82472 results about "Pharmaceutical Substances" patented technology

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

KRAS mutation inhibitors and pharmaceutical compositions comprising said inhibitors are useful for the treatment of a disease or disorder associated with KRAS mutation.

Compounds shown as formula (I) or stereoisomers thereof, or pharmaceutically acceptable salts, solvates or prodrugs thereof, a pharmaceutical composition comprising same, and the use of same in the preparation of drugs for preventing and / or treating diseases or disorders related to RAS protein activity, such as cancer.

The present invention encompasses compounds of formula (I), wherein R1a, R1b, R2a, R2b, Z, R3 to R5, ring A, ring B, p, q, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, 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.

Provided are a compound having the structure represented by formula (I) and capable of being used as a KRAS inhibitor, a pharmaceutical composition comprising the compound, a method for preparing the compound, and a use of the compound in treatment of cancer.

Compounds or their pharmaceutically acceptable salts can modulate the G12D mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

The present disclosure relates to a fused heteroaryl compound, a preparation method therefor, and a use thereof in medicine. Specifically, the present disclosure relates to a fused heteroaryl compound represented by general formula (I'), a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof as a therapeutic agent, especially a use thereof in the preparation of a medicament for inhibiting KRAS amplification and / or mutant activity. Each group in general formula (I') is as defined in the description.

Dosage forms, drug delivery systems, and methods related to immediate or sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Provided are novel compounds useful as inhibitors of KRAS, in particular KRAS G12D and / or other KRAS G12 mutants, as well as pharmaceutical compositions comprising these compounds and methods of treatment by administration of these compounds or the pharmaceutical compositions.

Provided herein are compounds, and pharmaceutically acceptable salts thereof, useful as KRAS inhibitors, methods of making and using the same (singly or in combination with additional agents), and pharmaceutical compositions thereof.

Provided herein are compounds, and pharmaceutically acceptable salts thereof, useful as KRAS inhibitors, methods of making and using the same (singly or in combination with additional agents), and pharmaceutical compositions thereof.

The present invention relates to a compound of formula (I), or a stereoisomer, a tautomer, a deuterated compound or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof as a drug for treating and / or preventing KRAS-mediated diseases.

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Disclosed is a nitrogen-containing heterocyclic compound, pharmaceutical composition thereof and application thereof. The present disclosure provides a nitrogen-containing heterocyclic compound of formula I, a pharmaceutically acceptable salt thereof, a prodrug thereof, a stereoisomer thereof, a tautomer thereof or an isotopically labeled compound thereof. The nitrogen-containing heterocyclic compounds as represented in Formula I in the present disclosure have good inhibitory effects on cells of various mutations such as KRAS G12C, KRAS G12D, KRAS G12V, KRAS Q61H and other mutations, as well as on KRAS-amplified wild-type cells, and are expected to treat and / or prevent a wide range of diseases associated with Ras.

The present invention covers spirocyclic compounds of general formula (I), in which R1, R2, X, Y, and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant KRAS signaling, as a sole agent or in combination with other active ingredients.

A benzo nitrogen-containing heterocyclic derivative regulator, a preparation method therefor and a use thereof. Particularly, the present invention relates to a compound represented by general formula (XIX), a preparation method therefor, a pharmaceutical composition containing the compound, and a use of the compound as a regulator in the preparation of drugs for treating metabolic diseases and related diseases, wherein each substituent in the general formula (XIX) is the same as the definition in the description.

There is provided herein a compound of formula (I) wherein R1, R2, R3, R4, A, X1, Y, L, Z, R5, R6a, R6b, W and R7 are as defined herein, for use in the treatment of colorectal and / or lung cancer.

A compound as represented by formula I-1, a stereoisomer or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing same, and the use thereof as a PARP-1 inhibitor in the preparation of a drug for treating related diseases. Each group in formula I-1 is as defined in the description.

Provided herein are compounds, such as compounds of Formula (I), Formula (l-A), Formula (l-AA), or Formula (l-BB), or pharmaceutically acceptable salts of any one thereof, useful for modulating KRAS GD12 and / or other G12 mutants.

A fused ring compound, a pharmaceutical composition comprising same, and the use thereof. The compound has a structure as represented by formula (I), or is a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer or a mixture form thereof, a metabolite, a metabolic precursor, an isotope-substituted form, a pharmaceutically acceptable salt, a hydrate, a solvate, a polymorph or a co-crystal thereof. The compound can be used for treating one or more cancers caused by KRAS mutation.

The present invention discloses substituted 2-amino-9-(3,3-difluoropiperidin-4-yl)-7,9-dihydro-8H-purin-8-one compounds compounds having the structural formula represented by formula (I)： The substituted 2-amino-9-(3,3-difluoropiperidin-4-yl)-7,9-dihydro-8H-purin-8-one compounds, derivatives and pharmaceutically acceptable salts thereof of the present invention are capable of acting as a drug characteristic of a protein kinase inhibitor, in particular for the expression of a protein through a DNA-dependent protein kinase (DNA-PK) and can be used to treat or prevent disorders associated with abnormal protein kinase activity, such as cancer, cancer with brain metastases, cancer with meningeal metastases, glioma, glioblastoma, DIPG, and the like either as monotherapy or combination with other treatments, such as radiation therapy or chemotherapy.

The invention relates to the technical field of medicines, and provides a use of a heterocyclic anti-tumor compound, in particular a use of the heterocyclic anti-tumor compound in the preparation of a medicine for preventing and / or treating tumors or cancers. The compound has a tri-heterocyclic structure (for example, a structure as shown in formula (B)), has a novel structure, and provides a new direction for the development of SOS1 inhibitor drugs.

A pyrimido-pyridine compound, a pharmaceutical composition thereof and the use thereof. The compound and the pharmaceutical composition thereof as KRAS G12D inhibitors can be used for preparing a drug for preventing or treating KRAS G12D-related diseases, and can be particularly used for preparing a drug for preventing or treating cancers.

Compounds are provided which can inhibit KRAS G12D. Also provided are pharmaceutical compositions and medical uses of the same, including the use in treating or preventing conditions such as cancers.

Provided herein are compounds, such as compounds of Formula (I), Formula (l-A), Formula (l-AA), or Formula (l-BB), or pharmaceutically acceptable salts of any one thereof, useful for modulating KRAS GD12 and / or other G12 mutants. (I)

The present invention relates to crystalline forms of salts of the KRas G12C inhibitor 2-[(2b)-4- [7-(8-chloro-1-naphthyl)-2-[[(25)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H -pyrido [3,4- d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile, pharmaceutical compositions comprising the crystalline forms, processes for preparing the crystalline forms and methods of use thereof.

A compound having the following structure of Formula (I): (I) or a stereoisomer of the compound, tautomer of the compound, pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, A, X, Z, and Y are as defined herein. Pharmaceutical composition comprising the compounds, and their use in methods of treating diseases are also described.

Provided herein is a method or a use for treating a cancer, comprising administering to a subject a therapeutically effective amount of Compound A, a pharmaceutically acceptable salt, or a co-crystal thereof at a daily dose of 100 mg to 3600 mg on salt-free basis, wherein Compound A has the following structure:

The present invention provides substituted tricyclic compound of formula (I), which are therapeutically useful as KRAS degraders. These compounds are useful in the treatment and / or prevention of diseases or disorders dependent upon KRAS. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt or a stereoisomer or a tautomer thereof thereof.