215 results about "Indazole" patented technology

The invention belongs to the technical field of pyrimidine [1, 2-b] indazole derivative synthesis, and particularly relates to a fluoro pyrimidine [1, 2-b] indazole compound and a preparation method thereof. The preparation method specifically comprises the following steps: by taking an enamine compound as shown in a formula 1, heteroarylamine as shown in a formula 2 and polyfluoroalkyl halide as shown in a formula 3 as reaction substrates, mixing the reaction substrates, a catalyst and a solvent, and carrying out cyclization reaction in a protective gas atmosphere and under blue light irradiation to obtain the fluoropyrimidine [1, 2-b] indazole compound. The fluorine atom substituted or multi-fluoroalkyl substituted pyrimidine [1, 2-b] indazole derivative can be selectively constructed in the same reaction system, the diversity of the structure is obviously expanded, and the reaction conditions are mild and green and environment-friendly.

The invention relates to a preparation method of 3-[(1S, 2S)-1-[5-[(4S)-2, 2-dimethyl oxacyclohexane-4-yl]-2-[(4S)-2-(4-fluoro-3, 5-dimethyl phenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6, 7-dihydro-4H-pyrazolo [4, 3-c] pyridine-5-carbonyl] indol-1-yl]-2-methylcyclopropyl]-4H-1, 2, 3-triazolo [4, 3-c] pyridine-5-carbonyl] indol-1-yl]-2-methylcyclopropyl]-1, 2, 4-triazolo [4, 3-c] pyridine-5- The invention relates to synthesis of 1, 2, 4-oxadiazole-5-one or a salt thereof, and related synthesis intermediate compounds.

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 invention discloses an HPK1 small-molecule inhibitor based on a novel indazole skeleton and application of the HPK1 small-molecule inhibitor, and belongs to the technical field of medical chemistry. The HPK1 small-molecule inhibitor is a compound as shown in a formula (I) or an enantiomer thereof, a mixture of the enantiomer, a mixture of two or more diastereoisomers, a tautomer, a mixture of two or more tautomers, or an isotope variant or a pharmaceutically acceptable salt, a solvate, a hydrate or a prodrug thereof. The novel HPK1 small-molecule inhibitor skeleton disclosed by the invention shows a very strong inhibition effect on HPK1 and has a relatively good application prospect.

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 invention belongs to the technical field of medical fertilizers, and particularly relates to a medical fertilizer for preventing and treating corn sheath blight. The invention relates to a bactericidal active component. The bactericidal active component is formed by binary compounding of amisulbrom and bixafen according to the mass ratio of (1-15): (7-1). The amisulbrom and the bixafen are compounded according to the mass ratio of (1-15): (7-1), the prevention and treatment effect on the corn sheath blight can be improved, and support can be provided for developing a compound medicament for preventing and treating the corn sheath blight. Besides, when the pesticide-fertilizer granules are applied, nutritional ingredients needed by corn growth can be supplemented, the prevention and treatment effect on corn sheath blight can be improved, the dual effects of pesticide and fertilizer can be achieved through one-time application, and the pesticide-fertilizer granules have good application prospects.

The present disclosure relates to indazole containing macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer.

The present disclosure relates to compounds that act as inhibitors of the NLRP3 inflammasome, pharmaceutical compositions containing the compounds, and methods for treating inflammation and inflammation-aging-related disorders, including neurosensory disorders and other diseases associated with aging.

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.

To provide cell permeable PARG inhibitors.SOLUTION: Provided herein are a compound having the following formula, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, Ar, X1, X2, and ring B have the meanings as provided herein. The provided compounds are useful Poly ADP-ribose glycohydrolase (PARG) inhibitors.SELECTED DRAWING: None

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 provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.

The invention discloses a synthesis method of 1H-indazole-7-tert-butyl formate, and belongs to the technical field of organic synthesis. The synthesis method of the 1H-indazole-7-tert-butyl formate comprises the following steps: dissolving 7-carboxyl-1H-indazole in an organic solvent I, then adding 1, 1-di-tert-butoxy-N, N-dimethyl methylamine, heating, and carrying out a stirring reaction to obtain a reaction solution; and performing post-treatment. According to the synthesis method, one-step conversion of indazole carboxylic acid into indazole tert-butyl formate is achieved, reaction conditions are mild, aftertreatment and purification are simple, cost is low, and manufacturability amplification can be achieved.

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.