38 results about "Trametinib" patented technology

The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and / or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis.

The present invention provides a method of providing adjuvant treatment to a human patient which comprises administering to such a patient therapeutically effective doses of debrafenib and trametinib for a time period sufficient to increase relapse-free survival (RFS).

Disclosed are compounds of formula (I) and formula (II): (I) (II) wherein R1, R2, A, and B are as defined herein. Also disclosed is a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula (I) or (II) either alone or in combination with a second compound selected from elesclomol, NSC174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.

The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and / or salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.

The invention belongs to the field of biomedicine, and relates to an inducer for inducing mesenchymal stem cells to differentiate into islet cells. The invention discloses the inducer for inducing mesenchymal stem cells to be differentiated into islet cells. The inducer is prepared from the following components: GLP-1, parathyroid hormone, acetaminophen, rapamycin, icariin, trametinib, EPO and VEGF. According to the inducer for inducing and differentiating the mesenchymal stem cells into the islet cells, all the components are safe and non-toxic, the number of steps needed by induced differentiation is small, the time is short, and the induction efficiency is high.

The invention discloses a method for synthesizing trametinib. The method comprises the steps of dehydrating N-(2-fluoro-4-iodophenyl)-N'-methylurea to form carbodiimide, then enabling the product to be subjected to a cyclization reaction with 2-methyl-3-oxo-diethyl glutarate to obtain 2-(2-fluoro-4-iodophenylamino)-4-hydroxyl-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-nonanoic acid-ethyl ester; after that, carrying out cyclization on the obtained product with N-(3-nitrophenyl)-N'-cyclopropyl urea to obtain 3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-methyl-1-(3-nitrophenyl)pyrido[4,3-d]pyrimidine-2,4,7(1H,3H,6H)-trione; finally, reducing a nitro group first, then performing acetylation to obtain the trametinib. The invention provides a new synthesis route of the trametinib by means of retrosynthetic analysis, and can greatly shorten the technological process; furthermore, expensive reagents are not used in a preparation process; the method has the advantages of being simple and convenient to operate and lower in cost; a reference is provided for the preparation of the trametinib.

The invention belongs to the technical field of medicine, and discloses application of trametinib in preparation of a drug for treating Parkinson's disease, wherein trametinib is used for preparing the drug to delay the degeneration of dopaminergic neuron. The obtained product can effectively delay the degenerative death of dopaminergic neuron, to treat Parkinson's disease fundamentally; the drug can be taken orally without injection to achieve the treatment effect, has excellent curative effect for Parkinson's disease caused by a variety of reasons, and has important significance for the treatment and curing of Parkinson's disease.

The invention discloses a method for synthesizing a key intermediate of trametinib, which uses monoformamide monoethyl malonate and methylmalonic acid to complete the cyclization reaction to obtain a crude pyridinetrione compound; the obtained pyridinetrione The crude compound is directly cyclized with N-(2-fluoro-4-iodophenyl)-N'-cyclopropylurea to obtain the key intermediate of trametinib. The present invention adopts monoethyl malonate and methylmalonic acid to complete the cyclization reaction to obtain a pyridinetrione compound, which is directly cyclized with a urea compound without purification to obtain a key intermediate for synthesizing trametinib. The method steps are short, the total yield is 47.3%, and it has the potential of scale-up in pilot scale, which provides a new scheme for the synthesis of trametinib.

The invention belongs to the technical field of medicine application, and discloses an application of trametinib in preparing a medicine for reversing multi-medicine resistance of tumors. Trametinib can be used for significantly reversing the multi-medicine resistance of the tumors mediated by membrane transport protein to ensure that the sensitivity of P-glycoprotein high expression cells to anti-cancer medicines can be restored. According to the medicine for reversing the multi-medicine resistance of the tumors, disclosed by the invention, trametinib and the anti-cancer medicines can be combined to ensure that the effects of treating and controlling resistant tumors can be achieved by restoring the sensitivity of resistant cells to the anti-cancer medicines.