138 results about "Imidazopyridine" patented technology

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.

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 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 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.

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 invention discloses imidazopyridine derivatives and application thereof, a pharmaceutical composition and a pharmaceutical preparation, and belongs to the technical field of medical chemistry. The technical problems to be solved are that the existing P2X3 receptor inhibitor is poor in safety, low in P2X3 or P2X2 / 3 selectivity, poor in metabolic stability and the like. According to the key points of the technical scheme, the imidazopyridine derivative is selected from a compound as shown in a formula I or a racemate, a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, an isotope label, a solvate, a polymorphic substance, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof.

The present invention relates to a novel salt of an imidazo[1,2-a] pyridine compound, and more specifically, to azetidin-1-yl\{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl\}methanone diphosphate and a method for preparing same. The azetidin-1-yl\{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl\}methanone diphosphate according to the present invention has excellent solubility, volume density, light / temperature stability, acid / base stability, and the like, and thus can be usefully used in the formulation of pharmaceuticals.

The present invention provides a novel imidazopyridine compound, an optical isomer thereof, or a pharmaceutically acceptable salt thereof. The novel compound according to the present invention effectively inhibits the enzymatic activity of Bruton's tyrosine kinase (BTK), and thus can be advantageously used as a pharmaceutical composition for the prevention or treatment of BTK-mediated diseases, such as autoimmune diseases or cancers.

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]pyridin-2(3H)-one are described.

The application discloses an imidazopyridine derivative and application, a pharmaceutical composition and a pharmaceutical preparation, and belongs to the technical field of medicinal chemistry. The technical problems to be solved are that existing P2X3 receptor inhibitors have poor safety, low selectivity for P2X3 or P2X2 / 3 and poor metabolic stability. The technical solution is that an imidazopyridine derivative is selected from the compounds shown in the formula I or racemates, stereoisomers, geometric isomers, tautomers, nitroxides, hydrates, isotopically labeled compounds, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts or prodrugs.

The invention relates to a stable imidazo [1, 2-a] pyridine derivative pharmaceutical composition and application thereof.The pharmaceutical composition comprises an active pharmaceutical ingredient and auxiliary materials, the active pharmaceutical ingredient is (azetidine-1-yl) (8-(2, 6-dimethyl benzylamino)-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl) ketone or salt thereof, and the auxiliary materials are selected from the group consisting of 2-(2, 6-dimethyl benzylamino)-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl)-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl) ketone or salt thereof. The auxiliary material comprises one or more selected from cyclodextrin or salts thereof, and the pharmaceutical composition also comprises a nitrite scavenger.

The present invention relates to a compound of formula (I) or a stereoisomer, or tautomer, (I) wherein A1, A2, R1 and R2, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and / or treatment of an infection caused by pestivirus in an animal.

The present disclosure relates to [18F]-labeled imidazopyridine derivatives or salts thereof as positron emission tomography (PET) radiotracers suitable for imaging the stress-signaling non-receptor tyrosine kinase c-abl, and their use in in vivo diagnosis, preclinical and clinical imaging, patient stratification on the basis of mutational status of c-abl and assessing response to therapeutic treatments. The present disclosure furtherrelates to the use of [18F]-labeled imidazopyridine derivatives as PET radiotracers. Thedisclosure also provides a process for the radiosynthesis of [18F]-labeled imidazopyridinederivatives.

Macrocyclic peptides (MPs) are a class of compounds that have been shown to be particularly well suited for engaging difficult protein targets. However, their utility is limited by their generally poor cell permeability and bioavailability. The present disclosure reports an efficient solid-phase synthesis of novel MPs by trapping a reversible intramolecular imine linkage with a 2-carbonyl pyridine to create an imidazopyridinium (IP+)-linked ring. This chemistry is useful for the creation of macrocycles of different sizes and geometries, including head-to-side and side-to-side chain configurations. Many of the IP+-linked MPs exhibit far better passive membrane permeability than expected for "beyond Rule of 5" molecules, in some cases exceeding that of much lower molecular weight, traditional drug molecules. This chemistry has been demonstrated to be suitable for the creation of libraries of IP+-linked MPs and show that these libraries can be mined for protein ligands.

The application belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of Zolpidem. The method uses 2-(6-methyl-2-(p-tolyl) imidazo[1,2-a]pyridine-3-yl) acetaldehyde as a reaction raw material, and prepares Zolpidem through catalytic oxidation reaction with N,N-dimethylformamide. The preparation method has the advantages of safe operation, simplicity, environmental friendliness, short reaction steps, and high yield and purity of the prepared Zolpidem.

This invention discloses a method for synthesizing an intermediate of retinoic acid, relating to the field of pharmaceutical organic synthesis technology, comprising the following steps: S1, in the presence of a base, 2-amino-3-chloropyridine and 4-bromopiperidine undergo a nucleophilic substitution reaction in solvent A to prepare compound III; S2, in the presence of a catalyst and ammonia solution, compound III undergoes an amination reaction in solvent B to prepare compound II; S3, compound II is dissolved in solvent C, and sequentially undergoes CDI cyclization and hydrogen chloride solution salt formation to prepare compound I, namely 1-(piperidin-4-yl)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one. This invention is low-cost, uses mild reaction conditions, has a simple synthesis process, high yield, and eliminates the need for expensive and potentially unsafe excipients, effectively improving reaction safety, being environmentally friendly, and suitable for industrial production.

To provide a new compound useful for treatment, prevention and / or diagnosis of seizure or the like in diseases accompanied by epileptic seizure or convulsive seizure (including multidrug-resistant seizure, intractable seizure, acute symptomatic seizure, febrile seizure and status epilepticus).SOLUTION: There are provided a compound represented by formula [I] and a salt thereof. Ring C is selected from pyridazine, pyrimidine, indole, pyrrolopyridine, indazole, pyrazolopyridine, imidazopyridine, imidazopyrazine, imidazopyridazine, triazolopyridine, pyrazolopyrimidine, imidazopyrimidine, triazolopyrimidine, isoquinoline, naphthyridine, quinazoline, quinoxaline, benzodioxole, oxazine, oxazepine, benzothiazole, and triazolopyridazine, with the proviso that pyrimidine-2, 4-dione and dihydropyrimidine-2, 4-dione are excluded.SELECTED DRAWING: None

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 relates to a compound corresponding to formula (I): in which - R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and pharmaceutical composition comprising the said compound for the treatment and prevention of diseases requiring a modulation of b-FGFs.

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 or prodrug thereof. These compounds are TLR9 inhibitors useful for the treatment, prevention or slowing of a fibrotic disease, such as liver fibrosis, kidney fibrosis, biliary fibrosis or pancreatic fibrosis, nonalcoholic steatohepatitis (NASH), nonalcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic nephropathy, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

The present invention relates to different forms of the compound 6-chloro-2-ethyl-N-(4-(4-(4-(trifluoromethoxy) phenyl) piperidin-1-yl) benzyl) imidazo [1, 2-a] pyridine-3-carboxamide and to processes for preparing these forms / compounds. The invention also relates to the mono-acid addition salts thereof and to methods of making these mono-acid addition salts as well as to pharmaceutical compositions comprising any of the aforementioned compounds. Furthermore, the invention relates to the use of any of these compounds.