DOMINGUEZ, Esteban,GUO, Deqi,MADER, Mary Margaret,NGUYEN, Anh-Quan Hannah,DEL PRADO, Miriam Filadelfa,RICHETT, Michael Enrico,RODRIGUEZ, Michael John,YIP, Yvonne Yee Mai,YU, Kuo-Long
申请号：
PE2018000313
公开号：
PE20181025A1
申请日:
2016.08.22
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
A compound that inhibits the activity of tissue lysine methyltransferase, a homogenous enhancer of zeste 2 (EZH2),Where x is - ch2-o-ch2-ch2Y'es-nr4r5, - CH (CH3) - cyclohexyl-4-il-n-methyl-n-methylilo, etc.； R4 is cyclohexane-4-il, replaced by n-methyl-n-methylamine, n-methyl-n-cyclopolamine, etc.； R5 is methyl or ethyl； R6 is methyl or chlorine. It also refers to a composition and combination, including these compounds. A preferred compound is 5 - [(4,6-dimethyl-2-oxo-1,2-dihydropyridine-3-il) methyl] - 2 - (1R) - 1 - [4 - (3-methoxy-1-il) epoxy] ethyl} - 3-methyl-5,6,7,8-tetrahydro-4h-tieno [3,2-c] azerbaijani-4-ona. These compounds can be used to treat cancer, such as ovarian cancer, gastric cancer, rectal cancer and so on.Se refiere a compuestos que inhiben la actividad de la histona lisina metiltransferasa, potenciador del homologo de Zeste 2 (EZH2), donde: X es -CH2- o -CH2-CH2-； Y' es -NR4R5, -CH(CH3)-ciclohexil-4-il-N-metil-N-metoxietilo, entre otros； R4 es ciclohex-4-il sustituido con N-metil-N-metoxietilamino, N-metil-N-ciclopropilamino, entre otros； R5 es metilo o etilo； R6 es metilo o cloro. Tambien se refiere a una composicion y a una combinacion que comprende a dichos compuestos. Un compuesto preferido es 5-[(4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil]-2-{(1R)-1-[4-(3-metoxiazetidin-1-il)ciclohexil]etil}-3-metil-5,6,7,8-tetrahidro-4H-tieno[3,2-c]azepin-4-ona. Dichos compuestos son utiles para el tratamiento del cancer tales como cancer de ovario, gastrico, colorrectal, entre otros
