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 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 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 novel organic nitric oxide donor salts of a antimicrobial compounds, and novel compositions and kits comprising at least one organic nitric oxide donor salt of an antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and / or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. In one embodiment the antimicrobial compounds of the invention are aztreonam, ciprofloxacin, doripenam, duramycin and tobramycin. The organic nitric oxide donors that form salts are preferably organic nitrates, organic nitrites, nitrosothiols, thionitrites and heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and / or oxatriazole-5-imines. The methods of the invention are preferably for the treatment of bacterial infections associated with pulmonary diseases such as cystic fibrosis and for treating Bacillus anthracis infections.

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 novel synthesis method of furoxan, and belongs to the fields of organic chemistry and medicine. The synthesis method comprises the following steps: weighing alpha-nitroxime and sulfonyl chloride, adding the weighed alpha-nitroxime and sulfonyl chloride into a solvent, placing the mixture into a reactor, carrying out reactions at a temperature of -10 to 50 DEG C under stirring, adding alkali, keeping on stirring, and finally carrying out separation and purification after the reactions completely finish, so as to obtain the furoxan. The reaction conditions are mild, asymmetrical furoxan compounds with different substituents can be obtained, the application range of the method is wide, the price of the raw material sulfonyl chloride is lower than that of NCS, the whole reaction period is short and lasts about 20 minutes, the cost is low, the yield can reach 95% or more and is higher than that of methods which have been reported before, moreover, no pollutant is discharged, and thus the method is environment-friendly.

The invention discloses a composite energetic material with an embedded structure and a preparation method thereof. A solvent-non-solvent method is used to prepare a composite energetic material of 3,4-dinitrofurazanylfuroxan / aluminum powder with an embedded structure. Material, dissolve 3,4-dinitrofurazanylfuroxan in ethyl acetate, drop into the n-hexane suspension of aluminum powder, control the dropping speed, stirring speed and preparation time to obtain the composite of embedded structure Energetic materials. The method provided by the invention can effectively reduce the diffusion distance between 3,4-dinitrofurazanylfuroxan and aluminum powder, optimize the crystal morphology and surface state of 3,4-dinitrofurazanylfuroxan, The prepared composite energetic material has the advantages of high bulk density, low sensitivity and high detonation heat, which can effectively improve the detonation heat of 3,4-dinitrofurazanyl oxide furazanyl press-packed aluminum-containing explosives. The mass percentage of the embedded structure composite energetic material of the present invention is composed of: 60-75% of 3,4-dinitrofurazanyl oxide furazan; 25-40% of aluminum powder.

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.

The invention provides a 3,4-bis(1-hydro-5-tetrazolyl)furoxan ionic salt containing energy and a preparation method thereof, which belongs to the technical field of energy materials. A synthetic method for the 3,4-bis(1-hydro-5-tetrazolyl)furoxan ionic salt comprises the following steps: subjecting 3,4-bis(1-hydro-5-tetrazolyl)furoxan and equimolar organic base to an acid-base neutralization reaction to obtain corresponding ionic salts or 3,4-bis(5-tetrazolyl)furoxan barium salt and equimolar sulfate of corresponding cations (wherein a part of sulfate is prepared through a reaction of a chlorine salt or an iodine salt and silver sulfate); filtering a precipitate; and removing a solvent in a filtrate through steaming so as to obtain a target product. The synthetic method provided by the invention is simple and is easy for industrialization. 16 energy-containing salts prepared in the invention have good heat stability, calculated detonation performances of all the energy-containing salts are much better than those of TNT, and a part of the energy-containing salts have detonation performances close to those of RDX, but have a degree of percussion sensitivity lower than that of RDX and can be used as a green substitute for RDX.

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 belongs to the field of chemical synthesis, and specifically discloses a method for synthesizing 3,4-bis(4'-aminofurazan-3'-yl)furazan oxide in one step using a microchannel reactor. ‑Amidoxime furazan solution and sodium nitrite aqueous solution are simultaneously pumped into the micro-mixer of the microchannel reactor, and after mixing, they are passed into the microreactor for reaction to obtain 3,4-bis(4'-aminofurazan -3'-yl) reaction solution of furazan oxide. The reaction process of the invention realizes one-step direct synthesis from the raw material AAOF to the target product DATF, has the advantages of short reaction time, high conversion rate of raw materials, high yield of target product, etc., and has good industrial application prospects.

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 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 belongs to the field of chemical synthesis, and particularly discloses a method for synthesizing 3, 4-bis(4'-aminofurazan-3'-yl) furoxan by a one-step method by using a micro-channel reactor. The method comprises the following steps of respectively pumping a 3, 4-bis(4'-aminofurazan-3'-yl) furoxan solution and a sodium nitrite aqueous solution into a micro-mixer of a micro-channel reactor at the same time, mixing, and introducing into the micro-reactor to react, thereby obtaining the reaction solution containing 3, 4-bis(4'-aminofurazan-3'-yl) furoxan. The reaction process provided by the invention realizes one-step direct synthesis from the raw material AAOF to the target product DATF, has the advantages of short reaction time, high raw material conversion rate, high targetproduct yield and the like, and has good industrial application prospects.

The present invention relates to nitric oxide furoxan derivative compounds which showed to be active in the treatment of tumors. In addition, they may be used as adjuvants in cancer immunotherapy.

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.

The invention provides a method for preparing a press-packed aluminum-containing explosive, which uses 3,4-dinitrofurazanylfuroxan and aluminum powder as main raw materials, and directly Method granulation. The method first dissolves 3,4-dinitrofurazanylfuroxan in ethyl acetate at a temperature of 50°C to 60°C, then adds a surfactant, stirs for 20 minutes, and then adds the above solution to the aluminum powder. Stir as you add. Finally, add the binder and desensitizing agent solution and stir for 30 minutes. After the whole material forms a paste, it is sieved to form particles of 1 mm to 2 mm, and dried to obtain the aluminum-containing explosive molding powder. The mixed explosive with good formability and high detonation velocity can be prepared by adopting the preparation method of the aluminum-containing explosive provided by the invention, which overcomes the defects of the traditional direct preparation method in the background technology.

The present invention provides: a furoxan compound having a fluorine atom as a substituent group on the ring structure thereof; and a novel nitric oxide donor including the compound. The present invention relates to a fluorofuroxan compound represented by general formula (1) or (2). The compound of formula (1) can be manufactured by reacting a fluoride salt with a nitrofuroxan compound to substitute the nitro group with a fluoro group. The compound of formula (2) can be manufactured by subjecting the compounds of formula (1) to isomerization by irradiation with light.