225 results about "Imidazopyridine" patented technology

The invention discloses an imidazo [4, 5-b] pyridine compound capable of blocking mRNA translation of tumor cells and an application of the imidazo [4, 5-b] pyridine compound in preparation of antitumor drugs for blocking mRNA translation of tumor cells, and the imidazo [4, 5-b] pyridine compound has a structure shown in a formula (I) or a pharmaceutically acceptable salt of the imidazo [4, 5-b] pyridine compound. The mRNA translation of cancer promoting protein is crucial to the occurrence and development of malignant tumors, but a small molecular compound for targeted inhibition of mRNA translation is lacked clinically at present. The invention provides an imidazo [4, 5-b] pyridine compound, which can be combined with a translation initiation factor eIF4A and inhibit the ATP-dependent RNA helicase function of the translation initiation factor eIF4A so as to block the translation of mRNA and present proliferation inhibition and apoptosis promotion functions in various tumor cells. # imgabs0 #

Disclosed herein are improved synthetic pathways for the preparation of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo [4, 5-c] pyridine-2 (3H)-one (toltinib). Also disclosed herein are novel compounds for use in the synthesis of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo [4, 5-c] pyridine-2 (3H)-one.

The invention provides an imidazo [1, 2-alpha] pyridine stimuli-responsive molecule with a D-A twisted structure as well as a preparation method and application of the imidazo [1, 2-alpha] pyridine stimuli-responsive molecule, belongs to the technical field of intelligent materials, and is used for solving the technical problem that intelligent materials for developing stimuli-responsive molecules for data encryption and information anti-counterfeiting are insufficient. The preparation method of the compounds N1 and N3 comprises the following steps: 2-aminopyridine and 2, 4 '-dibromoacetophenone are subjected to an amphiphilic reaction to obtain a compound a; the compound a and POCl3 are subjected to a Vilsmeier-Haack reaction, and a compound b is obtained; carrying out Suzuki coupling reaction on the compound a or the compound b and triphenylamine boric acid to obtain a compound N1 or N2; the compound N2 and malononitrile are subjected to a Knovenagel condensation reaction, and a compound N3 is obtained. The compound prepared in the invention has good fluorescence emission capability in a solution and a solid state and a grinding solvent acid / alkali stimulated fluorescence discoloration behavior, and can realize good data encryption and information anti-counterfeiting.

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a 6,5-heterocyclic structure (e.g., compounds having a imidazopyridine, imidazopyrimidine, imidazopyrazine, imidazopyridazine, imidazotriazine, benzoimidazole, benzotriazole, benzoisoxazole, purine, indazole, triazolotriazine, triazolopyridazine, triazolopyrimidine, triazolopyrazine, triazolotetrazine, triazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolopyridazine, pyrazolotriazine, pyrazolopyridine, isoxazolopyrazine, isoxazolopyrimidine, isoxazolopyrdiazine, isoxazolotriazine, or isoxalopyridine structure) which function as inhibitors of DYRK1A, DYRK1B, and Clk-1, and their use as therapeutics for the treatment of Alzheimer's disease, Down syndrome, diabetes, glioblastoma, autoimmune diseases, cancer (e.g., glioblastoma, prostate cancer), inflammatory disorders (e.g., airway inflammation), and other diseases.

The invention discloses an mRNA (messenger Ribonucleic Acid) vaccine of varicella-zoster virus as well as a preparation method and application of the mRNA vaccine. According to the mRNA vaccine provided by the invention, a gE antigen sequence is subjected to codon optimization; then selecting a proper promoter, 5 'UTR, 3' UTR and 3 '-terminal PolyA to combine into complete mRNA nucleic acid for coding the varicella-zoster virus, screening to obtain two groups of mRNA nucleic acid for coding the varicella-zoster virus with both expression level and stability, and adopting a novel cationic lipid imidazopyridyl lipid compound to prepare a vaccine liposome. The targeting property in drainage of lymph nodes is improved, and the humoral immunity and cellular immunity levels excited by the vaccine in animal bodies are remarkably improved.

The invention relates to the field of biological medicine, in particular to a pyruvate-based respiratory system medicine synergist as well as a preparation method and application thereof. The synergist is a modified betulin derivative, and the preparation method comprises the following steps: adding betulin and triphenylphosphine into a solvent, uniformly stirring, and adding ammonia water for reaction to prepare aminated betulin; the preparation method comprises the following steps: adding (7-chloroimidazo [1, 2-A] pyridine-2-) methanol and phosphorus oxychloride into a solvent, carrying out heating reaction, and after the reaction is completed, carrying out post-treatment on a reaction solution to obtain an intermediate 1; adding aminated betulin, the intermediate 1 and magnesium sulfate into a solvent for reaction, and performing post-treatment on the reaction liquid after the reaction to obtain an intermediate 2; and adding 1-cyclopropyl-1, 3-dihydroimidazo [4, 5-C] pyridine-2-ketone, NaH and the intermediate 2 into a solvent, carrying out a stirring reaction, and carrying out post-treatment on the reaction liquid to obtain the 1, 3-dihydroimidazo [4, 5-C] pyridine-2-ketone. The modified betulin derivative disclosed by the invention is matched with pyruvate for use, so that the treatment effect of the pyruvate is remarkably enhanced.

Provided is a method for synthesizing a compound 2-[(2R,5S)-5-[2-[(R)-1-hydroxyethyl]furo[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1 / TYK2 kinase inhibitor. The compound is prepared by nucleophilic substitution, palladium on carbon reduction, and cyclization reaction using 7-chloro-6-nitrofuro[3,2-b]pyridine as a starting material. The synthesis method has mild reaction conditions, high product yield, and high purity, and is suitable for industrial production. Further provided are a crystal form of the compound, crystal forma of its salts, and their preparation methods. The crystal form of the compound and the crystal forms of its salts have good physical and chemical properties and are suitable for drug development.

A compound can have a structure of Formula A, or derivative thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combination thereof:wherein ring A is a phenyl, indolyl, naphthyl, or benzothiazolyl; X is S, SO, or SO2; Y is a linker or bond; Z is CH, CR2, or N; Z1 is C or N to form an imidazopyridine; each Z2, Z3, or Z4 is independently CH, CR2, or N; each Z5 or Z6 is C or CH; each R1, R2, and R3 is independently a substituent, and at least one of R1, R2, or R3 is a substituent other than a hydrogen; m is 0, 1, 2, 3, or 4; and n is 0 or a positive integer. The compounds can have specific substituent patterns.

Novel imidazo[1,5-a]pyrido[4,3-e]pyrazine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The imidazo[1,5-a]pyrido[4,3-e]pyrazine compounds, identified as CK2 inhibitors, are useful as anticancer and / or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

The present invention relates to an mRNA vaccine composition for the prevention of enterovirus A71 (EV-A71) infection. The composition comprises an mRNA encoding the VP1 protein of EV-A71 and lipid nanoparticles (LNPs) comprising specific cationic lipids. Compared with the conventional cationic lipid system, the imidazopyridyl cationic lipid A5 with strong membrane fusion capability is adopted, so that obvious neutralizing antibody and cellular immune response can be induced under single-time and low-dose immune conditions, and excellent safety and children applicability are shown.

The present disclosure relates to the field of therapeutic Bruton's tyrosine kinase (BTK) inhibitors. Pharmaceutical formulations of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo [4, 5-c] pyridine-2 (3H)-one are described, as well as methods for preparing the pharmaceutical formulations.

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a 6,5-heterocyclic structure (e.g., compounds having a imidazo-pyridine structure, or compounds having a pyridinyl-purine structure) which function as inhibitors of DYRK1A, DYRK1B, and Clk-1, and are useful as therapeutics for the treatment of Alzheimer's disease, Down syndrome, diabetes (e.g., any type or form of diabetes, including type-1 or type-2), autoimmune diseases, inflammatory disorders (e.g., airway inflammation), cancer (e.g., glioblastoma, prostate cancer), diabetes, and other diseases.

The invention belongs to the technical field of biomedicine, and particularly relates to application of a sorted protein SNX3 inhibitor in preparation of drugs for proliferative retinopathy. The invention verifies that the overexpression of the sorted protein (SNX3) induces pathological angiogenesis and is a new target of pathological neovascular diseases, and a small-molecule inhibitor W1122 is identified based on the protein structure of the SNX3. The chemical structural formula of the small-molecule inhibitor W1122 is as shown in formula 1, the small-molecule inhibitor W1122 belongs to imidazo [1, 2-a] pyridine derivatives, the chemical name of the small-molecule inhibitor W1122 is N-(1, 1-dioxobenzo [b] thiophene-6-yl)-2-(7-methoxy-2-phenyl imidazo [1, 2-a] pyridine-3-yl) acetamide, the chemical formula of the small-molecule inhibitor W1122 is C24H19N3O4S, the molecular weight of the small-molecule inhibitor W1122 is 445.49 g / mol, and the small-molecule inhibitor W1122 can effectively inhibit pathological retinal angiogenesis. The result of the embodiment of the invention shows that the small-molecule inhibitor W1122 can effectively prevent and treat proliferative retinopathy by inhibiting the expression of SNX3, and shows that the sorted protein SNX3 provides a new drug target for treating the proliferative retinopathy.

The invention discloses a small molecular probe based on an imidazo [1, 5-a] pyridine skeleton, a preparation method and application, and belongs to the field of activatable small molecular fluorescent probes. The preparation method of the small molecular probe based on the imidazo [1, 5-a] pyridine skeleton comprises the following steps: dissolving 2-benzoylpyridine and ammonium acetate in acetic acid, adding salicylaldehyde, heating and stirring to generate a compound 3; and dissolving the compound 3 in dichloromethane, adding pyridine, stirring, adding 4-bromobutyryl chloride, and continuously stirring to obtain a compound 1, namely the small molecule probe. The small molecule probe can be used for detecting hydrazine in a biological system or drinking water.

The present invention addresses the problem of providing a novel method for efficiently producing an aptamer having a high affinity for a target substance. Provided is a single-stranded nucleic acid molecule library comprising a plurality of single-stranded nucleic acid molecules, the multiple single-stranded nucleic acid molecules comprise a single-stranded nucleic acid molecule containing Ds / Pa ', and the single-stranded nucleic acid molecule containing Ds / Pa' comprises a pair of primer binding regions located at the 5'terminal and the 3 'terminal of the single-stranded nucleic acid molecule and a variable region located between the pair of primer binding regions. The pair of primer binding regions is composed of a base sequence shared among the plurality of single-stranded nucleic acid molecules, and the variable region comprises a non-natural base Ds (7-(2-thienyl)-3H-imidazo [4, 5-b] pyridine-3-yl) represented by general formula (I) and a non-natural base Pa'represented by general formula (II).

The invention discloses a preparation method of methoxy imidazo [1, 5-a] pyridine, which comprises the following steps: firstly, taking a compound P1, specifically 1-methylamino-3-methoxypyridine, as an initial raw material, and carrying out carbamylation reaction in a formylation reagent to prepare a compound P2, specifically N-[(5-methoxypyridine-2-yl) methyl]; further carrying out intramolecular ring closing reaction on the compound P2 to obtain a compound P3 which is specifically 7-methoxy imidazo [1, 5-a] pyridine; then, a selective bromination experiment at the C3 position is carried out by taking a compound P3 as a parent skeleton and cyanogen bromide (CNBr) as a bromination reagent, and finally, specific bromination of the C3 site of the imidazo [1, 5-a] pyridine with the selectivity of 100% is realized. A solid theoretical basis is laid for efficient specific modification of the low-reaction-activity C3 site, and an efficient synthesis path is provided for rapid construction of the imidazopyridine derivative, so that the imidazopyridine derivative has a wide application prospect.

The present invention relates to imidazo[1,2-a]pyridine and [1,2,4]triazolo[1, 5-a]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, nonalcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

The invention provides a bidentate cobalt complex containing an imidazo [1, 2-alpha] pyridine group as well as a preparation method and application of the bidentate cobalt complex, and belongs to the technical field of organic chemical synthesis. The structural formula of the bidentate cobalt complex is shown in the specification, and the preparation method comprises the following steps: carrying out bromination reaction and cyclization reaction on 2-methoxy-6-acetylpyridine to obtain a bidentate ligand with methoxy and imidazo [1, 2-alpha] pyridyl, and carrying out demethylation reaction on the ligand to obtain another bidentate cobalt complex with hydroxyl and imidazo [1, 2-alpha] pyridyl. The imidazo [1, 2-alpha] pyridyl-containing bidentate cobalt complexes are prepared from imidazo [1, 2-alpha] pyridyl-containing bidentate ligands, and the two ligands react with anhydrous cobalt chloride respectively to obtain various imidazo [1, 2-alpha] pyridyl-containing bidentate cobalt complexes. The electron effect of the complex is adjusted by changing substituent groups on imidazo [1, 2-a] pyridine groups, then the activity of the complex in catalytic reaction is adjusted, and the complex can be further applied to hydrosilylation reaction of styrene and has very important application prospects.

This blue phosphorescent material includes: a central metal containing iridium; and a phenyl-imidazopyridine ligand which is a bidentate ligand of the central metal and has an iridium-carbon bond with the central metal, wherein the ligand may include a ligand in which a 2,6-dimethylphenyl functional group has been introduced to a phenyl group of the ligand. The present application relates to a blue phosphorescent material, a production method thereof, and photophysical properties thereof, the blue phosphorescent material having an iridium-carbon bond and including a phenyl-imidazopyridine ligand to which a sterically hindered functional group has been introduced.

Provided herein are pharmaceutical formulations of the AKT1 E17K selective inhibitor 4-((1-(4-(2-(2-aminopyridin-3-yl)-5-(5-fluoropyridin-2-yl)-3H-imidazo[4,5-b]pyridin-3-yl)benzyl)piperidin-4-yl)amino)pyrimidine-2-carbonitrile maleate.

Provided is a compound selected from a compound of chemical formula 1 having lysine-specific demethylase-1 (LSD1) inhibitory activity, and a tautomer, a stereoisomer, and a solvate thereof, and pharmaceutically acceptable salts of the aforementioned components. The compound is effective in the prevention or treatment of diseases caused by abnormal activation of LSD1. Also disclosed is a composition containing the compound as an active ingredient and its uses in preventing and / or treating diseases caused by abnormal activation of LSD1.

The present invention provides compounds capable of inhibiting ERK5. Also provided are pharmaceutical compositions and pharmaceutical uses thereof, including in the treatment or prevention of conditions such as cancer.

The disclosure provides a method of treating, ameliorating, and / or preventing retinal degenerations, such as but not limited to anterior segment ocular disorders and / or age-related macular degeneration (AMD), in a subject. In certain embodiments, the method comprises administering to the subject a therapeutically effective amount of a compound of the disclosure. In certain embodiments, the compound of the disclosure prevents and / or minimizes cellular assault, such as oxidative stress-related cellular assault, and / or promote cell viability.

In the novel salt of the imidazo [1, 2-a] pyridine compound, the crystal form thereof and the preparation method of the novel salt of the imidazo [1, 2-a] pyridine compound, the novel salt of the imidazo [1, 2-a] pyridine compound is azetidine-1-yl {8-[(2, 6-dimethyl benzyl) amino]-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl} ketone citrate.

An imidazopyridine pyrimidone compound, a preparation method therefor and a use thereof. The imidazopyridine pyrimidone compound, or a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutically acceptable salt thereof or a mixture thereof has a structure represented by formula I or formula II. R1 and R2 are each independently selected from phenyl, naphthyl, and phenyl substituted by at least one of halogen, C1-6 alkyl, C1-6 alkoxy, halogen-substituted C1-6 alkyl, and cyano; R3 is one or more substituents; and R3 is selected from C1-4 alkyl, halogen-substituted C1-4 alkyl, and halogen. The compound can have a better HsClpP protease agonist effect than the currently reported positive compounds, and can be used for treating HsClpP receptor agonist-related diseases.

Provided herein are various forms and compositions of N- (5- (5-((1R, 2S) -2-fluorocyclopropyl) -1, 2, 4-oxadiazol-3-yl) -2-methylphenyl) -7- ( (2-hydroxy-2-methylpropoxy) methyl) imidazo [1, 2-a] pyridine-3-carboxamide useful as a selective inhibitor of c-kit kinase and uses of the same in the treatment of c-kit kinase associated diseases.

The present invention relates to a compound selected from (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine and a pharmaceutically acceptable salt thereof, and in particular to the phosphate salt of (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, both having preferably an enantiomeric excess of the (R) form higher than or equal to 97%. Furthermore, the present invention relates to pharmaceutical compositions comprising the same, their use as a medicament and in methods of treatment of diseases and disorders in humans including women of child bearing potential and pediatric patients in which aldosterone over-exposure contributes to the deleterious effects of said diseases or disorders, as well as processes for preparing said inventive compounds.

This disclosure relates to the field of therapeutic Bruton's tyrosine kinase (BTK) inhibitors. Pharmaceutical formulations of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo[4,5-c]pyridin-2(3H)-one are described.