36 results about "Teriflunomide" patented technology

This invention is related to the use of the combination of teriflunomide or a pharmaceutically acceptable salt thereof and glatiramer acetate for treating multiple sclerosis.

The invention belongs to the technical field of medicinal chemistry and discloses a preparation method of teriflunomide and an intermediate thereof. The preparation method of the teriflunomide provided by the invention comprises the following steps: getting a compound with a structure as shown in formula I and an azide in an organic solvent to generate nucleophilic substitution reaction to generate a compound with the structure as shown in formula II; getting and mixing the compound with the structure as shown in the formula II with the organic solvent, heating to obtain the compound with the structure as shown in formula III; under inert-gas protection and alkaline conditions, getting the compound with the structure as shown in the formula III and the compound with the structure as shown in the formula IV to generate electrophilic addition and isomerization reaction in the organic solvent to obtain the teriflunomide. According to the preparation method of the teriflunomide provided by the invention, the reaction intermediate is not needed to be purified, operation is simple, yield of the teriflunomide is improved, production cost of the teriflunomide is lowered, and therefore, the preparation method is more beneficial to industrial production of the teriflunomide.

The invention discloses application of leflunomide and teriflunomide or derivatives or pharmaceutically acceptable salt thereof to preparation of medicines for treating leukemia. The leflunomide and the teriflunomid have remarkable inhibition effect on the leukemia comprising acute lymphoblastic leukemia (ALL), acute myelocytic leukemia (AML), chronic granulocytic leukemia, chronic lymphocytic leukemia and the like; and new material basis is laid for the development of the medicines for treating leukemia.

The invention belongs to the technical field of medicine preparation, and discloses a preparation method for a compound pellet capsule and the prepared compound pellet capsule. The capsule structure comprises a medicine-carrying pill, a delayed-release layer and a rapid-release layer; the medicine-carrying pill is prepared by employing an extrusion-spheronization process; and the delayed-release layer and the rapid-release layer are prepared by employing a fluidized bed coating process. The prepared capsule is substantial in curative effect, safe, stable, convenient to take, small in side effect and low in production medical cost. The medicine effective compositions dimethyl fumarate and teriflunomide are different in drug action mechanism, also medicine administration is simple and convenient, and the curative effect of the two medicine effective compositions generates synergic effect, the indication scope is larger than that of a single medicine, multiple sclerosis is treated through multiple targets, and the curative effect is better than that of a single medicine.

This invention is related to the use of the combination of teriflunomide and interferon beta thereof, for the preparation of a medicament for use in treating multiple sclerosis.

The invention relates to the application of teriflunomide in the preparation of medicines for preventing foot-and-mouth disease virus infection, and belongs to the technical field of veterinary medicines. The application of the invention can provide a class of highly efficient, safe and quality-controllable anti-foot-and-mouth disease virus medicine for further controlling the spread of foot-and-mouth disease.

The invention discloses a teriflunomide microemulsion, a preparation method and application. The preparation method includes: well mixing an emulsifier and a co-emulsifier, then adding an oil phase; dissolving teriflunomide into deionized water to obtain a teriflunomide solution aqueous phase; in the process of stirring, dropwise adding a teriflunomide solution into a mixed oil phase to form a transparent drug-containing microemulsion, wherein a proportion of the oil phase, the aqueous phase, the emulsifier and the co-emulsifier is optimized according to a pseudo-ternary phase diagram. Percutaneous administration, the microemulsion can improve solubleness of slightly soluble drug, form high concentration gradient and promote drug absorption; a hydrophobic portion of the microemulsion interacts with cuticle to disturb lipid bilayer structure, a hydrophilic portion can hydrate the cuticle, combined action of the hydrophobic portion and the hydrophilic portion can enhance permeability ofthe drug on the cuticle, and permeation and absorption of the drug are facilitated. A new dosage form is provided for clinic application of teriflunomide.

The invention belongs to the technical field of medicinal chemistry and discloses a preparation method of teriflunomide and an intermediate thereof. The preparation method of the teriflunomide provided by the invention comprises the following steps: getting a compound with a structure as shown in formula I and an azide in an organic solvent to generate nucleophilic substitution reaction to generate a compound with the structure as shown in formula II; getting and mixing the compound with the structure as shown in the formula II with the organic solvent, heating to obtain the compound with the structure as shown in formula III; under inert-gas protection and alkaline conditions, getting the compound with the structure as shown in the formula III and the compound with the structure as shown in the formula IV to generate electrophilic addition and isomerization reaction in the organic solvent to obtain the teriflunomide. According to the preparation method of the teriflunomide provided by the invention, the reaction intermediate is not needed to be purified, operation is simple, yield of the teriflunomide is improved, production cost of the teriflunomide is lowered, and therefore, the preparation method is more beneficial to industrial production of the teriflunomide.

The present invention relates to a process for preparing Teriflunomide of formula (I).

The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.

The present invention provides a process for preparing Teriflunomide of formula (I).

The present invention relates to a method of treating MS in a human patient in need of such treatment and comprises administering to said patient a combination therapy in a single oral dosage form (e.g. a tablet or capsule) of dim ethyifurrta rate and one agent selected from teriflunomide (or its prodrug leflunomide), fingolimod and laquinimod. This combination is more effective than the single agents alone and / or has reduced side effects and better tolerability than the single agents alone and / or can be given in a reduced frequency. Moreover, the present invention is directed to a pharmaceutical composition suitable for the oral treatment of multiple sclerosis consisting of dimethylfumarate and one agent selected from teriflunomide, fingolimod and laquinimod as active ingredients and one or more pharmaceutically acceptable excipients.