Immune agonists
AssigneesShenzhen University, Shenzhen Conjugenix Pharmaceutical Technology Company Limited
InventorsGuangyi Jin, Zhulin Wang, Ji Zhou, Mian Qin, Sumei Ren, Yajuan Cheng, Shuxian Tan
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Abstract
The present application provides a novel series of small molecular immune agonists of Toll-like receptor 7, having a structure represented by Formula I. The present application further provides use of the immune agonist for activating and amplifying immune cells and lymphocytes, and for preparing an immunomodulatory drug, an immune anti-tumor small molecule drug, and an immune anti-tumor macromolecular drug.
Claims15
A compound having a structure represented by Formula I:
- wherein
- R1 represents any one of the following alkoxy groups and alkylamino groups:
- L represents a connection chain, and the connection chain comprises any one of a polyethylene glycol chain, an alkyl chain, and a heterocyclic chain;
- n represents an integer between 1 and 20;
- R2 represents a functional group or a functional carrier;
- the functional group comprises at least one of a carboxyl group, a phosphate group, an amino group, an isothiocyano group, an isocyanate group, a thiourea group, an azide group, an unsaturated double bond, and an unsaturated triple bond;
- or consists of at least one of a targeted drug or a precursor thereof, a protein, a polypeptide, an antibody, a virus, a bacteria, and a cell;
- and
- the functional carrier comprises:
- a biocompatible material capable of binding the Formula I, a carrier capable of binding the Formula I, a biocompatible material capable of supporting the Formula I, and a carrier capable of supporting the Formula I.
An immune agonist compound, being selected from the group consisting of:
- SZU-194, having a structural formula of
- SZU-195, having a structural formula of
- SZU-213, having a structural formula of
- SZU-215, having a structural formula of
- SZU-251, having a structural formula of
- SZU-254, having a structural formula of
A starting compound of a compound having a structure represented by Formula I:
- wherein
- R1 represents any on of the following alkoxy groups and alkylamino groups:
- L represents a gonnegtion chain, and the gonnegtion chain comprises any one of a polyethylene glycol chain, an alkyl chain, and a heterocylic chain;
- n represents an integer between 1 and 20;
- R2 represents a functional group or a functional carrier;
- the functional group comprises at least one of a carboxyl group, a phosphate group, an amino group, an isothiocyano group, an isocyanate group, a thiourea group, an azide group, an unsaturated double bond, and an unsaturated triple bond;
- or consists of at least one of a targeted drug or a precursor thereof, a protein, a polypeptide, an antibody, a virus, a bacteria, and a cell;
- the functional carrier comprises:
- a biocompatible material capable of binding the Formula I, a carrier capable of binding the Formula I, a biocompatible material capable of supporting the Formula I, and a carrier capable of supporting the Formula I;
- and
- the starting compound is one selected from the group consisting of the following compounds:
- GY100, having a structural formula of
- GY115, which is an alkynyl-containing compound derived from GY100 and has a structural formula of
- GY121, which is an alkynl-containing compound derived from GY100 and has a structural formula of
- and
- GY122, which is an alkynyl-containing compound derived from GY100 and has a structural formula of
Dependencies are inferred from the claim text.