39 results about "Triazolopyridine" patented technology

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 preparation method of trazodone hydrochloride. The preparation method comprises the following steps: activating 1, 2, 4-triazolo [4, 3-a] pyridine-3 (2H)-ketone by using an inorganic strong base, adding an inorganic weak base as an acid-binding agent to react with 1-(3-chlorphenyl)-4-(3-chloropropyl) piperazine hydrochloride, filtering to remove inorganic salt after the reaction is finished, crystallizing to obtain trazodone free base, salifying to obtain a trazodone hydrochloride crude product, and purifying to obtain the trazodone hydrochloride. And finally, recrystallizing by using a mixed solvent of an organic solvent and water to obtain a trazodone hydrochloride finished product. The preparation method of trazodone hydrochloride provided by the invention is simple and efficient to operate, the product purity is high, genotoxic impurities and residue on ignition meet the requirements of laws and regulations, and the preparation method has obvious industrialization and commercialization advantages.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a method for preparing a triazolopyridine compound which has a PHD inhibiting effect and can be used for treating or preventing diseases caused by reduction of production of EPO and the like.

The invention discloses a compound with a triazolopyridine structure as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The compound has a brand-new chemical structure, the unique skeleton and the optimized molecular weight endow the compound with excellent patent medicine potential, hydroxyl and other functional groups in the compound provide a wide space for chemical modification, and the development prospect of diversified pharmacological activity derivatives is indicated; the compound significantly inhibits uric acid activity, has efficacy superior to that of a traditional drug benzbromarone, has lower cytotoxicity, and is an ideal uric acid-reducing drug candidate; the synthetic route is simple, the conditions are mild, the raw materials are easy to obtain, industrial production is facilitated, the high purity of the product is ensured through an efficient separation means, a powerful guarantee is provided for clinical medication safety, and novel uric acid lowering drugs are expected to be developed.

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.

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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 invention relates to the technical field of medicines, in particular to a preparation process of a Fikatinib intermediate 4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-oxy)-3-methylaniline, which comprises the following steps: step 1, in a nitrogen atmosphere, carrying out substitution reaction on a compound B and a compound C in a formula in an alkali and organic solvent system to obtain a compound D in a formula; step 2, adding the compound D into a reduction catalysis solution system protected by nitrogen, reacting at 70-120 DEG C for 8-30 hours, tracking by TLC until the reaction is complete, adding water which is 2-8 times of the volume of the compound D, and performing post-treatment and purification to obtain a compound A; wherein the reduction catalysis solution system comprises a reducing agent, a catalyst and inorganic acid, the reducing agent comprises reducing phosphoric acid, and the catalyst comprises iodine or metal salt of iodine. According to the preparation process of the 4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-oxy)-3-methylaniline intermediate, the reaction condition is mild, the prepared product is high in yield and purity, the preparation process is environmentally friendly, and the preparation process can be used for industrial production.

Compounds of Formula I, Formula Ib, or Formula Ic, and pharmaceutically acceptable salts, esters, and prodrugs thereof are provided, which are DGAT2 inhibitors. Also provided are methods of preparing compounds of Formula I, Formula Ib, or Formula Ic, pHARMACEUTICAL COMPOSITIONS COMPRISING COMPOUNDS OF Formula I, Formula Ib OR Formula Ic AND USE OF THEIR FOR THE TREATMENT OF LIVER STEATIVE DEGENERATION, NON-ALCOHOLIC STEATIVE HEPATITIS (NASH), FIBROSIS, TYPE 2 DIABETES, OBESITY, HYPERLiPIA, HYPERCHROCHROLEASE, Atherosclerosis, DECIDERATION OF COGNITION, DEmentia, HEART-KITE DISEASES (e.g. And methods of treating diseases and conditions related thereto, comprising administering to a patient in need thereof a compound of Formula I, Formula Ib, or Formula Ic. # imgabs0 #

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.

The invention provides a naphthenic base substituted triazolopicolinamide compound as well as a preparation method and application thereof, and belongs to the technical field of pesticides. According to the cycloalkyl substituted triazolo picolinamide compound provided by the invention, unsubstituted or substituted cyclohexyl and unsubstituted or substituted cyclopentyl are introduced to a triazole ring, so that the cycloalkyl substituted triazolo picolinamide compound has an excellent inhibition effect on phytophthora capsici in important oomycetes diseases, and the EC50 of the cycloalkyl substituted triazolo picolinamide compound to the phytophthora capsici is as low as 0.3 mu mol / L; the naphthenic base substituted triazolopicolinamide compound and the derivative thereof have a significant effect on rhizoctonia solani, rhizoctonia cerealis, sclerotinia sclerotiorum, fusarium graminearum, gaeumannomyces graminis, botrytis cinerea, phytophthora infestans, phytophthora capsici, alternaria solani, fusarium moniliforme, potato dry rot pathogen, phytophthora capsici and the like. Cucumber colletotrichum gloeosporioides and magnaporthe oryzae also have broad-spectrum antibacterial activity, and the compound has a good application prospect in preparation of drugs for resisting plant pathogenic fungi.

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 present invention discloses a flavonol derivative containing triazolopyridine, which is characterized by a structural formula as shown in Formula S: #imgabs0#, wherein: R1 is hydrogen, alkyl or alkoxy; R2 contains one or more halogens, alkyl or alkoxy groups at the ortho, meta or para position on the benzene ring; and n is 3 or 4. The present invention conducts a plant fungus inhibition activity test on the disclosed flavonol derivative containing triazolopyridine, and proves that the disclosed flavonol derivative containing triazolopyridine has good fungus inhibition activity and can be used in the preparation of a plant pathogen inhibition agent.

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.

Disclosed is the use of a JAK inhibitor [1,2,4]-triazolo-[1,5-a]0pyridine compound in the preparation of drugs for treating autoimmune, inflammatory or allergic diseases, or diseases such as transplant rejection. The JAK inhibitor [1,2,4]-triazolo-[1,5-a]-pyridine compound comprises a compound as shown in formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof. The JAK inhibitor has a good efficacy in animal model tests of diseases such as autoimmune, inflammatory or allergic diseases.

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 invention relates to the field of chemical technology, and in particular to a 1,2,4-triazolo[4,3-a]pyridine sulfone derivative, a method for preparing the 1,2,4-triazolo[4,3-a]pyridine sulfone derivative compound, and use of the 1,2,4-triazolo[4,3-a]pyridine sulfone derivative in treating citrus Huanglongbing disease. The derivative is formed by combining a [1,2,4]triazolo[4,3-a]pyridine structure with a sulfone structure.

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 solid state forms of (E)-1-(4-(4-((4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)pyrrolo[2,1-f][1,2,4]triazin-5-yl)piperidin-1-yl)-4-(dimethylamino)but-2-en-1-one and salts thereof. Such solid state forms re useful in preparation of pharmaceutical compositions for the treatment of diseases.

This application relates to novel triazole-pyridine substituted pyrrolidinyl, tetrahydro-2H-pyranyl, cyclohexyl, and piperidinyl acetic acid compounds, their manufacture, pharmaceutical compositions comprising them, and their use as medicaments for treating a disease associated with dysregulation of lysophosphatidic acid receptors (LPA).