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公开(公告)号:US20140235614A1
公开(公告)日:2014-08-21
申请号:US14183864
申请日:2014-02-19
发明人: Setsuo Funasaka , Toshimi Okada , Keigo Tanaka , Satoshi Nagao , Isao Ohashi , Yoshinobu Yamane , Yusuke Nakatani , Yuki Karoji
IPC分类号: C07D409/14 , C07D401/14 , C07D401/12
CPC分类号: C07D409/14 , C07D401/12 , C07D401/14
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US20210230177A1
公开(公告)日:2021-07-29
申请号:US16628504
申请日:2018-07-06
发明人: Yoshito Kishi , Yanran Ai , Ning Ye , Qiaoyi Wang , Kenzo Yahata , Kentaro Iso , Santhosh Reddy Naini , Shuji Yamashita , Jihoon Lee , Isao Ohashi , Takashi Fukuyama
IPC分类号: C07D493/22
摘要: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A)
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公开(公告)号:US08933099B2
公开(公告)日:2015-01-13
申请号:US14183864
申请日:2014-02-19
发明人: Setsuo Funasaka , Toshimi Okada , Keigo Tanaka , Satoshi Nagao , Isao Ohashi , Yoshinobu Yamane , Yusuke Nakatani , Yuki Karoji
IPC分类号: A61K31/445 , C07D401/14 , C07D409/14 , C07D401/12
CPC分类号: C07D409/14 , C07D401/12 , C07D401/14
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US20230128195A1
公开(公告)日:2023-04-27
申请号:US18058441
申请日:2022-11-23
发明人: Yoshito Kishi , Yanran Ai , Ning Ye , Qiaoyi Wang , Kenzo Yahata , Kentaro Iso , Santhosh Reddy Naini , Shuji Yamashita , Jihoon Lee , Isao Ohashi , Takashi Fukuyama
IPC分类号: C07D493/22
摘要: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A):
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公开(公告)号:US11548898B2
公开(公告)日:2023-01-10
申请号:US16628504
申请日:2018-07-06
发明人: Yoshito Kishi , Yanran Ai , Ning Ye , Qiaoyi Wang , Kenzo Yahata , Kentaro Iso , Santhosh Reddy Naini , Shuji Yamashita , Jihoon Lee , Isao Ohashi , Takashi Fukuyama
IPC分类号: C07D493/22
摘要: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
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