84 results about "Diastereomer" patented technology

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.

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.

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.

This invention belongs to the field of organic ligand technology, and specifically discloses a phosphoxazolin ligand having the structure shown in general formula I or general formula II, or its tautomers, enantiomers and diastereomers: , R 1 Selected from hydrogen, alkyl, perfluoroalkyl, alkoxy, aryl; R 2 Selected from hydrogen, alkyl, perfluoroalkyl, alkoxy, aryl; R 3 Selected from alkyl, cycloalkyl, alkenyl, and aryl; R 4 Selected from alkyl, cycloalkyl, alkoxy, perfluoroalkyl, aryl, and fluorine atoms; R 5 Selected from hydrogen, alkyl, cycloalkyl, alkoxy, perfluoroalkyl, aryl, and fluorine atoms; R 6 The substituents are selected from hydrogen, alkyl, cycloalkyl, alkoxy, perfluoroalkyl, aryl, and fluorine atoms; n and m are the number of substituents, where n+m≤5. This invention also discloses a method for preparing phosphosoxazoline ligands and their application in catalytic allylation, bicyclization, intermolecular desymmetry, or intramolecular condensation reactions of nitrile derivatives.

This invention relates to a phosphate-containing chiral diastereomeric oxime ester compound, its preparation method, and its applications, belonging to the field of organic synthesis technology. This invention introduces a chiral center at a specific location in the molecular structure of the oxime ester compound to form a mixture of diastereomeric stereoisomers. The introduction of the chiral center interferes with intermolecular chiral recognition, thereby effectively suppressing the π-π stacking effect and crystal growth between the aromatic ring cores. Furthermore, the introduction of the phosphate ester structure into the product effectively improves its solubility in propylene glycol methyl ether acetate or cyclohexanone solvents. The photocurable ink prepared using the diastereomeric oxime ester compound of this invention exhibits excellent storage stability and better photosensitivity.

The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, solvates, adducts, polymorphs, isomers such as stereoisomers and diastereomers, or derivatives thereof, that are useful as orexin antagonists, their preparation, their use in pharmaceutical compositions, and methods of using orexin antagonists to treat or prevent a disease or disorder mediated by orexin receptor activity.

The present invention provides pyridazine-3-carboxamide compounds of general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention also provides pharmaceutical compositions comprising said compounds, processes for their preparation and their use in the treatment or prevention of TYK2 kinase-mediated diseases.

The invention provides a method for chiral resolution of (trans)-2,2-dichloro-3-(3-chloro-4-fluorophenyl)cyclopropane-1-carboxylic acid. The method comprises the steps of: (a) treating (trans)-2,2-dichloro-3-(3-chloro-4-fluorophenyl)cyclopropane-1-carboxylic acid with a chiral base selected from the list consisting of: quinine, R )-1-cyclohexylethan-1-amine, S )-1-cyclohexylethan-1-amine and L )-leucinamide, in an organic solvent to form a suspension, (b) separating the desired enantiomer and diastereomeric salt of the chiral base from the suspension, and (c) optionally, treating the separated diastereomeric salt with an acid to obtain the desired enantiomer of 2,2-dichloro-3-(3-chloro-4-fluorophenyl)cyclopropane-1-carboxylic acid.

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.

The present invention relates to a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof and to pharmaceutical compositions comprising a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, in the treatment of fibrotic diseases, preferably idiopathic pulmonary fibrosis (IPF) or non-alcoholic steatohepatitis (NASH). Further aspects of the present invention include combination therapies in which a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, is used in combination with a known anti-fibrotic or anti-inflammatory agents for fibrotic diseases.

The present application relates to an amide compound, a pharmaceutical composition thereof, and use thereof. The amide compound is selected from a compound of formula (I), a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, an atropisomer thereof, and a pharmaceutically acceptable salt thereof. The present application develops a series of novel amide compounds. The amide compound has excellent anti-HIV activity and the ability to inhibit HIV capsid protein binding, and is suitable for intravenous administration, oral administration, and subcutaneous administration. The amide compound has a long half-life and high drug exposure in vivo, and thus possesses the potential to develop long-acting drugs. Also, the amide compound has good metabolic stability, low or medium penetrability and a high protein binding rate in cells, no significant inhibitory effects on various CYP enzymes, and high safety. The amide compound is promising for use against HIV infection.

The application belongs to the field of medicinal chemistry, and specifically discloses a kind of protein tyrosine phosphatase (PTPN) inhibitor as shown in formula I and enantiomers, diastereoisomers, tautomers or pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition and a pharmaceutical use thereof.The application also discloses a method for treating cancer, metabolic diseases and other related diseases using the protein tyrosine phosphatase inhibitor.I.

The present invention provides pyridazine-3-carboxamide compounds of general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention also provides pharmaceutical compositions comprising said compounds, processes for their preparation and their use in the treatment or prevention of TYK2 kinase-mediated diseases.

This invention belongs to the field of compound analysis and provides a method for detecting the content and isomer ratio of hydroxypropyltetrahydropyranotriol using high-performance liquid chromatography-differential refractive index (HPLC-DRI). The method includes the following steps: qualitative and quantitative analysis of prepared standard solutions and test solutions using HPLC-DRI. The method provided by this invention uses a simple and clean mobile phase with no impact on human health, simplifies sample pretreatment, has a low detection limit for hydroxypropyltetrahydropyranotriol, exhibits good linearity within the linear range, high correlation coefficient, high resolution of diastereomers, and good repeatability. It provides an effective detection method for ensuring the quality of hydroxypropyltetrahydropyranotriol and screening for superior grades.

Disclosed are a pyrimidine carboxamide compound and an application thereof. Further provided are a pyrimidine carboxamide compound represented by formula (I), or a tautomer, mesomer, racemate, enantiomer, or diastereomer thereof, a mixture form thereof, or a pharmaceutically acceptable salt thereof. The compound can be used as a Vanin enzyme inhibitor, and can be used to prepare a drug for treating various diseases, including Crohn's disease, ulcerative colitis, and so on.

Disclosed in the present invention are a nitrogen-containing heteroaryl compound, a preparation method therefor and the use thereof. The present invention specifically relates to a compound represented by formula (I) for treating cancer, and an isotope-labelled substance, enantiomer, diastereomer, atropisomer, solvate, prodrug or pharmaceutically acceptable salt thereof. The compound of the present invention has good inhibitory activity against WRN, and has good application prospects.

The application discloses a tricyclic compound as shown in general formula I or an enantiomer, a diastereomer, a racemate and a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, the compound has strong STING agonistic activity in THP1-Dual cells, can be used for preparing a medicine for treating diseases related to the function of STING protein, has the prospect of being used for preparing a medicine for treating inflammatory diseases, autoimmune diseases, infectious diseases or tumor-related diseases, and provides a reliable way for clinical application.

Provided in the present invention are a nitrogen-containing compound and the use thereof. The nitrogen-containing compound of the present invention is a compound as represented by formula (I), or a solvate, tautomer, enantiomer, diastereomer, isotopically labeled compound (preferably a deuterated compound) or pharmaceutically acceptable salt of the compound as represented by formula (I). The compound can be used in the preparation of a drug for preventing or treating inflammation-related diseases and / or diseases associated with necroptosis and autophagy.

Provided is a compound represented by general formula (I), or a tautomer, mesomer, racemate, enantiomer, diastereomer, or pharmaceutically acceptable salt thereof, and use thereof for preparing an antiviral protease inhibitor drug.

The present invention relates to a NMDA receptor antagonist and a use thereof. The NMDA receptor antagonist of the present invention is a compound of formulas II and III below, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a tautomer, a solvate, an isotopic substituent, a polymorphic substance, a prodrug or a metabolite thereof. The present invention also provides a pharmaceutical composition comprising these compounds, and a use of these compounds in treating or preventing NMDA receptor-mediated diseases.

The application discloses a preparation method of a Ledipasvir intermediate (S)-5-(tert-butoxycarbonyl)-5-azaspiro[2,4]heptane-6-carboxylic acid and an intermediate compound thereof, and belongs to the technical field of synthesis of pharmaceutical intermediates. The method uses N-tert-butoxycarbonyl glycine and (R)-alpha-methyl benzylamine as starting materials, and generates a diastereoisomer mixture of (S)-3A and (R)-3B through amide condensation and intramolecular N-alkylation ring closure reaction, and obtains the target configuration intermediate compound (S)-3A through solvent recrystallization and mother liquor racemization reaction and recrystallization. Further, (S)-3A is further subjected to one-pot deprotection of double protection groups and amino protection to obtain the target product. The yield of the target intermediate configuration obtained by the application can reach 86.7%, the chiral purity of the product is greater than 99%, the operation is simple, the conditions are mild, the reaction stability is high, the recycling of non-target configuration compounds is realized, and the industrialized production is easy.

This invention relates to pharmaceutically acceptable salts, entantiomers or diastereomers of novel compounds of the Formula (Im1) wherein R1, R2, R3, A1, Cy1 and E are as defined in the specification, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention furhter relates to pharmaceutical compositions of the pharmaceutically acceptable salts, enantiomers or diastereomers of novel compounds for use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

The application provides a resolution method of clemastine fumarate intermediate, comprising the following steps: 1) reacting racemic N-methyl-2-(2-chloroethyl)pyrrolidine with a chiral resolving agent in a first organic solvent to obtain a diastereomeric salt solution; 2) purifying the material after the reaction in step 1) by cooling and crystallization, and filtering to obtain R-N-methyl-2-(2-chloroethyl)pyrrolidine resolving agent salt; 3) dissolving the R-N-methyl-2-(2-chloroethyl)pyrrolidine resolving agent salt obtained in step 2) in a second organic solvent-water two-phase system, adjusting the pH value to 9-13, then separating the organic phase, and concentrating to obtain R-N-methyl-2-(2-chloroethyl)pyrrolidine; wherein the chiral resolving agent is at least one selected from L-di(3,5-dinitrobenzoyl) tartaric acid and L-di-p-chlorobenzoyl tartaric acid. By using a specific chiral resolving agent, the resolution efficiency of racemic N-methyl-2-(2-chloroethyl)pyrrolidine is significantly improved, and combined with cooling and crystallization and two-phase acid adjustment replacement, the operation is simple, and the cost is controllable.

This invention provides a method for detecting related substances in Reganosine starting materials. The method is a high-performance liquid chromatography (HPLC) method. The related substances include residual impurities in the starting materials, process by-product impurities, and diastereomers of the Reganosine starting materials. The chromatographic conditions are: mobile phase A: aqueous acetic acid; mobile phase B: methanol; gradient elution. The method provided by this invention can effectively separate 2-chloroadenosine and its impurities. Furthermore, studies on the specificity, accuracy, precision, limit of detection, limit of quantitation, linear range, and robustness of the method demonstrate that this detection method has high specificity and high sensitivity.

Disclosed herein are novel catalysts for producing remdesivir in one-pot manner, in which a diastereomerically enriched form of an intermediate, which following acidic hydrolysis would give rise to the desired remdesivir, was produced with the aid of the disclosed novel catalysts. Also disclosed herein is an improved process for the preparation of remdesivir without the need to separate one of the enantiomers while minimizing the formation of undesired isomers, thus offers economic advantages for operation on a commercial scale.

The specification relates to a compound of formula (I), its enantiomer, diastereomer, or its physiologically acceptable salt thereof, along with a composition containing the same; wherein Q, J, R1, R2, R3, R4 and Ra are as disclosed herein The compound or composition have potential for use as a cryopreservation agent or an ice crystal recrystallization inhibitor. In addition, disclosed is a method for cryopreserving a biological material. Further, disclosed is a process for preparation of the compound.

The present invention provides a method for preparing finerenone by means of resolving a racemate with a diastereomeric tartaric ester, and also relates to diastereomer salts (VIIa), (VIIb), (VIIc) and / or (VIId). The resolving method uses a chiral substituted tartaric ester represented by general formula (VIa) or (VIb) as a resolving agent to resolve a racemate represented by formula (V) to obtain a compound represented by formula (Va) and / or (Vb). The racemate is firstly added into a solvent mixture to be heated until completely dissolved; then the resolving agent is added to obtain a homogeneous system; and resolution is performed by stirring for crystallization.