72 results about "Ras Inhibitor" patented technology

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.

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.

Disclosed herein are compounds, and salts thereof, which inhibit targeted Ras mutants, pharmaceutical formulations, and methods of treatment of NRAS-, KRAS, or HRAS-mediated diseases, such as certain cancers.

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 present invention relates to crystalline forms of RAS inhibitors, compositions containing the same, and methods of using the same. The present disclosure features crystalline forms of Ras inhibitors, pharmaceutical compositions thereof, and uses thereof in the treatment of cancer.

Combinations, compositions and uses of a cyclin dependent kinase 2 (CDK2) inhibitor INX-315, or a pharmaceutically acceptable salt thereof described herein, in combination with a CDK4 / 6 inhibitor for the treatment of disorders characterized by mutation of Kirsten rat sarcoma (KRAS), including but not limited to the treatment of tumors and cancers. In addition, the invention includes a method to delay acquired resistance to a RAS inhibitors in a KRAS mutant cancer, comprising administering the CDK2 inhibitor INX-315 optionally in combination or alternation with a KRAS inhibitor.

This disclosure provides compounds of Formula (I) or (II) (e.g., Formula (II-a), (Il-b), or (II-c)), or pharmaceutically acceptable salts thereof, that inhibit a Ras GTPase (e.g., a KRas, NRas, and / or HRas GTPase). In some embodiments, the Ras protein is a dysregulated Ras protein that has a mutation (referred to herein as a mutant Ras protein). These compounds are useful, for example, for treating a disease, disorder, or condition in which increased and / or sustained (e.g., excessive) Ras activation, such as Ras activation associated with a mutant Ras protein, contributes to the pathology and / or symptoms and / or progression of the disease, disorder, or condition (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing compounds of Formula (I) or (II) (e.g., Formula (II-a), (Il-b), or (II- c)), or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

The invention relates to a compound with a pan-RAS inhibition effect as shown in a formula (A), or an isotope derivative, a stereoisomer or pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing the compound, and the use of the compound of formula (A) for the prevention and / or treatment of cancer, tumors, inflammatory diseases, autoimmune diseases or immune-mediated diseases.

The present application relates to a broad-spectrum RAS inhibitor having a macrocyclic structure as represented by formula (I). Specifically, the present invention relates to a compound as represented by formula (I), a preparation method therefor, and a pharmaceutical composition thereof, and further relates to the use of the compound and pharmaceutical composition thereof in the preparation of a drug for treating KRAS protein-related diseases, for example, for treating cancer.

Provided are compounds, or pharmaceutically acceptable salts thereof, capable of regulating biological processes involving Ras, alone or in combination with other therapeutic agents, pharmaceutical compositions, and protein conjugates thereof.SOLUTION: Provided is a compound having the structure of Formula I: A-L-B (Formula I) or a pharmaceutically acceptable salt thereof, wherein A is a Ras binding moiety, L is a linker, and B is a selective crosslinking group, wherein when the compound, or pharmaceutically acceptable salt thereof, is contacted with a sample containing a Ras protein, at least 20% of the Ras protein in the sample covalently reacts with the compound, or pharmaceutically acceptable salt thereof, to form a conjugate.SELECTED DRAWING: None

The present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a RAS inhibitor and other therapeutic agents.

Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as cancer.

The present disclosure features macrocyclic compounds capable of inhibiting Ras proteins, as well as pharmaceutical compositions and protein complexes thereof, and their use in the treatment of cancer.