1597 results about "Tautomer" patented technology

A spiro compound, and a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite, or prodrug thereof, a pharmaceutical composition comprising the compound, a preparation method therefor, and a use thereof in preparation of a drug for preventing or treating KRAS-mediated related diseases.

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

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, isotopic variant, tautomer or stereoisomer thereof as a KRAS mutant inhibitor. The present invention also provides a pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt, isotopic variant, tautomer or stereoisomer thereof, and a use in treating cancer.

Compounds are provided having the following structure:or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein a, b, c, d, G1, G2, L1, L2, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8 and X are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, nanoparticles comprising the compounds and methods for their use and preparation are also provided.

Provided in the present invention is a compound of formula (X), or an isotopic variant, a tautomer or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as a KRAS mutant inhibitor. Further provided in the present invention are a pharmaceutical composition containing the compound, or the isotopic variant, the tautomer or the stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and the use thereof in the treatment of cancers.

The invention discloses a nitrogen-containing fused ring compound as well as a preparation method and application thereof, and particularly relates to a nitrogen-containing fused ring compound as shown in a general formula I, or pharmaceutically acceptable salt thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof, and a preparation method and application thereof in pharmacy, and particularly relates to a nitrogen-containing fused ring compound as shown in a general formula I, or pharmaceutically acceptable salts thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof. Wherein the definition of each group is described in the specification. # imgabs0 #

The present invention provides a compound as an APJ receptor agonist. The compound is a compound represented by formula (I), or an isotopic variant, tautomer, stereoisomer or pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition comprising the compound, and a use thereof in the treatment or prevention of diseases associated with APJ.

Compounds having the structure of Formula (I): or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof; wherein R1, R2, R3, R4, R5, L1, L2, a and z are as defined herein, are disclosed. Use of these compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds, and methods for their use and preparation are also provided.

The invention provides a benzofuranone compound as well as a pharmaceutical composition and application thereof, and relates to the technical field of medicines. The benzofuranone compound is a compound as shown in a formula I, a stereoisomer thereof, a tautomer thereof, a crystalline hydrate thereof, a solvate thereof, a prodrug thereof or a pharmaceutically acceptable salt thereof. The benzofuranone compound and the pharmaceutical composition and the pharmaceutical preparation prepared from the benzofuranone compound can prevent or treat organ injury diseases, and have good treatment effects in kidney injury, liver injury, lung injury, brain injury and heart injury.

The invention discloses a nitrogen-containing heterocyclic ring compound as well as a preparation method and application thereof, and particularly relates to a nitrogen-containing heterocyclic ring compound as shown in a general formula (I), or pharmaceutically acceptable salts thereof, or enantiomers, diastereoisomers, tautomers, torsion isomers, solvates, polymorphic substances or prodrugs thereof, and a preparation method and pharmaceutical application thereof. Wherein the definition of each group is described in the specification. # imgabs0 #

Provided in the present invention are compounds as VAV1 degradation agents and the use thereof. Specifically provided are compounds represented by formula (II), and tautomers, stereoisomers, pharmaceutically acceptable salts or prodrugs thereof. The compounds provided by the present invention have good efficacy, and can be used for preparing drugs for treating or preventing VAV1-related diseases.

The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.

The invention discloses a compound as shown in a formula (I), and / or pharmaceutically acceptable salts thereof, and / or a raceme mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and belongs to the technical field of medicines. The invention also discloses a pharmaceutical composition containing the compound as shown in the formula (I), and the compound as shown in the formula (I) and / or a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and / or the pharmaceutical composition, a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof. The invention further discloses application of the cGAS agonist in preparation of the cGAS agonist and a medicament for treating diseases responding to activation of the cGAS-STING signal channel.

The present invention provides a compound of formula (I) as a WRN inhibitor, a compound or a pharmaceutically acceptable salt, isotope variant, tautomer or stereoisomer thereof. The invention also provides a pharmaceutical composition comprising the compound, and its use in the treatment of cancer.

The invention relates to a benzopyrimidine derivative and application thereof in medicine, in particular to a compound shown in a general formula (I) or a stereoisomer, a racemate, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, an intermediate of the compound and application of the compound to inhibition or degradation of KRAS related diseases such as cancers. And B-L-K (I).

Formula (I): JPEG2025536322000043.jpg74140 (in the formula, L, R 1 , R 2 , R 3 and W is as defined in the specification. and their enantiomers, diastereomers, racemates, tautomers, prodrugs, hydrates, solvates and pharmaceutically acceptable salts are useful in the treatment of diseases and conditions affected by the inhibition of Mer kinase, such as cancer.

Compounds of formula I (Formula I),where the substituents R1 through R5 are defined herein, and agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of the compounds of Formula (I). In addition, methods and uses of compounds of Formula I as, for example, insecticides. Compositions having compounds of Formula (I) and their uses in controlling insects, particularly in crops of useful plants. Methods and intermediates related to the synthesis of compounds of Formula (I).

The invention discloses a quinazolinone compound as well as a preparation method, a pharmaceutical composition and application thereof, and relates to the technical field of pharmaceutical chemistry. In particular to a quinazolinone compound as shown in a formula I or pharmaceutically acceptable salt, prodrug, stereoisomer, diastereoisomer, enantiomer, tautomer, solvate, salt of solvate, polymorphic substance and isotope labeled compound of the quinazolinone compound. The quinazolinone compound designed and synthesized by the invention can effectively inhibit TAK1 protein activity, achieves an excellent curative effect at a molecular level, and can be applied to preparation of medicines for treating and / or preventing inflammation, chronic fibrosis diseases, hyperproliferative diseases and cardiovascular diseases.

The invention provides an m-diamide compound as well as a preparation method and application thereof. The m-diamide compound is a compound represented by a formula I, or a stereoisomer, a tautomer, an isotope derivative and a pesticide acceptable salt thereof. The m-diamide compound disclosed by the invention has high insecticidal activity, still has a good insecticidal effect under a low dosage, and is more beneficial to environmental protection; moreover, the insecticidal composition has excellent persistence and quick-acting property on killing pests, and does not easily generate cross resistance with existing m-diamide compounds; the plant safety is realized.

The invention relates to a pyrrolo [2, 3-d] pyrimidine-4-amine derivative and application thereof in medicine, in particular to a compound shown in a formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, and application of the compound in preparation of medicines for treating sGC-related diseases.

Provided are covalent organic frameworks (COFs). Also provided are methods of making the COFs and methods of using the COFs. The COF sheets define a plurality of pores, and stack in an eclipsed configuration to form sheets that assemble to form nanoparticles. Each COF sheet may be a co-condensate of p-phenylenediamine (PA) and (i) triformylbenzene (TFB) and triformylphloroglucinol (TP) or (ii) triformylphloroglucinol (TP). A COF of the present disclosure has the following structure: Formula (I) and / or Formula II where each X2 is Formula (III) where earch X1 is Formula (IV) Formula (V) Formula (VI) Formula (VII) Formula (VIII) Formula (IX) Formula (X) Formula (XI) Formula (XII) Formula (XIII) or any tautomer thereof, where at least one X1 is not Formula (XIV).

An aqueous pharmaceutical composition including compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[({2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl}amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclododecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

A method of selectively inhibiting pathogenic microbes includes: providing an antimicrobial compound that is functional having a structure of Formula 1, or derivative thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combination thereof; and contacting a microbe with the compound such that the microbe is selectively inhibited;

Disclosed herein are compounds used as inhibitors of KAT6 and pharmaceutical compositions comprising the compounds. Also disclosed are methods for treating a disorder or disease responsive to the inhibition of KAT6 activity in a subject. In an embodiment, the compounds are of formula (I) or a pharmaceutically acceptable salt thereof, or a deuterated analog thereof, or an N-oxide thereof, or a tautomer thereof, wherein values for the variables (e.g., ring B, A', A2, A3, A4, A5, Xl, L, R62, R63, R64, R7, and n) are disclosed herein.

The invention provides a compound as shown in a formula (I), and a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. As a GLP-1R agonist, the compound and the pharmaceutical composition thereof can be used for preparing drugs for treating and / or preventing diseases mediated by GLP-1R. # imgabs0 #

The invention discloses a compound which is a compound as shown in a formula (I) or a stereoisomer, a tautomer, a solvate and a pharmaceutically acceptable salt of the compound as shown in the formula (I). As a liposome, the compound provided by the invention has high transfection efficiency, and especially can be used for delivering nucleic acid molecules (such as siRNA, mRNA and pDNA) to regulate expression of protein, or delivering CRISPR gene editing tools to realize knockout or repair of lesion genes.

Disclosed in the present application are a compound as represented by formula (I), a pharmaceutically acceptable salt, a stereoisomer, a tautomer, or an N-oxide, and the use thereof in the preparation of a drug for treating, preventing or alleviating voltage-gated sodium ion channel-related diseases.

The present invention relates to the technical field of medicine. Specifically, the present invention relates to a KRAS inhibitor compound, a pharmaceutical composition thereof, and a use thereof. Specifically, the present invention relates to a compound as represented by formula (I), or a stereoisomer, tautomer, nitrogen oxide, solvate, metabolite, pharmaceutically acceptable salt, or prodrug of the compound as represented by formula (I). The compound and the pharmaceutical composition thereof provided in the present invention can be used for preparing medicaments for preventing or treating diseases related to KRAS amplification or mutations such as KRAS G12A, KRAS G12C, KRAS G12D, KRAS G12R, KRAS G12S, KRAS G12V, KRAS G13D, or KRAS Q61H, and can especially be used for preparing medicaments for preventing or treating cancer.