8 results about "RAS Mutation" patented technology

The present invention discloses nitrogen-containing macrocyclic compounds, pharmaceutical composition and use thereof. The present invention provides a compound represented by formula 0, a solvate, a pharmaceutically acceptable salt thereof or a solvate of the pharmaceutically acceptable salt thereof. The compounds of the present disclosure are orally bioavailable pan-RAS inhibitors which can target a wider range of RAS mutations than traditional mutant-selective RAS inhibitors, and have high exposure, long half-life and good pharmacokinetic properties, may be useful for the treatment of RAS-driven cancers and effective in patients who have not responded to other therapies.

The invention relates to a PI4K inhibitor and application thereof, in particular to application in blocking or inhibiting autophagy caused by RAS mutation or treating RAS mutation tumors. In addition, the invention discloses that the mechanism of the autophagy caused by RAS mutation is completely different from that of the existing starvation-induced autophagy, the pathway of the autophagy caused by RAS mutation is P38-ULK1-PI4KB-WIPI2, especially S256 and T263 sites of P14KB phosphorylated by ULK1, and experiments prove that the specificity of the pathway can be used as a diagnostic marker and a therapeutic target of tumors.

The present disclosure relates to an antibody-drug conjugate, and in particular, to an antibody-drug conjugate (ADC) loaded with an Ras mutation inhibitor, a composition comprising the ADC molecule, and therapeutic use thereof.

The present invention relates to an antibody-drug conjugate, and in particular, to an antibody-drug conjugate (ADC) carrying a Ras mutation inhibitor, a composition comprising the ADC molecule, and therapeutic use thereof.

A PI4K inhibitor and use thereof, especially use in blocking or inhibiting autophagy caused by RAS mutations or treating tumors associated with RAS mutations. In addition, the present invention reveals that autophagy caused by RAS mutations is completely different in mechanism from existing starvation-induced autophagy. The pathway of autophagy caused by RAS mutations is P38-ULK1-PI4KB-WIPI2, especially the S256 and T263 sites of ULK1 phosphorylated PI4KB. It has been experimentally confirmed that the specificity of the pathway can be used as a diagnostic marker and a therapeutic target of tumors.

This disclosure relates to antibody-drug conjugates, and more specifically to antibody-drug conjugates (ADCs) carrying Ras mutation inhibitors, compositions containing said ADC molecules, and their therapeutic applications.

This invention discloses nitrogen-containing macrocyclic compounds, pharmaceutical compositions thereof, and uses. The invention provides compounds represented by Formula 0, their solvates, pharmaceutically acceptable salts thereof, or solvates of pharmaceutically acceptable salts thereof. The disclosed compounds are pan-RAS inhibitors with oral bioavailability, targeting a wider range of RAS mutations compared to conventional mutation-selective RAS inhibitors. They exhibit high exposure, long half-life, and favorable pharmacokinetic properties, and can be used to treat RAS-driven cancers, showing efficacy in patients unresponsive to other therapies.

This invention provides cyclic compounds effective against RAS-mutated cancers, as well as non-natural amino acids and peptide compounds useful for their production, particularly peptide compounds that exhibit sufficiently selective KRAS inhibitory activity against HRAS and NRAS. [Solution] The present invention provides a cyclic compound having a specific amino acid sequence that interacts with and selectively inhibits amino acid residues specific to KRAS, or a salt thereof, or a solvate thereof. The pharmacological effect of the cyclic compound is to inhibit the proliferation of tumor cells having RAS mutations.