462 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 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 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 #

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 belongs to the technical field of traditional Chinese medicine biology, and particularly relates to application of a phenolic compound in preparation of a medicine for preventing or treating hepatic fibrosis. A pair of phenolic diastereoisomers (+)-fresh bamboo juice phenol C and (-)-fresh bamboo juice phenol C are separated from fresh bamboo juice, and an anti-hepatic fibrosis activity screening test shows that (+)-fresh bamboo juice phenol C has a remarkable inhibition effect on human hepatic stellate cells LX-2, has clinical application potential in anti-hepatic fibrosis treatment, and has broad application prospects. The method can be used for preparing medicines for preventing or treating hepatic fibrosis, and a new basis is provided for pharmacological research of fresh bamboo juice.

The invention belongs to the technical field of traditional Chinese medicine biology, and particularly relates to a phenolic diastereoisomer and a preparation method and application thereof.The phenolic diastereoisomer has the chemical structural formula shown in the formula I and the formula II, the formula I is dextroisomer and is named as (+)-fresh bamboo juice phenol D, and the formula II is levoisomer and is named as (-)-fresh bamboo juice phenol D. A pair of phenolic diastereoisomer compounds (+)-fresh bamboo juice phenol D and (-)-fresh bamboo juice phenol D are successfully obtained from fresh bamboo juice, and an anti-neurotoxicity activity test shows that (+)-fresh bamboo juice phenol D has a remarkable protection effect on PC12 cell injury caused by glutamic acid and can be used for preparing medicines for preventing or treating neurodegenerative diseases; wide application prospects are realized.

The invention belongs to the technical field of biological medicines, and particularly relates to a royal jelly acid derivative and a synthesis method, a pharmaceutical composition and application thereof. The royal jelly acid derivative is a compound shown as a formula (I), or an enantiomer, a diastereoisomer and a tautomer thereof, or a solvate or a pharmaceutically acceptable salt thereof. A series of royal jelly acid derivatives with novel structures are constructed by using a natural component royal jelly acid derived from royal jelly as an initial raw material, the royal jelly acid derivatives can play a role in resisting pulmonary fibrosis by inhibiting the activity of fibroblasts, the effect of the royal jelly acid derivatives is equivalent to that of pirfenidone, and the royal jelly acid derivatives are expected to be developed into candidate drugs for resisting pulmonary fibrosis. The ceramide NP has excellent effects in anti-inflammatory, anti-allergic and itching-relieving aspects, has a better effect than known ceramide NP, and can be used for preparing health care products, cosmetics and medicines. And # imgabs0 #.

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.

The invention discloses a trifluoromethyl-containing polysubstituted phosphorus-doped six-membered ring phosphine oxide compound as well as a preparation method and application of the trifluoromethyl-containing polysubstituted phosphorus-doped six-membered ring phosphine oxide compound. A diene-containing three-stage phosphine oxide compound is used as a raw material, a trifluoromethyl reagent and a nucleophilic reagent are used, in the presence of a transition metal copper catalyst and a pyridine-oxazoline ligand, a free radical domino cyclization reaction is initiated to obtain the compound, C-O, C-N and C-C coupling is realized, and the variety of the nucleophilic reagent can be changed, so that the structure of the product is diversified. The diastereoisomers can be separated, the yield of a single diastereomer can reach 85%, and the diastereoisomers have excellent diastereoselectivity. The invention provides a novel reaction mode of constructing a polysubstituted phosphorus-doped six-membered ring by mediation of free radicals, the reaction condition is mild, the operation is simple, the substrate universality is good, a novel skeleton structure of an organic phosphine reagent is provided, and the variety diversity of the organic phosphine reagent is expanded. The synthesized compound can be used as a catalyst to be applied to Appel reaction, and has a good application prospect.

A camptothecin compound and a conjugate thereof, or a tautomer thereof, an enantiomer thereof, a diastereomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition thereof, a preparation method therefor, and use thereof. The compound and the conjugate can be used for treating proliferative diseases related to abnormal cell activity.

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 invention relates to imidazoquinoline or benzindazolone compounds, their pharmaceutically acceptable salts, hydrates, solvates, enantiomers, diastereoisomers, tautomers or prodrugs; their use in the prevention and treatment of inflammatory diseases; and intermediates for their preparation. By using the compounds of the present invention as substrates of NQO1 to activate the redox reaction of NQO1, the expression and activity of inflammatory cytokines can be inhibited, and thus they can be used for preventing or treating diseases related to NQO1 activity.

Provided are a compound of formula (I) or a tautomer, enantiomer, diastereomer, isotope-labeled compound, solvate, or pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and use thereof in the preparation of a drug for preventing and treating pyroptosis-related autoimmune diseases, infections, and non-infectious diseases.

The present invention relates to the field of pharmacological research, and specifically relates to a compound as shown in general formula (I), or a pharmaceutically acceptable salt, tautomer, enantiomer, diastereomer, racemate, hydrate, ester, solvate, metabolic precursor or prodrug thereof, a preparation method therefor, a pharmaceutical combination comprising same, and a use of the compound in the prevention and / or treatment of respiratory diseases caused by viruses (such as SARS-CoV2, SARS-CoV, and MERS-CoV) and in the inhibition of nonstructural proteins of the related viruses, such as a papain-like protease protein.

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 present invention relates to compounds of formula (I), their diastereoisomers and their salts, for use for inhibiting cancer-related inflammation, notably via STING interaction.

The present invention belongs to the field of organic chemical ligands and discloses a nitrogen-nitrogen-phosphorus ligand having a structure of the general formula I or its tautomers, enantiomers, and diastereomers: #imgabs0#R 1 、R 5 R is independently selected from hydrogen, alkyl, alkoxy, cycloalkyl, alkenyl, alkynyl, hydroxyl, aldehyde, carboxyl, ester, halogen, trifluoromethyl, cyano, acyl, amide, amino, nitro, phenyl, benzyl, sulfonyl, sulfonic acid, and mercapto; 2 is selected from one of the following structures: alkyl, alkoxy, cycloalkyl, alkenyl, alkynyl, phenyl, benzyl, phenethyl, naphthylmethyl, -CHPh2, ester, -CH2OBn, or substituted phenyl or benzyl, or R 2 With R 4 connected to form a five-membered ring and an acene ring; the R 3 is selected from hydrogen or alkyl; said R 4 is selected from hydrogen, alkyl, alkoxy, alkenyl, alkynyl, phenyl, benzyl; W is PR2 or P(O)R2, and R is selected from phenyl, naphthyl, cyclohexyl, and substituted phenyl. The present invention also discloses a preparation method and use of nitrogen-nitrogen-phosphorus ligands.

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.

Disclosed in the present invention are a compound as shown in formula 1, or a tautomer, mesomer, racemate, enantiomer and diastereomer thereof, a mixture form thereof, or a pharmaceutically acceptable salt thereof. The compound has excellent NLRP3 inhibitory activity, and the compound of the present invention lays a new material basis for the development of therapeutic drugs for NLRP3-related diseases.

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.