106 results about "Ras Inhibitor" patented technology

The disclosure provides compounds, e.g., compounds of Formula I, and their use in treating medical diseases or disorders, such as cancer. The compounds are contemplated to be modulators of Ras (e.g., K-Ras).

Related to macrocyclic compounds and therapeutic uses thereof. Disclosed a compound of formula (I), or a pharmaceutically acceptable salt thereof, a solvate thereof or a solvate of the pharmaceutically acceptable salt, and their use for the preparation of a medicament of treatment of cancer. Provided herein are useful compounds for the inhibition of RAS mutant and the compound shows good inhibitory activity against RAS.

This disclosure provides cyclic peptide compounds of formula (A) or formula (II) as inhibitors of Ras kinase, and compositions and use of the same in treating diseases associated with Ras kinase.

The present invention relates to a compound as shown in formula (A) having a pan-RAS inhibitory effect, or an isotopic derivative or stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound, and the use of the compound of formula (A) in the prevention and / or treatment of cancers, tumors, inflammatory diseases, autoimmune diseases or immune-mediated diseases.

The present invention provides macrocyclic compounds, the use thereof for selectively inhibiting the activity of RAS mutants, and pharmaceutical compositions comprising the compounds, e.g., for treatment of various diseases including cancer.

Provided are a compound represented by formula (I) and a pharmaceutical composition comprising the compound, and a use of a compound of formula (A) for preventing and / or treating cancer, tumor, inflammatory disease, autoimmune disease, or immune-mediated disease.

The present disclosure relates to a polycyclic compound, a preparation method therefor, and the pharmaceutical use thereof. Specifically, the present disclosure relates to a polycyclic compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof as a therapeutic agent, in particular, the use as an RAS inhibitor and the use in the preparation of a drug for treating and / or preventing RAS-mediated or dependent diseases or conditions, wherein each group in general formula (I) is as defined in the description.

Provided are a fused tricyclic compound, a preparation method therefor and a pharmaceutical use thereof. Specifically, provided are a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, particularly a use as an RAS inhibitor and a use in the preparation of a drug for treating and / or preventing RAS-mediated or RAS-dependent diseases or disorders. The groups in general formula (I) are as defined in the description.

Lung cancer is the leading cause of cancer deaths worldwide. Metastatic non-small-cell lung cancer (NSCLC) has recently benefited from two consecutive breakthroughs: the identification of oncogene drivers, such as KRAS mutations, leading to the development of targeted therapies, and the understanding of the cancer immunity cycle leading to the development of immune checkpoint inhibitors. KRASG12C mutations can be found in approximately 13% of patients with non-small-cell lung cancer (NSCLC) and historically have been associated with a poor prognosis. Now, data from a phase II trial demonstrate the efficacy of the novel KRASG12C-specific inhibitor sotorasib for patients with advanced-stage NSCLC harbouring this alteration with disease progression on at least one standard-of-care therapy. However one could expect that resistance to Ras inhibitors could occur and that there is a need for identifying new therapeutic avenues for limiting said resistance. The inventors now show that when use alone, sotorasib and tipifarnib did not show a significant anti-tumor effect on lung cancer cells harboring the G12C KRAS mutation, whereas the combination potently induced cell death, suggesting a synergism between these drugs. The present invention thus relates to the combination of Ras inhibitors and famesyltransferase inhibitors for the treatment of cancers.

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as a medicament, in particular for use in treating proliferative disorders, inflammatory diseases and / or genetic disorders. The present invention relates further to a pharmaceutical composition comprising the compounds of formula (I). Moreover, the present invention relates to a method of inhibiting growth, proliferation or metastasis of cancer cells in a subject in need thereof, in particular which may encompass subsets of patients defined by their mutational status of the RAS oncogene or patients who might have developed resistance to the standard of care or treatment with RAS mutation specific inhibitors. The present invention also relates to a method of inhibiting RAS molecules in treating genetic disorders like RASopathies or inflammatory disorders like Adenomyosis where KRAS gene is mutationally activated. In addition, the present invention relates to a method of inhibiting proliferation and or secretion of factors from a cell population sensitive towards inhibiting RAS activation in vitro, in particular sensitive towards inhibiting KRAS. HRAS and NRAS activation in vitro. Furthermore, the present invention relates to a kit containing a formulation comprising a pharmaceutical composition comprising a compound of formula (I).

The invention discloses an application of mRNA (messenger Ribonucleic Acid) for coding p16 protein in preparation of a medicine for treating pancreatic cancer. The mRNA for coding the p16 protein comprises a nucleic acid sequence as shown in SEQ ID NO.1-3. The invention also provides an application of the mRNA for coding the p16 protein and a universal RAS inhibitor daraxonrasib in the preparation of a medicine for treating pancreatic cancer in combination with the mRNA for coding the p16 protein and the universal RAS inhibitor daraxonrasib. Further, the mRNA encoding the p16 protein can be entrapped in a lipid nanoparticle. Experiments show that the function of CDKN2A is recovered by delivering p16 mRNA, the sensitivity of pancreatic cancer cells to the daraxonrasib can be enhanced, the drug resistance of the daraxonrasib can be reversed, and a remarkable synergistic anti-tumor effect is shown in various pancreatic cancer mouse models. The invention provides a new combined treatment strategy for the treatment of pancreatic cancer, especially pancreatic ductal adenocarcinoma.

This disclosure features the crystalline forms of Ras inhibitors, their pharmaceutical compositions, and their use in the treatment of cancer.

The present disclosure provides compounds of Formula (Vc) and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of uses as therapeutic, diagnostic and research tools. In particular, the subject compositions and methods are used to reduce signal transduction output of oncogenic proteins.

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as a medicament, in particular for use in treating proliferative disorders, inflammatory diseases and / or genetic disorders. The present invention relates further to a pharmaceutical composition comprising the compounds of formula (I). Moreover, the present invention relates to a method of inhibiting growth, proliferation or metastasis of cancer cells in a subject in need thereof, in particular which may encompass subsets of patients defined by their mutational status of the RAS oncogene or patients who might have developed resistance to the standard of care or treatment with RAS mutation specific inhibitors. The present invention also relates to a method of inhibiting RAS molecules in treating genetic disorders like RASopathies or inflammatory disorders like Adenomyosis where KRAS gene is mutationally activated. In addition, the present invention relates to a method of inhibiting proliferation and / or secretion of factors from a cell population sensitive towards inhibiting RAS activation in vitro, in particular sensitive towards inhibiting KRAS, HRAS and NRAS activation in vitro. Furthermore, the present invention relates to a kit containing a formulation comprising a pharmaceutical composition comprising a compound of formula (I).

The present disclosure provides macrocyclic compounds capable of inhibiting Ras proteins, as well as pharmaceutical compositions and protein complexes thereof, and their use in the treatment of cancer. The present invention relates to RAS inhibitors.