50 results about "Sulfonylurea" patented technology

Oil dispersion compositions comprising sulfonylurea-florpyrauxifen-benzyl mixtures, having improved stability, are disclosed.

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 application discloses a sulfonylurea herbicide hydrolytic enzyme TsmE mutant, a coding gene thereof and a use thereof. The amino acid sequence of the mutant is shown in SEQ ID NO. 4. The mutant M6 provided by the application has deesterification activity to macromolecular sulfonylurea herbicides methyldisulfuron and sodium salt of methyl iodosulfuron, and therefore has a good application prospect in sulfonylurea herbicide residual pollution bioremediation and anti-herbicide transgenic engineering.

Disclosed in the present invention are a compound as shown in formula 1, or a tautomer, mesomer, racemate, enantiomer and diastereomer thereof, a mixture form thereof, or a pharmaceutically acceptable salt thereof. The compound has excellent NLRP3 inhibitory activity, and the compound of the present invention lays a new material basis for the development of therapeutic drugs for NLRP3-related diseases.

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 belongs to the field of plant genetic engineering technology and specifically relates to a sulfonylurea herbicide-resistant rapeseed gene, protein, primer set, recombinant expression vector, engineered bacteria, and applications thereof. The sulfonylurea herbicide-resistant rapeseed gene of the present invention comprises one or more of BnALS1m1, BnALS1m2, BnALS3m1, and BnALS3m2; the nucleotide sequences of BnALS1m1, BnALS1m2, BnALS3m1, and BnALS3m2 are shown in SEQ ID NO. 1, SEQ ID NO. 2, SEQ ID NO. 3, and SEQ ID NO. 4, respectively. Transgenic expression of the sulfonylurea herbicide-resistant rapeseed gene of the present invention in crops can improve the crop's tolerance and resistance to sulfonylurea herbicides, thereby assisting in the breeding of new crop varieties with high sulfonylurea herbicide resistance.

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.

The present invention discloses a low-cost rapeseed hybrid seed production method, which relates to the field of utilizing hybrid vigor in Brassica napus. The method comprises: (1) hybridizing an Ogura CMS sterile line as the female parent with a plant containing a sulfonylurea herbicide resistance locus to obtain an Ogura CMS sterile line containing the sulfonylurea herbicide resistance locus; (2) planting the Ogura CMS sterile line containing the sulfonylurea herbicide resistance locus as the female parent and an Ogura CMS restorer line as the male parent in a 5:1 ratio in a seed production field, employing conventional field management methods, and harvesting the Brassica napus seeds when mature; and (3) planting the harvested seeds in a conventional field and spraying the sulfonylurea herbicide at the seedling stage to obtain Brassica napus hybrid seeds of higher purity. The present invention mixes the improved Ogura CMS sterile line with the female sterile restorer line in a seed production field to obtain the first generation of offspring, and sprays herbicides at the seedling stage to obtain rapeseed hybrids with higher purity. This method can greatly reduce the cost of seed production. The present invention also provides an effective method for the reproduction of the restorer line 9538R.

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 BnaALS1 linkage mutant protein based on gene editing, a mutant gene and an application of the BnaALS1 linkage mutant protein and the mutant gene. According to the invention, the BnaALS1 gene is edited by using a gene editing technology, and a germplasm resource with linkage mutation is created, so that the BnaALS1 gene has the characteristics of resisting sulfonylurea and imidazolone herbicides at the same time. The BnaALS1 linked mutant germplasm can effectively solve the problem of inhibition of soil residues on rape growth caused by application of imidazolone herbicides to preceding crops, and can also safely apply sulfonylurea herbicides during the rape planting period for field weed prevention and control.

The present application relates to the preparation technology field of sulfonylurea herbicide, propose a trifloxysulfuron synthesis method, including the following steps: S1, 3-(2,2,2-trifluoroethoxy) pyridine-2-sulfonamide is dissolved in solvent, obtain mixed solution, the solvent is acetonitrile and acrylonitrile;S2, 4, 6-dimethoxy pyrimidine-2-yl carbamic acid phenyl ester and catalyst are added to the mixed solution, and reaction is carried out to obtain trifloxysulfuron. Through the above technical scheme, the problem of low purity and low yield of trifloxysulfuron synthesis in the prior art is solved.

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 relates to a kind of preparation method of furan sulfonyl ketone and its intermediate, with 2-chloro-3-methyl-4-methylsulfonyl benzoic acid as raw material, directly bromination is obtained 2-chloro-3-bromomethyl-4-methylsulfonyl benzoic acid;Then 2-chloro-3-bromomethyl-4-methylsulfonyl benzoic acid and tetrahydrofurfuryl alcohol substitution reaction is obtained 2-chloro-4-(methylsulfonyl)-3-(((tetrahydrofuran-2-yl) methoxy) methyl) benzoic acid;Then intermediate acyl chloride is formed;Acyl chloride intermediate and cyclohexanedione are condensed under the action of triethylamine, finally catalyst acetone cyanohydrin is added and rearrangement reaction is obtained target product furan sulfonyl ketone.Compared with prior art, the present application reduces the esterification protection of raw material 2-chloro-3-methyl-4-methylsulfonyl benzoic acid in the step of preparing furan sulfonyl ketone and the deprotection step in subsequent step, and the bromide removed in the reaction can be recycled and reused, shorten the reaction step, improve the overall yield, more green and environmental protection.

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 present disclosure relates to a method for preparing a sulfonylurea derivative. Specifically, the present disclosure relates to a method for preparing a compound represented by formula (I), comprising the step of preparing the compound represented by formula (I) from a compound represented by formula (II) in the presence of LiOtBu. The method has a high yield and mild reaction conditions and thus is suitable for industrial production.

The present invention relates to a composition and a method capable of predicting sulfonylurea dependence in diabetic patients by identifying the variants of: rs777077261(C>A) of KCNB2(Potassium Voltage-Gated Channel Subfamily B Member 2); rs202112906(C>T) of GHSR(Growth hormone secretagogue receptor); rs28944173(T>C) of NOS2(Nitric oxide synthase 2); rs3792268(C>A) of CAPN10(Calpain 10); rs199670165(C>A), rs17848945(C>T), rs755372392(G>A), rs200840955(G>A), rs200842352(C>A) or rs45489599(C>T) of FASN(Fatty acid synthase); rs185358392(G>A), rs769120237(G>A), rs201884071(G>A) or rs766766661(C>T) of KCNH6(Potassium Voltage-Gated Channel Subfamily H Member 6); rs14847401(G>A), rs37551700(G>A) or rs774656238(A>G) of DIS3L2(DIS3 like 3'-5' exoribonuclease 2); or rs74315349(G>A) or rs150546920(C>G) of NR0B2(Nuclear Receptor Subfamily 0 Group B Member 2).

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 present invention relates to compounds of formula (I): wherein Q is selected from O or S; r1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, where R1 is attached to the sulfur atom of the sulfonylurea group via a ring carbon atom, and where R1 may optionally be substituted; and R2 is a cyclic group substituted in the alpha position, wherein R2 may optionally be further substituted. The invention also relates to salts, solvates and prodrugs of such compounds; pharmaceutical compositions comprising such compounds; and to the use of such compounds in the treatment and prophylaxis of medical conditions and diseases, most particularly in the treatment and prophylaxis of medical conditions and diseases by inhibition of NLRP3.

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.