2809 results about "Tautomer" patented technology

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.

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.

Compounds represented by general formula (I), or stereoisomers, tautomers, deuterated substances, solvates, prodrugs, metabolites, and pharmaceutically acceptable salts or eutectic crystals thereof, an intermediate thereof, and the use thereof in diseases related to KRAS inhibition or degradation such as cancers.

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.

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.

A fused ring compound, a pharmaceutical composition comprising same, and a use. The compound has a structure represented by formula (I) or a tautomer, mesomere, racemate, enantiomer, diastereomer or mixture thereof, metabolite, metabolic precursor, isotope substitution form, pharmaceutically acceptable salt, hydrate, solvate, polymorph or eutectic thereof. The compound can be used for treating a cancer caused by KRAS mutations, and said cancer is selected from one or more cancers caused by KRAS G12C, KRAS G12V, KRAS G12A and G12D mutations. In particular, the compound can serve as a G12D inhibitor and has relatively high inhibitory activity.

Provided herein are KRAS modulating compounds, such as compounds of Formula (I), (I-A), (I-B), or pharmaceutically acceptable salts, solvates, stereoisomers, atom labelled, or tautomers of any of the foregoing. The compounds provided herein are useful for modulating KRAS GD12 and / or other G12 mutants.

Provides heterocyclic compounds and use thereof, specially relates to a compound represented by Formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a solvate thereof, a crystal form thereof, a metabolite thereof or a prodrug thereof, further relates to a PROTAC comprising a compound of Formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a solvate thereof, a crystal form thereof, a metabolite thereof or a prodrug thereof. The heterocyclic compounds can be used for preventing or treating a SOS l-associated disease.

Provided herein are compounds of Formula (I) or tautomers, atropisomers, stereoisomers, or pharmaceutically acceptable salts thereof. These compounds are useful as KRAS mutant degraders and / or inhibitors.

A compound targeting a KRAS protein degradation agent, and a use thereof. The compound is a compound having an F-L-M structure, or a tautomer, racemate, enantiomer, or diastereomer thereof, or a mixture thereof or a pharmaceutically acceptable salt thereof, wherein F is a KRAS protein binding fragment, L is a linking unit for linking F and M, and M is a VHL binding fragment. The compound can be used for treating diseases caused by KRAS mutation or amplification.

Provided herein are compounds, or salts, esters, tautomers, prodrugs, zwitterionic forms, or stereoisomers thereof, as well as pharmaceutical compositions comprising the same. Also provided herein are methods of using the same in modulating (e.g., inhibiting) KRAS (e.g., KRAS having a Q61H, G12D, G12V, G12C, G12S, G12A, G12R, or G13D mutation or wild-type KRAS, including wild-type amplified KRAS) and treating diseases or disorders such as cancers in subjects in need thereof.

The invention provides a tetrahydropyridinopyrazole derivative and application thereof in medicine, and particularly relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic of the compound, and an intermediate and a preparation method of the tetrahydropyridinopyrazole derivative. The invention also relates to application in preparation of related medicines for treating diabetes mellitus. # imgabs0 #

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 R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the 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 discloses a compound represented by a formula (1), or a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a mixture form thereof, or a pharmaceutically acceptable salt, a prodrug or a solvate thereof, the structure of the formula (1) is represented as follows: # imgabs0. Strong hydrophilic sulfonic acid inner salt and / or phosphoric acid inner salt side chains are introduced at the position of (AAA and the like)-PAB (self-destruction group), so that the druggability (including hydrophilicity and stability) of the antibody drug conjugate corresponding to the compound is greatly enhanced, the in-vivo drug removal effect is reduced, and the tumor treatment effect is improved.

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, L, L1, L2, L3, L4, M, q, w and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

The invention provides a compound as shown in a formula I, or pharmaceutically acceptable salt, stereoisomer or tautomer thereof. The compounds have been demonstrated to be good GLP-1 receptor agonists. In addition, the compound is simple in preparation method and has a certain application prospect. # imgabs0 #

The invention discloses a polysubstituted pyrrolidine derivative represented by a general formula (I), a stereoisomer, a tautomer, a deuterated derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application of the compound. The invention also relates to pharmaceutical compositions comprising these compounds, stereoisomers, tautomers, deuterated derivatives or pharmaceutically acceptable salts thereof, uses of the compounds as sodium channel subtype Nav1.8 inhibitors, and uses thereof in the treatment and prevention of pain-related diseases. # imgabs0 #

Provided in the present invention are a tetrahydropyridopyrazole derivative and use thereof in medicine. Specifically provided is a compound as shown in general formula (I) or a racemate, stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate thereof, a preparation method therefor, and use thereof in the preparation of a related drug for treating diabetes or obesity.

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer, or salt thereof, wherein R1, R2, R3, R4, R5, L1a, L1b, L2, L3, L4, L5, L6, L7, M1, M2, q, w, m and n are as defined herein. Compounds of structure (I) find utility in a number of applications, including use as therapeutic agents for various treatment methods.

The present disclosure provides a class of compounds represented by formula (I '), or tautomers, stereoisomers or pharmaceutically acceptable salts thereof. The compound disclosed by the invention has a relatively strong agonistic effect on GLP-1R, can be used for treating diseases such as diabetes mellitus, metabolism-related fatty liver diseases, Alzheimer's disease and the like or has an effect of reducing weight. # imgabs0 #

Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.

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 relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or co-crystal of the compound, an intermediate of the compound, and application of the compound in inhibiting or degrading KRAS related diseases such as cancers. # imgabs0 #

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.

A compound as an LPAR1 antagonist, a pharmaceutical composition thereof and a use thereof. A compound represented by formula (I), as well as a racemate, stereoisomer, tautomer, nitrogen oxide, or pharmaceutically acceptable salt thereof. The compound of the LPAR1 antagonist has a good inhibitory effect on LPAR1, has excellent pharmacokinetic properties, and has good druggability.

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.