325 results about "Diastereomer" patented technology

Disclosed in the present invention are a KRAS G12D degradation agent as well as a preparation method therefor and the use thereof. The present invention provides compounds as shown below, and / or stereoisomers, enantiomers, diastereoisomers, atropisomers, deuterated compounds, hydrates, solvates, prodrugs and / or pharmaceutically acceptable salts thereof. The compounds provided by the present invention can effectively degrade and / or inhibit KRAS G12D protein in cells, and can be used for preparing drugs for treating and / or preventing related diseases or disorders caused by KRAS G12D mediation. G-L-E I

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.

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.

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 discloses an HPK1 small-molecule inhibitor based on a novel indazole skeleton and application of the HPK1 small-molecule inhibitor, and belongs to the technical field of medical chemistry. The HPK1 small-molecule inhibitor is a compound as shown in a formula (I) or an enantiomer thereof, a mixture of the enantiomer, a mixture of two or more diastereoisomers, a tautomer, a mixture of two or more tautomers, or an isotope variant or a pharmaceutically acceptable salt, a solvate, a hydrate or a prodrug thereof. The novel HPK1 small-molecule inhibitor skeleton disclosed by the invention shows a very strong inhibition effect on HPK1 and has a relatively good application prospect.

The invention discloses a 3-aryl piperidine-2, 6-diketone compound as shown in a general formula I or an enantiomer, a diastereoisomer, a raceme and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the 3-aryl piperidine-2, 6-diketone compound, the compound is used as a VAV1 targeted molecular glue degradation agent, and can degrade VAV1 protein in a targeted manner, so that the VAV1 protein can be degraded in a targeted manner. The invention has the application of preparing medicines for treating and / or preventing inflammatory diseases and autoimmune diseases.

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 discloses a TYK2 selective inhibitor and its use, specifically relates to a compound of formula (I) or its tautomer, mesomer, racemate, enantiomer, diastereoisomer or pharmaceutically acceptable salt thereof, and its use for preparing a drug for treating a disease mediated by TYK2.

The present invention refers to a method for the preparation of a compound according to formula (45), its enantiomers, diastereomers, a racemic mixture, and the pharmaceutically acceptable salts thereof. Furthermore the invention refers to a compound of formula (45) prepared by said method for use in treatment of neurodegenerative disorders and to pharmaceutical compositions.

The invention provides a carboxylic acid compound as well as a preparation method and application thereof. Relates to a carboxylic acid compound as shown in a formula (I), and an isotope label, an enantiomer, a diastereoisomer, a solvate or a pharmaceutically acceptable salt thereof for treating cancers. The carboxylic acid compound is shown as a formula (I), and the compound has better inhibitory activity on eIF4E and has a good application prospect.

The present invention provides a novel tetrahydroisoquinoline compound, a preparation method therefor, a pharmaceutical composition comprising the compound, and a use thereof. Specifically, the present invention provides a nitrogen-containing heterocyclic compound as shown in Formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, or racemate thereof. The compound of the present invention is capable of effectively reducing the synthesis of fatty acids and cholesterol esters, thereby alleviating the development and deterioration of metabolic diseases.

The application discloses a preparation method of 4AA diastereoisomer. Specifically disclosed is a preparation method of compound A5, which comprises the following steps: performing a reduction reaction on compound A3 in a solvent under the action of a reducing agent and a Lewis acid to obtain compound A5. The predetermined diastereoisomer is obtained through directional synthesis starting from commercial 4AA, and the reaction route is short and the yield is high.

A composition of stereoisomers of sulfoxaflor, where these stereoisomers are selected from diastereomers A and B at a selected A:B ratio, are provided as a mixture of crystal structures, and are water soluble with water solubility of at least about 0.7±0.07 mg / ml, methods for preparing them and insecticides and / or pesticides preparations comprising them.

Provided herein are pharmaceutical formulations comprising glucokinase activator, or a prodrug, or a pharmaceutically acceptable salt, an isotope labeled analogue, a crystalline form, a hydrate, a solvate, or a diastereomeric or enantiomeric form thereof and the use thereof for treating diseases; the pharmaceutical formulations are in the form of immediate-release formulations, extended-release formulations, or combination of immediate-release formulation and extended-release formulations. The pharmaceutical formulations achieved once-a-day therapy for some diseases, in particular, type II Diabetes Mellitus with obesity. The pharmaceutical formulations exhibit sustained 24 hours of glucose-lowering effects. The pharmaceutical formulations also achieved lower Cmax, extended T1 / 2 as well as maintained similar bioavailability and increased MRT compared with commercial Dorzagliatin tablet, enhanced the pharmacology effect of restoring the glucose stimulated GLP-1 secretion in diabetes with obesity.

The invention discloses a fused ring compound, a pharmaceutical composition containing the fused ring compound and application. The compound has a structure as shown in a formula (I) or a tautomer, a meso-mer, a raceme, an enantiomer, a diastereoisomer or a mixture form, a metabolite, a metabolism precursor, an isotope substitution form, a pharmaceutically acceptable salt, a hydrate, a solvate, a polymorphic substance or an eutectic substance thereof, the compound can be used for treating one or more cancers caused by KRAS mutation.

The application belongs to the technical field of chemical synthesis, and particularly relates to a method for asymmetrically synthesizing adjacent halogenated alcohol compounds. The cis adjacent halogenated alcohol compound is prepared through catalytic hydrogenation of asymmetric dynamic kinetic resolution of alpha halogenated ketone. The method has mild reaction conditions, excellent enantiomer and diastereomer selectivity, high efficiency and good yield, and has good application prospect.

The invention relates to the cosmetic and non-therapeutic use of a composition consisting essentially of a compound of formula I below: (I) or its enantiomers, isomers or diastereoisomers, or a mixture thereof, or a salt or a solvate thereof, wherein R1 and R2, independently of each other, are a C3-C6 sugar, a uronic acid, or a glucoside, for bleaching or whitening the skin and skin appendages of a healthy individual.

The invention discloses a fused ring compound, a pharmaceutical composition containing the fused ring compound and application. The compound has a structure as shown in a formula (I) or a tautomer, a meso-mer, a raceme, an enantiomer, a diastereoisomer or a mixture form, a metabolite, a metabolism precursor, an isotope substitution form, a pharmaceutically acceptable salt, a hydrate, a solvate, a polymorphic substance or an eutectic substance thereof. The compound can be used for treating cancers caused by KRAS mutation, the cancers caused by KRAS mutation are selected from one or more of cancers caused by KRASG12C, KRASG12V, KRASG12A and G12D mutation, and particularly, the compound can be used as a G12D inhibitor and has relatively high inhibitory activity.

Provided are a bicyclic compound of formula I that achieves a degradative or inhibitory effect on NRF2 by means of activating KEAP1, an isotopically labeled form, an enantiomer, a diastereomer, an atropisomer, or a pharmaceutically acceptable salt thereof, a method for preparing the compound, and use thereof in treating cancers.

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.

To provide a compound or a salt thereof which is rapidly metabolized to produce fulvestrant in the body.SOLUTION: The compound is a compound of formula (IV), an enantiomer, a diastereomer, a racemate, a pharmaceutically acceptable salt or a solvate thereof: Wherein R7 comprises certain phosphorus-containing esters and R8 represents certain substituents.SELECTED DRAWING: None

The invention discloses a chiral phenol calix [4] aryl porous organic molecular cage material as well as a preparation method and application thereof. A chiral calix [4] arene raceme and an acyl chloride chiral auxiliary agent are used as initial raw materials to react to prepare a pair of diastereoisomers, gram-grade separation is achieved through silica gel column chromatography, then the chiral auxiliary agent is removed respectively, and the single enantiomer chiral phenol calix [4] arene compound with the ee value being 99.9% or above can be obtained. The preparation method comprises the following steps of: synthesizing tetraaldehyde chiral phenol calix [4] arene by introducing an aldehyde group unit on the tetraaldehyde chiral phenol calix [4] arene through Duff reaction, and assembling the tetraaldehyde chiral phenol calix [4] arene serving as a construction element with a polyamino organic synthesizer to prepare the chiral phenol calix [4] arene porous organic cage with a larger cavity. The preparation method of the chiral porous organic cage does not need a catalyst, the preparation process is simple, operation is easy and convenient, expansibility is good, the yield is high, and the prepared chiral molecular cage is large in cavity, large in specific surface area and good in repeatability and can be used for chiral recognition and gas adsorption.

This disclosure relates to heterogeneous nuclear ribonucleic acid A2B1 (hnRNPA2B1) agonist compounds and their use in combination with chemotherapeutic agents for antitumor treatment. Specifically, this disclosure relates to fused ring compounds of formula (I), their cis-trans isomers, their enantiomers, their diastereomers, their racemic mixtures, their solvates, their hydrates, or their pharmaceutically acceptable salts or prodrugs thereof, compositions comprising any of the former, and products thereof, as well as the use of the aforementioned substances as hnRNPA2B1 agonists in the preparation of products for the prevention and / or treatment of tumors, said products may further comprise or be used in combination with chemotherapeutic agents. This disclosure has broad application prospects for the prevention and treatment of tumors.

The invention discloses a phosphabicyclo [3, 2, 0] organic phosphorus compound as well as a preparation method and application thereof. Diallyl-containing tertiary phosphine oxide and phosphine sulfur compounds are used as raw materials, 10-phenyl phenothiazine is used as a photocatalyst, the photocatalyst is excited under a light source of 390 nm to activate double bonds, high-stereoselectivity [2 + 2] cycloaddition reaction is realized, the phosphorus heterocyclic bicyclo [3, 2, 0] organophosphorus compound containing two quaternary carbon centers is synthesized, diastereoisomers can be separated, and the yield is high. A single diastereoisomer product is as high as 97%, and excellent diastereoselectivity is achieved. The invention provides a green reaction mode for photocatalytic synthesis of the phosphabicyclo [3, 2, 0] organophosphorus compound, the conditions are mild, and the substrate universality is good. The obtained phosphabicyclo [3, 2, 0] organophosphorus compound is applied to a primary alcohol chlorination reaction as a catalyst, shows high reaction activity, and has more excellent catalytic activity compared with a reported catalytic system.

An aromatic heterocyclic compound, a pharmaceutical composition and use thereof. Specifically disclosed are a compound as shown in formula I, a stereoisomer thereof, a diastereomer thereof, or a pharmaceutically acceptable salt of any one of the foregoing, or a crystal form or solvate of any one of the foregoing. The aromatic heterocyclic compound has a novel structure, good CDK7 inhibitory activity, and good selectivity.

To provide: a more efficient transfection composition or a formulation for transfecting a nucleic acid molecule into a cell; and a method for transfecting a nucleic acid molecule using the composition or formulation comprising such a composition for administration to cells.SOLUTION: The invention relates to a composition suitable for transfecting a nucleic acid molecule into a cell, preferably a eukaryotic cell, including (i) at least one compound of general formula (III), or a tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or an acceptable salt thereof, and (ii) an acceptable excipient, buffering agent, cell culture medium, or transfection medium.SELECTED DRAWING: Figure 5

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 application discloses an ether bond connected linker-drug molecule and an antibody conjugated drug, a preparation method and application thereof, and particularly discloses a compound represented by formula (1) or (2), or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer or a mixture form thereof, or a pharmaceutically acceptable salt, a prodrug or a solvate thereof, a composition containing the same or a use thereof. The compound of the application is connected with a drug molecule through an ether bond through a polypeptide (VC, VA, AAA)-PAB (self-elimination group) on a linker, greatly enhances the drugability (including hydrophilicity and stability) of the compound to an antibody drug conjugate, reduces the drug clearance in the body, and improves the tumor treatment effect.

The invention relates to pyridazinone or pyridazine compounds as well as derivatives and pharmaceutical compositions thereof. Specifically, the invention provides a pyridazinone or pyridazine compound as shown in a formula (I) or (Ia) or a stereoisomer, a tautomer, an enantiomer, a diastereoisomer, a resonator, a pharmaceutically acceptable salt, a hydrate, a solvate or a crystal form of the pyridazinone or pyridazine compound. The compound shown in the formula (I) or (Ia) has excellent agonistic effect and pharmacodynamic performance on a thyroid hormone beta receptor.