21 results about "Triazolopyridine" patented technology

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 application relates to the technical field of medicines, in particular to a preparation process of a Tucatinib intermediate 4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylaniline, which comprises the following steps: step 1: under a nitrogen atmosphere, a substitution reaction is carried out on a compound B and a compound C in a base and an organic solvent system to obtain a compound D; step 2: the compound D is added into a reduction catalytic solution system protected by nitrogen, after 8-30h of reaction at 70-120 DEG C, TLC tracking is carried out until the reaction is completed, 2-8 times the volume of the compound D is added into water, post-treatment and purification are carried out, and the compound A is obtained; wherein the reduction catalytic solution system comprises a reducing agent, a catalyst and an inorganic acid, the reducing agent comprises a reducing phosphoric acid, and the catalyst comprises iodine or a metal salt of iodine. The preparation process of the Tucatinib intermediate 4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylaniline in the application has mild reaction conditions, high product yield and high purity, the preparation process is environment-friendly, and can be used for industrial production.

The application provides a cycloalkyl-substituted triazolopyridine amide compound and a preparation method and application thereof, and belongs to the technical field of pesticides. The cycloalkyl-substituted triazolopyridine amide compound provided by the application introduces an unsubstituted or substituted cyclohexyl group or an unsubstituted or substituted cyclopentyl group on a triazole ring, has excellent inhibitory effect on pepper Phytophthora capsici Leonian, and has an EC 50 as low as 0.3 micromole / L; and the cycloalkyl-substituted triazolopyridine amide compound and derivatives thereof also have broad-spectrum inhibitory activity on rice Helminthosporium leaf spot fungus, wheat Helminthosporium leaf spot fungus, brassica sclerotinia, wheat Gibberella zeae, wheat take-all fungus, tomato botrytis cinerea, potato late blight fungus, pepper Phytophthora capsici Leonian, tomato early blight fungus, rice bacterial wilt fungus, potato dry rot fungus, cucumber anthracnose fungus and rice rice blast fungus, and have a good application prospect in the preparation of anti-plant pathogenic fungus drugs.

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 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 provides a novel tetrahydroisoquinoline or isoindoline-substituted [1,2,4] triazolo [1,5-a] pyridine derivative selectively inhibiting JAK1, and a pharmaceutical composition comprising same as an active ingredient for preventing or treating cancer, rheumatoid arthritis, psoriatic arthritis, atopy, Crohn's disease, or ulcerative colitis.

The invention relates to the technical field of medicine synthesis, in particular to a preparation method of a triazolopyridine compound. The triazolopyridine compound is N-[7-hydroxy-5-(2-phenethyl) [1, 2, 4] triazole [1, 5-a] pyridine-8-carbonyl] glycine, the preparation method takes a compound I and a compound II as initial raw materials, and a target product is prepared through the following steps in sequence: firstly, carrying out alkylation reaction by taking carbonate as an acid-binding agent to synthesize an intermediate I, and then, carrying out reaction on the intermediate I and the intermediate II to obtain the triazolopyridine compound. Carrying out hydrolysis-decarboxylation reaction on the intermediate I to generate an intermediate II; then, the intermediate II generates an acyl chloride intermediate III under the catalysis of N, N-dimethylformamide, and the acyl chloride intermediate III does not need to be separated and is directly subjected to an acid amine condensation reaction in a water-containing heterogeneous solution; finally, the intermediate III is subjected to a hydrolysis reaction with water as a single solvent, and the triazolopyridine compound can be obtained.

The invention relates to a crystal form of a quinazoline derivative and a preparation method thereof. Specifically, the invention provides an E crystal form, a D crystal form and an H crystal form of 1-(inner-3-((4-((4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-yloxy)-2-fluoro-3-methylphenyl) amino) quinazoline-6-yl) oxy)-8-azabicyclo [3.2. 1] oct-8-yl) prop-2-en-1-one, and the E crystal form, the D crystal form and the H crystal form have good stability and can be better used for clinical treatment. Formula (I).

Relates to a pharmaceutically acceptable salt of a quinazoline derivative, and a crystal form and application thereof. Specifically, the invention provides a medicinal salt, a crystal form and a preparation method of 1-(inner-3-((4-((4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-yloxy)-2-fluoro-3-methylphenyl) amino) quinazoline-6-yl) oxy)-8-azabicyclo [3.2. 1] oct-8-yl) prop-2-en-1-one, and the corresponding salt has good stability and can be better used for clinical treatment.

Provided are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

The invention provides a triazole pyridine extractant-hollow tetrazinyl COF composite material as well as a preparation method and application thereof, and relates to the technical field of material preparation. The preparation method comprises the following steps: firstly, taking hydroformylated SiO2 as a hard template, carrying out step-by-step polymerization and alkali etching to obtain a tetraazinyl covalent organic framework (COF) material of an ethylene connecting bond with a hollow structure, and then further introducing an extracting agent molecule with a specific multi-tooth coordination structure into a cavity of the tetraazinyl covalent organic framework (COF) material by utilizing a pressure difference-concentration difference method to obtain the composite material. According to the composite material, the high specific surface area and short mass transfer path of the hollow structure, the strong coordination capability of the tetrazine group and the high selective recognition function of the extraction agent are synergistically integrated, so that the composite material shows high adsorption capacity, fast adsorption kinetics, excellent selectivity and good reusability on thorium ions; the method has important application value in the field of efficient separation and recovery of actinide elements in radioactive wastewater.

The application discloses a triazolopyridine bromodomain-containing protein 4 (BRD4) small molecule inhibitor and a preparation method and application thereof, a compound or a pharmaceutically acceptable salt or a racemate thereof, the general formula of which is shown as formula (I). The novel synthetic triazolopyridine compound effectively regulates the occurrence and development process of related diseases by inhibiting the activity of BRD4 protein. In addition to the advantage of inhibiting the activity of BRD4 protein, the compound has good water solubility and liver microsomal stability, which means that it can be better absorbed and distributed in the body, thereby improving the therapeutic effect. The compound also has good drugability, so that it can be better applied to various inflammatory, autoimmune diseases and tumor drugs. The application provides a new choice for the treatment of related diseases and is expected to play an important role in clinical practice.

The invention relates to the field of medicinal chemistry, in particular to a preparation method of a triazolopyridine compound, which comprises the following steps: reacting a compound 6 with aniline and diphenyl phosphite in the presence of isopropanol to obtain a compound 7; and reacting the compound 5 with the compound 7 to obtain the compound as shown in the formula I. The method avoids use and production of heavy metal substances, and is environment-friendly, simple, efficient, mild in reaction condition, easy to control in operation, safe, reliable, low in cost, good in economic benefit and suitable for industrial production.

The present application relates to the field of artificial board, and discloses a mildew-proof and water-resistant bamboo-based artificial board and a preparation method thereof, wherein the board blank of the artificial board is formed by bamboo shaving glue mixing and paving; the components for glue application include melamine, formaldehyde, modified bamboo powder, modified nano silicon dioxide, plant oil acid and water; the modified bamboo powder is made by grafting modified silane coupling agent with bamboo powder; the modified silane coupling agent is made by reacting functional modifier obtained by the reaction of 3-chloro-2-hydrazine pyridine intermediate made from 3-chloro-2-hydrazine pyridine and carbon disulfide, hydrophobic modified ultraviolet absorber made from 5-chloro-2-(2',4'-dihydroxyphenyl)-2H-benzotriazole and glycidyl ester tertiary carbonic acid, and p-phenylenediamine, and then reacting with vinyl trimethoxysilane; the modified nano silicon dioxide is made by modifying with silicon-phosphorus coupling modifier obtained from DOPO and vinyl triethoxysilane and tetraethyl orthosilicate, so as to prepare the artificial board with good ultraviolet resistance, antibacterial and mildew-proof property, water resistance and flame retardance.

Provided herein are 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)thiophene-2-carboxamide and 4-([1,2,4]triazolo[1,5-a]pyridin-7-yl)thiophene-2-carboxamide derivatives. Such compounds are useful, for example, for the treatment and / or prevention of neurodegenerative diseases or disorders such as ophthalmological neurodegenerative disorders. This disclosure also features compositions containing the same as well as methods of using and making the same.

Provided are compounds of Formula I, Formula Ib or Formula Ic and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, Formula Ib or Formula Ic, pharmaceutical compositions comprising compounds of Formula I, Formula Ib or Formula Ic, and methods of using these compounds to treat hepatic steatosis, non-alcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

The present application relates to triazolopyridopyrimidine and dihydroimidazopyridopyrimidine compounds having activity as inhibitors of generally regulated repressor protein 2 (GCN2) kinase, processes for their preparation, compositions comprising them and their use, for example in therapy. More specifically, the present application relates to compounds useful in the treatment of diseases, disorders or conditions treatable by inhibition of GCN2 kinase, such as cancer and neuronal diseases. (I)

A crystal form of a triazolopyridine-substituted indazole compound and a preparation method thereof, and specifically discloses a crystal form of a compound shown in formula (I) and a preparation method thereof.

Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for the treatment of retinal binding protein (RBP4) related diseases, such as obesity and the like.

The present invention relates to compounds of formula (I), and enantiomers and diastereoisomers, stereoisomers, pharmaceutically acceptable salts thereof, which are useful as kinase modulators, including RIPK1 modulation. All variables are as defined herein.