公开(公告)号：US08933099B2

公开(公告)日：2015-01-13

申请号：US14183864

申请日：2014-02-19

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Setsuo Funasaka ,  Toshimi Okada ,  Keigo Tanaka ,  Satoshi Nagao ,  Isao Ohashi ,  Yoshinobu Yamane ,  Yusuke Nakatani ,  Yuki Karoji

IPC: A61K31/445 ,  C07D401/14 ,  C07D409/14 ,  C07D401/12

CPC classification number: C07D409/14 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.

Abstract translation: 本发明提供了具有FGFR抑制活性的新化合物或其药学上可接受的盐，以及含有该化合物的药物组合物。 具体地说，本发明提供由下式（I）表示的化合物或其药学上可接受的盐：其中n表示0〜2; A表示亚芳基或亚杂芳基; G表示单键，氧原子或-CH 2 - ; E表示含氮非芳族杂环; R1表示烷氧基等; R2表示氢原子等; 并且R 3表示氢原子，烷基，烷氧基等，条件是当E表示氮杂环丁烷环且R 2或R 3存在于氮杂环丁烷环上的氮原子上时，R 2或R 3不表示 氢原子。

公开(公告)号：US20140235614A1

公开(公告)日：2014-08-21

申请号：US14183864

申请日：2014-02-19

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Setsuo Funasaka ,  Toshimi Okada ,  Keigo Tanaka ,  Satoshi Nagao ,  Isao Ohashi ,  Yoshinobu Yamane ,  Yusuke Nakatani ,  Yuki Karoji

IPC: C07D409/14 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D409/14 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.

Abstract translation: 本发明提供了具有FGFR抑制活性的新化合物或其药学上可接受的盐，以及含有该化合物的药物组合物。 具体地说，本发明提供由下式（I）表示的化合物或其药学上可接受的盐：其中n表示0〜2; A表示亚芳基或亚杂芳基; G表示单键，氧原子或-CH 2 - ; E表示含氮非芳族杂环; R1表示烷氧基等; R2表示氢原子等; 并且R 3表示氢原子，烷基，烷氧基等，条件是当E表示氮杂环丁烷环且R 2或R 3存在于氮杂环丁烷环上的氮原子上时，R 2或R 3不表示 氢原子。