16-08-2012 дата публикации
Номер: US20120208811A1
Автор:
Naoki Taka,
Masayuki Ohmori,
Kyoko Takami,
Masayuki Matsushita,
Tadakatsu Hayase,
Ikumi Hyodo,
Masami Kochi,
Hiroki Nishii,
Hirosato Ebiike,
Yoshito Nakanishi,
Toshiyuki Mio,
Lisha Wang,
Weili Zhao,
TAKA NAOKI,
OHMORI MASAYUKI,
TAKAMI KYOKO,
MATSUSHITA MASAYUKI,
HAYASE TADAKATSU,
HYODO IKUMI,
KOCHI MASAMI,
NISHII HIROKI,
EBIIKE HIROSATO,
NAKANISHI YOSHITO,
MIO TOSHIYUKI,
WANG LISHA,
ZHAO WEILI
A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a Caryl group; Rand Rindependently represent H, OH, X, CN, NO, a Chaloalkyl group, a Calkyl group, or the like ; Rrepresents H, a Calkyl group, a Caryl group, a Calkyl group, or a Chaloalkyl group; and Rrepresents H, X, a Calkyl group, a Chaloalkyl group, OH, CN, NO, or the like.) 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein A represents benzene claim 1 , indole claim 1 , azaindole claim 1 , benzofuran claim 1 , benzothiophene claim 1 , benzothiazole claim 1 , quinoline claim 1 , or pyrrole.3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Rrepresents hydrogen claim 1 , Calkyl claim 1 , Caryl Calkyl claim 1 , or Cperfluoroalkyl.4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Rrepresents hydrogen claim 1 , halogen claim 1 , Calkyl claim 1 , Cperfluoroalkyl claim 1 , cyano claim 1 , methanesulfonyl claim 1 , hydroxyl claim 1 , alkoxy claim 1 , or amino.5. The compound of or a pharmaceutically acceptable salt thereof claim 1 , which is selected from the group consisting of:(1) [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1H-indol-2-yl)-methanone;(2) [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(6-pyrrolidin-1-ylmethyl-1H-indol-2-yl)-methanone;(3) [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-[6-(4-hydroxy-piperidin-1-ylmethyl)-1H-indol-2-yl]-methanone;(4) [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1H-pyrrolo[3,2-c]pyridin-2-yl)-methanone;(5) [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(6-piperazin-1-ylmethyl-1H- ...
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