28 results about "Sulfonylurea" patented technology

To provide an adjuvant that can maintain the therapeutic effect while reducing the dose of the SU drugs since sulfonylurea drugs (hereinafter also referred to as "SU drugs"'), which are antidiabetic drugs, induce pancreatic β cell exhaustion when used long-term in addition to the side effects of hypoglycemia and weight gain and have side effects of reduced efficacy (hypoglycemic effect) and renal damage.SOLUTION: If D-allulose is administered before or simultaneously with SU drug administration, the hypoglycemic effect of SU drugs will be enhanced. As a result, the above-mentioned problem is solved because the dose of SU drugs can be significantly reduced. Furthermore, since D-allulose has been eaten by humans, it can provide a highly safe drug when combined with SU drugs.SELECTED DRAWING: Figure 3

The present application relates to a preparation method of cyprosulfamide, and the cyprosulfamide is prepared by using a one-pot method, and the method specifically comprises the following steps: adding an organic base, a reaction solvent, 2-chloro-3-(2,2,2-trifluoroethoxy)methyl-4-methylsulfonylbenzoic acid and a Curtius condensing agent into a reaction container, heating and refluxing for 3-5 h to generate an active ester intermediate; after the reaction solution containing the active ester intermediate is cooled, 1,3-cyclohexanedione and acetone cyanohydrin are added to perform a condensation rearrangement reaction, and cyprosulfamide is generated. The one-pot synthesis process is adopted, the use of dimethyl sulfoxide is avoided, compared with a traditional process, the method is green, environmentally friendly, has low safety risks, has high yield and good purity, and is more suitable for industrialized production.

The invention discloses a sulfonylurea structure-containing compound as well as a preparation method and application thereof, and relates to the technical field of preparation and application of medical inhibitor compounds. The structure of the compound containing the sulfonylurea structure is shown in the specification. The preparation method comprises the following three steps: synthesizing an intermediate 1 from raw materials through Suzuki coupling reaction, obtaining an intermediate 2 through Sonogashira coupling reaction, and synthesizing a target compound through Williamson reaction. Through the synergistic effect of sulfonyl and ureido, accurate recognition and efficient embedding of a kinase ATP binding pocket are achieved, and the technical bottlenecks that a traditional c-Met inhibitor is poor in selectivity, drug resistance is likely to be generated and the synthesis process is complex are solved.

The present invention relates to a sulfonylurea derivative and medical uses thereof, specifically relating to the sulfonylurea derivative shown in general formula (I), a preparation method thereof, a pharmaceutical composition containing same, and a use of same for treating diseases and disorders affected by neuronal damage, for example: cerebral stroke, brain damage, neuropathic pain, migraines, inflammatory pain, chronic pain, or depression. The definition of each group in the general formula (I) is the same as that in the description.

The invention provides a pharmaceutical composition of a sulfonylurea derivative. Specifically, the present disclosure provides a pharmaceutical composition comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a stabilizer and a buffer agent. The composition has excellent stability. = = =

The invention discloses a herbicide-resistant gene StGSTF8 in sagittaria trifolia and application of the herbicide-resistant gene StGSTF8, and belongs to the technical field of genetic engineering. The bensulfuron methyl resistance gene StGSTF8 (glutathione-S-transferase F8) is identified from sagittaria trifolia for the first time by means of proteomics, molecular biology, transgenic function verification and the like, the nucleotide sequence is as shown in SEQ ID NO: 1, the coded amino acid sequence is as shown in SEQ ID NO: 2, and the nucleotide sequence is as shown in SEQ ID NO: 1. It is proved that the strain endows plants with resistance through mediating herbicide detoxification metabolism and oxidative stress resistance, and reference is provided for improvement of the resistance of plants to sulfonylurea herbicides and research and development of novel herbicides.

This invention discloses the application of the WAT1 gene in regulating the absorption and accumulation of sulfonylurea herbicides in plants. The invention found that knocking out the OsWAT1 gene in rice reduces the absorption and accumulation of bensulfuron-methyl, lowers the bensulfuron-methyl content in rice, and increases resistance to bensulfuron-methyl. Rice with the OsWAT1 gene knocked out also developed resistance to ethoxysulfuron and sulfadiazine. Furthermore, knocking out the NtWAT1 homolog of flue-cured tobacco K326, indoor resistance verification experiments showed that the tobacco mutant also acquired bensulfuron-methyl resistance, also achieved by reducing herbicide absorption and accumulation. This indicates that the WAT1 gene plays a role in regulating the absorption and accumulation of sulfonylurea herbicides in plants and can be used to create new plant varieties with resistance to sulfonylurea herbicides.

Novel gene repressor systems are provided that are useful in animal cells that include engineered repressors with altered ligand-binding domains (LBDs) and DNA-binding domains (DBDs), as well as mutated operator sequences. In one aspect, the systems enable independent, drug-inducible control of multiple genes within a single animal or animal cell line. In one aspect, the disclosure provides both tetracycline-responsive repressors and sulfonylurea (SU)-responsive repressors — e.g., variants that respond specifically to ethametsulfuron-methyl (Es) or chlorsulfuron (Cs). Mutations are introduced to either the LBD (to alter ligand specificity), DBD (to alter operator binding), or the operator sequence itself, resulting in orthogonal systems.

The present invention relates to aqueous dispersions comprising an ALS inhibitor, typically a sulfonylurea herbicide, specifically from the class of triazolinones herbicides, a HPPD inhibitor, specifically a triketone as from the class of 2-benzoyl-1,3-cyclohexanedione herbicides, optionally a safener from the class of the sulfonamides, a water-soluble herbicide present as a salt, specifically glyphosate and to dispersions resulting from dispersing the concentrate suspension in water, to a method of making the aqueous suspension and to a method of controlling unwanted plants using these dispersions.

This invention belongs to the field of plant genetic engineering and plant stress resistance biotechnology, and discloses... ZmCYP81Q32 Application of genes in improving nicosulfuron resistance in plants. This invention provides... ZmCYP81Q32 The nucleotide sequence of the gene, as shown in SEQ ID NO:1, encodes a cytochrome P450 enzyme that can directly bind to sulfonylurea herbicides and promote their hydroxylation metabolism. This reduces the accumulation of the parent herbicide in the plant, alleviates herbicide-induced growth inhibition, leaf chlorosis, and oxidative damage, and significantly improves plant tolerance to sulfonylurea herbicides, especially enhancing plant resistance to nicosulfuron. This invention can be widely used for crop herbicide resistance improvement, herbicide-tolerant germplasm creation, and related molecular breeding.

The invention discloses a morin derivative and a preparation method and application thereof, the morin derivative has the following molecular structure expression, the derivative not only has significantly improved hypoglycemic effect, but also is beneficial to improvement of biosafety compared with existing sulfonylurea drugs; .

The present disclosure describes sulfonylurea derivatives compounds of Formula (I), and pharmaceutically acceptable salts thereof, compositions, methods, and uses thereof. Such compounds are believed to be therapeutically useful as inhibitors of KAT6A with improved selectivity particularly in the treatment and / or prevention of diseases and disorders mediated by KAT6A in a subject.

The present application relates to sulfonylurea derivatives or pharmaceutically acceptable salts thereof and uses thereof. In particular, the present application relates to the use of sulfonylurea derivatives or pharmaceutically acceptable salts thereof as NLRP3 inflammasome inhibitors, wherein the structure of the sulfonylurea derivatives is according to Formula I, wherein the definitions of the substituents are as described in the specification.

The present application provides a kind of fluorine sulfonylureas in the emulsifiable concentrate of loxylone and its preparation method, the fluorine sulfonylureas in the emulsifiable concentrate of loxylone is composed of the following weight percentage components: fluorine sulfonylureas 2-30%, loxylone 2-30%, solvent A 5-20%, basic substance 0.1-5%, alcohol 2-10%, plant oil derivative product 2-20%, emulsifier 2-30%, solvent B makes up the rest.This emulsifiable concentrate of loxylone containing fluorine sulfonylureas is stable at low dilution, can be applied to aerial application, compared with traditional fluorine sulfonylureas and loxylone emulsifiable concentrate, the effect of weed control is better.

This invention provides a gene for Brassica napus resistant to the sulfonylurea herbicide bensulfuron-methyl, encoding the amino acid sequence shown in SEQ ID NO:2, exhibiting resistance to the sulfonylurea herbicide bensulfuron-methyl. Preferably, the nucleotide sequence of the Brassica napus resistant gene to bensulfuron-methyl is shown in SEQ ID NO:1. The invention also provides the application of the above-mentioned Brassica napus resistant gene to bensulfuron-methyl in detecting plants, plant cells, or plant tissues resistant to the sulfonylurea herbicide bensulfuron-methyl, and in cultivating plants, plant cells, or plant tissues resistant to the sulfonylurea herbicide bensulfuron-methyl. The Brassica napus resistant gene to bensulfuron-methyl of this invention provides stable resistance to the sulfonylurea herbicide bensulfuron-methyl. Brassica napus with this gene recovers quickly from herbicide damage, exhibits excellent plant type, normal fruit setting, and can be safely used at the recommended field concentration.

The application discloses an ALS inhibitor sulfonylurea herbicide and a preparation method and application thereof, relates to the technical field of herbicides, and comprises 22 compounds with structures as shown in general formula I or optical isomers, crystal forms, pharmaceutically acceptable salts, hydrates or solvates of each of the compounds and a preparation method and application thereof. After reasonable collocation, the medicine has good prevention and control effects on gramineous plants or broad-leaved plants. The herbicide does not cause harm to soil and environment.

The present disclosure relates to compounds of Formula (I)and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

The application discloses a new sulfonylurea herbicide-resistant mutation gene of Brassica napus and application thereof, and relates to the field of plant molecular breeding. The application provides a breeding method for creating sulfonylurea (SU) herbicide-resistant rapeseed through interspecific distant cross of Brassica napus and self-crossing for 6 generations, and specifically comprises the following steps: creating a new sulfonylurea herbicide-resistant Brassica napus NR9 through interspecific distant cross of Brassica napus and self-crossing for 6 generations; performing PCR amplification on the NR9 by using specific primers of an acetolactate synthase gene (ALS3) to obtain three new nucleotide mutation site sequences of the NR9 on the ALS3, and the three new nucleotide mutation site sequences are respectively a 312th nucleotide, a 535th nucleotide and an 816th nucleotide; and introducing the gene containing the mutation site into other rapeseed germplasm which is not resistant to sulfonylurea herbicide by using plant conventional breeding methods such as hybridization and backcrossing to improve the tolerance of the target variety or strain of the ALS3 gene mutation nucleic acid sequence to the sulfonylurea herbicide.

The application relates to the technical field of organic synthesis, and particularly discloses a synthesis method and application of 2-chloro-4-methoxy-6-methylthio-1,3,5-triazine. The synthesis method of 2-chloro-4-methoxy-6-methylthio-1,3,5-triazine comprises the following steps: 2,4,6-trichloro-1,3,5-triazine is added into methanol, sodium bicarbonate is added, and stirring and mixing are carried out to obtain a mixed solution; methyl mercaptan is added into the mixed solution at -10-0 DEG C, and stirring reaction is carried out at 10-30 DEG C for 2-3 hours to obtain a reaction solution; ice water is added into the reaction solution, standing is carried out, solid is collected through filtration, and drying is carried out to obtain 2-chloro-4-methoxy-6-methylthio-1,3,5-triazine. The 2-chloro-4-methoxy-6-methylthio-1,3,5-triazine disclosed by the application can be used for synthesizing sulfonylurea herbicides, and has the characteristics of easy degradation, low toxicity, high activity and low cost.

Novel gene repressor systems are provided that are useful in animal cells that include engineered repressors with altered ligand-binding domains (LBDs) and DNA-binding domains (DBDs), as well as mutated operator sequences. In one aspect, the systems enable independent, drug-inducible control of multiple genes within a single animal or animal cell line. In one aspect, the disclosure provides both tetracycline-responsive repressors and sulfonylurea (SU)-responsive repressors — e.g., variants that respond specifically to ethametsulfuron-methyl (Es) or chlorsulfuron (Cs). Mutations are introduced to either the LBD (to alter ligand specificity), DBD (to alter operator binding), or the operator sequence itself, resulting in orthogonal systems.

The utility model belongs to sulfonylurea production technical field discloses a kind of production device of sulfonylurea, including reaction kettle main body, and the inside of reaction kettle main body has hollow interlayer;Spiral heat exchange mechanism, spiral heat exchange mechanism includes by concentric arrangement inner spiral guide vane and outer spiral cooling pipe, and the rotation direction of inner spiral guide vane and outer spiral cooling pipe is opposite;Dispersion mechanism, dispersion mechanism includes with the vertical and rotation installation drive shaft of reaction kettle main body, and drive shaft is driven by drive motor mounted on reaction kettle main body, and three layers of dispersion disc are installed on drive shaft, and inner spiral guide vane is welded to the inner wall of reaction kettle main body, and the inclination angle of inner spiral guide vane is 45 °, and the plate height of inner spiral guide vane is one sixth of reaction kettle main body diameter.The utility model not only can realize dynamic strengthening heat exchange, but also can guarantee the efficiency of mass transfer in high viscosity stage, while it can solve the problem of local overheating caused by sulfonation heat release.

The present invention relates to a composition and method for predicting sulfonylurea dependency in diabetes mellitus patients by identifying the mRNA level of GIPR (gastric inhibitory polypeptide receptor), the level or activity of GIPR protein, or mutations inhibiting the level or activity of GIPR, and for modulating such dependency by regulating these factors.

The present invention relates to novel compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions in which interleukin 1β activity is implicated.

The invention discloses a method for evaluating the medicine curative effect of a sulfonylurea medicine for treating MODY3. According to the application disclosed by the invention, the fact that after the MODY3 is treated by the sulfonylurea medicine, the expression of the Phosphoryl-1d-myo-inositol, the expression of the Phosphoryl-L-serine, the expression of the Sphingosine-1-phosphate, the expression of the Triacylglycinol, the expression of the 1, 2-diacyl-3-(alpha 1-6 alpha beta 1)-s-glycinol, the expression of the 1-acyl-1-glycinol, the expression of the Phosphoryl-glycinol and / or the expression of the 1-acyl-1-glycinol, the expression of the Phosphoryl-glycinol and the expression of the 1-acyl-1-glycinol are changed is found for the first time.

A Sorghum seed comprising in its genome at least one polynucleotide encoding a polypeptide having an alanine to tyrosine substitution at position 93 of the Sorghum AHAS protein large subunit. The plant has increased resistance to one or more herbicides, for example from the imidazolinone group, as compared to wild-type Sorghum plants. The Sorghum plant may comprise in its genome, one, two, three or more copies of a polynucleotide encoding a mutated large subunit of Sorghum AHAS or a Sorghum AHAS polypeptide of the invention. In this context, the Sorghum plant may be tolerant to any herbicide capable of inhibiting AHAS enzyme activity. For example, the Sorghum plant may be tolerant to herbicides of the imidazolinones type, such as imazethapyr, imazapir, and imazapic or to herbicides of the sulfonylurea group.

The invention discloses a compound as shown in a formula 1, or a tautomer, a meso-mer, a raceme, an enantiomer, a diastereoisomer, a mixture form or a pharmaceutically acceptable salt thereof. The compound has excellent NLRP3 inhibitory activity, and the compound provided by the invention lays a new material basis for development of drugs for treating NLRP3 related diseases.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a urea derivative based on a sulfonylurea skeleton and a preparation method and application thereof. The urea derivative based on the sulfonylurea skeleton provided by the invention has a typical acid center as a primary pharmacophore of a prostaglandin E receptor 4, and molecular docking shows that a sulfonylurea part and a key amino acid residue Arg316 form a metal ionic bond, so that the urea derivative based on the sulfonylurea skeleton has high inhibitory activity on human EP4. Meanwhile, the urea derivative based on the sulfonylurea skeleton provided by the invention has a typical urea structure as a primary pharmacophore of sEH, and molecular docking shows that the urea structure can be combined with a key catalytic triad of soluble epoxide enzyme protein, so that the urea derivative based on the sulfonylurea skeleton has high inhibitory activity on human-derived sEH and mouse-derived sEH; the compound has small side effects and can be used as an EP4 / sEH double-target inhibitor.

The application discloses a sulfonylurea-containing compound and a preparation method and application thereof, and relates to the technical field of preparation and application of pharmaceutical inhibitors. The sulfonylurea-containing compound has the structure of: The preparation method is realized through three steps: raw materials are subjected to a Suzuki coupling reaction to synthesize an intermediate 1, subjected to a Sonogashira coupling reaction to obtain an intermediate 2, and subjected to a Williamson reaction to synthesize a target compound. Through the synergistic effect of a sulfonyl group and a urea group, precise recognition and efficient embedding of a kinase ATP binding pocket are realized, and the technical bottlenecks of poor selectivity, easy drug resistance and complex synthesis process of traditional c-Met inhibitors are solved.