1009 results about "Tautomer" patented technology

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.

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.

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 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.

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.

Provided herein are novel triazine compound derivatives, compositions containing the compounds, and preparation methods and uses thereof. The triazine compound derivatives are compounds represented by Formula (I) or (II), or tautomers, stereoisomers, prodrugs, crystal forms, isotopically labeled forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compounds and compositions of the present disclosure can be used to treat diseases or disorders mediated by USP1, in particular, cancer. Formula (I) Formula (II)

The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt tautomer, solvate, hydrate thereof. Also disclosed are methods of using such compounds and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of proliferative disorders, such as cancer.

The invention provides a diketone biphenyl compound serving as a VAV1 degradation agent and application of the diketone biphenyl compound. Specifically provided are a compound represented by formula (I), a tautomer, a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof. The compound provided by the invention is good in drug effect and can be used for preparing drugs for treating or preventing VAV1 related diseases.

Described herein are methods of for treating and / or preventing Major adverse cardiovascular events (MACE). by administering to a subject in need thereof, a combination of a sodium-glucose transport protein 2 (SGLT2) inhibitor and a compound of Formula I or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof, wherein the variables of Formula I are as defined herein.

The present application provides the use of betaine in preventing the occurrence of autism spectrum disorder (ASD). Specifically, the present application provides the use of betaine or a pharmaceutically acceptable salt, stereoisomer, tautomer, nitroxide, solvate, metabolite or prodrug thereof in the preparation of a medicament for preventing the occurrence of ASD, optimizing fetal neural development or reducing the risk of fetal neural development disorder. By using betaine or a pharmaceutically acceptable salt, stereoisomer, tautomer, nitroxide, solvate, metabolite or prodrug thereof as an active ingredient, the occurrence of ASD can be effectively prevented, fetal neural development can be optimized, or the risk of fetal neural development disorder can be reduced.

Provided in the present invention are a compound as represented by formula (I), or a pharmaceutically acceptable salt, a tautomer, a geometrical isomer, an optical isomer, a solvate or an isotopic derivative thereof, and the use thereof. The compound of the present invention has a significant inhibitory activity on PRMT5, has a significant inhibitory effect on tumor cells and in vivo tumor models, also has a good administration performance, and has clinical application potential for preventing and / or treating diseases which are at least partially mediated by PRMT5.

The invention provides a compound as shown in a formula I which can be used as a sodium channel regulator, and a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition containing the compound and the stereoisomer, the tautomer or the pharmaceutically acceptable salt thereof and a carrier or excipient, and a pharmaceutical application of the pharmaceutical composition as a NaV1.8 inhibitor (such as pain, respiratory diseases, neurological disorders, mental diseases and the like).

The invention relates to an aromatic ring-containing compound serving as a WRN inhibitor and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer, a hydrate, a solvate, pharmaceutically acceptable salt or prodrug of the compound, a preparation method of the tautomer, the stereoisomer, the hydrate, the solvate and the pharmaceutically acceptable salt or prodrug of the compound and application of the tautomer, the stereoisomer, the hydrate, the solvate and the pharmaceutically acceptable salt or prodrug in preparation of drugs for treating WRN-related diseases.

The invention provides a compound as shown in a formula I, and a tautomer, a stereoisomer, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The compound can be used as an antagonist of TRPM3.

The present invention relates to a compound represented by formula (I) or a stereoisomer, tautomer, solvate or pharmaceutically acceptable salt of a compound represented by formula (I), TIFF2026503201000033.tif3981X1, X2 and X3 are each independently an optionally substituted C1-C 15 alkylene, and R and R are each independently an optionally substituted C-C 40 Alkyl, optionally substituted C-C 40 Heteroalkyl, optionally substituted C-C 40 Alkenyl, optionally substituted C-C 40 Heteroalkenyl, optionally substituted C-C 40 Alkynyl or optionally substituted C-C 40 The present invention provides a compound comprising heteroalkynyl, wherein R3, R4, R5, and R6 are each independently H, halogen, or optionally substituted C1-C3 alkyl, and the substituents are independently selected from halogen, -OH, -SH, -NH2, -NO2, cyano, and C1-C3 alkyl, which has the advantages of low cytotoxicity, strong delivery ability, and strong immunostimulatory effect.

The invention relates to a pyrimidine derivative as well as a pharmaceutical composition and application thereof, and particularly provides a compound as shown in the following formula H, and a raceme, a stereoisomer, a tautomer, an isotope label, a solvate, a polymorphic substance, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound.

A pharmaceutical composition or a pharmaceutical preparation, the pharmaceutical composition or the pharmaceutical preparation comprising a therapeutically effective amount of an active ingredient M and a pharmaceutical excipient, the active ingredient M being selected from a compound of general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic thereof, the pharmaceutical composition or the pharmaceutical preparation comprises 1-600 mg of an active ingredient M. The invention also relates to application of the pharmaceutical composition or the pharmaceutical preparation in preparation of related medicines for treating cancers.

The invention provides a compound as shown in a formula (I), and a stereoisomer, a tautomer, an isotope label, nitrogen oxide, a solvate, a polymorphic substance, a metabolite, ester, pharmaceutically acceptable salt or prodrug thereof, or a pharmaceutical composition thereof, which have better antibacterial and anti-inflammatory effects, can be used as an antibiotic, and can be used for preparing a pharmaceutical preparation for preventing and treating diseases. The compound can treat infection caused by pathogenic microorganisms resistant to erythromycin and telithromycin, and simultaneously acts on double targets of ribosome and topoisomerase.

Provided herein are compounds of formula (I), or their tautomers, stereoisomers, or pharmaceutically acceptable salts. These compounds are useful as KRAS(G12D) proteolytic agents and / or inhibitors. [Case 1] TIFF2026511222000314.tif64165

The present invention relates to the field of medicines and relates to a fused five-membered and six-membered heterocyclic compound, a preparation method therefor, and a use thereof in the field of pharmaceuticals. Specifically, the present invention provides a compound having a structure represented by formula (I), or a stereoisomer, a tautomer, a solvate, a metabolite, a pharmaceutically acceptable salt, or a prodrug thereof. The compound and a pharmaceutical composition thereof of the present invention can be used for preparing a medicament for treating HIF-2α-mediated related diseases, such as renal anemia, chronic kidney disease, chronic metabolic disease, neurodegenerative disease, infection, inflammatory disease, pulmonary edema, and acute respiratory distress syndrome.

The application relates to the field of agricultural disease control technology, and particularly relates to the use of indole compounds and pharmaceutically acceptable salts, solvates, crystal forms, prodrugs, stereoisomers and tautomers thereof for preparing a medicine for inhibiting pathogenic key protein kinase CgSlt2 of pathogenic fungi. The application first proposes a new type of CgSlt2-targeted inhibitor, specifically, indole compounds ((S)-N-(1-(1H-indol-3-yl)-4-(methylamino)-4-oxobutan-2-yl)-8-bromo-1,6-naphthyridine-2-carboxamide) and ((S)-N-(2-((1H-indol-3-yl)-1-(methylamino)-1-oxopropyl)-8-bromo-1,6-naphthyridine-2-carboxamide) are used as CgSlt2 inhibitors, have the characteristics of high target specificity and high activity, and exhibit excellent pathogenicity inhibition of a strain of the complex group of Colletotrichum gloeosporioides.

The invention discloses a lipid compound for delivering a therapeutic agent as well as a preparation method and application of the lipid compound, and particularly discloses a compound shown in a formula I or pharmaceutically acceptable salt, stereoisomer, tautomer, solvate, chelate, non-covalent complex or precursor of the compound, the ionizable lipid compound can effectively deliver nucleic acid molecules, small molecule compounds and other drugs, and through comparison, the lipid nanoparticles are good in particle size distribution and high in encapsulation efficiency, the delivery effect can be obviously better than that of contrast lipid nanoparticles, and the requirement of in-vivo delivery can be met. (I)

Disclosed in the present invention are a heterocyclic compound, a pharmaceutical composition, and a use of the heterocyclic compound or the pharmaceutical composition. Provided is a heterocyclic compound, or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorphic substance, solvate, isotope derivative, or prodrug thereof. The heterocyclic compound has a structure represented by formula (I). The heterocyclic compound provided in the present invention has inhibitory activity against a TEAD protein, can effectively inhibit the interaction between TEAD and YAP, and thus can treat diseases related to abnormal regulation of the TEAD protein or an abnormal Hippo pathway.

This specification provides novel acetylene compound derivatives, compositions containing such compounds, methods for producing the sames, and uses thereof. The acetylene compound derivatives are compounds of the following chemical formula (I), or their tautomers, stereoisomers, prodrugs, crystalline forms, isotopically labeled forms, pharmaceutically acceptable salts, hydrates, or solvates. The compounds and compositions of the present invention can be used in the treatment of polθ-mediated diseases or disorders, particularly cancer. JPEG2026522774000373.jpg51149

The invention discloses a compound for inhibiting SMARCA2 or pharmaceutically acceptable salt, ester, stereoisomer, tautomer, polymorphic substance, solvate, metabolite, isotope labeled compound or prodrug of the compound, and a pharmaceutical composition containing the compound and the pharmaceutically acceptable salt, ester, stereoisomer, tautomer, polymorphic substance, solvate, metabolite, isotope labeled compound or prodrug. The compound and the pharmaceutical composition are used for preventing or treating diseases, symptoms or disorders related to SMARCA2.

Disclosed are compounds having the formula (I), or an enantiomer, diastereomer, or tautomer or atropisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, wherein R1, R2, A and n are defined herein. Also disclosed are methods of preparing such compounds, as well as pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of inflammatory disorders, allergic disorders, skin disorders, mast cell disorders, pain disorders, and pruritus disorders. (I)

The present application relates to a kind of thieno [2, 3-c] pyridazine derivatives, and its isotope form, stereoisomer, tautomer, cis-trans isomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, hydrate, prodrug and polymorph, these compounds can be used as cholinergic M4 receptor positive allosteric modulator, it has good application prospect in preparation for preventing and / or treating the drug for the disease related to abnormal muscarinic acetylcholine receptor.

Disclosed herein is an isoquinoline-1 (2H)-one derivative of formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof wherein the values of the variables (e.g., L2A, R1, R2A, R3, R4A, R4B, R4C, R4D, Q2, Q3, Q4) are as described herein. Also disclosed is a pharmaceutical composition comprising such derivatives, and a method of using such derivatives to treat or prevent a condition or disease responsive to inhibition of PI3K [alpha] activity in a subject.

The present invention relates to compounds of formula (I), and stereoisomers, tautomers, N- oxides, and pharmaceutically acceptable salts thereof that are useful for modulating, preferably inhibiting three-prime repair exonuclease (TREX1). The present invention further relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising said compounds. Further, the present invention relates to compounds of formula (I) and pharmaceutical compositions comprising said compounds for use in the treatment of cancer, such as breast, small cell lung cancer and colorectal cancer, in particular cancers with chromosomal instability, TREX1-mediated autoimmune diseases, inflammatory myocarditis, Aicardi-Goutières syndrome (AGS), familial chilblain lupus (FCL), systemic lupus erythematosus (SLE) and retinal vasculopathy with cerebral leukodystrophy (RVCL).

Provided in the present invention are a compound as represented by formula I which can be used as a sodium channel modulator, and a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof. Further provided are a pharmaceutical composition containing the compound and the stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and a carrier or an excipient, and the pharmaceutical use thereof as an NaV1.8 inhibitor (against, for example, pain, respiratory diseases, neurological disorders, and mental diseases).