2515 results about "Stereochemistry" patented technology

This invention provides a tetrahedral antibody comprising a first, second, third, and fourth domain, wherein the first and second domains are Fab or Fc domains; wherein each of the first and second domains comprise a first polypeptide chain comprising a first N-terminus of the domain, and a second polypeptide chain comprising a second N-terminus of the domain; wherein the first N-terminus of the first domain and the first N-terminus of the second domain are joined to each other by a non-peptidyl linkage, which can be a covalent linkage or a non-covalent linkage between first and second dimerizing polypeptides attached to the first N-termini of the first and second domains, respectively; and wherein the third and fourth domains are attached at their respective C-termini to the second N-termini of the first and second domains, respectively, or the N-termini of the first and second dimerizing polypeptides.

The invention discloses a cyclic nonapeptide with repairing and anti-oxidation effects and application of the cyclic nonapeptide, the amino acid sequence of the cyclic nonapeptide is cyclic (arginine-glycine-aspartic acid-serine-arginine-lysine-valine-lysine-serine), the prepared cyclic nonapeptide has the repairing and anti-oxidation effects, and the cyclic nonapeptide has the repairing and anti-oxidation effects. The composition can be applied to preparation of cosmetics with repairing and / or anti-oxidation effects.

Compositions for delivering ketone bodies to a subject include one or more beta-hydroxybutyrate salts, one or more acetoacetate salts, beta-hydroxybutyric acid, and optionally acetoacetic acid. The compositions may optionally include one or more ketone body esters, such as one or more beta-hydroxybutyrate esters and / or one or more acetoacetate esters. An example composition contains about 2% to about 98% on a molar basis of the one or more beta-hydroxybutyrate salts and the one or more acetoacetate salts, about 2% to about 98% on a molar basis of the beta-hydroxybutyrate free acid and optionally the acetoacetate free acid, and optionally about 2% to about 98% on a molar basis of one or more ketone body esters.

Disclosed in the present invention is a novel substituted heterocyclic compound having VAV1 target degradation activity. Specifically disclosed is a compound serving as a VAV1 target degradation agent and having the structure of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer of the compound. The compound can be used for preventing or treating diseases related to VAV1 targets or signaling pathways.

The present invention relates to a process for producing a chiral aromatic amine, said process comprising the steps of: a) providing an aromatic imine, and b) contacting said aromatic imine from step a) with an imine reductase, thereby stereoselectively reducing said aromatic imine to a chiral aromatic amine with said imine reductase; and to novel imine reductases capable of catalytic reactions.

A method for producing an aromatic heterocycle-substituted difluoroacetic acid derivative having a partial structure represented by the formula (III), by reacting an N-oxido aromatic heterocyclic compound having a partial structure represented by the formula (I) with tetrafluoroethylene in the presence of a compound represented by the formula (II): R—YH, in a solvent selected from an aromatic hydrocarbon solvent, an ester solvent and an ether solvent:

The invention discloses hydrolysis-resistant liquid phosphite ester and a preparation method and application thereof.The hydrolysis-resistant liquid phosphite ester is prepared by the steps that 2, 2, 4-trimethyl-1, 3-pentanediol and phosphorus trichloride or phosphite triester serve as raw materials, a cyclization reaction is conducted firstly, and then the hydrolysis-resistant liquid phosphite ester is obtained; and then carrying out nucleophilic substitution on Cl or aryl and alkyl on the cyclized intermediate by using higher saturated monohydric alcohol with more than C8, wherein the molecular structure is as shown in formula I in the specification. The liquid phosphite ester is novel liquid phosphite ester, the main body of the liquid phosphite ester is of a six-membered ring structure, the basic structure of the phosphite ester is reserved to the maximum extent, and the anti-oxidation effect of the phosphite ester is guaranteed; hydrophobic aliphatic chain structures on phosphorus atoms and branched chains of the phosphorus atoms prevent water molecules from approaching P-O bonds, so that the phosphorus atoms and the branched chains are prevented from being attacked by the water molecules, and the hydrolysis resistance is improved under the conditions that any additional amine hydrolysis-resistant agent is not used and any steric hindrance group is not introduced; good practical value, economic value and market prospect are realized.

The invention relates to a synthesis method of a diunsaturated ester compound catalyzed by N-heterocyclic carbene, and belongs to the field of organic synthesis. According to the preparation method, the synergistic effect of N-heterocyclic carbene and light is utilized, gamma-oxo unsaturated aldehyde and Katritzky salt are taken as starting raw materials, the Katritzky salt generates alpha-ester free radicals through a single electron transfer process under the illumination condition, the free radicals react with a nucleophilic trienol intermediate generated through catalysis of the N-heterocyclic carbene, and the alpha-ester free radicals react with the nucleophilic trienol intermediate to generate the gamma-oxo unsaturated aldehyde. Target products are obtained with good yield and high regioselectivity, so that a series of epsilon-alkylated diunsaturated ester compounds are efficiently synthesized. The method is simple and convenient to operate, green and efficient, has the advantages of no transition metal participation, wide substrate applicability and the like, provides a new way for synthesis of the diunsaturated ester compound, and has a wide application prospect.

The present invention provides compounds of formula I for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), interferonosis, nonalcoholic steatohepatitis (NASH), interstitial lung disease (ILD), and idiopathic pulmonary fibrosis (IPF). JPEG2026504613000125.jpg8493 (in the formula, R 1 , R 2 , R 3 , R 4 , A, D, E, G, J, K, and L are as defined in claim 1), and prodrugs, deuterated analogs, and pharmaceutically acceptable salts thereof.

The invention relates to a stevioside composition, which comprises at least one stevioside and at least one of siamenoside I, mogroside V, mogroside III-E and mogroside II-E, and is characterized in that the stevioside composition comprises at least one stevioside and at least one of siamenoside I, mogroside V, mogroside III-E and mogroside II-E; wherein the stevioside has a higher solubility in the composition than in an equivalent composition lacking siamenoside I, mogroside V, mogroside III-E, and mogroside II-E. The invention also relates to a method for preparing the stevioside composition. The composition may be an aqueous solution.

The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).

The invention belongs to the field of organic synthesis, and discloses an aldol condensation reaction method and a catalyst thereof.The method comprises the steps that in the presence of a composite catalyst, a substrate 1 and a substrate 2 are subjected to an aldol condensation reaction, after the reaction is finished, an aldol condensation product is collected from reaction products, according to the method, aldol condensation reaction of fatty aldehyde or aromatic aldehyde is catalyzed by adopting the novel composite catalyst, and the method has the advantages of being mild in reaction condition, environmentally friendly, efficient and simple in post-treatment.

The present disclosure is directed to HLA class II molecules having a higher affinity for CD4 than naturally occurring HLA class II molecules. In certain aspects, the HLA class II molecule comprises a DQ beta chain having (i) an amino acid other than leucine at a position corresponding to amino acid residue 114 of SEQ ID NO: 1, (ii) an amino acid other than valine at a position corresponding to amino acid residue 143 of SEQ ID NO: 1, (iii) or both (i) and (ii). Certain aspects of the present disclosure are directed to nucleic acid molecules encoding the HLA class II molecules, vectors comprising the nucleic acid molecule, cells comprising the same, and methods of use thereof.

The invention provides a reduced coenzyme Q10 and gamma-aminobutyric acid eutectic crystal and a preparation method and application thereof, and belongs to the technical field of eutectic crystal manufacturing. In the eutectic crystal, the molar ratio of the reduced coenzyme Q10 to the gamma-aminobutyric acid is 1: 2, and the structural formula of the eutectic crystal is as shown in formula I. The eutectic crystal has the advantages of good stability, low cytotoxicity and strong oxidation resistance.

The invention relates to a CHRM4 receptor agonist and application thereof. The invention discloses a compound shown as a formula (I), or a stereoisomer, a deuterated compound, a solvate, a co-crystal or a pharmaceutically acceptable salt of the compound, a pharmaceutical composition of the stereoisomer, the deuterated compound, the solvate, the co-crystal or the pharmaceutically acceptable salt, and application of the stereoisomer, the deuterated compound, the solvate, the co-crystal or the pharmaceutically acceptable salt in preparation of drugs for treating / preventing CHRM4-mediated diseases, and all groups in the formula (I) are defined as in the specification.

The present invention relates to a process for preparing B-[(7α,17β)-17-hydroxy-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-trien-3-yl]-boronic acid, also known as Fulvestrant-3-boronic acid or ZB716, whose structure is reported below.

The invention discloses a polypeptide compound, a composition containing the same and application, and belongs to the technical field of medicines. The invention discloses a polypeptide compound as shown in a formula I, an isomer thereof or a pharmaceutically acceptable salt thereof, and also discloses a composition which comprises the polypeptide compound, the isomer thereof or the pharmaceutically acceptable salt thereof. The invention discloses application of a polypeptide compound, an isomer or pharmaceutically acceptable salt thereof and a composition in preparation of a medicine for treating or / and preventing CaSR receptor related diseases. The polypeptide compound shown in the formula I shows relatively high agonistic activity on CaSR, and is safe and effective.

The invention relates to an L-proline heterocyclic intermediate, alpha-methyl-L-proline hydrochloride and a preparation method thereof, which comprises the following steps: step 01, cyclization upper protection: taking L-proline as a raw material, which is shown in a formula (1), to react with trichloracetic aldehyde hydrate under an acidic condition, and performing upper protection to obtain a heterocyclic intermediate as shown in a formula (2); the molar weight of chloral hydrate is 1-2.5 times of the molar weight of the L-proline shown in the formula (1), preferably 1.5 times of the molar weight of the L-proline shown in the formula (1). 02, methylation: reacting the heterocyclic intermediate as shown in the formula (2) obtained in the step 01 with lithium diisopropylamide, and after the reaction is completed, adding dimethyl sulfate for methylation to obtain an intermediate as shown in a formula (3); 03, deprotection: adding the intermediate as shown in the formula (3) obtained in the step 02 into a deprotection reagent for hydrolysis so as to obtain the alpha-methyl-L-proline hydrochloride as shown in the formula (4), so that the problems that the preparation cost of the existing alpha-methyl-L-proline hydrochloride is relatively high and the yield is relatively low can be solved.

Provided herein are multispecific antigen-binding polypeptide constructs comprising at least two different heterodimers, each comprising a heavy chain and a light chain. At least one heterodimer comprises a Fab region comprising a lambda light chain and at least one heterodimer comprises a Fab region comprising a kappa light chain. One or more of the immunoglobulin heavy and light chains that form the antigen-binding polypeptide construct comprise amino acid modifications that promote correct pairing between the heavy and light chains to form the desired multispecific antigen-binding polypeptide construct. The amino acid modifications may be in the CH1 and / or CL domains, in the VH and / or VL domains, or a combination thereof.

The present invention relates to the preparation of cyantraniliprole, comprising the preparation of 8-methyl-2,4-dioxo-1,4-dihydro-2H-benzo[d][1,3]oxazine-6-carbonitrile key intermediate via 2-amino-5-((hydroxyimino)methyl)-3-methylbenzoic acid. Wherein hydroxylamine attacks a benzylic formyl group, to obtain the 2-amino-5-((hydroxyimino)methyl)-3-methylbenzoic acid, that undergoes simultaneously or by consecutive steps dehydrogenation and cyclization to obtain the benzo[d][1,3]oxazine group and the cyano group of the desired product. In addition, an improved method for the synthesis of the benzylic formyl group is also displayed.

The invention relates to the technical field of compound synthesis, in particular to an intermediate of gepodalin, a preparation method of the intermediate and a preparation method of gepodalin. The intermediate of gepodamycin is selected from any one of compounds shown in the following structural formula, and in the formula, X represents halogen, and R1 represents a hydroxyl protecting group; r2 represents an amino protecting group, and R3 represents a C1-C10 alkyl group. The intermediate can be synthesized to obtain the core intermediate of gepodamycin through a series of new synthesis steps, and the yield, the purity and the post-treatment difficulty of the core intermediate can be improved, so that the production cost of gepodamycin is greatly reduced.

Described herein is GLP-1R agonists and pharmaceutical compositions comprising the said compound. The subject compound and compositions are useful for the treatment of a GLP-1 associated disease or disorder, including Type 2 diabetes or obesity.

A novel salt form of Compound (I) represented by the following structural formula, and its corresponding pharmaceutical compositions, are disclosed.Particular single crystalline forms of 1:1 Compound (I) tartrate salt are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms are also disclosed. The present disclosure also provides methods of treating cancer in a subject.

The invention provides a preparation method of milbemycin oxime A4, which comprises the following steps: under an acidic condition, carrying out hydrolysis disaccharide removal reaction on tenvermectin B to obtain tenvermectin B aglycone; the preparation method comprises the following steps: carrying out silicon-based protection on tenvermectin B aglycone by adopting a silicon-based protection reagent to obtain 5-hydroxyl silicon-based tenvermectin B aglycone; the preparation method comprises the following steps: brominating 5-hydroxyl silicon-based tenvermectin B aglycone by adopting a brominating reagent to obtain 13-bromine-5-hydroxyl silicon-based protected tenvermectin B aglycone; the preparation method comprises the following steps: reducing 13-bromo-5-hydroxyl silicon group protected tenvermectin B aglycone by using a reducing agent to obtain 5-hydroxyl silicon group protected milbemycins A4; the milbemycins A4 protected by the 5-hydroxyl silicon group is subjected to desilicication protection treatment, and the milbemycins A4 is obtained; oxidizing milbemycins A4 by adopting an oxidizing agent to obtain 5-ketomilbemycins A4; the preparation method comprises the following steps: reacting 5-ketomilbemycins A4 with hydroxylamine hydrochloride to obtain milbemycins A4, and efficiently preparing the active component milbemycins A4 single component by taking tenvermectin B as a raw material.

The present invention relates to a compound of the formula (i) wherein Ar represents a phenyl or a 6-membered heteroaryl group, R1 and R2 represent independently a hydrogen atom or a deuterium atom, R3 represents (1) a —COR4 group, (2) a —BOR5OR6 group, (3) a —X—Z group, (4) a (C1-C6)alkyl group or a (C1-C6)alkenyl group, (5) a —X—S(O)n(R7)p(R8)q group, (6) a halogen atom, a —NH2 group or a —CN group, (7) a —O—R11 group, (8) a —NH—COR9 group, (9) a —C(═NH)NHOH group, (10) a —NH—C(NH)—R9′ group, or (11) a —NHCOCOOR12 group or a —NHCOCONR12′R12″ group, X represents a bond, a —NH— group, a —CONH— group or a —CO— group, Z represents a 4 or 5-membered cycloalkyl, a 4 or 5-membered heterocylcloalkyl group, a 4 or 5-membered heteroaryl group or a phenyl group or a pharmaceutically acceptable salt thereof. The present invention further relates to a medicament comprising said compound of formula (I) and to said compound of formula (I) for use as an inhibitor and degrader of estrogen receptors.

The invention relates to the technical field of pharmaceutical preparations, in particular to a pure drug-based nano preparation constructed by super-solubilization of a natural polyphenol material and a biguanide drug and a preparation method of the pure drug-based nano preparation. The pure drug-based nano preparation constructed by super solubilization of the natural polyphenol material and the biguanide drug provided by the invention is composed of the natural polyphenol material and the biguanide drug, and a phenolic hydroxyl group of the natural polyphenol material and an amino group of the biguanide drug are self-assembled into the nano preparation through electrostatic interaction and hydrophilic and hydrophobic effects, namely the pure drug-based nano preparation. The mass ratio of the natural polyphenol material to the biguanide drug is 1: (0.0001-10000). The pure drug-based nano preparation provided by the invention has the advantages of high drug loading capacity, simple preparation process, greenness, high efficiency, safety and suitability for industrial application.