136 results about "Indazole" patented technology

The invention belongs to the field of analytical chemistry, relates to material preparation, and particularly discloses a preparation method of a copper-doped covalent organic framework and application of the copper-doped covalent organic framework in adrenaline colorimetric detection. Firstly, 1H-indazole-4, 7-diamine (Iz) and 1, 3, 5-triformyl phloroglucinol (Tp) are used as monomers to synthesize a novel covalent organic framework (Iz-Tp COF) through a Schiff base reaction, copper ions are introduced into the Iz-Tp COF framework to prepare a novel metal covalent organic framework (Iz-Tp (at) Cu), and then according to the phenomenon that the Iz-Tp (at) Cu can catalyze oxidation color development of epinephrine, the metal covalent organic framework (Iz-Tp (at) Cu can catalyze oxidation color development of epinephrine. According to the present invention, the simple, sensitive and efficient adrenaline colorimetric detection method is established, the test conditions are finally optimized, the standard addition method is combined to accurately determine the adrenaline concentration in the urine, and the good practical application value is provided.

The present invention relates to a novel polymorph of (1R,2R,3aS,3bR,10aS,10bR,11S,12aS)-5,10b-difluoro-1-(((fluoromethyl)thio)carbonyl)-11-hydroxyl-2,10a,12a-trimethyl-7-phenyl-1,2,3,3a,3b,7,10,10a,10b,11,12,12a-dodecylhydrocyclapenta[5,6]napththo[1,2-F]indazole-1-furan-2-carboxylate ester as shown in formula (I), a preparation method therefor, and a use thereof. The crystal form of the present invention has characteristics such as a significant pharmaceutical effect, good stability, high yield, and high purity, and is beneficial for the selection and design of a drug administration route and the determination of a drug preparation process parameter, thereby improving drug production quality.

The present invention relates to an indazole derivative or a pharmaceutically acceptable salt thereof, and a composition for preventing, treating, or ameliorating cancer, comprising, as an active ingredient, the derivative or a pharmaceutically acceptable salt thereof. The indazole derivative of the present invention is designed to provide strong binding to the C-terminal domain of Hsp90, and does not affect the composite structure of Hsp90 and HSF-1, thus not inducing the activation of HSF-1 or the expression of Hsp genes, thereby effectively promoting apoptosis of cancer cells. Thus, the indazole derivative of the present invention can be used in the prevention, treatment, or amelioration of cancer.

The present invention relates to the preparation of compositions comprising sodium trans-[tetrachlorobis(1H-indazole)ruthenate (III)]. Synthesis and formulation preparation is detailed. Impurity profiles are also discussed. Compositions herein are useful for anti-cancer applications.

The present application provides a kind of compound with indazole group, THR beta receptor agonist and use, compound with indazole group or its pharmaceutically acceptable salt.The present application develops a kind of THR beta selective agonist with better specificity and drugability, the present agonist is better selective agonist THR beta and avoids the activation of THR alpha, separates the harmful influence of thyroid hormone excess from potential beneficial effects such as lowering cholesterol and blood lipids, provides a kind of new type of treatment drug with broad prospects for treating a series of major metabolic diseases in urgent need of solution.

The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and / or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and / or prophylaxis of diseases, especially for treatment and / or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.

The invention provides a method for preparing a chiral helicene compound through cyclization reaction of an iridium-catalyzed 3-aryl indazole biaryl compound and disubstituted alkyne. The method comprises the following steps: under the action of an iridium catalyst, a chiral cyano phosphorus-oxygen ligand and an additive, carrying out an intermolecular asymmetric carbon-hydrogen bond activation reaction on a 3-aryl indazole biaryl compound and disubstituted alkyne, and after the reaction is finished, separating to obtain the chiral diazaspirene-containing compound, according to the invention, synthesis of the chiral helicene compound is realized through a transition metal catalysis asymmetric carbon-hydrogen bond activation method, the research technology of Cp metal catalysis asymmetric carbon-hydrogen bond activation is further developed, and the synthesis strategy of the chiral helicene compound is expanded at the same time; reaction substrates are wide in universality, and chiral control in the reaction process is realized through the chiral cyano phosphine oxide, so that the product has very high enantioselectivity; various chiral helicene compounds are synthesized, the synthesis method is simple and convenient, and the atom economy is high.

The present disclosure relates to an indazole-pyrazole skeleton compound and use thereof. Specifically, the present disclosure provides a compound as shown in formula I or a pharmaceutically acceptable salt thereof. The compound of the present disclosure has good inhibitory effect on PDE4 and good therapeutic effect on acute lung injury.

The invention provides new indazole derivatives of formula (I):or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

The invention discloses a perfluoroalkyl-substituted pyrimido [1, 2-b] indazole ketone compound and a preparation method thereof, and belongs to the technical field of compounds containing two or more heterocyclic rings. Comprising the following steps: with enaminone, a perfluoroalkane compound and aminoindazole as raw materials, carrying out a reaction under blue light irradiation in the presence of an organic solvent and alkali to prepare the perfluoroalkyl-substituted pyrimido [1, 2-b] indazole ketone compound; according to the invention, through visible light mediated dehalogenation and cyclization free radical addition, high-yield synthesis of the perfluoroalkyl substituted pyrimido [1, 2-b] indazole ketone compound is realized; the prepared perfluoroalkyl-substituted pyrimido [1, 2-b] indazolone compound has excellent antibacterial activity, can be used for preparing antibacterial drugs, and has outstanding industrial application value.

The application discloses a synthesis method of aromatic aldehyde, comprising the following steps: under inert atmosphere, a compound shown in formula I and a compound shown in formula II are reacted in an organic solvent containing a photocatalyst, a nickel catalyst, a ligand, a base and water under blue light irradiation to obtain aromatic aldehyde shown in formula III; formula I, formula II and formula III are structures as follows, ring A is selected from benzene, pyridine, thiophene, furan, pyridazine, indazole, indole, isoquinoline, quinoline, naphthalene, benzothiophene, dibenzofuran or dibenzothiophene; the application generates formyl radicals under the nickel synergistic photo-oxidation and reduction catalytic condition, and the formylation of bromobenzene and its derivatives is realized in a simple and efficient one-pot way, aromatic aldehyde is constructed, and the reaction has the characteristics of cheap and easily available raw materials, mild reaction conditions, controllable synthesis process, high separation yield / yield, green environmental protection, wide substrate applicability and the like.

The invention belongs to the technical field of chemical synthesis, and particularly relates to an indazole alkaloid derivative as well as a preparation method and application thereof. Comprising the following steps: under an alkaline condition, carrying out alkylation reaction on a compound a and an alkylating agent to obtain a compound b; performing demethylation reaction on the compound b and a demethylation reagent to obtain a compound c; carrying out glycosylation reaction on the compound c and sugar bromide to obtain a compound d; in a sodium methoxide and solvent system, removing acetyl on glycosyl of the compound d to obtain the indazole alkaloid derivative. Or carrying out oxidation reaction on the compound d and methyl iodide to obtain an intermediate; and removing acetyl on glycosyl of the intermediate in a sodium methoxide and solvent system to obtain the indazole alkaloid derivative. The invention provides a preparation method of an indazole alkaloid derivative, which is green, simple, convenient and efficient.

The present disclosure relates to indazole macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer comprising administering a therapeutically effective amount of a compound to a subject in need thereof.

The invention discloses a method for preparing a GLP-1 agonist intermediate 5-bromine-4-fluorine-1-methyl-1H-indazole, according to the method, 2, 6-difluorobenzonitrile which is low in price is used as a starting raw material, the regioselectivity of bromination reaction is improved and the yield is increased by optimizing the reaction, and the whole reaction synthesis operation is simple, the safety risk is low, and the method is suitable for industrial production. The method is more suitable for industrial production, and a new way is provided.

The invention relates to extended-release formulations comprising substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof that can activate adenosine 5'-monophosphate- activated protein kinase (AMPK). The invention further relates to methods of treating a condition comprising administering an extended-release formulation comprising AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof.

The application aims to provide a synthesis method of 6-bromo-5-fluoro-3-iodo-1-methyl-1H-indazole, which adopts 5-bromo-2,4-difluorobenzonitrile as raw material, and obtains the target product 6-bromo-5-fluoro-3-iodo-1-methyl-1H-indazole through two-step reaction; the synthesis method has a short process route, the raw material and auxiliary material are cheap and easy to obtain, the reaction activity is high, there is no isomer, the operation is simple and easy to control, the yield of the obtained target product is high, and the industrialization is convenient.

The present disclosure provides methods of large-scale preparation of alpha-1 antitrypsin (AAT) activity modulators useful for treating alpha-1 antitrypsin deficiency (AATD), such as 4-(5-(4-fluorophenyl)-6-(tetrahydro-2H-pyran-4-yl)-1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid (Compound 1), 3-[5-(4-fluorophenyl)-6-isopropyl-1H-pyrrolo[2,3-f]indazol-7-yl]propanoic acid (Compound 2), or any pharmaceutically acceptable salt of any of the foregoing.

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 provides a preparation method of 2-(pyridine-3-yl)-2H-indazole-4-carboxylic acid, which comprises the following steps: A) adding an electrolyte, 2-(pyridine-3-yl)-2H-indazole, a cyanation reagent, an additive and a solvent into an electrolytic bath, inserting an inert electrode, and stirring to react under a constant current condition; and B) after the reaction is finished, acidizing, separating and purifying to obtain the 2-(pyridine-3-yl)-2H-indazole-4-carboxylic acid. Compared with the prior art, the method has the advantages that raw materials and catalysts are easy to obtain, expensive metal catalysts and ligands are not needed, an electrochemical synthesis strategy is utilized, energy consumption is low, pollution is low, use of easily-exploded and highly-toxic reagents is avoided, and the method is environmentally friendly, efficient, short in synthesis route, easy to operate, high in stability, mild in condition and easy to implement.

The present application provides a compound shown in formula (I) and its racemate, stereoisomer, tautomer, isotopically labeled, nitroxide, solvate, polymorph, metabolite, ester, prodrug or pharmaceutically acceptable salt thereof. Such compounds have good FGFR2 / 3 inhibitory effect, and can be used for treating or preventing FGFR2 / 3 mediated disorders and diseases, and preparing drugs for treating or preventing such disorders and diseases.

The invention provides a preparation method of nirapalide tosylate, which is characterized in that 1H-indazole-7-carboxyl methyl ester, 2, 4-dimethoxybenzylamine and (S)-3-(4-bromophenyl) piperidine-1-carboxylic acid tert-butyl ester are used as raw materials to react to prepare the nirapalide tosylate. The method has the advantages of simple process operation, few side reaction products and high purity of the obtained product, and is suitable for industrial production of nirapalide tosylate.