833 results about "Diastereomer" patented technology

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.

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.

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.

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.

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 present application relates to a multi-specific bioconjugate linker and a method for synthesizing the same, and specifically to a compound or its tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt thereof. The present application also relates to a method for preparing the compound and its use in tumor treatment.

The invention belongs to the technical field of traditional Chinese medicine biology, and particularly relates to a pair of diastereoisomers in fresh bamboo juice as well as a preparation method and application of the diastereoisomers, in the diastereoisomers, a formula I is a dextroisomer and is named as (+)-fresh bamboo juice phenol A, and a formula II is a levoisomer and is named as (-)-fresh bamboo juice phenol A. According to the invention, a pair of diastereoisomer compounds (+)-fresh bamboo juice phenol A and (-)-fresh bamboo juice phenol A are successfully obtained from fresh bamboo juice, and an in-vitro cell test shows that the (+)-fresh bamboo juice phenol A has a remarkable inhibition effect on gastric cancer cells, liver cancer cells, colorectal cancer cells, bladder cancer cells and lung cancer cells of a human body; the compound can be used for preparing medicines for preventing or treating tumors, and has a wide application prospect.

A compound represented by formula (1), or a tautomer, mesomer, racemate, enantiomer, and diastereomer thereof, or mixture form thereof, or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein the structure of formula (1) is as shown below: formula (1). According to the compound, a strong hydrophilic sulfonate inner salt and / or phosphate inner salt side chain are introduced at the position of polypeptide (VC, VA, AAA, etc.)-PAB (self-immolative group) of a linker, greatly enhancing the druggability (comprising hydrophilicity and stability) of an antibody drug conjugate corresponding to the compound, reducing the in-vivo drug clearance effect, and improving the tumor treatment effect.

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 belongs to the technical field of traditional Chinese medicine biology, and particularly relates to a phenolic compound and a preparation method and application thereof.The phenolic compound is a pair of diastereoisomers, the formula I of the phenolic compound is dextroisomer and is named as (+)-fresh bamboo juice phenol B, and the formula II of the phenolic compound is levoisomer and is named as (-)-fresh bamboo juice phenol B. A pair of diastereoisomer phenolic compounds (+)-fresh bamboo juice phenol B and (-)-fresh bamboo juice phenol B are successfully obtained from fresh bamboo juice, and the diastereoisomer phenolic compounds (+)-fresh bamboo juice phenol B and (-)-fresh bamboo juice phenol B have remarkable inhibition effects on gastric cancer cells, liver cancer cells, colorectal cancer cells, bladder cancer cells and lung cancer cells of a human body through in-vitro cell tests; the compound can be used for preparing medicines for preventing or treating tumors, and has a wide application prospect.

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 present invention relates to the field of medicine, and in particular to a PRMT5 inhibitor, as well as a preparation method therefor and a use thereof. The PRMT5 inhibitor is a compound as shown in formula (I), an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug, an isotope variant, or a pharmaceutically acceptable salt thereof. The present invention has better activity, selectivity, pharmacokinetic characteristics, safety or a wider treatment window.

The invention provides a method for detecting diastereoisomers in a nerofloxacin malate sodium chloride injection. The method comprises the following steps: separating optical isomers of the nerofloxacin malate sodium chloride injection by adopting a liquid chromatography; wherein the chromatographic condition of the liquid chromatography comprises a mobile phase, the mobile phase comprises a mobile phase A and a mobile phase B, the mobile phase A is a trifluoroacetic acid solution, and the mobile phase B is methanol-tetrahydrofuran. According to the technical scheme, a trifluoroacetic acid solution is adopted as a mobile phase A, methanol-tetrahydrofuran is adopted as a mobile phase B, tetrahydrofuran is added in the mobile phase B, the peak pattern of a main peak is improved, the trailing factor is 1.06, the operation time can be shortened, and the peak pattern of the main peak is improved.

The invention belongs to the technical field of biocatalysts, and discloses an alkene reductase mutant and application of the alkene reductase mutant in catalytic preparation of a brivaracetam synthesis intermediate. The amino acid sequence of the alkene reductase mutant is as shown in SEQ ID NO.1, a compound enzyme composed of the mutant, carbonyl reductase K1 and glucose dehydrogenase can take a compound 5-hydroxy-4-n-propyl-2-furanone as a substrate, double bonds are reduced, hydroxyl is removed, a compound (R)-4-propyl dihydrofuran-2 (3H)-ketone is obtained, and the compound (R)-4-propyl dihydrofuran-2 (3H)-ketone can be used for preparing the alkene reductase. The ee value of the (R)-4-propyl dihydrofuran-2 (3H)-ketone obtained through catalysis reaches 93.0%, the (R)-4-propyl dihydrofuran-2 (3H)-ketone with the ee value larger than 99.8% can be further obtained through diastereoisomer crystallization, and the method can be used for efficient and green preparation of the brivaracetam key intermediate (R)-4-propyl dihydrofuran-2 (3H)-ketone.

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.

Provided herein are pharmaceutical compositions, each comprising a phenylsulfonamide, for example, a compound of Formula I, or an enantiomer, a mixture of enantiomers, a mixture of tow ore more diastereomers, a tautomer, a mixture of two or more tautomers, or an isotopic variant thereof; or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof; and a pharmaceutically acceptable excipient. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurodegenerative disease.

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 a pyrazinamide compound, which is a compound with a structure as shown in a general formula (I) or a tautomer, an enantiomer, a diastereomer, a racemate, a metabolite or a metabolic precursor of the compound, or pharmaceutically acceptable salt, ester and prodrug of the compound, or a hydrate of the compound, the invention also discloses a preparation method of the pyrazinamide compound and an application of the pyrazinamide compound in preparation of medicines for preventing and treating GPR52 related diseases. The invention also discloses a preparation method of the pyrazinamide compound and an application of the pyrazinamide compound in preparation of medicines for preventing and treating GPR52 related diseases.

The present invention provides a compound or an enantiomer, diastereomer, racemate, tautomer, stereoisomer, geometric isomer, nitrogen oxide, metabolite or pharmaceutically acceptable salt, ester, solvate, hydrate, isotope-labeled compound, or prodrug thereof, having good prospects in the treatment of hyperproliferative diseases, particularly cancer, more particularly cancer associated with KAT6A and / or KAT6B.

The invention provides an application of a compound as shown in a formula I, cis-trans isomers, enantiomers, diastereoisomers, racemes, solvates, hydrates or pharmaceutically acceptable salts or prodrugs of the compound in preparation of drugs for prevention, alleviation, adjuvant therapy or treatment of lung injury, and application of the compound in preparation of drugs for prevention, alleviation, adjuvant therapy or treatment of lung injury in preparation of drugs for prevention, alleviation, adjuvant therapy or treatment of lung injury in preparation of drugs for prevention, alleviation, adjuvant therapy or treatment of lung injury. The compound shown in the formula I can obviously reduce proinflammatory cytokine tumor necrosis factor alpha (TNF-alpha) and interleukin 6 (IL-6) of an acute lung injury rat model, improve infiltration of inflammatory cells (including mononuclear / macrophage, lymphocyte and neutrophil) in lung tissues, improve pathological injury of the lung tissues, improve lung functions, and improve the curative effect of the lung. The above results show that the compound represented by the formula I can be used for prevention, alleviation, adjuvant therapy or treatment of lung injury, especially acute lung injury or a combined disease thereof or acute respiratory distress syndrome or a combined disease thereof.

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 pyrimidine compound as well as a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is shown in a formula I, and the compound further comprises enantiomers, diastereoisomers, racemes, cis-trans-isomers, deuterated compounds, metabolites, prodrugs, solvates, hydrates, pharmaceutically acceptable salts or co-crystals of the compound. The compound has high-efficiency and high-selectivity inhibitory activity on various mutants of EGFR single mutation, double mutation and triple mutation, has low activity and low toxicity on wild type EGFR, and has a good treatment effect on cancers; the problems that an existing EGFR inhibitor is poor in effect, low in selectivity, resistant to drugs and the like are solved. # imgabs0 #

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.

Provided in the present application is a compound represented by formula (I), 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 or a prodrug thereof. The compound represented by formula (I) of the present application has a relatively ideal inhibitory activity with regard to KAT6A and / or KAT6B.

Stereoselective synthesis of 3,4-diamino-1,2-diols possessing a long hydrocarbon chain was carried out via olefin cross-metathesis between a commercial tetradec-1-ene and known diastereoisomeric trichloroacetamides prepared in our laboratory. Subsequent modification of the obtained coupling products used an approach based on functional group interconversions, which was accompanied by the rational choice of deprotection protocols. The resulting molecules represent novel isomeric amino analogues of natural D-ribo-phytosphingosine, which on the basis of their structure could have the status of skin sphingomimetics, i.e. substances that can affect the properties of the skin and dermis in terms of improving the quality of the lipid matrix (e.g. change in permeability, hydration), or stimulating the biosynthesis of procollagen in deeper structures. The cytotoxic effect of the prepared aminoisophytosphingosines was examined on two human non-malignant cell lines (BJ and HaCaT) and the screening results confirmed the safety in at least three representatives of the prepared series of compounds. In addition, the ability of the synthesized derivatives to inhibit cancer cell proliferation was also investigated. The results of preliminary anticancer screening showed weaker antiproliferative potential of these unusual sphingoid bases.

The invention provides an oxime-containing compound and application thereof. The oxime-containing compound provided by the invention has a structure as shown in a formula (I) or enantiomers, diastereoisomers, racemate, tautomers, stereoisomers, geometric isomers, nitrogen oxides, metabolites or pharmaceutically acceptable salts, esters, solvates, hydrates, isotope labeled compounds or prodrugs of the structure as shown in the formula (I). The oxime-containing compound provided by the invention can be used for preventing and / or treating cancers and other hyperproliferative diseases and diseases related to Hippo pathway dysfunction. # imgabs0 #

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 #.