75 results about "Mutant RAS" patented technology

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The present disclosure provides quinazoline- and azaquinazoline-based compounds and pharmaceutically acceptable salts thereof, and methods of using the same as modifiers of mutant Ras protein. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic protein.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

Disclosed are RAS(ON) multi-selective inhibitor compositions and methods of treating RAS protein-related diseases or disorders using an intermittent dosing regimen. RAS(ON) multi-selective inhibitors having tight binding to cyclophilin A (CypA) result in high exposure levels, prolonged tissue retention, and / or slow clearance rates, thereby increasing the risk of inhibition of wild-type RAS in normal tissues. Accordingly, provided herein are methods for the safe and effective dosing of low KD1 RAS(ON) multi-selective inhibitors using an intermittent dosing regimen. Also provided are methods of selecting or identifying such RAS(ON) multi-selective inhibitors suitable for intermittent administration.

The present disclosure provides compounds and their methods of use. In particular, the compounds of the present disclosure may be useful for inhibiting RAS proteins, such as KRAS proteins. The disclosed compound may be used in the treatment of cancer and be highly selective for KRAS proteins having the G12D mutation. Alternatively or additionally, said compounds may have broad spectrum activity across a range of KRAS proteins.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The present invention encompasses compounds of the formula (I), wherein R1, R2.a, R2.b, R3.a, R3.b, R4.a, R4.b, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, Rx, n and Q have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments / medical uses, especially as agents for treatment and / or prevention of oncological diseases.

The present disclosure generally relates to quick release pharmaceutical dose unit tablets containing small molecule API drugs. In some examples, the API is an inhibitor of Ras proteins, such as K-Ras, H-Ras, and N-Ras, with a G12C mutation. The tablet also contains a disintegrating agent and an excipient. More specifically, the present disclosure relates to pharmaceutical dosage unit tablets containing divariclisib or a pharmaceutically acceptable salt thereof, an ex-particulate disintegrant, and an ex-particulate excipient, as well as a method for preparing the tablets from particles formed by dry granulation.

The present application relates to compounds of formula (A) that inhibit the growth of cancers that express G12D mutant Ras proteins. The molecules of the specification are thus indicated for use in the treatment of cancer that express G12D mutant Ras protein.

The invention discloses an additive for resisting cow ovarian aging and its application. The additive is made of a composition of anthocyanidins, glycyrrhizic acid and wolfberry glycopeptide. When the composition is used in clinical veterinary treatment of cow ovarian aging, the role of primary cow ovarian granulosa cells is clarified through transcription, which is mainly involved in regulating programmed cell death, Ras protein signal transduction, tissue development, cell serine, tryptophan kinase activity, MAPK signaling pathway, PI3K-AKT signaling pathway, and laser confocal results show that the composition can significantly reduce the production of mitochondrial reactive oxygen; at the same time, the therapeutic effect on the persistent corpus luteum of the main cow is achieved by improving the intestinal flora structure, and more specifically, the colony is significantly changed upstream at the genus and species level; B-ultrasound results reveal that for a persistent corpus luteum cow, more large follicles can be detected on the ovaries after one month of gavage with the additive composition.

The present invention relates to a compound that may be useful for inhibiting RAS protein. More specifically, the present invention relates to a compound for inhibiting broad-spectrum KRAS mutant protein. Therefore, the compound of the present invention can be used to treat conditions mediated by KRAS protein. For example, the compound can be used to treat cancer.

The present invention is based on the discovery of extracellular accessible Ras proteins on cancer cells. The present invention provides an antigen binding protein (ABP), such as an antibody or chimeric antigen receptor (CAR), where the ABP comprises at least one first antigen binding domain capable of binding to an extracellular Ras antigen. Further provided are isolated nucleic acids and expression constructs for expressing the ABP of the invention, as well as recombinant host cells expressing the ABP of the invention. The invention also relates to a pharmaceutical composition, a pharmaceutical combination, a compound for medicine and a compound for diagnosing, preventing and / or treating cancer. Finally, the present invention relates to a combination of the ABP, CAR, isolated nucleic acid, expression construct, recombinant host cell or pharmaceutical composition as defined herein with a chemical compound, such as a cerebron (CRBN) inhibitor or a polar organic solvent, such as DMSO, for a method of diagnosis, prevention and / or treatment of cancer.

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 disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

A biomarker composition for predicting susceptibility to a therapeutic agent for neurofibromatosis by using Ras activity; and a pharmaceutical composition for preventing or treating neurofibromatosis, including a Ras activity inhibitor. The biomarker composition can accurately diagnose susceptibility to a therapeutic agent for neurofibromatosis by measuring the expression levels of a GTP-bound and activated Ras (Ras-GTP) protein and an activated p-ERK protein or a gene encoding the same in a biological sample of an individual. The pharmaceutical composition inhibits the activity of Ras proteins, and thus can be effectively used for the prevention or treatment of neurofibromatosis in which the activity of the Ras proteins is increased.