41 results about "Monomethylfumarate" patented technology

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 present invention provides pharmaceutical compositions comprising compounds of Formula (I), and methods of treating neurological disorders comprising administering to a subject in need thereof a pharmaceutical composition comprising a compound of Formula (I).

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 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.

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 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.