41 results about "Monomethylfumarate" patented technology

The invention discloses a preparation method of monomethyl fumarate. A main material of maleic anhydride and methanol are subjected to alcoholysis reaction, thus producing monomethyl maleate, which is then isomerized to produce the monomethyl fumarate. The preparation method comprises the following steps: the main material of the maleic anhydride and the methanol are subjected to the alcoholysis reaction, thus producing the monomethyl maleate; then the monomethyl maleate solution is added with ethyl acetate and is then added with fumaryl chloride at 80-100DEG C for reacting for 60-120 minutes, then the ethyl acetate is removed by distillation, water is added, the product is heated to dissolve, and after cooling, centrifugal separation and vacuum drying, the monomethyl fumarate is obtained. The alcoholysis reaction process can be completed at room temperature, which saves energy and has short reaction time; and the isomerization reaction of the monomethyl maleate and the alcoholysis reaction of the maleic anhydride can adopt the same set of equipment, and the isomerization reaction can be carried out as soon as the alcoholysis reaction is completed, thus having no need for new devices.

Provided herein are compositions containing compounds, or pharmaceutically acceptable salts, that metabolize to monomethyl fumarate with certain pharmacokinetic parameters and methods for treating, prophylaxis, or amelioration of neurodegenerative diseases including multiple sclerosis using such compositions in a subject, wherein if the compositions contain dimethyl fumarate, the total amount of dimethyl fumarate in the compositions ranges from about 43% w / w to about 95% w / w.

The invention features a method of treating a subject in need of treatment for multiple sclerosis. The method involves orally administering to the subject in need thereof a pharmaceutical composition in unit dosage form consisting essentially of (a) from about 120 mg to about 240 mg of dimethylfumarate formulated for delayed release, and (b) one or more pharmaceutically acceptable excipients, wherein following the orally administering of the unit dosage form monomethylfumarate appears in the plasma of the subject upon hydrolysis of dimethylfumarate and the Cmax of the monomethylfumarate in the plasma of the subject is between about 0.4 and about 2 mg / L, and wherein about 480 mg of dimethylfumarate per day is orally administered to the subject.

The efficient compound mildew inhibitor for feed additive has lactic acid and / or phosphoric acid, propionic acid, monomethyl fumarate, potassium iodide, etc. as effective components, and oyster shell powder, corn cob, rice bran and other green functional stuffing and carrier. It is prepared through a mixing, pelletizing and coating process, and has no volatilization of mixed acid, lasting mildew inhibiting effect, low use amount and other advantages. It has wide bactereostasis spectrum and mildew inhibiting period over 65 days.

The invention discloses a preparation method of a scale inhibitor. According to the preparation method, the scale inhibitor is prepared through copolymerization reaction of a monomer A and a monomer Bunder the action of a catalyst and an initiator; the initiator comprises an oxidizing agent and a reducing agent; the monomer A is at least one ingredient selected from itaconic acid, maleic anhydride, maleic acid, a monomethyl maleate, a monoethyl maleate, a monoisopropyl maleate, a isobutyl maleate, a mono-tert-butyl maleate, fumaric acid, monomethyl fumarate, monoethyl fumarate, and acomitic acid; and the monomer B is at least one selected from acrylic acid, methyl acrylate, ethyl acrylate, hydroxyethyl acrylate, hydroxy-propyl acrylate, methacrylic acid, hydroxyethyl methylacrylate, hydroxypropyl methacrylate, and vinyl acetate. The preparation method is simple in operation, and low in cost.

A composite anti-mildew agent especially suitable for storage of tobacco leaf is prepared from monomethyl (or dimethyl) fumarate and vanillin through proportional mixing. Its advantages are low irritation to human skin and mucosa and high effect.

A process for preparing monomethyl fumarate from maleic acid anhydride as raw material includes such steps as alcoholizing by methanol at 30-70 deg.C for 1.5-5 hr while stirring, adding concentrated hydrochloric acid and isomerizing reaction at 30-80 deg.C for 20-60 hr (or adding ethyl acetate and then concentrated hydrochloric acid and isomerizing at 20-70 deg.C for 3-8 hr while stirring), centrifugal separation and vacuum drying. Its advantages include high output rate (95%), very low energy consumption and no environmental pollution.

The invention provides a preparation method of polyacrylamide for an incense making adhesive. The preparation method comprises the following steps: S1, mixing acrylamide, acrylic acid, chitosan and deionized water to obtain a monomer solution A; S2, mixing methyl methacrylate, styrene, monomethyl fumarate and ethanol to obtain a monomer solution B; S3, mixing the monomer solution A and the monomersolution B, adding polyethylene and urea, and adjusting pH to be 5.5-6.5; S4, cooling to the temperature of 0-4 DEG C, introducing nitrogen and displacing oxygen, and then adding a DMAP catalyst anda chain extender; S5, heating to the temperature of 10-15 DEG C, and adding a cross-linking agent, a chain transfer agent, a reducing agent and an oxidizing agent into the mixture every 3 min; S6, heating to the temperature of 75-85 DEG C, carrying out heat-insulation reaction for 1-1.5 h, taking out an adhesive, adding caustic soda, hydrolyzing at the temperature of 80-90 DEG C for 1-2 h, and drying, crushing, granulating and carrying out secondary drying to obtain the final product. The polyacrylamide prepared by the invention has certain hydrophobic and water-resistant performance, the molecular weight reaches 30,000,000, and the polyacrylamide has the advantages of strong adhesive force, low moisture absorption rate, corrosion resistance and antibiosis, environmental protection and nopollution after combustion, and the like.

The invention provides preparation of a novel composite antibacterial agent. The preparation comprises the following steps: adding chitosan, monomethyl fumarate and ultrapure water to a reactor according to a molar mass ratio of 1:1:0.2, stirring by a magnetic force for dissolution, carrying out a sealed reaction for 3 hours at the temperature of 45 DEG C, thus obtaining a bright yellow reaction solution, after natural cooling, carrying out freeze drying, dissolving an obtained solvent in distilled water, and then preparing the antibacterial solution. The invention further provides preparation and application of master batches of the novel composite antibacterial agent. The novel composite antibacterial agent can be taken as an additive, and can be used for preparing a long-acting antibiotic film and a long-acting antibacterial bottle cap. The novel composite antibacterial agent disclosed by the invention can improve the antibacterial ability of chitosan and enable the chitosan to be easily processed, and also has an excellent antibacterial effect no matter in a neutral environment or a weak alkaline environment.

The present invention relates to novel compounds for use as a medicament. In particular, the present invention relates to a medicament, preferably in the treatment and / or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis and psoriasis.

The invention discloses application of fumarate in preparing drugs for treating hepatopathy. The application of fumarate in preparing the drugs for treating the hepatopathy includes application of dimethyl fumarate (DMF) and application of monomethyl fumarate (MMF) in treating various hepatic diseases. According to the application of fumarate in preparing the drugs for treating the hepatopathy, DMF and MMF are adopted to activate the express of nuclear factor-E2-related factor 2 (Nrf2) in various human hepatoma carcinoma cells and mice liver cells and the express of downstream antioxidant genes of the nuclear factor-E2-related factor 2 (Nrf2), a Keapl-Nrf2-ARE pathway which is the most important in a cellular anti-oxidation mechanism is started, in addition, the damage of oxidative stress in a mice hepatopathy model on the liver can be further prevented, and the liver protection effect is good. Fumarate has the potential of being developed into treatment drugs regarding the hepatopathy related to the oxidative stress damage, and has important development and application prospects in treating the various hepatic diseases such as fatty hepatopathy, drug induced hepatopathy, cholestatic hepatopathy, viral hepatitis, cirrhosis and liver cancer.

Provided herein are compositions containing compounds, or pharmaceutically acceptable salts, that metabolize to monomethyl fumarate with certain pharmacokinetic parameters and methods for treating, prophylaxis, or amelioration of neurodegenerative diseases including multiple sclerosis using such compositions in a subject, wherein if the compositions contain dimethyl fumarate, the total amount of dimethyl fumarate in the compositions ranges from about 43% w / w to about 95% w / w.

The invention relates to application of fumarate and pharmaceutically acceptable salt thereof in preparation of medicines for treating ferroptosis related diseases. According to the application, the fumarate comprises dimethyl fumarate and / or monomethyl fumarate. The application has the advantages that the influence of the fumarate and the pharmaceutically acceptable salt thereof on the level of key regulatory gene GPX4 protein for ferroptosis is disclosed for the first time, a theoretical basis is provided for research on a treatment strategy for the ferroptosis diseases, and an insertion site is provided for preparing the new medicines for treating the ferroptosis related diseases.

The invention relates to a preparation method of antiseptic mono-benzyl-methyl fumarate, which belongs to the technical field of food antiseptic, and comprises the following steps that: (1) preparing and isomerizating mono-benzyl-methyl fumarate: isomerized catalyst is added into maleic anhydride and phenylcarbinol after being reacted for a period of time under the reaction temperature, and the maleic anhydride and the penylcarbinol are isomerizated for a period of time to obtain the mono-benzyl fumarate under an isomerization temperature. (2) The mono-benzyl fumarate, methanol and catalyst with certain quantity are sequentially added into a flask to obtain the pure mono-benzyl-methly fumarate. The method adopts maleic anhydride, methanol and phenylcarbinol as raw materials to prepare novel fumarate - mono-benzyl-methyl fumarate, so the obtained compound simultaneously has a good bacteriostatic function and a good oxidation resistant function, and a novel though can be provided to develop a novel multifunctional food additive. The product is developed to a series of food additives having multiple functions.

The present invention relates to novel compounds for use as a medicament. In particular, the present invention relates to novel prodrugs of monomethyl fumarate (MMF) suitable as a medicament, preferably in the treatment and / or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis and psoriasis.

The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel prodrugs of monomethyl fumarate (MMF) suitable as a medicament, preferably in the treatment and / or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis, rheumatoid arthritis and psoriasis.

The invention discloses a preparation method of monomethyl fumarate. A main material of maleic anhydride and methanol are subjected to alcoholysis reaction, thus producing monomethyl maleate, which is then isomerized to produce the monomethyl fumarate. The preparation method comprises the following steps: the main material of the maleic anhydride and the methanol are subjected to the alcoholysis reaction, thus producing the monomethyl maleate; then the monomethyl maleate solution is added with ethyl acetate and is then added with fumaryl chloride at 80-100DEG C for reacting for 60-120 minutes, then the ethyl acetate is removed by distillation, water is added, the product is heated to dissolve, and after cooling, centrifugal separation and vacuum drying, the monomethyl fumarate is obtained. The alcoholysis reaction process can be completed at room temperature, which saves energy and has short reaction time; and the isomerization reaction of the monomethyl maleate and the alcoholysis reaction of the maleic anhydride can adopt the same set of equipment, and the isomerization reaction can be carried out as soon as the alcoholysis reaction is completed, thus having no need for new devices.

Methods and pharmaceutical compositions comprising one or more prodrugs (e.g., aminoalkyl prodrugs) of monomethyl fumarate (MMF) thereof are provided herein for the treatment of a heart failure disease, including heart failure with preserved ejection fraction. The compounds of the present disclosure are configured to be converted in vivo, upon oral administration, to monomethyl fumarate. Upon conversion, the active moiety (i.e., monomethyl fumarate) of various embodiments is effective in treating subjects suffering from a heart failure disease, including heart failure with preserved ejection fraction.

The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel prodrugs of monomethyl fumarate (MMF) suitable as a medicament, preferably in the treatment and / or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis and psoriasis.

The invention discloses a laser aluminum plating film for food packaging. The laser aluminum plating film comprises a film matrix layer and an aluminum plating layer. The film matrix layer is prepared from the following components in parts by weight: 10-24 parts of hexafluoroisopropyl p-toluenesulfonate, 23-39 parts of ethyl 2-cyano-3,3-diphenyl acrylate, 13-31 parts of 1-stearic acid-monomethyl fumarate-diglyceride, 30-42 parts of dodecafluoroheptyl methacrylate, 8-19 parts of cellulose acetate-propionate and 40-58 parts of poly(cyclohexylene-dimethylene terephthalate). The laser aluminum plating film for food packaging has higher oil proofness, and can prevent the oil stain of the product inside the package from seeping so as to influence the appearance of the package.

Disclosed are conjugates of monomethyl fumarate and a carrier group or aminocarrier group, or a pharmaceutically acceptable salt thereof. In the conjugates, monomethyl fumarate acyl is covalently bonded to the carrier group or aminocarrier group through a carbon-oxygen bond that is cleavable in vivo. The carrier group may include a core, e.g., a monosaccharide, a sugar acid (e.g., acid monosaccharide), a sugar alcohol, or a catechin polyphenol. The aminocarrier group may include a core, e.g., an aminomonosaccharide. The carrier group or aminocarrier group may include, e.g., at least one short chain fatty acid acyl, at least one tryptophan analogue, at least one ketone body, or at least one pre-ketone body. Also disclosed are pharmaceutical compositions containing the conjugates and methods of their use.

A gas-phase antiseptic, antimildew and antistaling agent with high safety and effect and broad spectrum for grain tobacco, medicine, vegetables, clothes, etc is prepared from methyl fumarate, dimethyl fumarate, calcium propioate, VC or VE, benzoic acid and nipagin ester through dissolving in alcohol, heating natural cooling while crystallizing, drying in air, pulverizing and packing in sealed mode.

A process for preparing monomethyl fumarate from maleic acid anhydride as raw material includes such steps as alcoholizing by methanol at 30-70 deg.C for 1.5-5 hr while stirring, adding concentrated hydrochloric acid and isomerizing reaction at 30-80 deg.C for 20-60 hr (or adding ethyl acetate and then concentrated hydrochloric acid and isomerizing at 20-70 deg.C for 3-8 hr while stirring), centrifugal separation and vacuum drying. Its advantages include high output rate (95%), very low energy consumption and no environmental pollution.

The invention discloses a method for preparing contact lenses with a two-dimension code. The method comprises the following steps: 1) preparing raw materials, namely, A, mixing hydrogel, an emulsion stabilizer and a monomethyl fumarate sodium salt in parts by weight, heating, and treating with infrared rays and microwaves alternatively twice, thereby obtaining a first mixture; B, mixing silicone hydrogel with glycerinum in parts by weight, thereby obtaining a second mixture; C, mixing the first mixture and the second mixture, thereby obtaining a third mixture; D, mixing the third mixture, nano-silver granules and nano ferric hydroxide granules, feeding into water, and treating in ultrasonic waves, thereby obtaining a fourth mixture; 2) molding. By adopting the contact lenses prepared by using the method disclosed by the invention, eyes can be prevented from abrasion caused by a two-dimension code graph when people wear the contact lenses with the two-dimension code, and wearing comfort can be further improved; moreover, due to the two-dimension code added on the contact lenses, the contact lenses can be widely used in fields such as a recognition system, a security protection system or an anti-theft system, and the like.

Disclosed are conjugates of monomethyl fumarate and a carrier group or aminocarrier group, or a pharmaceutically acceptable salt thereof. In the conjugates, monomethyl fumarate acyl is covalently bonded to the carrier group or aminocarrier group through a carbon-oxygen bond that is cleavable in vivo. The carrier group may include a core, e.g., a monosaccharide, a sugar acid (e.g., acid monosaccharide), a sugar alcohol, or a catechin polyphenol. The aminocarrier group may include a core, e.g., an aminomonosaccharide. The carrier group or aminocarrier group may include, e.g., at least one short chain fatty acid acyl, at least one tryptophan analogue, at least one ketone body, or at least one preketone body. Also disclosed are pharmaceutical compositions containing the conjugates and methods of their use.

The present invention describes an improved process for the industrial scale production of dimethyl fumarate. The process involves a one-pot ring opening reaction of maleic anhydride to monomethyl maleate and isomerization into the corresponding monomethyl fumarate in presence of a Lewis acid. Finally the mono methyl fumarate was converted into the dimethyl fumarate by an acid catalyzed esterification reaction.

The invention discloses a method for preparing contact lenses with a two-dimension code. The method comprises the following steps: 1) preparing raw materials, namely, A, mixing hydrogel, an emulsion stabilizer and a monomethyl fumarate sodium salt in parts by weight, heating, and treating with infrared rays and microwaves alternatively twice, thereby obtaining a first mixture; B, mixing silicone hydrogel with glycerinum in parts by weight, thereby obtaining a second mixture; C, mixing the first mixture and the second mixture, thereby obtaining a third mixture; D, mixing the third mixture, nano-silver granules and nano ferric hydroxide granules, feeding into water, and treating in ultrasonic waves, thereby obtaining a fourth mixture; 2) molding. By adopting the contact lenses prepared by using the method disclosed by the invention, eyes can be prevented from abrasion caused by a two-dimension code graph when people wear the contact lenses with the two-dimension code, and wearing comfort can be further improved; moreover, due to the two-dimension code added on the contact lenses, the contact lenses can be widely used in fields such as a recognition system, a security protection system or an anti-theft system, and the like.

The present invention comprises compounds of formula (I): where R1 may be PEG or other polymeric moieties. For example, R1 may be repeating PEG units —(CH2—CH2—O)n—, wherein n=1-455. R1 may also be other polymeric moieties of varying sizes and structures, for example, R1 may be poly(glycolide), poly(lactic acid), poly(lactide), poly(caprolactone), poly(lactide-co-caprolactone), poly(lactide-co-glycolide), or poly(lactic acid)-butanol. One or more embodiments of the invention may also relate to injectable pharmaceutical compositions comprising polymer conjugated monomethyl fumarate, and methods for treating relapsing-remitting multiple sclerosis and psoriasis.