363 results about "Pyridazine" patented technology

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 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 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 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).

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 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.

The present invention provides a compound having inhibitory activity against a Mas-related G protein-coupled receptor X2. The present invention provides a compound having the following structural formula or the like, or a pharmaceutically acceptable salt thereof.

A compound useful as an active ingredient in a pharmaceutical composition for the treatment of cancer related to the activation of immune cells or cancer resistant to treatment with anti-PD-1 / anti-PD-L1 antibodies is provided. The inventors hereof have conducted studies on a compound useful as an active ingredient in a pharmaceutical composition for the treatment of cancer related to the activation of immune cells or cancer resistant to treatment with anti-PD-1 / anti-PD-L1 antibodies and discovered that a pyridazinyl-thiazolcarboxamide compound has an inhibitory effect on DGKβ (DGKzeta), leading to the achievement of the present invention.The pyridazinyl-thiazolcarboxamide compound of the present invention has an inhibitory effect on DGK and can be used as a therapeutic agent for the treatment of cancer related to the activation of immune cells or cancer that offers resistance to treatment with anti-PD-1 antibodies / anti-PD-L1 antibodies.

The invention belongs to the technical field of pyridazine derivative preparation. The invention provides a preparation method of a pyridazine derivative. The preparation method comprises the following steps: adding a compound with a general formula 1, iron nitrate nonahydrate, potassium carbonate and 4CzIPN into tetrahydrofuran for reaction; the reaction equation is shown in the specification; in the formula (I), R is hydrogen, 4-methyl, 4-methoxyl, 3-methoxyl, 2-iodine or 4-chlorine. The method provided by the invention is simple and convenient to operate and does not need high temperature and oxidant. The target product simultaneously contains diaza and pyridazine skeletons.

Treatments of neuromuscular conditions, activity-induced muscle damage, metabolic myopathies, and movement disorders with compositions comprising 2-((5-fluoropyridin-3-yl)methyl)-6-(2-(2,2,2-trifluoroethoxy)pyrimidin-5-yl)pyridazin-3(2H)-one (Compound 1), as well as solid forms of Compound 1, and pharmaceutical compositions of Compound 1, and kits of Compound 1, are described herein.

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.

The invention provides a pyridazinone compound, or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, and also provides a method related to preparation and application of the compound, a pharmaceutical composition containing the compound and a treatment method of related metabolic diseases. The compound disclosed by the invention shows an excellent thyroid hormone receptor excitation effect and has a wide application prospect in the field of metabolic disease treatment.

The invention provides a production process of pyridaben, and belongs to the technical field of pesticides, and the production process comprises the following steps: adding a dichloropyridazinone-methanol solution and p-tert-butyl benzyl mercaptan into a condensation reaction kettle, dropwise adding an acid-binding agent, and carrying out a condensation reaction to obtain a pyridaben mixed solution; transferring the pyridaben mixed solution into a heating kettle, heating to completely dissolve the pyridaben, then carrying out filter pressing by a filter press into a crystallization kettle, carrying out cooling recrystallization, and then carrying out centrifugal separation and drying to obtain the pyridaben. According to the invention, pyridaben is produced by adopting a new process of directly heating, filtering and recrystallizing after condensation reaction, so that the use of high-toxicity and high-risk organic solvents such as methylbenzene in the recrystallization process is effectively avoided, the original production process is simplified, the product content is increased, the production cost is reduced, and the market demand can be fully met.

The invention belongs to the technical field of biological medicines, relates to application of a compound 1 in treatment or prevention of diseases related to RET fusion and / or RET mutation, and provides application of N (3-chloro-5 (trifluoromethyl) phenyl) 3 ((6 (4-hydroxypiperidine-1-yl) imidazo [1, 2-a] pyridin-2-yl)-1, 3, 4-triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4 The invention relates to application of (2R, 2R, 2b) pyridazin-3-yl) ethynyl) 2-methylbenzamide or pharmaceutically acceptable salts thereof in treatment or prevention of RET fusion and / or RET mutation related diseases, and application of the (2R, 2R, 2b) pyridazin-3-yl) ethynyl) 2-methylbenzamide or pharmaceutically acceptable salts thereof in treatment or prevention of RET fusion and / or RET mutation related diseases in treatment or prevention of RET fusion and / or RET mutation related diseases by utilizing broad-spectrum and efficient RET inhibition activity, excellent drug-resistant mutation covering ability and higher safety The technical problems of drug resistance, off-target toxicity, high medication frequency and the like of the existing RET inhibitor are solved, and a new effective means is provided for accurate treatment of RET-driven tumors.

The present invention relates to a pyridazinone derivative and a use thereof. Specifically, the present invention relates to a compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition thereof, and a use of the compound represented by general formula (I) or the pharmaceutical composition thereof in the preparation, prevention and / or treatment of Myosin-mediated diseases, wherein each substituent in general formula (I) is as defined in the description.

The invention discloses a pyridazinone compound as well as a pharmaceutical composition and application thereof. The structure of the compound is shown as a formula (I), and the compound comprises a racemate, a stereoisomer, a tautomer, a nitrogen oxide, a stable isotope compound, a metabolite, a solvate, a pharmaceutically acceptable salt or a mixture of the racemate, the stereoisomer, the tautomer, the nitrogen oxide, the stable isotope compound and the metabolite. The compound has a proper half-life period, can be decomposed in blood through injection or oral administration to generate a PARP7 inhibitor compound and dextroborneol, and the PARP7 inhibitor compound and dextroborneol can penetrate through a blood brain barrier, show a good synergistic interaction effect, are beneficial to medicine formation and have a clinical application prospect in prevention or / and treatment of cerebral apoplexy.

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 discloses a pyridazine ring compound as well as a pharmaceutical composition and application thereof. Specifically, the invention discloses a compound as shown in a formula (I), pharmaceutically acceptable salts thereof, solvates thereof or solvates of the pharmaceutically acceptable salts thereof. The pyridazine ring compound disclosed by the invention has good inhibitory activity on NLRP3 (Nuclear Link Receptor Protein 3).

The present invention provides a compound having the structure:whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 orC1-C4 alkyl;R6 is H, OH, or halogen;B is a substituted or unsubstituted heterobicycle, pyridazine, pyrazole, pyrazine, thiadiazole, or triazole,wherein the heterobicycle is other than chloro substituted indole; andthe pyrazole, when substituted, is substituted with other than trifluoromethyl,or a pharmaceutically acceptable salt thereof.

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.

The present invention provides a process for the preparation of aminopyridazine derivatives, and novel pyridazine-based and pyrazole-based compounds which are useful as either starting materials or intermediates in said process.

The present invention relates to an industrially advantageous process for the preparation of pyridazinone derivative. More specifically, the present invention relates to an efficient process which is operationally simple and suitable for industrial application and will eliminate or limit the presence of impurities in the pyridazinone derivative, an investigational new drug.