46 results about "Leflunomide" patented technology

The present invention relates to a transdermal administration preparation for external application such as ointment, cream and the like, which contains SMP-114 or leflunomide or a pharmaceutically acceptable acid addition salt thereof as an active ingredient. The present invention further relates to a pharmaceutical composition for transdermal administration which contains, a) as an active ingredient, N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide or an active motabolite thereof or a pharmaceutically acceptable salt thereof; and B)(1) a carrier for transdermal administration which contains a base for dissolution in a proportion of not less than 40 w/w %, or (2) a carrier for transdermal administration which contains a hydrophobic base for suspension having no polar group in a molecule in a proportion of not less than 70 w/w %. According to the present invention, a novel means of transdermal administration of SMP-114 or leflunomide or an active motabolite thereof or a pharmaceutically acceptable acid addition salt thereof can be provided.

The invention discloses application of leflunomide, teriflunomide, brequinar and derivatives thereof to treatment of virus infection, especially RNA virus infection. RNA viruses include but are not limited to influenza viruses, respiratory syncytial viruses, hand, foot and mouth viruses (EV71), dengue viruses (type-2 dengue viruses), Zika viruses and Japanese encephalitis viruses. The medicines have broad-spectrum and excellent antiviral activity and have relatively low toxicity to normal cells.

The invention relates to application of artesunate as a drug for treating systemic lupus erythematosus, adopting the artesunate with a molecular formula of C19H2808 for treating the systemic lupus erythematosus. The invention overcomes the defects that the prior common drug for treating SLE, such as cyclophosphamide, glucocorticoid, mycophenolate mofetil, hydroxychloroquine sulfate, leflunomide, azathioprine and the like has multiple side effects, is expensive, influences the life quality of a patient and even causes the patient to die because of some side effects, and the like. The invention has the advantages of cheap raw materials, easy availability, non or low toxicity, no pollution, mature production technology of a artesunate finished product, stable and reliable quality and little toxic side effects. Through comparison and study on a lupus mouse show that the efficacy of the artesunate is superior to a contrast group with little side effect. Therefore, the artesunate has a favorable prospect to treat the systemic lupus erythematosus.

Implantable medical devices having anti-restenotic coatings are disclosed. Specifically, implantable medical devices having coatings of certain anti-inflammatory agents, are disclosed. The-anti-inflammatory agents are selected from the group consisting of ENMD-0997, gusperimus hydrochloride, BMS-561392, CP-461, RDP-58, CNI-1493, CEP-1347, CMT-3, prinomastat, rebimastat, leflunomide, BX-471, DF-1681, BXT-51072, M-40403, LY-293111 sodium, and pharmaceutically acceptable derivatives thereof. The anti-restenotic medical devices include stents, catheters, micro-particles, probes and vascular grafts. Intravascular stents are preferred medical devices. The medical devices can be coated using any method known in the art including compounding the anti-inflammatory agent with a biocompatible polymer prior to applying the coating. Moreover, medical devices composed entirely of biocompatible polymer-anti-inflammatory agent blends are disclosed. Medical devices having a coating comprising at least one anti-inflammatory agent in combination with at least one additional therapeutic agent are also disclosed. Furthermore, related methods of using and making the anti-restenotic implantable devices are disclosed.

The present invention is within the field of industrial protein production. The invention provides a novel expression system using dihydroorotate dehydrogenase (DHODH) as a selection marker in combination with leflunomide or a metabolite thereof, notably for use in mammalian cell lines. Expression vectors encoding DHODH, cell lines comprising said vectors and methods of producing recombinant proteins are also provided.

The invention discloses a leflunomide tablet and a preparation technology and use thereof. The product is prepared from leflunomide, milk sugar, pregelatinized starch, hydroxypropyl methyl cellulose, carboxymethyl starch sodium, polysorbate-80, 12% slushing pregelatinized starch, magnesium stearate and a gastric soluble film coating premix. The production method comprises the steps of fabricating tablets and coatings, and the like. The leflunomide tablet disclosed by the invention is high in dissolution rate, good in stability, good in anti-inflammatory analgesic effect, and small in effect on erythrocyte sedimentation rate, and the total effective rate is 85%. The drug disclosed by the invention has the characteristics of being fewer in medication administration times, stable in plasma concentration, long in lasting time and the like.

The invention discloses a crystal form compound of leflunomide. In an XRD pattern of the crystal form compound, characteristic diffraction peaks occur when the value of 2theta is 8.04 DEGs +/- 0.2 DEG, 10.83 DEGs +/- 0.2 DEG, 14.29 DEGs +/- 0.2 DEG, 18.72 DEGs +/- 0.2 DEG, 20.48 DEGs +/- 0.2 DEG and 24.92DEGs +/- 0.2 DEG. The novel crystal form of leflunomide has better stability than all the reported crystal forms of leflunomide and has high purity and good reproducibility. The invention also discloses a preparation method for the crystal form compound. The preparation method is simple in process and can be easily implemented. The invention further provides application of the crystal form compound in the fields of preparations and medicines.

The present invention relates to c-Abl-, PDGF-R- or c-kit-tyrosine kinase inhibitors such as 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3 -((4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, bis(1H-2-indolyl)-1-methanone, AG1295, CT52923, RP-1776 , GFB-111, pyrrolo[3,4-c]-β-carboline-diketones, SU 102, AG1296, RPR101511A, CDP 860, Zvegf3, CP 673451, PD 170262, KI 6783, KN 1022, AG 13736 , CHIR 258, MLN 518, SU 11248, leflunomide or their pharmaceutically acceptable salts in the preparation of medicines for treating diabetes such as type I diabetes and type II diabetes.

The invention belongs to the field of biology and discloses a molecular cloning and identifying method for a silkworm gene. The sequence of the silkworm gene is SEQ ID NO:1; and the silkworm gene is named BmDHODH. The method disclosed by the invention has the advantages that leflunomide is used for treating silkworm cells and has great inhibitory effect on BmDHODH expression and cell proliferation; as a component in pyrimidine synthesis, BmDHODH is a necessary biological enzyme closely related with cell growth and proliferation, can become a new gene target for killing lepidoptera pests, provides new opinion for eco-friendly pest control and provides a new target and a new theoretical method for developing an environment-friendly pesticide; and as a biological model for the lepidoptera pests, basic knowledge of the lepidoptera pests can be enriched for silkworm BmDHODH, and a new method is provided for environment-friendly pest control.

The invention discloses a high bioavailability Leflunomide tablet and a preparing method thereof. The Leflunomide tablet is prepared from, by weight, 1-5 parts of Leflunomide, 5-60 parts of filler, 1-15 parts of disintegrating agent, 0.5-5 parts of lubricant, 0.1-2 parts of surface active agent, 2-10 parts of adhesive, 0.1-5 parts of threonine, 1-3 parts of glutamine, 1-5 parts of beta-carotene and 0.1-2 parts of glutathione. The Leflunomide tablet is high in dissolution rate and bioavailability and little in side effect, and has a positive meaning of ensuring safety and effectiveness of clinical medication.

The present invention relates to a method for preparation of Teriflunomide, comprising steps of: (a) adding Leflunomide to an alcoholic solvent to give solution (I); (b) adding an aqueous sodium hydroxide solution slowly into the solution (I) to give solution (II); (c) acidifying the solution (II) with inorganic acid for precipitation to give solution (III); and (d) filtering the solution (III) to give Teriflunomide.

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.

The invention discloses a leflunomide tablet for treating adult rheumatoid arthritis, and belongs to the technical field of medicines. The composition is prepared from leflunomide, lactose, starch, hydroxy propyl cellulose, lauryl sodium sulfate, superfine silica powder, polyethylene glycol 6,000, sodium carboxymethyl starch and magnesium stearate. The leflunomide is a novel crystal compound. An experiment shows that the medicine is fast to dissolve, simple in preparation technology and applicable to mass production.

The present invention provides an application of lyfluomite in preparation of medicine for curing ankylosing spondylitis. The lyfluomite can utilize its action of inhibiting the hyperlasia of fibrolast to reduce hyperplasia of fibrous tissue between joint and bone trabecula. Besides, it also can inhibit the hyperplasia of activated lymphocytes and conversion of B-lymphocyte into plasmocyte, and can reduce infiltration of lymphocyte and plasmocyte in articular synovium of ankylosing spondylitis. The therapeutic effect is reliable, and its toxic side effect is less, so it is an effective medicine for curing ankylosing spondylitis.

The invention discloses a medicine for curing rheumatism. The medicine is prepared form the following raw materials in parts by weight: 2 to 5 parts of an auxiliary material, 3 to 7 parts of dendrobium nobile stem solution, 1 to 2 parts of sodium salicylate, 0.2 to 1.5 parts of leflunomide, 2 to 4 parts of oryzanol, 0.2 to 1 part of vitamin E, 2 to 4 parts of lysine, 1 to 4 parts of caffeine, 4 to 9 parts of cucurbitacine, 0.5 to 2.5 parts of aspirin, 0.4 to 2 parts of terramycin, 3 to 6 parts of glycerinum and 10 to 18 parts of normal saline. The invention further discloses a preparation method of the medicine. The medicine is wide in raw material source, simple in preparation technology and suitable for large-scale industrial production; as the ingredients of the dendrobium nobile stem solution, the cucurbitacine and the sodium salicylate have an synergistic effect, the medicine is reasonable in formula, convenient to use, short in curing time, capable of curing the rheumatism completely, low in relapse possibility, free of toxic and side effects and good in use effect.

The invention provides a simple preparation method of teriflunomide, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps of: (1) mixing 5-methylisoxazole-4-formic acid and a condensing agent in a solvent under an alkaline condition, and carrying out condensation reaction to obtain an active ester system; (2) mixing the active ester system and 4-trifluoromethylaniline in a solvent, and carrying out condensation reaction to obtain an intermediate leflunomide; and (3) carrying out alkali treatment and acid treatment on the obtained intermediate leflunomide to obtain teriflunomide. According to the method, the 5-methylisoxazole-4-formic acid reacts with the 4-trifluoromethylaniline in the form of active ester, so that the reaction activity of the 5-methylisoxazole-4-formic acid and the 4-trifluoromethylaniline is improved, the reaction condition is mild, the obtained intermediate leflunomide does not need to be purified, and the yield of teriflunomide is improved.

The invention discloses an environmental-protection simple preparation method of teriflunomide; leflunomide is used as a starting material, a heterogeneous reaction is adopted, an organic solvent is avoided from being used in a synthesis reaction process, and thus the high-purity teriflunomide can be prepared.

The invention discloses a crystal form compound of leflunomide V. The crystal form is different from X-ray powder diffraction and differential scanning patterns of the leflunomide, which are publishedin the existing document, and is a novel crystal form; and the X-ray powder diffraction pattern has characteristic diffraction peaks different from a reported crystal form at 2theta of 7.8255 degrees, 8.7099 degrees, 9.1789 degrees, 9.6017 degrees, 11.1488 degrees, 14.9436 degrees, 15.6434 degrees, 18.6293 degrees, 19.3055 degrees, 20.2744 degrees, 23.3166 degrees, 23.5235 degrees, 30.1244 degrees, 30.6877 degrees, 31.5469 degrees and 37.2453 degrees. The solubility of the crystal form is better than that of other all crystal forms in existing reports, the purity is high and the repeatabilityis good; and the invention further discloses a preparation method of the crystal form.

New leflunomide Form III is disclosed, along with processes for preparing it. The present invention also provides an economic process for preparing leflunomide Form II and a process for preparing leflunomide Form I from leflunomide Form III. Pharmaceutical compositions and dosage forms containing the new form and methods of using them for the treatment of rheumatoid arthritis are also disclosed.