910 results about "Pyridazine" patented technology

Provided herein are compounds of Formula (I) and Formula (II) and compositions thereof that capable of disrupting, interrupting, and / or preventing an interaction between a small GTPase protein and a PI3K protein (e.g., PI3Kα). The present disclosure also provides methods of treating cancers and other indications with such compounds or compositions thereof. (I) (II)

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 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 present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.

The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.

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 disclosure relates to inhibitors of NLRP3 of Formula (I):or a pharmaceutically acceptable salt, solvate, clathrate, hydrate, stereoisomer, tautomer, isotopically labeled compound, or prodrug thereof, wherein Ring A is a 5- to 8-membered monocyclic heterocycloalkyl comprising at least one O ring atom, p is 0 or 1, and R1, R2, R3, R4, and X are as defined herein, useful in the treatment of diseases and disorders inhibited by said protein.

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.

To provide: herbicidal substituted phenyl-pyridazine-diones and substituted phenyl-pyridazinone derivatives of formula (I); and processes and intermediates used for the preparation of such derivatives.SOLUTION: The present invention relates to: herbicidal substituted phenyl-pyridazine-diones and substituted phenyl-pyridazinone derivatives of formula (I); and processes and intermediates used for the preparation of such derivatives. The invention further provides: herbicidal compositions comprising such derivatives; and the use of such compounds and compositions in controlling undesirable plant growth, in particular the use in controlling weeds, such as broad-leaved dicotyledonous weeds, in crops of useful plants.SELECTED DRAWING: None

To provide: herbicidal substituted phenyl-pyridazine-diones and substituted phenyl-pyridazinone derivatives of formula (I); and processes and intermediates used for the preparation of such derivatives.SOLUTION: The present invention relates to: herbicidal substituted phenyl-pyridazine-diones and substituted phenyl-pyridazinone derivatives of formula (I); and processes and intermediates used for the preparation of such derivatives. The invention further provides: herbicidal compositions comprising such derivatives; and the use of such compounds and compositions in controlling undesirable plant growth, in particular the use in controlling weeds, such as broad-leaved dicotyledonous weeds, in crops of useful plants.SELECTED DRAWING: None

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.

Described herein are crystalline forms of 6-(6-(((1R,2R,3S,5S)-2-fluoro-9-azabicyclo[3.3.1]nonan-3-yl)(methyl)amino)pyridazin-3-yl)-2-methylbenzo[d]oxazol-5-ol (compound A), a small molecule splicing modulator (SMSM) of mRNA, such as pre-mRNA, encoded by genes, for the treatment of Huntington's disease.

The present invention relates to compounds of formula I. The compounds of the present invention are SMARCA4 protein degradation agents for the treatment of cancer. # imgabs0 #

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.

The invention discloses a preparation method of silver-coated copper powder. The preparation method comprises the following steps: reacting copper-containing complexing mother liquor, a silver source and a reducing agent; the copper-containing complexing mother liquor is prepared from the following raw materials: copper powder, a chelating agent, a dispersing agent and a modification additive; the modification additive comprises at least one of ethylenediamine, ammonium carbonate, ammonia water, tetraethylenepentamine, polyethylene polyamine, imidazole, pyridazine, pyrimidine and pyrazine. According to the preparation method of the silver-coated copper powder, the silver coating layer of the prepared silver-coated copper powder is uniform and compact, and controllable preparation of the silver-coated copper powder with different appearances is achieved.

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.

The present invention relates to a compound of formula (I) A-L1-RCG1 (I) wherein A is of formula (A), R1 is H, an optionally substituted alkyl, alkenyl, alkynyl, R2 is halogen, alkyl; alkenyl; alkynyl; alkylthio; alkylthioalkyl; alkyl-S(O)-; alkyl-S(O2)-; alkyl-S(O)-alkyl-; alkyl-S(O2)-alkyl-; alkoxy; alkoxyalkyl; haloalkoxyalkyl; cycloalkyl-O-alkyl; alkyl-NH- alkyl; (alkyl)2-N-alkyl; alkyl-NH; and (alkyl)2N; R3 is deuterium; H, alkyl; alkenyl; alkynyl; alkylthio; -OR6, -NR7R8, heterocycloalkyl, heteroaryl, aryl, cycloalkyl; L1 is a linker, RCG1 is a reactive chemical group. The present invention also relates to a compound of formula A- L1-G-BA (II) wherein G is the product of reaction between RCG1 and a reactive group RCG2 and BA is a binding agent, a pharmaceutical composition comprising it and its therapeutic uses, for instance for treating cancer.

Described herein is 6-(6-(((lR,2R,3S,5S)-2-fluoro-9- aza bicyclo[ 3.3.1 ]nonan-3-y l)(methyl)a mino) pyridazin-3-y l)-2- methylbenzo[d]oxazol-5-ol (structure B) as a small molecule splicing modulator (SMSM) of mRNA, such as pre-mRNA, encoded by genes, for the treatment of neurological and neurodegenerative diseases, such as e.g. Huntigton's disease, and brain cancer.

The compound shown in the formula (I) shows good activity on various pests and pest mites in agriculture or other fields. Moreover, the compounds can obtain good prevention and treatment effects at a very low dosage, so that the compounds can be used for preparing insecticides and / or acaricides. # imgabs0 #

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.