34 results about "Benzothiadiazine" patented technology

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 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.

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.

The invention provides a compound structure showed in a formula I, a synthetic method and application of pharmaceutically acceptable salt or mixture thereof in terms of preparation of medicines for preventing and/or curing diabetes complications. The compound is used as an aldose reductase inhibitor, accumulation of sorbite in a human body is reduced effectively by means of suppressing activity of aldose reductase, and accordingly an effect of preventing and/or curing the diabetes complications is achieved. The invention further provides a medicine composition which comprises the compound and has an effect of preventing and/or curing diabetes.

The present invention provides a method for preparing 1,2,4-benzothiadiazine-1,1-dioxo compounds in high yields from readily available starting materials, short steps and under mild reaction conditions. The preparation method of the 1,2,4-benzothiadiazine-1,1-dioxo compound represented by the general formula (I), is characterized in that the compound represented by the general formula (III) and the compound represented by the general formula (IV) The compound or the compound represented by the general formula (V) is reacted in the presence of an acid, and after synthesizing the nitrous ether compound represented by the general formula (III), the ring-closing reaction of the iminoether compound occurs in the presence of a base; A method for preparing a 1,2,4-benzothiadiazine-1,1-dioxo compound represented by the general formula (I) by subjecting a compound represented by the general formula (II) to a ring-closing reaction. ∴ In general formula (I)~(V), R ₁ represents a substituted or unsubstituted alkyl or aryl group. R ₂ represent substituents. n represents an integer from 0 to 4. Multiple R when n is 2 or more ₂ Each may be the same or different, and may be combined with each other to form a ring. R ₃ represents a hydrogen atom or a substituent. R ₄ represents a substituted or unsubstituted alkyl group.

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

The invention relates to a benzothiadiazine compound, application thereof and a positron drug of AMPAR (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor). The structure of the benzothiadiazine compound is shown as the specification, wherein R is selected from one of Br, Cl, F, I and the groups shown as the specification. A marked benzothiadiazine compound prepared by taking the above benzothiadiazine compound as a precursor has high standard uptake value and high specificity to AMPAR.

The invention relates to a synthesis method of a 4H-1, 2, 4-benzothiadiazine-1, 1-dioxide derivative. The method comprises the following steps: under a heating condition, taking an aprotic solvent as a reaction medium, mixing N-aryl amide with a structure represented by a general formula I with chlorosulfonyl isocyanate, and carrying out a continuous reaction process of [2+2]-cyclization/carbon dioxide removal/sulfonylation so as to generate the 4H-1, 2, 4-benzothiadiazine-1, 1-dioxide derivative with a structure represented by a general formula II in one step, wherein the structure of the general formula I is shown in the specification, the structure of the general formula II is shown in the specification, Ar represents a substituted or unsubstituted monocyclic or polycyclic aromatic ring, and R1 and R2 represent a hydrogen atom and a substituted or unsubstituted hydrocarbon group. The method is low in cost, non-toxic and high in synthesis efficiency.

The invention provides benzothiadiazine methoxy acrylate derivatives and a preparation method and application thereof, and the benzothiadiazine methoxy acrylate derivatives have the following chemicalstructural general formula VII as shown in the description, wherein R1 is hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, methoxy or nitro; and R2 is hydrogen, methyl or benzyl. According to the invention, an active group 3, 4-dihydro-2H-1, 2, 4-benzothiadiazine-1, 1-dioxo substitutes the side chain part of the methoxy acrylate bactericide and then is reasonably spliced with the pharmacophore of the methoxy acrylate bactericide, so that the bactericide with novel structure, broad spectrum, high efficiency and low toxicity is synthesized, the bactericide can be alternately used with the existing bactericide, the generation of resistance is avoided or delayed, the preparation conditions are conventional, the subsequent treatment is simple and convenient, and the industrialization is easy to realize.

The invention relates to a preparation method of a chiral 3, 4-dihydrobenzothiadiazine compound, which comprises the following steps: under the conditions of no water, no oxygen and protective atmosphere, adding molecular sieves into compounds shown in a formula (1) and a formula (2) under the action of a catalyst, and reacting in an organic solvent at -40-40 DEG C to obtain the chiral 3, 4-dihydrobenzothiadiazine compound shown in a formula (4); the catalyst comprises a chiral TADDOL type rare earth metal complex or a combined catalyst of a chiral TADDOL ligand and a rare earth metal amide complexed with lithium chloride, the reaction route is as follows, in which R1 is selected from hydrogen, C1-C4 alkyl or halogen; R2 is selected from hydrogen, C1-C2 alkyl or phenyl; and R3 is selectedfrom a C1-C5 alkyl group, a C3-C6 cycloalkyl group, a phenyl group, a benzyl group, a phenylpropyl group, a C1-C4 alkyl substituted phenyl group, a C1-C4 alkoxy substituted phenyl group, a halogenatedphenyl group, a furyl group or a thienyl group.

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 relates to a synthesis method of a benzothiadiazine-1, 1-dioxide compound, and develops a novel solvent-free synthesis method of the benzothiadiazine-1, 1-dioxide compound. No solvent is added in the reaction process, and even part of the product can be obtained through separation without post-treatment. Therefore, the separation and purification process of the product is easy to implement, the reaction time is shortened, the yield of the product is increased, the yield can reach 73%-98%, the purity can reach 96%-99%, the use of toxic solvents is reduced to the greatest extent, and the problems of resource waste, environmental pollution and the like caused by the solvents are fundamentally solved. The method thoroughly eliminates the heavy metal pollution problem in the product from the source, is suitable for preparation of active pharmaceutical ingredients (API), biological agents and the like, and meets the requirements of green chemistry concept.