugate is obtained by the reaction between a coupling precursor and a biotic ligand, and is a compound of formula (I): wherein R2 represents the biotic ligand, X1 represents OH or SH, R1 represents linear alkyl, branched alkyl, substituted alkyl, unsubstituted alkyl or alkoxyalkyl, X2 represents a coupling group; and m and n each are an integer selected from 1 to 10; When the coupling precursor is a compound of formula 1: X2 represents the group thiocarbonyl When the coupling precursor is a compound of formula 2: X2 represents the group When the coupling precursor is a compound of formula 3: X2 represents the groupin which u is an integer selected from 0 to 12;
or when the coupling precursor is a compound of formula 4: X2 represents the groupin which PEG represents a polyethylene glycol group.