38 results about "Trametinib" patented technology

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 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 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.