C07D211/10

LIGHT-EMITTING RADICAL CATION PROBE IN SITU GENERATED BY ACID INDUCTION, AND PREPARATION THEREFOR AND APPLICATION THEREOF
20250305953 · 2025-10-02 ·

The present invention belongs to a technical field of a medical material. Disclosed are a light-emitting radical cation probe generated in situ by acid induction, and preparation therefor and application thereof. The light-emitting radical cation probe is obtained by oxidation of a compound of formula I in an acidic condition, and has a structure of formula II. A preparation method for the light-emitting radical cation probe is further disclosed. The radical cation probe of the present invention is generated by an in situ reaction in an acidic environment without a seperation, has the advantages of emitting red to near-infrared light, high generation efficiency and good stability, and can be used in fluorescence imaging. The radical cation probe of the present invention can achieve in situ imaging in an acidic stomach environment and gastrointestinal imaging. The probe of the present invention is further used in preparing a probe for monitoring and measuring a food digestion process in a stomach or preparing a reagent for monitoring and measuring treatment of anti-gastric drug that neutralizes gastric acid.

##STR00001##

Compounds

The present disclosure relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or hydrate thereof, ##STR00001## The present disclosure further relates to pharmaceutical compositions comprising a compound of formula (Ia) and methods of treating a disease or disorder (e.g., cancer) by administering a compound of formula (Ia).

Compound, preparation method thereof, and use thereof

The present invention relates to a method for preparing a biomaterial having selectively functionalized tyrosine, a biomaterial having selectively functionalized tyrosine, and a pharmaceutical composition containing the same as an active ingredient. The method for preparing a biomaterial to which a compound represented by formula 2 is coupled, of the present invention, allows the compound represented by formula 2 to be selectively coupled, in a high yield in a biomaterial, to tyrosine, which is present on the surface of an aqueous solution such that the coupling thereof to amino acids other than tyrosine does not occur and, when only one tyrosine is present, heterogeneous mixtures are not present and the inherent activity of the biomaterial is maintained, and thus the compound can be effectively used as a pharmaceutical composition containing a biomaterial drug as an active ingredient. In addition, the method can selectively functionalize tyrosine, and thus can be effectively used for tyrosine functionalization in a biomaterial.

Compound, preparation method thereof, and use thereof

The present invention relates to a method for preparing a biomaterial having selectively functionalized tyrosine, a biomaterial having selectively functionalized tyrosine, and a pharmaceutical composition containing the same as an active ingredient. The method for preparing a biomaterial to which a compound represented by formula 2 is coupled, of the present invention, allows the compound represented by formula 2 to be selectively coupled, in a high yield in a biomaterial, to tyrosine, which is present on the surface of an aqueous solution such that the coupling thereof to amino acids other than tyrosine does not occur and, when only one tyrosine is present, heterogeneous mixtures are not present and the inherent activity of the biomaterial is maintained, and thus the compound can be effectively used as a pharmaceutical composition containing a biomaterial drug as an active ingredient. In addition, the method can selectively functionalize tyrosine, and thus can be effectively used for tyrosine functionalization in a biomaterial.