34303 results about "Medicinal chemistry" patented technology

The present application relates to the technical field of medicines, and relates to a macrocyclic compound containing amide substitution, in particular to a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof in the treatment of disease.

Provided herein are compounds having the following structure (I), wherein the substituents are as defined herein, compositions comprising a compound, and methods for modulating the activity of KRAS G12D.

The present embodiments provide compounds of Formula I, compositions of the compounds, and methods for treating diseases such as cancer.

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).

Provided are a pyrimidine polycyclic derivative inhibitor, a preparation method therefor and the use thereof. In particular, provided are a compound as shown in the general formula, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in the treatment of cancers and other related diseases.

The invention relates to a fused ring compound, a preparation method thereof and application of the fused ring compound in medicine. Specifically, the invention relates to a fused ring compound as shown in a general formula (IN), a preparation method thereof, a pharmaceutical composition containing the compound and application of the fused ring compound as a therapeutic agent, in particular to application of the fused ring compound in preparation of drugs for inhibiting KRAS G12D. Wherein each group in the general formula (IN) is as defined in the specification. # imgabs0 #

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.

The present invention is directed to the compounds of Formula (IV) inhibitors of KRAS(G12D). The inhibitors described herein can be useful in the treatment of diseases or disorders associated with KRAS(G12D), such as Lung cancer, Pancreatic cancer, Colorectal cancer et al. In particular, the invention is concerned with compounds and pharmaceutical compositions inhibiting KRAS(G12D), methods of treating diseases or disorders associated with KRAS(G12D), and methods of synthesizing these compounds.

Provided herein are compounds having the following structure (I), wherein the substituents are as defined herein, compositions comprising a compound, and methods for modulating the activity of KRAS G12D and / or G12V.

The invention relates to compounds of formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a prodrug thereof, a deuterated molecule thereof or a PROTAC molecule thereof that selectively inhibit the activity of K-Ras G12D protein, compositions comprising the same, the methods of using the same and related intermediates.

Drug products adapted for nasal delivery comprising formulations with epinephrine and devices comprising such formulations are provided. Methods of treating anaphylaxis with epinephrine products are also provided.

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.

A tricyclic compound as a VHL ligand, a preparation method therefor, and a use of the compound or a pharmaceutical composition thereof for preventing and / or treating a series of diseases, disorders, and conditions.

The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides Tmax value of less than 30 minutes upon said administration. Other aspects and embodiments are contemplated and described.The invention also provides a pharmaceutical composition for intranasal administration comprising a triptan, a pharmaceutically acceptable vehicle and a mucosal permeation enhancer, wherein upon said administration said composition provides a Tmax substantially equivalent to subcutaneous administration of said triptan. Other aspects and embodiments are contemplated and described.

Disclosed in the present invention are a quinazoline compound, and a pharmaceutical composition thereof and the use thereof. Provided in the present invention is a compound as represented by formula I, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The compounds of the present invention have a good degradation effect on the KRAS protein with a G12D mutation, have a good inhibitory activity against the proliferation of tumor cells with a KRAS G12D mutation, and exhibit good pharmacokinetic properties.

The application provides a process method for preparing (2-(3,6-dimethoxy-9H-carbazol-9-yl)ethyl) phosphonic acid, and particularly relates to the technical field of organic synthesis. The process method is that, under alkaline conditions, a halogenated phosphonate compound is added into a 3,6-dimethoxy-9H-carbazole solution to perform a reaction, hydrochloric acid aqueous solution is added after the reaction to perform acidolysis degreasing, and finally (2-(3,6-dimethoxy-9H-carbazol-9-yl)ethyl) phosphonic acid is obtained through extraction, reflux adsorption and beating purification. The process method uses 3,6-dimethoxy-9H-carbazole as a starting material, realizes the synthesis of the target product through one-pot reaction, has mild reaction conditions, uses non-toxic raw materials which are easy to obtain, has simple synthesis process, is convenient to operate, and has high separation yield.

Disclosed in the present invention are a polycyclic derivative, and a preparation method therefor and the use thereof. In particular, the present invention relates to a compound represented by general formula (I) or a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in the preparation of a drug for treating diseases. The compound has a structure as represented by formula (I).

Disclosed herein are compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C. The compounds have a general Formula (I): or pharmaceutically acceptable salts thereof, wherein the variables of Formula (I) are as defined herein. Also provided herein are pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C disorder.

This disclosure provides methods of treating cystic fibrosis or a CFTR-mediated disease comprising administering Compound I, a deuterated derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. The disclosure also provides pharmaceutical compositions comprising Compound I, a deuterated derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing, and optionally comprising one or more additional CFTR-modulating agents.

The invention relates to a furan ring-containing compound as well as a pharmaceutical composition and application thereof. Specifically disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound provided by the invention has one or more of the following advantages: (1) the structure is novel; (2) the compound has a good retarding effect (inhibiting effect) on the activity of a Nav1.8 channel; and (3) the compound has good selectivity to other subtypes of Nav and is high in safety. # imgabs0 #

The present disclosure relates generally to compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

The invention relates to a fused ring compound, a preparation method thereof and application of the fused ring compound in medicine. Specifically, the invention relates to a fused ring compound as shown in a general formula (IN), a preparation method thereof, a pharmaceutical composition containing the compound and application of the fused ring compound as a therapeutic agent, in particular to application of the fused ring compound in preparation of drugs for inhibiting KRAS G12D. Wherein each group in the general formula (IN) is as defined in the specification. # imgabs0 #

Described herein are GLP-1R agonists and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of a GLP-1 associated disease or disorder, including Type 2 diabetes or obesity.

Compositions for inducing and maintaining a state of flow in a subject include optically pure S-beta-hydroxybutyrate or non-racemic mixtures enriched with the S-enantiomer. The S-beta-hydroxybutyrate enantiomer modulates the effect of ketone bodies in the subject and controls the rate at which ketosis is achieved. Beta-hydroxybutyric acid is more rapidly absorbed and utilized by the body than salts or esters, enhances taste, and reduces the need to include citric acid or other edible acids. Beta-hydroxybutyrate salts are more slowly absorbed and utilized by the body and can provide one or more electrolytes. Compositions for controlling ketone body level in a subject may contain a dietetically or pharmaceutically acceptable carrier and optically pure S-beta-hydroxybutyrate or non-racemic mixture enriched with S-beta-hydroxybutyrate, wherein the compositions contain from about 50.5% to 100% by enantiomeric equivalents of S-beta-hydroxybutyrate and from about 49.5% to 0% by enantiomeric equivalents of R-beta-hydroxybutyrate.

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

Herbicidally active 3-phenylisoxazoline-5-carboxamides of cyclopentenylcarboxylic acid derivativesThe invention relates to 3-phenylisoxazoline-5-carboxamides of cyclopentenylcarboxylic acid derivatives of the general formula (I) and their agrochemically acceptable saltsand to their use in the crop protection sector.