72 results about "Pyridazine" patented technology

To provide a compound superior in an ATX inhibitory action and useful for the prophylaxis or treatment of a disease involving ATX.SOLUTION: The invention provides a carboxylic acid compound represented by the general formula (1), or a pharmaceutically acceptable salt thereof.SELECTED DRAWING: None

The present application relates to a kind of thieno [2, 3-c] pyridazine derivatives, and its isotope form, stereoisomer, tautomer, cis-trans isomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, hydrate, prodrug and polymorph, these compounds can be used as cholinergic M4 receptor positive allosteric modulator, it has good application prospect in preparation for preventing and / or treating the drug for the disease related to abnormal muscarinic acetylcholine receptor.

The present disclosure relates to solid state forms of Compound (1) freebase. The present disclosure also relates to processes for the preparation of the solid state forms, the pharmaceutical compositions comprising the forms, and the use thereof, e.g., in the treatment and prevention of disorders in which NLRP3 activity is implicated.

In the production of crops in agriculture, horticulture, and the like, the occurrence of damage by pests and the like has been still a major issue, and therefore the development of new agricultural / horticultural pesticides has been demanded due to such as the emergence of pests resistant to existing chemicals.　It is discovered that a compound represented by general formula (1) {in the formula, X and Y each represent an oxygen atom or a sulfur atom, Z represents a hydroxyl group or the like, R1 represents an alkoxycarbonyl group or the like, R2 represents a substituted phenyl group or the like, R3 represents a hydrogen atom or the like, and R4 represents a substituted phenyl group or the like} or a salt thereof exhibits a high pesticidal effect on pests and the like in the field of agricultural / horticultural, and the present invention provides an agricultural / horticulturalpesticide using same as active ingredients, and a method for using same.

This invention relates to a novel and improved method for preparing substituted N-(2-chloroethyl)-N'-hydroxy-3-phenoxypyridazine-3-formamidinium, which can be converted into substituted 3-(3-phenoxypyridazine-4-yl)-5,6-dihydro-4H-1,2,4-oxadiazine. Specifically, this invention relates to the preparation of 3-(3-chloro-2-fluoro-phenoxy)-N-[1-(chloromethyl)-2-(2-chloro-4-methyl-phenyl)ethyl]-N'-hydroxy-6-methylpyridazine-4-formamidinium, which can be converted into 3-[3-(3-chloro-2-fluorophenoxy)-6-methylpyridazine-4-yl]-5-(2-chloro-4-methylbenzyl)-5,6-dihydro-4H-1,2,4-oxadiazine; More specifically, it involves 3-(3-chloro-2-fluoro-phenoxy)-N-[1-(chloromethyl)-2-(2-chloro-4-methyl-phenyl)ethyl]-N'-hydroxy-6-methyl-pyridazin-4-formamidinium, which can be converted into (5S)-3-[3-(3-chloro-2-fluorophenoxy)-6-methylpyridazin-4-yl]-5-(2-chloro-4-methylbenzyl)-5,6-dihydro-4H-1,2,4-oxadiazine.

This application discloses an F-18-labeled pyridazinone compound, its preparation method, and its applications, relating to the field of radiolabeling. Its general structural formula is: [Formula omitted for brevity]. Wherein, R1 is an alkyl group with 1-5 carbon atoms; R2 is a halogen or methyl group; R3 is one of the following structural formulas: [Formula omitted for brevity], ...

The present invention provides compounds of formula (I) and / or salts thereof and / or biologically active metabolites thereof and / or prodrugs thereof and / or solvates thereof and / or hydrates thereof and / or polymorphs thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 positive allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

This invention relates to deuterated 3-oxo-2,3-dihydropyridazine-4-carboxamide inhibitors, their preparation methods, and applications. Specifically, the compounds of this invention have the structure shown in formula (I). This invention also discloses the preparation method of the compounds and their use as AhR inhibitors. The compounds of this invention exhibit excellent selective inhibition of AhR and possess better pharmacodynamic and pharmacokinetic properties, as well as lower toxicity.

The present invention provides pyridazine-3-carboxamide compounds of general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention also provides pharmaceutical compositions comprising said compounds, processes for their preparation and their use in the treatment or prevention of TYK2 kinase-mediated diseases.

This invention belongs to the field of pharmaceutical chemistry technology, and discloses a compound and its uses. Specifically, it relates to a CRBN small molecule ligand compound based on a pyridazine-glutarimide core skeleton (PDG), its composition, and its application. It also relates to a protein degrading agent based on a CRBN small molecule ligand compound based on a pyridazine-glutarimide core skeleton (PDG) and its application. Specifically, the CRBN small molecule ligand compound is shown in (Ⅰ): wherein R... 1 and R 2 Selected from one or more of the following: fused rings attached to a pyridazine core, H, alkyl, OR, F, CN, CF3, NR2, Ph, 4-Py; Y selected from one or more of CH, CD, CF, and N; R 3 Selected from one or more of OR, NR2, CHR2, and C≡CR; R 4 Selected from H or alkyl.

Provided are a method for preparing a metalloenzyme inhibitor compound 1-cyclopropyl-2-(6-(difluoromethyl)pyridazin-4-yl)-5,6-difluoro-1H-benzo[d]imidazole, and an important intermediate for preparing the compound.

This invention belongs to the technical field of preparing tetrahydropyridazine derivatives. The method provided by this invention is simple to operate and does not require an external metal catalyst. The target product contains both a diazoxide and a tetrahydropyridazine skeleton, making it a potential intermediate in the pharmaceutical and materials fields. This invention provides a method for preparing tetrahydropyridazine derivatives, which involves adding a compound having general formula 1, tert-butyl peroxide, and sodium bicarbonate to a solution of acetone, as shown in the following reaction equation:

The present invention provides pyridazinone compounds, their stereoisomers, tautomers, or pharmaceutically acceptable salts, as well as methods related to the preparation and use of these compounds, pharmaceutical compositions containing these compounds, and methods for treating related metabolic diseases. The compounds of the present invention exhibit excellent thyroid hormone receptor activating effects and show promising potential for application in the field of metabolic disease treatment.

The present invention provides pyridazine-3-carboxamide compounds of general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention also provides pharmaceutical compositions comprising said compounds, processes for their preparation and their use in the treatment or prevention of TYK2 kinase-mediated diseases.

To provide treatment or preventive medication for autism spectrum disorder. [Solution] The present invention provides a PDE10A inhibitor for treating or preventing autism spectrum disorder. The inhibitor is 1-[2-fluoro-4-(1H-pyrazole-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazole-5-yl)pyridazine-4(1H)-one or a salt thereof, and is a therapeutic or prophylactic agent for autism spectrum disorder selected from the group consisting of childhood disintegrative disorder, Rett syndrome, Cleefstra syndrome, Pitt-Hopkins syndrome, Angelman syndrome, Kabuki syndrome, Asperger syndrome, Heller syndrome, and pervasive developmental disorder.

The present invention provides a pyridazine-3-carboxamide compound represented by general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention further provides a pharmaceutical composition including the compound, a preparation method therefor and a use thereof in treating or preventing a TYK2 kinase-mediated disease.

Disclosed in the present invention are a 4-amino substituted pyridazinone compound, and a preparation method therefor and the use thereof. The 4-amino substituted pyridazinone compound of the present invention has a structure as represented by formula I, wherein the definition of each substituent is as described in the description and claims. The compound of the present invention can be used in the preparation of anti-tumor drugs, particularly in the preparation of drugs for treating tumors such as melanoma.

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof 【Chemical 1】 TIFF2026516783000088.tif45170(wherein ring B is a monocyclic aromatic group which may be substituted with one or more substituents selected from halo, CN, OH, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, hydroxycycloalkyl, O-cycloalkyl, alkoxy, haloalkoxy, heterocycloalkyl, O-heterocycloalkyl, aryl, heteroaryl, O-aryl, NHCO-alkenyl, NHCO-aryl, -(CH2) q -O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl and CO2-alkyl, and the aryl group, heteroaryl group, heterocycloalkyl group, O-cycloalkyl group, NHCO-aryl group, -(CH2) q -O-heteroaryl group, CONH-aryl group, aryloxy-alkyl group, O-aralkyl group and O-aryl group are each independently selected from halo, alkyl, haloalkyl, alkoxy, NHCO-alkyl, NR 13 R 13 ’, SO2-alkyl, CN, hydroxyalkyl, CONR 14 R 14 ’, alkyl-NR 15 R 15 ’, heterocycloalkyl, alkyl-heterocycloalkyl, alkyl-cycloalkyl, aryl, (CH2) m -NHSO2-alkyl, CO2R 16 、alkoxy-alkyl, haloalkoxy, O-heterocycloalkyl, heteroaryl, alkoxy-alkoxy and O-(CH2) p -cycloalkyl, and may be further substituted with one or more groups independently selected therefrom, and in the latter groups, the cycloalkyl may be further substituted with one or more halo groups, haloalkyl groups, alkyl groups or alkoxy groups, m is an integer from 0 to 3, p and q are each independently from 0 to 3, Y is CR 10 R 10 ’ and R 10 and R10 ' is independently selected from H, F, alkyl and haloalkyl, and R a and R b Each is independently selected from H and alkyl, and R6 is selected from H, alkyl, cycloalkyl and hydroxyalkyl, R 13 , R 13 ', R 14 , R 14 ', R 15 , R 15 'and R 16 A method for preparing a compound of formula (IV) (wherein B is as defined above) and a compound of formula (V) (wherein R is independently selected from H, alkyl, haloalkyl and alkoxyalkyl), wherein (i) a compound of formula (IV) (wherein B is as defined above) is used to prepare a compound of formula (V) (wherein R is independently selected from H, alkyl, haloalkyl and alkoxyalkyl), the method comprising: (i) a compound of formula (IV) (wherein B is as defined above) 21 (ii) Treating the compound of formula (III) with a phenyl which may be substituted with 1 to 5 fluorine atoms to form a compound of formula (III), and (ii) treating the compound of formula (III) with a compound of formula (II) or a pharmaceutically acceptable salt thereof (wherein Y, R a , R b The present invention relates to a method comprising the steps of treating (and R6 as described above) to form a compound of formula (I). Further embodiments relate to intermediates useful in the claimed method.

In crop production, including agriculture and horticulture, damage caused by pests remains significant, and the development of new agricultural and horticultural insecticides is desired due to factors such as the emergence of pests resistant to existing pesticides. [Solution] The present invention relates to the general formula (1) TIFF2026086692000149.tif39170 {In the formula, X and Y represent oxygen atoms or sulfur atoms, Z represents a hydroxyl group, etc., R 1 R represents an alkoxycarbonyl group, etc. 2 R represents a substituted phenyl group, etc. 3 R represents a hydrogen atom, etc. 4 The compound represented by} or its salts exhibits high insecticidal efficacy against pests in the agricultural and horticultural fields, and provides an insecticide for agricultural and horticultural use containing these as active ingredients, as well as a method of using the same.

This invention belongs to the field of chemical synthesis technology, specifically relating to a method for synthesizing 6-(benzyloxy)pyridazine-3-amine. Using 6-chloropyridazine-3-amine as a raw material, this invention synthesizes 6-(benzyloxy)pyridazine-3-amine in one step through the action of sodium hydrogen. This synthesis is simple, easy to operate, and has a high yield.

This invention provides a novel compound, its use in inhibiting CDK12 and / or CDK13 activity and degrading cyclin K, a pharmaceutical composition comprising the compound, and its use in treating diseases (e.g., cancer) associated with CDK12 and / or CDK13 and / or cyclin K. According to the invention, these compounds exhibit excellent inhibitory activity and selectivity against CDK12 and / or CDK13, inducing the degradation of cyclin K, and therefore can be used for the treatment of cancers (e.g., breast cancer or gastric cancer).

The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):

This invention discloses a C5-position selective photocatalytic hydrogenation dechlorination method for 4,5-dichloropyridazinone. The method includes: dissolving 4,5-dichloropyridazinone (Formula I), a photocatalyst, and an organic amine reducing agent in an organic solvent under inert gas protection, and reacting under visible light irradiation to obtain 4-chloropyridazinone (Formula II); wherein R is selected from aryl, heteroaryl, alkyl, benzyl, or acylalkyl; the photocatalyst is disodium eosin Y or tetrabromofluorescein; the organic amine reducing agent is N,N-diisopropylethylamine; the organic solvent is DMF, DMSO, or acetonitrile; and the visible light wavelength is 420-520 nm. This method has advantages such as high regioselectivity, mild reaction conditions, and a wide range of applicable substrates.

This invention belongs to the field of pesticide chemistry. This invention provides an isoxazoline pyridazine derivative, which is a compound represented by general formula I or II or its stereoisomers, polymorphs, isotope labels, or pharmaceutically acceptable salts. The isoxazoline pyridazine derivative of this invention exhibits significant insecticidal activity and broad spectrum, achieving a corrected mortality rate of 23.81%–100.00% against diamondback moth, 17.78%–88.89% against Asian corn borer, and 20.00%–93.33% against peach aphid. The isoxazoline pyridazine derivative of this invention also shows LC50 activity against zebrafish. 50 ≥10 mg / L, which falls under the low-risk category for aquatic organisms and has low environmental risk.

Disclosed herein are solid forms of 7-((2R,4S)-4-((2,3-Dihydrobenzo[b][1,4]dioxin-6-yl-2,2,3,3-d4)oxy)-2-methylpiperidin-1-yl)-8-methyl-4H-pyrimido[1,2-b]pyridazin-4-one hydrochloride, including a crystalline Form X of exhibiting at least X-ray lines (in degrees 2θ ± 0.2°) at 6.69, 8.52, 10.29, 17.42, 20.64, 21.08, 26.22 and 29.52 in a powder diffraction pattern when measured using Cu Kα radiation. Also disclosed herein are pharmaceutical compositions containing the same, and to methods of their use and preparation.

Disclosed are compounds according to Formula (A), and related tautomers and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (A).