613 results about "Pyridazine" patented technology

The compounds represented by formula (I) of this invention exhibit excellent activity against a variety of pests and mites in agriculture or other fields. Furthermore, these compounds achieve good control effects at very low doses, and therefore can be used to prepare insecticides and / or acaricides.

Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof, and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

The invention relates to a conjugated microporous polymer based on a dicarbazole structure and a preparation method and application thereof, the conjugated microporous polymer has a dicarbazole structure unit and a nitrogen-containing aromatic structure unit, the dicarbazole monomer structure is represented by the formula (I): # imgabs0 #, in the structure represented by the formula (I): R = H, R1 = C = H or R1 = H, R = C = H; the structure of the nitrogen-containing aromatic monomer is shown as a formula (II): # imgabs 1 #, wherein the aromatic structure in the structure shown as the formula (II) is any one of benzene, pyridine, pyrimidine, pyrazine and pyridazine. A plurality of conjugated microporous polymers with excellent photocatalytic performance are obtained by changing aromatic monomers with different nitrogen contents, and the conjugated microporous polymers can be applied to high-efficiency production of hydrogen peroxide under photocatalytic conditions.

The present application relates to a various novel crystalline forms of 2- [3,5-dichloro -4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy) phenyl]-3,5- dioxo- 2,3,4,5-tetrahydro [1,2,4] triazine-6-carbonitrile represented by the following structural formula-1, which is referred to as Resmetirom. The present application also relates to process for the preparation of various novel crystalline polymorphic forms of compound of formula-1.

The present invention relates to a new and improved process for the preparation of substituted N-(2- chloroethyl)-N´-hydroxy-3-phenoxypyridazine-3-carboxamidines, which can be converted to substituted 3-(3-phenoxypyridazin-4-yl)-5,6-dihydro-4H-1,2,4-oxadiazines. In particular, the present 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-methyl-pyridazine-4-carboxamidine, which can be converted to 3-[3-(3- chloro-2-fluorophenoxy)-6-methylpyridazin-4-yl]-5-(2-chloro-4-methylbenzyl)-5,6-dihydro-4H-1,2,4- oxadiazine, more specifically to 3-(3-chloro-2-fluoro-phenoxy)-N-[1-(chloromethyl)-2-(2-chloro-4- methyl-phenyl)ethyl]-N'-hydroxy-6-methyl-pyridazine-4-carboxamidine, which can be converted to (5S)- 3-[3-(3-chloro-2-fluorophenoxy)-6-methylpyridazin-4-yl]-5-(2-chloro-4-methylbenzyl)-5,6-dihydro-4H- 1,2,4-oxadiazine.

Stable and bioavailable formulations and dosage forms comprising a dispersion (e.g., spray-dried dispersion) of solid amorphous 6-(cyclopropancamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide (Formula (I): BMS-986165) in a solid polymer matrix are provided for the treatment of auto-immune and auto-inflammatory diseases such as an inflammatory bowel disease (IBD) and psoriasis.

The present invention relates to solid forms of the poly(ADP-ribose) polymerase 7 (PARP7) inhibitor 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl]amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, and salts thereof, including methods of preparation thereof, where the inhibitor is useful in the treatment of cancer.

A novel additive, an electrolyte, and a lithium ion battery, relating to the technical field of lithium ion batteries. The electrolyte comprises a lithium salt and a non-aqueous solvent for dissolving the lithium salt, the electrolyte further comprises an electrolyte additive, the electrolyte additive comprises a positive electrode film-forming additive and a negative electrode film-forming additive, and the electrolyte additive further comprises a fluoro isocyanate-based pyridazine organic compound. The additive can absorb moisture and hydrofluoric acid in the electrolyte, reduce the dissolution of transition metals, improve the thermal stability of lithium hexafluorophosphate, and maintains the stability of a ternary material under high voltage; a sulfuric acid group on the novel additive can be oxidized by oxygen at a positive electrode, so that the oxygen generated when an LFO lithium supplementing agent is activated is absorbed, the capacity exertion, high temperature cycle and high temperature storage of the LFO lithium supplementing agent are significantly improved, and the DCIR of the battery will not obviously increase, thereby improving the stability of the battery.

The invention belongs to the technical field of pharmacy, and particularly relates to a method for preparing a pyridazinone compound and application of the pyridazinone compound, and the method comprises the following steps: step 1, reacting a compound as shown in a formula V with a Grignard reagent to obtain a compound as shown in a formula IV; 2, reacting the compound shown in the formula IV with succinic anhydride to obtain a compound shown in a formula III; 3, reacting the compound shown in the formula III with hydrazine hydrate to obtain a compound shown in a formula II; 4, oxidizing the compound shown in the formula II to obtain a pyridazinone compound; the pyridazinone compound or the pharmaceutically acceptable salt or prodrug of the pyridazinone compound can be used for inhibiting the activity of MET protein kinase and the mutant form of the MET protein kinase, and especially can be used as a Tepotinib intermediate.

Described herein are crystalline forms of the MAGL inhibitor 1,1,1,3,3,3-Hexafluoropropan-2-yl(S)-1-(pyridazin-3-ylcarbamoyl)-6-azaspiro[2.5]octane-6-carboxylate.

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl) thieno[2,3-d]pyrimidine-2,4 (1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

The invention discloses an all-organic polymer S-type heterojunction photocatalytic material and a preparation method and application thereof.The all-organic polymer S-type heterojunction photocatalytic material comprises a carrier and an organic polymer growing on the surface of the carrier, organic monomers are originally polymerized on the surface of carbon nitride to form an all-organic polymer S-type heterojunction, and the organic monomers are 1, 4-diacetylene benzene, 2, 4-diacetylene benzene and 2, 4-diacetylene benzene. The compound is 3, 5-diacetylene pyridine or 3, 6-diacetylene pyridazine; the preparation method comprises the following steps: (1) adding carbon nitride and a catalyst into a polar alkali solution, and uniformly mixing; and (2) putting an organic monomer into the mixed solution, and carrying out polymerization reaction to generate the all-organic polymer S-type heterojunction photocatalytic material in situ. The carbon nitride is selected as a carrier to be compounded with the organic conjugated polymer, the organic conjugated polymer can be adjusted to be matched with the energy band position of the carbon nitride by changing the molecular structure, an all-organic polymer S-shaped heterojunction is formed, the intramolecular charge transfer rate is higher, and the photocatalytic performance is improved.

Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof, and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

The invention provides a Zn-MOF material, a preparation method thereof and application of the Zn-MOF material in Congo red dye adsorption, and relates to the technical field of metal organic framework materials. The preparation method provided by the invention comprises the following steps: reacting 2-methylimidazole with 3, 6-dichloropyridazine in an alkaline solvent environment to generate 3, 6-bis (2-methylimidazole) pyridazine; the preparation method comprises the following steps: mixing and coordinating 3, 6-bis (2-methylimidazole) pyridazine, isophthalic acid and a zinc source to prepare a Zn-MOF material; the Zn-MOF material prepared by the preparation method disclosed by the invention can be used for effectively adsorbing Congo red.

The invention discloses a preparation method of 3, 6-dichloropyridazine, and belongs to the technical field of chemistry. According to the method, 3, 6-dihydroxypyridazine is used as a raw material, an organic solvent and triphenylphosphine oxide are combined to form a dichlorotriphenylphosphine intermediate state which is used as a chlorinating agent, dihydroxyl is substituted to generate 3, 6-dichloropyridazine, triphenylphosphine oxide and solid light are used as raw materials, heating reaction is performed to prepare 3, 6-dichloropyridazine, meanwhile, a one-pot method can be adopted in the two-step reaction, and operation is easy and convenient. The novel preparation method for synthesizing 3, 6-dichloropyridazine provided by the invention has the advantages of low raw material cost, high yield, high gas phase purity and no pollution, is suitable for industrial production, can meet industrial requirements, provides a new idea for later preparation of 3, 6-dichloropyridazine, has the remarkable advantages of high gas phase purity and high yield, and is suitable for industrial production. Wide application prospects are realized.

The present disclosure relates to heterocyclyl pyridazine compounds, processes and intermediates for their preparation as well as the uses thereof for controlling phytopathogenic microorganisms, such as phytopathogenic fungi.

The invention discloses a preparation method and application of a nitrogen-containing heterocyclic porous covalent organic framework material. The preparation method comprises the following steps: mixing trialdehyde phloroglucinol and a nitrogen heterocyclic ring-containing monomer according to a certain mass ratio, adding an organic catalyst and a mixed solvent, degassing, sealing, carrying out solvothermal reaction synthesis, washing with a polar solvent, carrying out Soxhlet extraction and purification, and drying to obtain the nitrogen heterocyclic ring-containing porous covalent organic framework material. According to the method, a pyridazine unit and trialdehyde phloroglucinol are used as monomers to construct a COF skeleton of a nitrogen heterocyclic ring, an asymmetric pi-conjugated structure is formed, efficient electron-hole space separation is achieved, active site charge distribution is optimized through the electron-rich characteristic of the pyridazine unit, and the oxygen molecule adsorption and activation capacity is enhanced. The method adopts a green solvent, is mild in reaction condition, avoids the use of toxic reagents, is green and environment-friendly, and provides a new way for photocatalytic synthesis of hydrogen peroxide.

Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α.

The present invention relates to a compound of formula (I) wherein R1 is a hydrogen atom, halogen or -(C1-C2)alkyl, R2 is -halo(C1-C2)alkoxy, and R3 and R4 form together with N to which they are attached an optionally substituted 5-7 membered monocyclic heterocycloalkyl ring or an optionally substituted 8-11 membered bicyclic heterocycloalkyl ring. The present invention also relates to a medicament and a pharmaceutical composition comprising said compound of formula (I), as well as their therapeutic uses, in particular as inhibitor of NOD-like receptor protein 3 inflammasome for preventing and / or treating Parkinson's disease, frontotemporal Dementia, Multiple System Atrophy, Alzheimer's disease, Multiple Sclerosis, Amyotrophic Lateral Sclerosis or brain injury.

Provided herein are crystalline salt and free base forms and amorphous forms of a compound having the following formula (I): (I) Compound 1. Also provided are pharmaceutical compositions comprising such crystalline and amorphous forms, processes for their manufacture and their use for the treatment of various conditions such as hemolytic anemia, sickle cell disease and MDS (very low risk MDS, low risk MDS, lower risk MDS and / or moderate risk MDS).

The invention discloses a crystal form, a salt form, a composition and a preparation method of a pyridazine compound, and particularly discloses a preparation method and application of a crystal form A and a composition of a compound shown as a formula (I), a crystal form B of a compound shown as a formula (II) and a crystal form C of a compound shown as a formula (III).

The invention belongs to the technical field of chemical synthesis, and particularly relates to a difluoroalkylated tetrahydropyridazine compound and a preparation method thereof. The preparation method of the difluoroalkylated tetrahydropyridazine compound comprises the following steps: by taking an acethydrazide compound and a difluoroalkyl compound as reaction raw materials, mixing the reaction raw materials, a photosensitizer, reaction alkali and a solvent under a nitrogen condition, and reacting under blue light to obtain the difluoroalkylated tetrahydropyridazine compound. A difluoroalkyl compound is reduced by a photosensitizer to generate a difluoroalkyl free radical, and the difluoroalkyl free radical and an acethydrazide compound are subjected to an addition reaction to obtain the difluoroalkylated tetrahydropyridazine compound. The method does not need to additionally add a metal catalyst or an oxidizing agent or a reducing agent, and is simple to operate, mild in reaction condition, wide in substrate universality, green and environment-friendly.

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 invention relates to a process for the preparation of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, where: Ring B is a monocyclic aromatic group; the present invention relates to a halogen-containing compound optionally substituted by one or more substituents selected from the group consisting of halogen, 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, wherein the aryl, heteroaryl, heterocycloalkyl, O-cycloalkyl, NHCO-aryl,-(CH2) q-O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and O-aryl groups are each optionally further independently selected from the group consisting of halogen, 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, wherein, in the latter group, the cycloalkyl is optionally further substituted by one or more halogen, haloalkyl, alkyl or alkoxy groups, and wherein, in the latter group, the cycloalkyl is optionally further substituted by one or more halogen, haloalkyl, alkyl or alkoxy groups, and wherein, in the latter group, the alkyl is optionally further substituted by one or more halogen, haloalkyl, alkyl or alkoxy groups; m is an integer from 0 to 3; p and q are each independently 0 to 3; y is CR10R10 ', wherein R10 and R10' are each independently selected from the group consisting of H, F, alkyl, and haloalkyl; ra and Rb are each independently selected from H and alkyl; r6 is selected from H, alkyl, cycloalkyl and hydroxyalkyl; the present invention relates to a process for the preparation of a compound of formula (I) wherein B is as defined above, and R13, R13 ', R14, R14', R15, R15 ', and R16 are each independently selected from H, alkyl, haloalkyl, and alkoxyalkyl, comprising the steps of: (i) treating a compound of formula (IV) with a compound of formula (V) to form a compound of formula (III) wherein B in formula (IV) is as defined above, R21 in formula (V) is phenyl optionally substituted by 1 to 5 fluorine atoms; and (ii) treating the compound of formula (III) with a compound of formula (II) in which Y, Ra, Rb and R6 are as described above, or a pharmaceutically acceptable salt thereof, to form a compound of formula (I). Other aspects of the invention also relate to intermediates useful in said processes.

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 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.

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.

The present invention is directed to morphic forms, co-crystals, salts, and amorphous solid dispersions of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile.

The application discloses a method for regionally selective C3-H alkyne of triazolopyridazine compounds, and belongs to the field of organic synthesis. The method uses triazolopyridazine and high-valence iodine (III) alkyne reagent as raw materials, and a double catalytic system composed of Ph3PAuNTf2 (5 mol%), AgOTf (5 mol%) and 1,10-phenanthroline (20 mol%) in dichloromethane, and after reaction at 50 DEG C, the C3 alkyne product is obtained through purification. The method solves the problems of catalyst deactivation and poor selectivity caused by nitrogen-rich heterocyclic rings through gold / silver synergistic catalysis, and realizes precise functionalization of the C3 position. The reaction condition is mild, the substrate is widely applicable (R¹ contains various aryl groups and heteroaryl groups, and R² is compatible with different substituted aryl groups), the yield is 60% to 95%, the step is economical, and the method is suitable for large-scale preparation.