342 results about "Sulfonilamide" patented technology

The present invention addresses the problem of providing a novel compound that has an OX2R agonist activity.　The present invention relates to a substituted sulfonamide compound which is represented by formula (I) or a pharmacologically acceptable salt thereof. A compound according to the present invention, or a pharmacologically acceptable salt thereof, has an agonist activity against OX2R, and is useful as, for example, a therapeutic agent for sleep disorders associated with OX2R (for example, narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorders, insufficient sleep syndrome, and extended sleep).

The invention belongs to the technical field of sulfonamide synthesis, and particularly relates to a green and environment-friendly sulfonamide amidation preparation method. Comprising the following steps: adding chlorosulfonic acid into a reactor, stirring, heating, adding o-nitrochlorobenzene, carrying out staged heat preservation, cooling, and adding thionyl chloride to obtain 2-nitro-4-chlorine sulfonate-chlorobenzene; the method comprises the following steps: separating and filtering 2-nitro-4-chlorine sulfonate-chlorobenzene, adding ammonia water, stirring, preserving heat, and carrying out filter pressing to obtain 2-nitro-4-amine sulfonate-chlorobenzene; the preparation method comprises the following steps: adding liquid caustic soda into 2-nitro-4-amine sulfonate-chlorobenzene, stirring, heating, and adjusting the pH value to obtain 2-nitro-4-amine sulfonate-phenol; the method comprises the following steps: adding water, a catalyst and hydrazine hydrate into 2-nitro-4-amine sulfonate-phenol, heating, stirring, and carrying out filter pressing to obtain 4-sulfonamide-2-amino-phenol. According to the preparation method of sulfonamide, generated tail gas is subjected to falling film absorption treatment, and the product prepared by the preparation method is high in purity.

The invention discloses a preparation method of alplsutentan and an alplsutentan intermediate, alplsutentan is obtained by taking a compound SM1 as a raw material through a one-step method or a multi-step method, and the multi-step method comprises the following steps: reacting the compound SM1 with a compound SM2 to obtain an intermediate I; reacting the intermediate I with 2-[(5-bromo-2-pyrimidinyl) oxy] ethanol to obtain an intermediate II, or reacting the intermediate I with ethylene glycol to obtain an intermediate I-b, and then reacting with 5-bromo-2-chloropyrimidine or 5-fluoro-2-chloropyrimidine to obtain the intermediate II; and finally, removing a protecting group from the intermediate II to obtain alpoxivan. The one-step method comprises the following steps: when X in a compound SM1 is a fluorine atom, the compound SM1 is 5-(4-bromophenyl)-4, 6-difluoropyrimidine, and the compound SM1 reacts with sulfonamide and 2-[(5-bromo-2-pyrimidinyl) oxy] ethanol to directly obtain alpoxivan. The synthesis route is short, and the reaction conditions are mild.

The present invention addresses the problem of providing a novel compound that has OX2R agonist activity.　The present invention relates to a substituted sulfonamide macrocyclic compound represented by formula (I) or a pharmacologically acceptable salt thereof. This compound, or a pharmacologically acceptable salt thereof, has agonist activity against OX2R, and is useful as a treatment agent, etc., for sleep disorders involving OX2R (e.g., narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorder, insufficient sleep syndrome, and extended sleep).

This invention discloses an analytical method for benzothiazole contaminants, comprising the following steps: detection by high performance liquid chromatography (HPLC), with the following chromatographic conditions: a phenylhexyl column as the stationary phase, mobile phase A being water, mobile phase B being acetonitrile, and gradient elution; wherein the benzothiazole contaminants are at least one of 2-aminobenzothiazole, 2-hydroxybenzothiazole, benzothiazole, 2-methylbenzothiazole, 2-mercaptobenzothiazole, 2,5-dimethylbenzothiazole, 2-cyanobenzothiazole, ethyl 2-carboxylate benzothiazole, 2-chlorobenzothiazole, 2-bromobenzothiazole, 2-methylthiobenzothiazole, phenylthiocyanate, N-tert-butyl-2-benzothiazole sulfenamide, 2-(2-hydroxyphenyl)-benzothiazole, N-cyclohexyl-2-benzothiazole sulfinamide, dibenzothiazole disulfide, and N,N-dicyclohexyl-2-benzothiazole sulfonamide.

The lithium (N-carbonyl) sulfonamide compound is represented by the following formula (I). In formula (I), R 1 and R 2 Each represents an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkynyl group having 2 to 10 carbon atoms, or an aryl group. 1 and L 2 Each represents a single bond or -O-. Among them, excluding L 1 and L 2 Each is a single bond.

The utility model discloses a flash dryer for producing a pesticide precursor, which relates to the field of pesticide production and comprises a base, a collecting box arranged on one side in the base, a processing tank arranged at the top end of the base, a cooling tank arranged on one side of the processing tank through a discharge pipe, and a precursor processing component arranged on one side of the processing tank and one side of the cooling tank. A precursor smashing assembly is arranged in the base, a screen is arranged on one side of the precursor smashing assembly, and a processing assembly is arranged on one side of the screen. According to the utility model, the precursor processing component is arranged, so that the vortex tube can be utilized to generate high-temperature airflow and low-temperature airflow, the high-temperature airflow can quickly dry sulfonamide, and the low-temperature airflow can cool the dried sulfonamide, so that the cleanliness and the stability of the sulfonamide can be ensured, and the sulfonamide degradation caused by overhigh temperature is avoided; the quality of sulfonamide as a pesticide precursor is influenced.

This invention discloses a method for preparing sulfonamide-modified benzo[a]fluorene-5-one derivatives, using 1,7-enyne and N Using sulfonylaminopyridine salts as raw materials, a series of sulfonated benzo[a]fluorene-5-one compounds were successfully synthesized by catalyzing the sulfonation / cyclization tandem reaction of 1,7-enynes under photocatalytic conditions. This method has excellent functional group tolerance and high economic applicability.

A use of a sulfonamide compound represented by formula (I) or a pharmaceutical composition comprising same in the preparation of a drug for treating pulmonary edema.

The present invention relates to a novel crystalline form of a helicase-primase inhibitor compound, and to pharmaceutical compositions comprising the novel crystalline form, to methods of production of the novel crystalline form, to the crystalline form in medicine and for use in the treatment of herpes viral infections.

The invention provides a crystalline form of N-{4-[2-(2-aminopyrimidin-5-yl)ethynyl]-3- fluoropyridin-2-yl}-5-chloro-2-methoxypyridine-3-sulfonamide characterized by a powder X- ray diffractogram (XRPD) having characteristic peaks at 2Ɵ = 8.6±0.2°, 13.5±0.2°, 22.6±0.2° and 24.7±0.2°. The invention further provides pharmaceutical compositions comprising the 5 crystalline form of the invention and uses of the crystalline form and the compositions. The crystalline form and the compositions are useful for the treatment or prevention of a variety of conditions, particularly cancer.

Rubber compositions including sulfonamides, and golf ball cores made from such compositions are disclosed. The type and concentration of components in the composition affect the properties of cores made therefrom, including, for example, coefficient of restitution and compression, and, thus, can be used to produce golf balls having desirable performance characteristics.

Mcl-1 selective inhibitors, Bcl-2 selective inhibitors, and Mcl-1 / Bcl-2 dual inhibitors and methods of using the same for the treatment of disease are disclosed.

Provided herein are amorphous and crystalline hemisulfate salt forms of the formula.Also provided are pharmaceutical compositions comprising the amorphous and crystalline hemisulfate salt forms, methods for their manufacture, and uses thereof for treating conditions associated with pyruvate kinase such as e.g., pyruvate kinase deficiency.

The invention provides a sulfonamide acetamide compound as well as a preparation method and application thereof. The structure of the sulfonamide acetamide compound is shown as a formula I. The sulfonamide acetamide compound provided by the invention can be used for treating cancers, inflammations and autoimmune diseases. The compound can effectively reduce the protein level of GSPT1 and / or ROR gamma.

The compounds of formula (I) wherein the substituents are as defined in claim 1 and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of these compounds may be used as insecticides. [Formula 1] JPEG2026501744000117.jpg33161

The invention discloses an indole pyridine chalcone compound and application thereof in medicine for treating colitis, and belongs to the technical field of biological medicine. The compound has a structure as shown in a formula I, wherein R1 is selected from C1-C8 alkyl, C1-C8 alkoxy, halogen, cyano, nitryl and morpholinyl, and R2 is selected from nitryl. According to the invention, multiple excellent pharmacophores such as indole, pyridine, chalcone, sulfonamide and the like are fused in the same molecule for the first time, the preparation method does not need pre-activation of a substrate, does not need a metal catalyst or an additive, and has the advantages of mild reaction conditions, high yield, good selectivity, low cost and environmental friendliness. The compound has strong inhibitory activity on hexokinase 2 (HK2), can significantly inhibit inflammatory response and regulate macrophage polarization, shows an excellent colitis treatment effect in in-vivo and in-vitro experiments, provides a new choice for developing novel colitis treatment drugs, and has a wide medical application prospect.

The application belongs to the method for improving the energy conversion efficiency and stability of organic-inorganic hybrid perovskite solar cells, and the main content is that ethyl benzene sulfonyl lactam (PSAD) containing sulfonamide functional group is combined with-NH2 and Pb 2+ in perovskite material respectively through hydrogen bond and coordination effect to passivate the crystal defects caused by the two kinds of functional groups and cations in perovskite crystal grains. The oxygen atom of the sulfoxide group in PSAD can not only fix the organic amine ion in perovskite through hydrogen bond, but also can form Pb 2+ …O coordination bond with Pb to passivate the defects caused by Pb. The method passivates the grain boundary, reduces the non-radiation recombination of carriers, enhances the charge transport of perovskite thin film, and significantly improves the energy conversion efficiency and stability of perovskite solar cells. The additive PSAD is cheap and easy to obtain, which provides the possibility for industrialization.

The invention provides a synthesis method of a negative charge highly delocalized sulfonyl imide alkali metal salt {[(R3SO2) (R2 (R1SO2N) SO) N] M), M = Li, Na, K, Rb or Cs}. The synthesis method comprises the following steps: carrying out oxidation and fluorination reaction on alkyl (S-alkyl sulfonyl imide) potassium sulfinate (or rubidium or cesium) and an N-fluorine electrophilic reagent to synthesize alkyl (S-alkyl sulfonyl imide) sulfonyl fluoride with the yield of 70-90%; the obtained alkyl (S-alkyl sulfimide) sulfonyl fluoride and sulfamide containing substituent R3 or alkali metal salt thereof are subjected to nucleophilic substitution reaction, the product is purified to obtain the high-purity negative-charge highly-delocalized sulfimide alkali metal salt, and the method has the characteristics that the operation is simple, the raw materials are low in price, the product is easy to separate and purify, the method is suitable for industrial mass production, and the like; and the prepared negative charge highly delocalized sulfimide alkali metal salt is high in chemical stability and good in solubility, and is a preferable electrolyte material for realizing high-specific-energy power and energy storage batteries.

The invention relates to an onium salt, a photoacid generator, a chemically amplified resist composition and a pattern forming method. The present invention is an onium salt represented by general formula (A). Thereby, provided is an onium salt used in a chemically amplified resist composition having excellent lithography performance such as high sensitivity, CDU, MEEF, and LWR in optical lithography using high-energy rays. In the formula, m1 is an integer of 1-4. And m2 is 1 or 2. R1 represents an electron-withdrawing group such as a hydrogen atom, a hydrocarbon group, or a cyano group; lA and LB each represents a single bond, a carbonyl group, an ether bond, an ester bond, an amide bond, a sulfonate bond, a sulfonamide bond, a carbonate bond, a urethane bond, or a hydrocarbylene group. W1 is a hydrocarbylene group containing an alicyclic structure, and a carbon atom forming the alicyclic structure has two atomic bonds. And W2 is a hydrocarbon group containing an alicyclic structure. Z + is an onium cation.

The present invention relates to a new process for the preparation of (3R)—N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, as well as to a novel intermediate useful for the synthesis of said compound at large scale.

The application provides a method for preparing alpha-sulfonamidyl acetal compounds from fatty aldehyde and sulfonamide, and belongs to the technical field of organic chemical synthesis, and comprises the following steps: step 1: fatty aldehyde, sulfonamide, sodium iodide, sodium carbonate peroxide and methanol or ethanol are added into a reaction container for mixing, a reaction mixture is obtained by reacting at a temperature of 50-80 DEG C for 16-24 hours; step 2: after the reaction mixture is purified, alpha-sulfonamidyl acetal compounds are obtained. The sulfonamide drugs used in the method are all commercially available, the fatty aldehyde is commercially available or is prepared by simply oxidizing commercially available fatty alcohol, and the pre-catalyst sodium iodide and the oxidant sodium carbonate peroxide are also cheap and easy to obtain; the method has a wide applicable range of substrates and good compatibility for sensitive groups; the reaction does not need transition metal catalysis, the alcohol used is used as a raw material and a solvent, and the only by-product is water, so that the method has the characteristics of high atom economy and green environmental protection.

Telomerase inhibitor compounds are provided. Some compounds contain a lactone or lactam group covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In other examples, a sulfonamide-containing moiety is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In some embodiments, the telomerase inhibitor compounds have an amide moiety and a vinyl sulfonamide group bonded to an aromatic group. In other examples, the inhibitor compounds have an isothiazolidine 1,1-dioxide core bonded to a phenyl group. Aspects of the present invention also include pharmaceutical compositions containing the telomerase inhibitor compounds of the present invention, as well as methods for treating telomerase-related diseases or conditions.

The application discloses a preparation method of a trans-7H-pyrrolo[2,3-d]pyrimidine compound, and the full name of the trans-7H-pyrrolo[2,3-d]pyrimidine compound is trans-N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexylmethanesulfonamide maleate, which is prepared from trans-4-[(tert-butoxycarbonyl)amino]cyclohexane carboxylic acid and 4-chloro-7H-pyrrolo[2,3-d]pyrimidine as starting materials through reduction, chlorination, substitution, oxidation, methylation, condensation and salt formation reactions. The preparation method has the advantages of few reaction steps, simple operation, low production cost, high production efficiency, high yield, high product purity and suitability for scale-up production.

To provide a solid electrolyte capable of improving ion conductivity.SOLUTION: Wherein the molecular crystal includes a sulfolane-based compound and 112233, - hexafluoropropane-1, 3-disulfonimide lithium (LiCFSA) as a lithium salt, and the inorganic filler is SiO2, A normalized surface area WA (1g / gSE) of the inorganic filler is 15 to m2 / gSE, where W (g / gSE) is a mass of the inorganic filler with respect to m2 of the inorganic filler, and A (900m2 / g) is a specific surface area of the inorganic filler.SELECTED DRAWING: Figure 1

The present invention relates to an aryl sulfonamide compound and its anti-influenza use, belonging to the technical field of biomedicine. The present invention provides a series of aryl sulfonamide compounds represented by the general formula I. Experimental verification shows that the aryl sulfonamide compounds have excellent antiviral activity. The toxicity of the compounds is evaluated by cytopathic effect assay. The compounds provided by the present invention have ideal safety and good development prospects.

The present technology relates to methods for the synthesis of a PFAS-free lithium single-ion polymer which comprises simultaneously reacting a sulfonyl chloride compound with an aromatic sulfonamide compound and a compound that is suitable to act as a quenching base. The simultaneous reaction of sulfonyl chloride with the aromatic sulfonamide compound and the compound that is suitable to act as a quenching base yields the single-ion monomer.

The present invention provides solid forms of (3R)-N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, salts and solvates thereof, as well as therapeutic uses thereof and pharmaceutical compostion comprising them.

The application relates to the technical field of aspirin pharmaceutical chemistry, in particular to an aspirin-sulfonamide hybrid, a preparation method and application thereof. The preparation method can synthesize a plurality of novel aspirin-sulfonamide hybrids by taking piperazine as a bridge, and by a three-step continuous method of "acyl chlorination, sulfonamidation and N-acylation" according to a "molecular hybridization principle". In the process, only one separation and purification is performed, and the preparation steps are simple. The aspirin-sulfonamide hybrid prepared by the method is most effective on human non-small cell lung cancer cells A549, and the activity is more than 33 times higher than that of a parent aspirin, and is similar to the activity of an anticancer drug irinotecan. The aspirin-sulfonamide hybrid 3k prepared by the method has a certain inhibitory effect on various cancer cells. The hybrid can induce human non-small cell lung cancer A549 cell apoptosis in a concentration-dependent manner, and can induce human non-small cell lung cancer A549 cell cycle arrest in the G0 / G1 phase, and inhibit cell growth.