5 results about "Druggability" patented technology

This invention relates to the field of chelating drug research, specifically to chelating ligand compounds, targeted chelating ligands and their complexes and applications. Compared with the prior art, the targeted molecule linking sites and linking methods disclosed in this invention have better targeting and in vivo stability. At the same time, the design of the targeted molecule linking sites in this invention can improve in vivo metabolism and distribution, thereby improving the druggability of preferred compounds and providing a better foundation for the clinical application of therapeutic radiopharmaceuticals.

The present application provides a compound or a pharmaceutically acceptable salt, ester, or solvate thereof. The compound provided in the present application has a structure represented by the following formula (I), wherein ring A is a benzene ring or a 5- or 6-membered heteroaromatic ring. Compared with a dual-motif CAIX inhibitor XYIMSR, the compound of formula (I) or the pharmaceutically acceptable salt, ester, or solvate thereof provided in the present application has relatively strong affinity for CAIX and a relatively small molecular volume. On the basis of the small-molecule structure, when the compound is used as a carrier for a radiopharmaceutical, the obtained small-molecule radiopharmaceutical has excellent pharmacokinetic properties and druggability, thereby providing a solution for clinical application.

The present invention belongs to the field of biomedicine. Provided are a bispecific antibody and the use thereof. The bispecific antibody contains a first antigen-binding domain targeting PD-L1 and a second antigen-binding domain targeting 4-1BB. The antibody retains the activity of an anti-PD-L1 antibody, achieves a balance between activity and safety, and has an excellent druggability potential.

Disclosed are compounds represented by formula (1), or their tautomers, meso compounds, racemic compounds, enantiomers, diastereomers, mixtures thereof, or pharmaceutically acceptable salts, prodrugs, or solvates thereof. The structure of formula (1) is shown below. By introducing strongly hydrophilic sulfonic acid inner salts and / or phosphate inner salt side chains at the polypeptide (VC, VA, AAA, etc.)-PAB (self-destructing group) position of the linker, the compounds significantly improve the druggability (including hydrophilicity and stability) of the antibody-drug conjugates corresponding to the compounds, reduce drug clearance in the body, and enhance tumor therapeutic effects. JPEG2026523005000202.jpg3882