公开(公告)号：US08933100B2

公开(公告)日：2015-01-13

申请号：US13752638

申请日：2013-01-29

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

Inventor： Keigo Tanaka ,  Tomoki Nishioka

IPC: A61K31/4525 ,  C07D405/12

CPC classification number: C07D405/12

Abstract: A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group.

Abstract translation: 由式（1）表示的化合物或其药理学上可接受的盐保留了帕罗西汀的主要治疗效果，并且具有改善的CYP抑制作用：其中R1是氢原子或C1-6烷基。

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。

公开(公告)号：US20130197045A1

公开(公告)日：2013-08-01

申请号：US13752660

申请日：2013-01-29

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

Inventor： Keigo Tanaka ,  Tomoki Nishioka

IPC: C07D413/14

CPC classification number: C07D413/14

Abstract: A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein R1 is a halogen atom, etc., R2 is a methyl group, etc., R3 is a C1-6 alkyl group, etc., and M is a group represented by: etc.

Abstract translation: 由式（1-1）或（1-2）表示的化合物或其药理学上可接受的盐保留了西他生坦的主要治疗效果，并且具有改善的CYP抑制作用：其中R1是卤素原子等，R2是 甲基等，R3为C1-6烷基等，M为由...表示的基团。

公开(公告)号：US20160168176A1

公开(公告)日：2016-06-16

申请号：US14904860

申请日：2014-07-18

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Keigo Tanaka ,  Takashi Fukuyama ,  Norio Murai ,  Wataru Itano ,  Shinsuke Hirota ,  Daisuke Iida ,  Hiroshi Azuma

IPC: C07F7/22 ,  C07F5/02 ,  C07D495/04 ,  C07D513/04 ,  C07D491/048 ,  C07D493/04

CPC classification number: C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.

Abstract translation: 由式（I）表示的化合物或其盐：其中环Z是环中具有一个或两个杂原子的5至6元杂芳环; X1是氢原子，羟基，羟基C1-6烷基，-B（OH）2，硼酸酯基，环状硼酸酯基，硼烷基，环状硼烷基，-BF3Mn1，-Sn （R 12）（R 13）（R 14），离去基团，羧基，甲酰基或-NR 16 R 17; X 2为氢原子或-CO 2 R 18。

公开(公告)号：US20130197033A1

公开(公告)日：2013-08-01

申请号：US13752638

申请日：2013-01-29

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Keigo Tanaka ,  Tomoki Nishioka

IPC: C07D405/12

CPC classification number: C07D405/12

Abstract: A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group.

Abstract translation: 由式（1）表示的化合物或其药理学上可接受的盐保留了帕罗西汀的主要治疗效果，并且具有改善的CYP抑制作用：其中R1是氢原子或C1-6烷基。

公开(公告)号：US20190231720A1

公开(公告)日：2019-08-01

申请号：US16260350

申请日：2019-01-29

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

Inventor： Keigo Tanaka ,  Tasuku Ishida ,  Masayuki Miyano ,  Raku Shinkyo

IPC: A61K31/166 ,  A61P19/10 ,  A61P29/00 ,  A61P7/06

CPC classification number: A61K31/166 ,  A61P7/06 ,  A61P19/10 ,  A61P29/00 ,  C07C233/73 ,  C07C235/60

Abstract: The present invention provides a compound represented by formula (1): or pharmaceutically acceptable salt thereof, wherein X and Y are the same or different from each other and represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group, wherein the C1-6 alkoxy group may be substituted with a C1-6 alkoxy group, and Z and W are the same or different from each other and represent a hydrogen atom, a halogen atom, or a C1-6 alkyl group.

公开(公告)号：US10406126B2

公开(公告)日：2019-09-10

申请号：US16260350

申请日：2019-01-29

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

Inventor： Keigo Tanaka ,  Tasuku Ishida ,  Masayuki Miyano ,  Raku Shinkyo

IPC: C07C233/73 ,  C07C235/60 ,  A61K31/166 ,  A61P7/06 ,  A61P29/00 ,  A61P19/10

Abstract: The present invention provides a compound represented by formula (1): or pharmaceutically acceptable salt thereof, wherein X and Y are the same or different from each other and represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group, wherein the C1-6 alkoxy group may be substituted with a C1-6 alkoxy group, and Z and W are the same or different from each other and represent a hydrogen atom, a halogen atom, or a C1-6 alkyl group.

公开(公告)号：US09975910B2

公开(公告)日：2018-05-22

申请号：US14904860

申请日：2014-07-18

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

Inventor： Keigo Tanaka ,  Takashi Fukuyama ,  Norio Murai ,  Wataru Itano ,  Shinsuke Hirota ,  Daisuke Iida ,  Hiroshi Azuma

IPC: C07D491/048 ,  C07F7/22 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02

CPC classification number: C07F7/2208 ,  C07D491/048 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F5/025 ,  C07F5/027

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.

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：US08592470B2

公开(公告)日：2013-11-26

申请号：US13752660

申请日：2013-01-29

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

Inventor： Keigo Tanaka ,  Tomoki Nishioka

IPC: C07D413/14

CPC classification number: C07D413/14

Abstract: A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein R1 is a halogen atom, etc., R2 is a methyl group, etc., R3 is a C1-6 alkyl group, etc., and M is a group represented by: etc.

Abstract translation: 由式（1-1）或（1-2）表示的化合物或其药理学上可接受的盐保留了西他生坦的主要治疗效果，并且具有改善的CYP抑制作用：其中R1是卤素原子等，R2是 甲基等，R3为C1-6烷基等，M为由...表示的基团。