42 results about "Furoxan" patented technology

The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders; (c) facilitating wound healing; (d) treating gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; (e) treating inflammatory disease states and/or disorders; (f) treating ophthalmic disorders; (h) treating peripheral vascular diseases; (i) treating diseases resulting from oxidative stress; (j) treating endothelial dysfunctions; and (k) treating diseases caused by endothelial dysfunctions. The organic nitric oxide enhancing compounds that form salts with the NSAIDs are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.

The invention describes novel diuretic compounds comprising at least one heterocyclic nitric oxide donor group, or pharmaceutically acceptable salts thereof, and novel composition comprising at least one diuretic compound comprising at least one heterocyclic nitric oxide donor group, and optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention comprising at least one heterocyclic nitric oxide donor group, and optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidatives stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; and (p) treating sexual dysfunctions. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.

The invention discloses a 4-nitro-3-(5-tetrazole) furoxan energetic ionic salt and a preparation method thereof, belongs to the technical field of energetic materials. A synthesis method of the 4-nitro-3-(5-tetrazole) furoxan energetic ionic salt is as follows: directly reacting the 4-nitro-3-(5-tetrazole) furoxan with a corresponding cation, and steaming for eliminating a solvent so as to obtain a target product; reacting the 4-nitro-3-(5-tetrazole) furoxan with the sulfate of the equimolar corresponding cation after mixing the 4-nitro-3-(5-tetrazole) furoxan with equimolar Ba(OH)2.8H2O, filtering and precipitating, steaming and eliminating the solvent in the filtrate to obtain the target product. The synthesis method provided by the invention is simple and easy to industrialize. The referred 9 energetic ionic salt has high density (rho: 1.55-1.84g/cm3), wherein the degree of percussion sensitivity of two compounds is more than 40J, and the energetic ionic salt belongs to insensitive explosive. The energetic ionic salt has excellent calculation detonation property and is a potential energetic material.

The invention describes compositions and kits comprising at least one organic nitric oxide enhancing salt of an angiotensin π antagonist, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia. The organic nitric oxide enhancing compounds that form salts with the angiotensin II antagonists are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.

The invention discloses a 3,4-di(3',5'-dinitryl-4'-methyl phenyl) furoxan compound, the structural formula of which is shown in the specification. The compound is mainly applied to energetic materials.

The invention discloses a preparation method of high-energy explosive 3,4-di(nitrofurazano)furoxan. Raw material 3-amino-4-acyl chloride oximidofurazan reacts with weak base solid silver carbonate in solvents such as tetrahydrofuran to generate an intermediate 3,4-di(amino furazano)furoxan with the yield of 80%. The preparation method disclosed by the invention overcomes the defects in the prior art, and no BAFF (B Cell Activating Factor) isomer 3,6-bi(3-amino furazan-4-base)-1,4-dioxa-2,5-diazacyclohexane-2,5-diene is generated; then, the BAFF is oxidized by using a mixture of hydrogen peroxide and concentrated sulfuric acid as an oxidant to generate the high-energy explosive BNFF, and the yield can reach 80%. The preparation method of the high-energy explosive BNFF is high in production efficiency, low in material cost, mature, stable, safe and reliable, and has engineering application prospect.

The invention discloses a synthesis method of 3,4-bi(4'-nitrophenyl) oxidized furoxan. The structure formula thereof is shown as (I), and the synthesis method adopts p-nitrobenzaldehyde as raw material; the structure formula thereof is shown as (II), and the synthesis method comprises the following steps: 1) adding the p-nitrobenzaldehyde and alcohol into a reaction flask, then adding hydroxylamine hydrochloride aqueous solution, using Na2CO3 aqueous solution to adjust pH of reaction liquid to 6 to 8, reacting for 1 to 2 hours at the temperature of 10 to 40 DEG C, obtaining p-nitrobenzaldoxime, with the molar ratio of the p-nitrobenzaldehyde and hydroxylamine hydrochloride of 1:1 to 1:1.5; and 2) adding the p-nitrobenzaldoxime, chlorosuccinimide and trichloromethane into the reaction flask, with the molar ratio of the p-nitrobenzaldoxime and chlorosuccinimide of 1:1 to 1:1.5, reacting for 1 to 3 hours at the temperature of 20 to 40 DEG C, using Na2CO3 solution to adjust pH of a system to 6 to 8 at the temperature of 0 to 5 DEG C, reacting for 1 to 4 hours and obtaining the objective product, namely the 3,4-bi(4'-nitrophenyl) oxidized furoxan. The synthesis method is mainly used for the 3,4-bi(4'-nitrophenyl) oxidized furoxan.

The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably β-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds. The heterocyclic nitric oxide donor groups are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.

The invention relates to a furoxan ring, and provides a synthesis method of 3, 4-dicarboxylic acid diethyl ester furoxan. The method adopts a monoethyl malonate potassium salt as a raw material and takes sodium nitrate/nitrite as an oxidizing agent. The substances are subjected to oxidation nitration and a ring formation reaction in a carbon tetrachloride solution, thus obtaining the target compound 3, 4-dicarboxylic acid diethyl ester furoxan with purity up to 98.7% and yield up to 94.2%. The synthesis method provided in the invention has the advantages of high purity and high yield.

The invention discloses a furoxan NO donor-type statin derivative and a preparation method thereof, and belongs to the technical field of medicinal chemical synthesis. The derivative has the structural formula represented by the following formula: wherein R is an alkyl, R1 is a statin residual group, and R2 is an aryl or an aryl sulfonyl. A statin drug is selected to "hybridize" with a NO donor, both NO and the statin drug have good therapeutic effects on atherosclerosis, and the problem of the mismatch of action mechanisms of NO and the statin drug is effectively avoided. In addition, 4-coumaric acid is selected as a linking group, and thus the therapeutic effect of the drug can be effectively enhanced. The compound can effectively release NO in vitro, and the useful attempt for the development of NO donor anti-atherosclerosis drugs is made.

The invention provides a synthetic method for 3-(4-aminofurazan-3-radical)-4-(4-nitrofurazan-3-radical) furazan. 3-(4-aminofurazan-3-radical)-4-(4-nitrofurazan-3-radical) furazan (ANTF) is a low-melting-point (100 DEG C) explosive, is expected to replace TNT to be used in casting explosives, and is also an intermediate for synthesizing other novel explosives. An existing synthetic method of ANTF has the defects of being large in acid use amount, low in synthesis yield, strict in reaction condition and the like. 3,4-bis(3'-aminofurazan-4'-radical) furoxan (BAFF) is adopted as a raw material, 3,4-bis(3'-aminofurazan-4'-radical) furoxan (BAFF) and SnCl2.2H2O are firstly subjected to a reduction reaction to obtain 3,4-bis(aminofurazan-4-raidcal) furazan, and then 3,4-bis(aminofurazan-4-raidcal) furazan and H2O2 are subjected to an oxidizing reaction to obtain the target product 3-(4-aminofurazan-3-radical)-4-(4-nitrofurazan-3-radical) furazan. 3,4-bis(aminofurazan-4-raidcal) furazan is adopted as the raw material, H2O2 (20%-30%) is adopted as an oxidizing agent, Na2WO4 is adopted as a catalyst, and 3-(4-aminofurazan-3-radical)-4-(4-nitrofurazan-3-radical) furazan is synthesized under the acidic condition through the oxidizing reaction. The synthetic method has the advantages of being easy and convenient to operate, high in safety, controllable in process and the like.

The invention discloses a 7-hydroxy difurazan and furoxan azacycloheptene compound. The structural formula thereof is shown as formula (I). The 7-hydroxy difurazan and furoxan azacycloheptene compoundis mainly applied to the fields of high explosives and propulsive agents.

The invention provides novel furoxan compounds, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for (a) treating cardiovascular diseases; (b) inhibiting platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device; (c) treating pathological conditions resulting from abnormal cell proliferation; (d) treating transplantation rejections, (e) treating autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; (f) reducing scar tissue or for inhibiting wound contraction; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; and (j) treating diseases caused by endothelial dysfunctions.

The invention discloses a synthesis method of a furazan oxide compound. The synthesis method comprises the following step of: oxidizing a glyoxime compound by taking iodobenzene diethyl ester as an oxidizing agent to carry out a reaction to obtain the furazan oxide compound. No heavy metal, acid or alkali participates in the reaction process. The method has the advantages of mild reaction conditions, high efficiency, green and environment-friendly process, simple post-treatment and the like, and is a synthetic method with a certain industrial value; besides, the reaction raw materials do not contain acyl chloride compounds with higher activity, no strict requirements are imposed on substituent groups of the furoxan compound, so that a new synthesis path is opened up for the furoxan compound containing groups which are easy to react with the acyl chloride compounds.

The invention discloses a method for continuously preparing 3, 4-bis(4'-aminofurazan-3'-yl) furoxan by adopting a micro-channel reactor The method comprises the following steps of (1) respectively pumping a 3-amino-4-amidoxime furazan solution and a sodium nitrite aqueous solution into a first micro-mixer in a micro-channel reactor device at the same time, mixing, and introducing into a first reaction module to carry out a first reaction, and (2) while the step (1) is carried out, respectively pumping the effluent of the first reaction module and a sodium carbonate solution into a second micro-mixer in the micro-channel reactor device at the same time, mixing, and introducing into the second reaction module to carry out a second reaction, thereby obtaining the effluent containing 3, 4-bis(4'-aminofurazan-3'-yl) furazan. The invention relates to an intermediate 3-amino-4-amidoxime furazan needing to be separated, and efficient and continuous preparation of 3, 4-bis(4'-aminofurazan-3'-yl) furoxan is realized through a one-pot two-step method.

Water soluble compounds having a furoxan structure which are capable of inhibiting metabolic pathways involved in the development of the tumours are provided. The use of such compounds as a medicament in the therapy of the tumours and as an adjuvant in the immunotherapy protocols against neoplasms is also described.

The invention discloses a method for directly synthesizing furoxan from methyl ketone, and belongs to the technical field of organic chemical synthesis. According to the method, methyl ketone is usedas a raw material, methyl ketone and a green nitration reagent tert-butyl nitrite (TBN) are subjected to a free radical reaction in an air or oxygen atmosphere with acetonitrile, toluene or 1, 4-dioxane as a reaction solvent to directly synthesize the furoxan. According to the method, a metal catalyst is not used in the synthesis process, acid and alkali are avoided, tert-butyl nitrite directly participates in the reaction, the tert-butyl nitrite is low in price and good in functional group compatibility, and the nitration reagent is very green. The methyl ketone can be directly purchased commercially, so that the reaction path is shortened and the workload of raw material preparation is saved compared with the traditional synthesis method. And meanwhile, the method only generates the target product furoxan, so that the environmental pollution and the difficulty of product post-treatment are reduced.