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Bicyclic Heterocycles as inhibitors of FGFR
专利权人:
INCYTE CORPORATION
发明人:
LU, Liang,SHEN, Bo,SOKOLSKY, Alexander,WANG, Xiaozhao,WU, Liangxing,YAO, Wenqing,YE, Yingda
申请号:
PE0014242017
公开号:
PE15142017A1
申请日:
2016.02.19
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
Refers to a bicyclic heterocycle derivative Compound of formula (i), in which: The Ring a is aryl or heteroaryl C6 C10 5-10 members R12 is c1-c6 alkyl, Halo, alquenilo C2 - C6Alquinilo C2 - C6, among others and N is 0, 1, 2 or 3 R2, R3 and R5 are h, alkyl, Halo, haloalquilo C1 - C3, C1 - C3, C1 - C3 FS or alkoxy R13 is H, CN, OR1, among others, R14 is H, CN, or4 conhr8,,Among others, it is cr10r11 X1 or x2 is nr7 n or Cr6.A Preferred Compound is 6 - (5 - amino - 2-methylphenyl) - 2 - (2,6 - difluoro - 3.5 - dimetoxifenil) - 1 - [h Spiro cyclopropane - 1,4 - [2,7] naftiridin] - 3 (2 (H) - One 6 - (5 - amino - 4 - fluoro - 2-methylphenyl) - 2 - (2,6 - difluoro - 3.5 - dimetoxifenil) - 1 - [h Spiro cyclopropane - 1,4 - [2,7] naftiridin] - 3 (2 (H) - One among others.These compounds are inhibitors of enzymes and fgfr4 FGFR3 and are used in the treatment of cancerSe refiere a un compuesto derivado de heterociclo biciclico de formula (I), en donde: el anillo A es arilo C6-C10 o heteroarilo 5-10 miembros R12 es halo, alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, entre otros y n es 0, 1, 2 o 3 R2, R3 y R5 son H, halo, alquilo C1-C3, haloalquilo C1-C3, CN o alcoxi C1-C3 R13 es H, CN, OR1, entre otros R14 es H, CN, OR4, CONHR8, entre otros X1 es CR10R11 o NR7 X2 es N o CR6. Un compuesto preferido es 6-(5-amino-2-metilfenil)-2-(2,6-difluoro-3,5-dimetoxifenil)-1H-espiro[ciclopropano-1,4-[2,7]naftiridin]-3(2H)-ona 6-(5-amino-4-fluoro-2-metilfenil)-2-(2,6-difluoro-3,5-dimetoxifenil)-1H-espiro[ciclopropano-1,4-[2,7]naftiridin]-3(2H)-ona entre otros. Estos compuestos son inhibidores de las enzimas FGFR3 y FGFR4 y se emplean en el tratamiento del cancer
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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