HORI, SEIJI,堀诚治,堀誠治,HASEGAWA, FUTOSHI,长谷川太志,長谷川太志,TOSAKI, SHINYA,户慎也,戶慎也,IMAZAKI, YUSUKE,今雄介,今雄介,KARASAWA, TOMOYA,柄泽智哉,柄澤智哉,UENO, HIROYUKI,上野博之,上野博之,MATSUMURA, YUTA,松村裕太,松村裕太,LI, CHIANG JIA,李嘉强,李嘉
申请号：
TW105117668
公开号：
TW201704227A
申请日:
2016.06.03
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
The present invention provides a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein X is nitrogen atom or CR5 Y is hydrogen atom, C1-6 alkyl, etc. R1a, R1b, R1c, R1d, and R1e are the same or different, hydrogen atom, halogen atom, hydroxy, etc. R4 is hydrogen atom, cyano, C1-6 alkyl, etc. R2, R3 and R5 are the same or different, hydrogen atom, halogen atom, hydroxy, C1-6 alkyl, etc. and Ar is monocyclic or polycyclic C6-10 aryl or monocyclic or polycyclic 5- to 10-membered heteroaryl, which exhibits antitumor activity by inhibiting plural kinases/signals such au CDK1, CDK2, CDK5, AURKA, AURKB, and JAK2 that are necessary for cell cycle, cell growth and survival of cancer stem cell, and has low side effect and high safety.本發明提供一種化合物,其包含下述式(1)所表示之化合物或其藥理上可容許之鹽,並且藉由阻礙細胞週期、細胞增生或癌幹細胞之存活所必需之CDK1、CDK2、CDK5、AURKA、AURKB、JAK2等複數種激酶及訊號而發揮抗腫瘤作用,減小副作用而安全性較高。[式(1)中,X表示氮原子或CR5,Y表示氫原子、C1-6烷基等,R1a、R1b、R1c、R1d及R1e相同或不同,表示氫原子、鹵素原子、羥基等,R4表示氫原子、氰基、C1-6烷基等,R2、R3及R5相同或不同,表示氫原子、鹵素原子、羥基、C1-6烷基等,Ar表示C6-10之單環式或多環式之芳基或5員~10員之單環式或多環式之雜芳基]
