278 results about "Indazole" patented technology

Disclosed herein are compounds and methods of treating diseases and / or conditions associated with FGFR inhibition.

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 invention relates to application of an amide ligand and a copper catalyst in preparation of an amino indazole piperidine compound. The indazole piperidine compound is prepared by reacting a halogen-substituted indazole piperidine compound with an ammonia reagent, the reaction is carried out under the action of an amide ligand and a catalyst, the amide ligand is # imgabs0, the structural formula of the amide ligand is # imgabs1 # or L-hydroxyproline, and the catalyst is a cuprous compound.

Indazolo-amino-pyrimidinone compounds of formula I; (I), for use in methods of inhibiting both Wee1 A kinase and Myt1 kinase.

Novel compounds of Formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control, and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, obesity, gout, pseudogout, CAPS, NASH, MASH, fibrosis, osteoarthritis, atherosclerosis, heart failure, idiopathic pericarditis, myocarditis, atopic dermatitis, hidradenitis suppurativa, inflammatory bowel disease, cancer, Alzheimer's Disease, Parkinson's Disease, dementia with Lewy bodies (DLB), and traumatic brain injury.

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.

Disclosed are processes for the preparation of the pesticide N-(1-methylcyclopropyl)-2-(3-pyridinyl)-2H-indazole 4-carboxamide. Also disclosed are methods for the preparation of intermediates of thereof N-(1-methylcyclopropyl)-2-(3-pyridinyl)-2H-indazole 4-carboxamide.

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.

An indazole derivative, a preparation method therefor, and a pharmaceutical application thereof. In particular, the present invention relates to an indazole derivative represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and a use of the derivative as an estrogen receptor modulator in the prevention and / or treatment of an estrogen receptor mediated or dependent disease or condition, the disease being particularly preferably breast cancer. The definition of each substituent in the general formula (I) is the same as that in the description.

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 invention provides a 2, 3-dimethyl-6-amino-2H-indazole solution concentration detection device, and relates to the technical field of solution detection.The 2, 3-dimethyl-6-amino-2H-indazole solution concentration detection device comprises a bottom plate, the outer surface of the bottom plate is fixedly connected with four supporting rods, one ends of the four supporting rods are jointly and fixedly connected with a liquid storage tank, the outer surface of the liquid storage tank is provided with a liquid pumping mechanism, and the liquid pumping mechanism is arranged on the outer surface of the liquid storage tank. The outer surface of the liquid storage tank and the inner wall of the liquid storage tank are both provided with stirring mechanisms, the outer surface of the bottom plate is fixedly connected with a supporting plate, an external solution can be pumped into the liquid storage tank through a liquid pumping mechanism, and the effect that the solution is conveniently added into the liquid storage tank for concentration detection is achieved; solution in the liquid storage tank is stirred through the stirring mechanism, the solution is evenly mixed, the concentration detection result of the solution is improved, the detection probe is driven to ascend and descend through the lifting mechanism, the height of the detection probe is controlled, then concentration detection of the solutions at different heights is achieved, and the accuracy of the concentration detection result is improved.

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.

This text describes bifunctional compounds that can be used as regulators of leucine-rich repeat kinase 2 (LRRK2). In particular, the heterobifunctional compounds of the present disclosure contain a moiety that binds to the cereblon E3 ubiquitin ligase at one end and a moiety that binds to LRRK2 at the other end, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of the target protein. The heterobifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities related to the degradation / inhibition of the target protein. Treat or prevent diseases or disorders caused by abnormal regulation of the target protein with the compounds and compositions of the present disclosure.

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.