34 results about "Benzothiadiazine" patented technology

A composition including diazoxide (7-chloro-3-methyl-2H-1,2,4-benzothiadiazine-1,1-dioxide) for the treatment and / or prevention of retinal ischemia and of diseases associated with retinal ischemia. The composition can also contain riluzole, a derivative active in neuroprotection of the latter, or a pharmaceutically acceptable salt of the latter.

A preparation method of 1,2,4-benzothiadiazine series compounds, the method adopts sulfoxide sulfonylimide and 3-aryl (alkyl) base-1,4,2-oxadiazol-5-ketone as The reaction substrate, under the co-catalysis of transition metal catalyst and co-catalyst, is heated by microwave reactor (reaction temperature is 100-120°C, reaction time is 2-3 hours) or heated by oil bath (reaction temperature is 110-130°C ℃, the reaction time is 15~18 hours) to react under the conditions of C-H / N-H bond to form a heterocyclic compound containing benzosulfoxide and dinitrogen, that is, to obtain 1,2,4 ‑Benzothiadiazine series compounds. The by-products obtained by this method are only carbon dioxide and water, which is convenient for separation and purification; the chemical selectivity of the reaction is high, and the substrate has wide applicability; no additional inert gas protection is required as the reaction environment, which is convenient and simple to operate; the reaction time under microwave conditions is short , with extremely low cost and few by-products, and can be applied to large-scale preparation.

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and / or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

Disclosed herein are 5-Substituted 4-amino-1H-benzo[c][1,2,6]thiadiazine 2,2-dioxide compounds useful as sweet flavor modifiers. Also disclosed herein are ingestible compositions that include one or more of these compounds in combination with a natural or artificial sweetener.

The invention provides a benzothiadiazine derivative and application of the benzothiadiazine derivative in agriculture. Specifically, the invention provides a compound as shown in a formula (I) and a preparation method thereof, application of the compound as shown in the formula (I) and a composition containing the compound as shown in the formula (I) in prevention and control of weeds, and a method for preventing and controlling the weeds by using the compound as shown in the formula (I) and the composition containing the compound as shown in the formula (I). Wherein the definition of each group in the formula (I) is shown in the invention.

The present invention proposes a class of benzothiadiazine methoxy acrylate derivatives and its preparation method and application. The substance has the following chemical structure formula VII: wherein, R 1 is hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, methoxy or nitro; R 2 is hydrogen, methyl or benzyl. In the present invention, the active group 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxy is replaced by the side chain part of the methoxyacrylate fungicide and its medicinal effect A class of novel structure, broad-spectrum, high-efficiency, and low-toxicity fungicides have been synthesized through reasonable splicing of groups, which can be used alternately with existing fungicides to avoid or delay the development of resistance. The preparation conditions are conventional, and the follow-up treatment is simple and easy to implement. industrialization.

The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system.

The invention provides a cyclohexanedione-benzothiadiazine compound and an application of the cyclohexanedione-benzothiadiazine compound. Specifically, the invention provides a compound as shown in a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide or a salt thereof of the compound as shown in the formula (I), a preparation method, a composition containing the compounds and application of the composition in agriculture, especially application of the composition as an active ingredient of a herbicide for preventing and treating unwanted plants, wherein A, R1, R2, R3, R4, R5, R6, R7, R8 and Q have the meanings as described in the invention.

The invention provides a preparation method of 1,2,4-benzothiadiazine-1-oxide series compounds. The method adopts a one-pot reaction, utilizes 2-bromophenyliminosulfone and aryl (alkyl) aldehydes that can be directly purchased commercially as reaction substrates, stable, cheap and non-toxic copper oxides as catalysts, and water as green Using a non-polluting solvent, react at 80-100°C for 12-15 hours in an air environment to synthesize 1,2,4-benzothiadiazine series compounds. The present invention uses water as a solvent, basically has no pollution to the environment, does not require alkali and inert gas protection, has no special requirements for reaction equipment, is easy to operate, adopts a one-pot reaction, and saves the operation of preparing and separating intermediates, so the synthesis cost extremely low. The product obtained in the present invention has excellent chemoselectivity, high production efficiency, wide compatibility of substrate functional groups, conforms to green reaction characteristics, is suitable for large-scale preparation, has excellent industrial application prospects, and is an environmentally friendly green product. chemical technology.

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and / or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

The invention provides a phenylalanine derivative containing benzothiadiazine-3-ketone 1,1-dioxide and a preparation method and application thereof. The derivative has the structure shown in the following general formula I. The invention also relates to a preparation method of the derivatives and their application as HIV-1 inhibitors in the preparation of anti-AIDS drugs.

The invention provides a synthetic method and agricultural biological activity of a benzothiadiazine compound and belongs to the field of organic synthesis. The synthetic method is simple in reactionsystem, a used catalyst is cheap, easy to obtain and less in dosage, other metals and carboxylates are not needed as additives, the yield is high, and the benzothiadiazines compound can be efficientlysynthesized. The invention adopts the technical scheme that the synthetic method comprises the following steps: respectively adding a sulfonimide compound and a nitrobenzene compound into a reactor and sealing under the air condition of 80-110 DEG C under the action of nickel diacetylacetone or nickel chloride and a solvent to react for 5-8 hours; after the end of reaction, performing column chromatography separation to obtain the benzothiadiazine compound. The benzothiadiazine compound can be applied to physalospora piricola.

The invention belongs to novel application of a bimetallic cationic complex, which is application of a bimetallic cationic complex [Ln(CH2CN)9]3<+>[(AlCl4)3]3<->.CH3CN as an efficient catalyst in preparation of dihydro-quinazolinone and 1,1-dioxo-dihydro-1,2,4-benzothiadiazine derivatives: under a water-free and oxygen-free condition and in an argon or nitrogen atmosphere, anthranilamide or 2-aminobenzenesulfonamide and aldehyde are used as reactants, the above bimetallic cationic complex is used as a catalyst and acetonitrile is used as a solvent to react to prepare the dihydro-quinazolinone derivative or the 1,1-dioxo-dihydro-1,2,4-benzothiadiazine derivative. The bimetallic cationic complex disclosed by the invention has the advantages of high catalyst activity, mild reaction conditions, short reaction time, high yield of the target product and simplicity in after-treatment.

This invention relates to benzothiadiazine compounds, their preparation method, composition containing the compounds, and the application of the compounds as KATP channel modulators in treating diseases related to central nervous system, cardiovascular system, lung system, gastrointestinal system and endocrine system.

The invention relates to a benzothiadiazine compound and application thereof, and a positron medicine of AMPAR. The structure of a benzothiadiazine compound is: wherein, the R is selected from one of Br, Cl, F, I, and . The labeled benzothiadiazine compound prepared by using the above-mentioned benzothiadiazine compound as a precursor has a high cross-brain volume and high specificity for AMPAR.

The present disclosure generally relates to various formulations and uses of the compound: N-(1-((4-amino-2,2-dioxo-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2-methyl-propan-2-yl)isonicotinamide, which is also referred to herein a “TM1” and comestibly acceptable salts thereof. In some aspects, the disclosure provides compositions that include TM1, or a comestibly acceptable salt thereof. In some embodiments, the compositions are ingestible compositions, including, but not limited to, packaged food and beverage products and tabletop sweeteners. In some aspects, the disclosure provides certain compositions that include such flavanone derivatives, such as compositions that include such flavanone derivatives and one or more other sweeteners. In some other aspects, the disclosure provides methods of reducing the caloric content of a sweetened article, such as a sweetened food or beverage product.