197 results about "Geometric isomer" patented technology

The invention relates to a PLpro protease small-molecule inhibitor for treating or preventing coronavirus infection and application of the PLpro protease small-molecule inhibitor. Specifically, the invention relates to a compound shown as a formula (I) or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof, and the use thereof in the preparation of a medicament for treating or preventing coronavirus infection or diseases or symptoms caused by coronavirus.

The invention relates to preparation and application of a substituted alkyl sulfide (sulfoxide) arylamine derivative. Specifically, the invention relates to a compound as shown in a formula (I), or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture thereof, or a pharmaceutically acceptable salt thereof, and an application of the compound in preparation of an acaricide for preventing and controlling pest mites, wherein the compound is used as a substituted alkyl sulfide (sulfoxide)-based arylamine derivative. The compound can achieve a better pest mite control effect at a lower dosage.

Provided in the present invention are an oxamide compound having a structure as shown in formula (I), or a pharmaceutically acceptable salt, isotope derivative or solvate thereof, or a stereoisomer, geometric isomer or tautomer thereof, or a prodrug molecule or metabolite thereof, and a pharmaceutical composition thereof and the use thereof. The compound involved in the present invention can efficiently inhibit STAT6 phosphorylation, can be used for preparing drugs for preventing and treating inflammatory diseases, and can be used for preparing anti-tumor drugs.

The invention discloses a separation method or an analysis method of astaxanthin geometric isomers and corresponding optical isomers thereof, and relates to the technical field of analysis. According to the method, four geometric isomers of all-trans astaxanthin, 9-cis astaxanthin and 13-cis / 15-cis astaxanthin can be effectively separated, and effective separation and detection of three optical isomers of all-trans astaxanthin, four optical isomers of 9-cis astaxanthin and eight optical isomers of 13-cis / 15-cis astaxanthin are further realized; therefore, effective separation and analysis of optical isomers corresponding to various geometric isomers can be realized. The method is high in specificity, good in separation degree and high in analysis accuracy of geometric isomers and optical isomers, and has important significance in developing research on the accurate correlation between the astaxanthin biological activity and the isomers.

Provided in the present invention is a small molecule compound, which is characterized in that it is a compound or a stereoisomer, geometric isomer, tautomer, racemate, hydrate, solvate, metabolite, and pharmaceutically acceptable salt or prodrug of the compound as represented by the following structural formula: formula (I). The small molecule compound of the present invention is applicable as a highly efficient and specific JAK kinase inhibitor, specifically a Tyk2 inhibitor and / or a JAK1 inhibitor, and / or a JAK1 / Tyk2 dual inhibitor.

The invention relates to a substituted arylthio thiazolidone derivative as well as preparation and application thereof. Specifically, the invention relates to a compound as shown in a formula (I), or an isotope-labeled compound, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture, or an acceptable salt of the compound, which is used as a substituted arylthio thiazolidone derivative, and application of the compound in preparation of insecticides for pest control, the compound can achieve a better pest control effect at a lower dosage, especially for pests such as tetranychidae, microcosaridae, acaridae, tarsonidae, aleuridae and root-knot nematode, and can be used for controlling pests such as tetranychidae, microcosaridae, gall mite, tarsonidae, aleuridae and the like.

The present invention relates to the preparation and use of novel trifluoroalkylthiophenylpyridine derivatives. Specifically, the present invention relates to compounds of formula (I-1) or formula (I-2) as trifluoroalkylthiophenylpyridine derivatives, or isotope labeled compounds thereof, or optical isomers, geometric isomers, tautomers or mixtures of isomers thereof, or agriculturally acceptable salts thereof, as well as the use of said compounds in the preparation of insecticides for pest control. These compounds are capable of achieving better pest control effects at lower dosages, especially against pests and mites such as Tetranychus cinnabarinus, Tetranychus urticae, and Panonychus citri.

Title: Process for treating keratinous materials using at least one polyester compound with acetoacetate functionalities. The present invention relates to a process for treating keratinous materials comprising applying to said keratinous materials, in one or more successive steps, at least: i) at least one polyester of formula (I) comprising at least two acetoacetate functionalities, as well as its optical, geometric, and / or solvate isomers, such as hydrates, or a composition containing it or them: (Z)–[OC(O)-C(Ra)(Rb)-C(O)-R4]u (I), formula (I) in which Z, u, R4, Ra, and Rb are as defined in the description, and ii) optionally, at least one crosslinking agent. Figure for the abstract: None

The invention discloses a preparation method and application of tanshinone IIA and cryptotanshinone amide derivatives. The tanshinone IIA and cryptotanshinone amide derivatives are compounds shown in a general formula (I) or stereoisomers, racemes, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, pharmaceutically acceptable salts or prodrugs of the compounds. The tanshinone IIA and cryptotanshinone amide derivative can be used for preparing anti-inflammatory drugs, antibacterial drugs, tumor drugs, drugs for treating cardiovascular and cerebrovascular diseases, drugs for treating burns and scalds and drugs for treating infectious diseases.

The present invention relates to a method for purifying (PU) at least one aqueous medium based on at least one C-glycoside derivative corresponding to formula (I) (preferably corresponding to formula (I') or (I''), and optical or geometric isomers thereof, and / or solvates (e.g., hydrates) thereof, and at least one salt, comprising at least one step of electrodialysis (PU1) of the aqueous medium. The present invention also relates to a method for preparing (PR) at least one C-glycoside derivative as described herein, comprising at least one step of electrodialysis (PU) of at least one aqueous medium containing at least the C-glycoside derivative and at least one salt. JPEG2026518301000030.jpg41170

Disclosed are a heterocycloalkyl carboxylic acid derivative, an intermediate, a preparation method therefor, and a use thereof, relating to the technical field of pharmaceutical chemistry. The heterocycloalkyl carboxylic acid derivative of the present invention is a compound represented by formula (I) below, or a stereoisomer, geometric isomer, tautomer, N-oxide, hydrate, solvate, pharmaceutically acceptable salt or prodrug thereof. By means of in vitro activity detection and animal behavioral experiments, it has been proven that said compound has good therapeutic effects for neurological diseases such as depression and bipolar disorder, as well as metabolic diseases such as diabetes and metabolic disorders.

The invention relates to the technical field of medicines, in particular to an STAT6 inhibitor, a preparation method of the STAT6 inhibitor and application of the STAT6 inhibitor in medicines. The invention provides an oxamide compound with a structure shown in a formula (III) or pharmaceutically acceptable salt, an isotope derivative and a solvate thereof, or a stereoisomer, a geometric isomer and a tautomer thereof, or a prodrug molecule and a metabolite thereof, as well as a medicinal composition and application of the oxamide compound, the salt, the isotope derivative and the solvate of the oxamide compound, the stereoisomer, the geometric isomer and the tautomer thereof, the prodrug molecule and the metabolite of the oxamide compound. The compounds may be used to treat or prevent STAT6 mediated diseases or disorders and related diseases or disorders.

The invention discloses a heterocyclic alkyl carboxylic acid derivative, an intermediate and a preparation method and application thereof, and relates to the technical field of medicinal chemistry. The heterocycloalkyl carboxylic acid derivative is a compound as shown in the following formula, and a stereoisomer, a geometric isomer, a tautomer, nitrogen oxide, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the heterocycloalkyl carboxylic acid derivative, and in-vitro activity detection and animal behavioral experiments prove that the compound has good treatment effect on neurological diseases, neurological diseases, neurological diseases, neurological diseases, neurological diseases, neurological diseases, neurological diseases, neurological diseases, neurological diseases and neurological diseases. The traditional Chinese medicine composition has a good treatment effect on diseases such as depression, bidirectional affective disorder and the like, and metabolic diseases such as diabetes mellitus, metabolic disorder and the like.

The present invention relates to novel heterocyclic compounds of formula (I) as inhibitors of PARG, their pharmaceutically acceptable salts, stereoisomers, solvates, polymorphs, tautomers, atropisomers, optical and geometric isomers, prodrugs, deuterated including other possible isotopes, combinations and use thereof in treating cancer. Formula (I) The present invention also relates to a process for the preparation of novel heterocyclic compounds of Formula (I), pharmaceutical compositions comprising them, and their use in the treatment of cancer.

The present application provides a compound having a structure shown in Formula I, II or III or its enantiomer, diastereoisomer, racemate, stereoisomer, geometric isomer, nitroxide, metabolite or its pharmaceutically acceptable salt, ester, solvate, hydrate, isotopically labeled compound or prodrug. The non-fenofibrate 4-position ether derivative of the present application has an excellent xanthine oxidase activity inhibitory activity.

Use of a compound, microarray chip substrate, microarray chip and use and method thereof. The present application provides use of a compound, or a geometric isomer, tautomer, isotopically labeled, hydrate, solvate or salt thereof in chip surface modification. Also provided is a microarray chip substrate modified by the compound, and a microarray chip comprising the microarray chip substrate. The microarray chip substrate of the present application can greatly improve the surface modification function by surface modification, improve nucleic acid synthesis yield, amplify detection signal, and avoid non-specificity and cross-talk. It has a wide application prospect.

The invention provides a compound or an enantiomer, a diastereoisomer, a racemate, a tautomer, a stereoisomer, a geometric isomer, nitrogen oxide, a metabolite or pharmaceutically acceptable salt, ester, solvate, hydrate, isotope labeled compound or prodrug thereof. The invention further provides a composition containing the compound and medical application. The compound has a good patent medicine prospect in the aspect of treating or preventing PTPN2-related diseases or symptoms.

The invention belongs to the field of medicinal chemistry. The invention discloses a heterocyclic compound as well as a preparation method and application thereof, and particularly relates to a series of blockers of sodium ion channels with novel structures as well as a preparation method and application thereof. The structure of the compound is shown as a general formula (I). The compounds or stereoisomers, racemes, geometric isomers, tautomers, prodrugs, hydrates, solvates or pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used for treating or / and preventing sodium ion channel (Nav)-mediated related diseases.

The invention discloses imidazopyridine derivatives and application thereof, a pharmaceutical composition and a pharmaceutical preparation, and belongs to the technical field of medical chemistry. The technical problems to be solved are that the existing P2X3 receptor inhibitor is poor in safety, low in P2X3 or P2X2 / 3 selectivity, poor in metabolic stability and the like. According to the key points of the technical scheme, the imidazopyridine derivative is selected from a compound as shown in a formula I or a racemate, a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, an isotope label, a solvate, a polymorphic substance, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof.

a kind of sp 2 C covalent organic framework functionalized silicon-based chromatographic stationary phases, their preparation methods, and applications. Preparation steps: (1) Preparation of SiO2-NH2: Aminated activated spherical silica particles are prepared using an amino-containing silane coupling agent; (2) SiO2@sp 2 C-COF preparation: Using TMT and TFPT as raw materials, sp was obtained through a Schiff base-mediated aldehyde-alcohol condensation reaction initiated by a self-assembled monolayer auxiliary surface. 2 A C covalent organic framework is loaded onto the surface of a silica matrix via C=N bonds. 2 C-COF possesses an in-plane π-conjugated, highly ordered, and robust framework structure. Its unique hydrophilic covalent triazine groups and hydrophobic benzene rings can provide various interactions such as hydrophobicity, π-π stacking, hydrogen bonding, and hydrophilicity. This enables the stationary relative shape-restricted and geometric isomers to exhibit special selectivity and separation capabilities, overcoming the instability of common imine-bonded COFs in liquid chromatography (HPLC) and the limited selectivity of relatively shape-restricted and geometric isomers stationed in traditional bonded silica gel.

The application discloses an imidazopyridine derivative and application, a pharmaceutical composition and a pharmaceutical preparation, and belongs to the technical field of medicinal chemistry. The technical problems to be solved are that existing P2X3 receptor inhibitors have poor safety, low selectivity for P2X3 or P2X2 / 3 and poor metabolic stability. The technical solution is that an imidazopyridine derivative is selected from the compounds shown in the formula I or racemates, stereoisomers, geometric isomers, tautomers, nitroxides, hydrates, isotopically labeled compounds, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts or prodrugs.

The invention relates to a cathepsin B sensitive fatty acid-adriamycin prodrug as well as albumin nanoparticles, a preparation method and application thereof, and belongs to the technical field of medicines. The cathepsin B sensitive fatty acid-adriamycin prodrug is a prodrug as shown in a formula (I), a geometric isomer thereof, and pharmaceutically acceptable salts, hydrates and solvates thereof, wherein n is equal to 0-14. The invention also relates to a combined albumin nanoparticle prepared by entrapping the cathepsin B sensitive fatty acid-adriamycin prodrug by using human / bovine serum albumin as a carrier. The albumin nanoparticles are small in particle size and uniform in form, have good placement stability and colloidal stability, can stably exist in systemic circulation and normal tissues, and release a parent drug adriamycin after being taken by tumor cells and hydrolyzed by cathepsin B; therefore, specific killing of tumor cells is realized without generation of serious toxic and side effects, and good clinical development prospects are achieved.

Applications of a diphenylpropenone compound of general formula (I), or a stereoisomer thereof, or a geometric isomer thereof, or a tautomer thereof, or a solvate thereof, or an acceptable animal feed salt, in the preparation of an animal feed additive or feed. Confirmed by animal breeding trials, the diphenylpropenone compound, or a stereoisomer thereof, or a geometric isomer thereof, or a tautomer thereof, or a solvate thereof, or an acceptable animal feed salt, can be used as the animal feed additive or animal feed. The weight of the animals can be effectively increased, survival rates can be enhanced, and the compound has a good effect on improving animal production performance.

The application discloses an ISR inhibitor and a preparation method and application thereof, and belongs to the technical field of biological medicines. The compound of the application is a compound with the structure of formula (I) or formula (II), a stereoisomer thereof, a geometric isomer thereof, a tautomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof or a solvate thereof. The compound provided in the application can be effectively combined with eIF2B, has good ATF4 inhibiting capacity, and can better restore protein synthesis when ISR is stimulated. Therefore, the compound of the application can be used as an ISR inhibitor and for treating various related diseases.

This present application discloses a pyrrolo [2, 3-b] pyridine derivative represented by formula (I), or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer, or a mixture of isomers thereof, or a pharmaceutically acceptable salt, or a prodrug thereof, or a metabolite thereof, as well as preparation method therefor, use as RET kinase inhibitor, and pharmaceutical composition comprising such derivative. Experimental results demonstrate that the compound according to the present invention can more effectively inhibit the activity of RET and its mutants compared to prior art drugs.

Provided are a compound for recovering a p53 mutation function and use thereof, particularly relating to a compound represented by Formula M, or an enantiomer, a diastereomer, a racemate, a tautomer, a stereoisomer, a geometric isomer, a crystal form, a nitrogen oxide, a metabolite or pharmaceutically acceptable salt, ester, solvate, hydrate, isotope-labeled compound or prodrug of the compound.

Disclosed are compounds of formula I, including all geometric and stereoisomers, N-oxides and salts thereof, wherein A, R 2 , R 4 , R 5 , L, and Q are as defined in this disclosure. Also disclosed are compositions containing the compounds of Formula 1, and methods for controlling and combating invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound or composition of the present disclosure. [Formula 1] TIFF2025542212000089.tif22170

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N oxides, and salts thereof, wherein R1, R2, R3, R4, R5, R6, m and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

The present application relates to a compound for inhibiting IRAK4 activity and a use thereof, and specifically provides a compound as represented by formula A, or an enantiomer, a diastereoisomer, a racemate, a tautomer, a stereoisomer, a geometric isomer, a nitrogen oxide, a metabolite or a pharmaceutically acceptable salt, an ester, a solvate, a hydrate, an isotope-labeled compound (preferably a deuterated substance), or a prodrug thereof,

The present application provides a DNA polymerase theta (Pol theta) inhibitor represented by structural formula (I) and its enantiomers, diastereomers, racemates, tautomers, stereoisomers, geometric isomers, deuterium compounds, nitroxides, metabolites or pharmaceutically acceptable salts, esters, solvates, hydrates, isotopically labeled compounds or prodrugs thereof, and corresponding preparation methods and applications. Biological experiments show that the compound of the present application has a Pol theta inhibitory effect, and can be used alone or in combination to treat tumors with high incidence of homologous recombination deficiency (HRD) or DNA damage response (DDR) deficiency.