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Alqueno and its application
专利权人:
EISAI RandD MANAGEMENT CO.; LTD.
发明人:
BOCK, Mark,HAO, Ming-Hong,KORPAL, Manav,NYAVANANDI, Vijay Kumar,PUYANG, Xiaoling,SAMAJDAR, Susanta,SMITH, Peter Gerard,WANG, John,ZHENG, Guo Zhu,ZHU, Ping
申请号:
PE2017002481
公开号:
PE20181083A1
申请日:
2016.05.27
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
1. The invention relates to a class II alqueno four substitute compound, which is characterized in that: R1 is selected from methyl, ethyl, cyclomethyldibutyl and other substance groups; R2 is selected from n or F; n is 0 or 1; R3 is selected when n = 1; m is 0 or 2; R4 is selected from F, CF3, Cl and other substance groups; P is 0 or 1; When R5 is selected from methyl, ethyl and propyl groups, it is f; R6 and R7 are f; R8 is h-o-ch3; R13, R14, R15 and R16 are selected from - h-o-ch3, respectively. 1. The preferred compound: (E) - 4 - ((2 - (4 - (E) - 1 - (1h-indazol-5-il) - 2-phenylbutyl-1-e n-1-il) phenyl ethyl) amine) - N, N-dimethyl ether-2-aniline;(e) - 4 - ((2 - (4 - ((E) - 1 - (3-fluoro-1h-indazol-5-il) - 2-fenil but-1-e n-1-il) phenyl) amino) - N, n-dimetibut-2-enamida, etc. The current invention is useful for the treatment of breast cancer.La presente invencion se refiere a un compuesto alqueno tetrasustituido de formula II caracterizado porque R1 se selecciona del grupo que consiste de metilo, etilo, ciclobutilo, entre otros; R2 se selecciona entre N o F; n es 0 o 1; R3 es F cuando n=1; m es 0 o 2; R4 se selecciona entre el grupo que consiste de F, CF3, Cl, entre otros; p es 0 o 1; R5 es F cuando p=1; R6 y R7 se seleccionan del grupo que consiste en metilo, etilo, propilo, entre otros; R8 es H o -CH3; R13, R14, R15 y R16 se seleccionan independientemente entre -H o -CH3. Son compuestos preferidos: (E)-4-((2-(4-(E)-1-(1H-indazol-5-il)-2-fenilbut-1-en-1-il)fenoxi)etil)amino)-N,N-dimetibut-2-enamida; (E)-4-((2-(4-((E)-1-(3-fluoro-1H-indazol-5-il)-2-fenil but-1-en-1-il)fenoxi)etil)amino)-N,N-dimetibut-2-enamida; entre otros. La presente invencion es util para el tratamiento del cancer de mama.
来源网站:
中国工程科技知识中心
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