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公开(公告)号：US08362236B2
公开(公告)日：2013-01-29
申请号：US12529222
申请日：2008-02-29
申请人： Nobuo Shimma , Takuo Tsukuda , Hiroshi Koyano , Atsushi Suda , Tadakatsu Hayase , Kihito Hada , Ken-Ichi Kawasaki , Susumu Komiyama , Naomi Ono , Toshikazu Yamazaki , Ryoichi Saitoh , Masami Kohchi , Kiyoshi Hasegawa
发明人： Nobuo Shimma , Takuo Tsukuda , Hiroshi Koyano , Atsushi Suda , Tadakatsu Hayase , Kihito Hada , Ken-Ichi Kawasaki , Susumu Komiyama , Naomi Ono , Toshikazu Yamazaki , Ryoichi Saitoh , Masami Kohchi , Kiyoshi Hasegawa
IPC分类号： C07D497/08 , C07D513/08 , C07D513/20 , A61K31/529 , A61K31/53 , A61K31/5377 , A61P35/00
CPC分类号： C07D497/08 , C07D513/08 , C07D513/18 , C07D513/20
摘要： The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.
摘要翻译： 本发明提供具有抑制HSP90酶的活性的新型化合物，可用作抗癌剂等，以及可用作其合成中间体的化合物。 具体而言，本发明提供下述式（1）表示的化合物及其药学上可接受的盐：其中X，R1，R2，R3，R4，R5，R6，R7，L1，L2和L3如 规范。
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公开(公告)号：US20100056510A1
公开(公告)日：2010-03-04
申请号：US12529222
申请日：2008-02-29
申请人： Nobuo Shimma , Takuo Tsukuda , Hiroshi Koyano , Atsushi Suda , Tadakatsu Hayase , Kihito Hada , Ken-ichi Kawasaki , Susumu Komiyama , Naomi Ono , Toshikazu Yamazaki , Ryoichi Saitoh , Masami Kohchi , Kiyoshi Hasegawa
发明人： Nobuo Shimma , Takuo Tsukuda , Hiroshi Koyano , Atsushi Suda , Tadakatsu Hayase , Kihito Hada , Ken-ichi Kawasaki , Susumu Komiyama , Naomi Ono , Toshikazu Yamazaki , Ryoichi Saitoh , Masami Kohchi , Kiyoshi Hasegawa
IPC分类号： A61K31/519 , C07D513/04 , A61P35/00 , A61K31/5377
CPC分类号： C07D497/08 , C07D513/08 , C07D513/18 , C07D513/20
摘要： The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.
摘要翻译： 本发明提供具有抑制HSP90酶的活性的新型化合物，可用作抗癌剂等，以及可用作其合成中间体的化合物。 具体而言，本发明提供下述式（1）表示的化合物及其药学上可接受的盐：其中X，R1，R2，R3，R4，R5，R6，R7，L1，L2和L3如 规范。
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公开(公告)号：US07745663B2
公开(公告)日：2010-06-29
申请号：US11658533
申请日：2005-07-26
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： C07C239/00 , C07C259/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07C229/00 , C07C251/00 , C07D265/00 , A61K31/535 , A01N37/18 , A61K31/16 , A61K31/165
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译： 本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。
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公开(公告)号：US06849709B2
公开(公告)日：2005-02-01
申请号：US09760949
申请日：2001-01-16
IPC分类号： A61K38/00 , A61K38/10 , A61P31/00 , A61P31/10 , C07K7/02 , C07K7/08 , C07K7/50 , A61K38/12 , C07K7/06
CPC分类号： C07K7/08 , A61K38/00 , Y10S435/911
摘要： The present invention relates to novel Aerothricins represented by the Formula (I), and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition comprising an Aerothricin of the Formula (I) and a pharmaceutically acceptable carrier. Furthermore, the present invention relates to the use of such Aerothricins for the preparation of medicaments, as well as to processes for the preparation of the Aerothricins of the Formula (I).
摘要翻译： 本发明涉及由式（I）表示的新型气丝菌素及其药学上可接受的盐。本发明还涉及包含式（I）的气丝菌素和药学上可接受的载体的药物组合物。 此外，本发明涉及这种气丝菌素用于制备药物的用途，以及制备式（I）的气丝菌素的方法。
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公开(公告)号：US06489440B1
公开(公告)日：2002-12-03
申请号：US09360476
申请日：1999-07-23
申请人： Masahiro Aoki , Masami Kohchi , Kazunao Masubuchi , Eisaku Mizuguchi , Takeshi Murata , Hiroaki Ohkuma , Takehiro Okada , Masahiro Sakaitani , Nobuo Shimma , Takahide Watanabe , Mieko Yanagisawa , Yuri Yasuda
发明人： Masahiro Aoki , Masami Kohchi , Kazunao Masubuchi , Eisaku Mizuguchi , Takeshi Murata , Hiroaki Ohkuma , Takehiro Okada , Masahiro Sakaitani , Nobuo Shimma , Takahide Watanabe , Mieko Yanagisawa , Yuri Yasuda
IPC分类号： C07K750
摘要： The present invention relates to novel Aerothricins represented by the Formula (I), wherein R1, R2, R3, R4, R5, X, Y, Z, and m are as defined in Claim 1; and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition comprising an Aerothricin of the Formula (I) and a pharmaceutically acceptable carrier. Furthermore, the present invention relates to the use of such Aerothricins for the preparation of medicaments, as well as to processes and intermediates for the preparation of the Aerothricins of the Formula (I).
摘要翻译： 本发明涉及由式（I）表示的新型气丝菌素，其中R1，R2，R3，R4，R5，X，Y，Z和m如权利要求1所定义; 本发明还涉及包含式（I）的气丝菌素和药学上可接受的载体的药物组合物。 此外，本发明涉及这种气丝菌素用于制备药物的用途，以及制备式（I）的气丝菌素的方法和中间体。
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公开(公告)号：US08575391B2
公开(公告)日：2013-11-05
申请号：US12752396
申请日：2010-04-01
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： C07C239/00 , C07C259/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07D265/00 , C07C229/00 , C07C251/00 , A61K31/535 , A01N37/18 , A61K31/16 , A61K31/165
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译： 本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。
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公开(公告)号：US20090233915A1
公开(公告)日：2009-09-17
申请号：US11658533
申请日：2005-07-26
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： A61K31/535 , C07C233/64 , A61K31/166 , C07D265/02 , C07D261/04 , A61K31/42 , C07C229/58 , A61P35/00
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译： 本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。
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公开(公告)号：US20100197676A1
公开(公告)日：2010-08-05
申请号：US12752396
申请日：2010-04-01
申请人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
发明人： Yoshiaki Isshiki , Yasunori Kohchi , Eisaku Mizuguchi , Hitoshi Iikura , Yasuaki Matsubara , Shinji Tsujii , Nobuo Shimma , Masanori Miwa , Satoshi Aida , Masami Kohchi , Takeshi Murata , Kosuke Aso
IPC分类号： A61K31/539 , A61P19/02 , A61K31/16 , C07C259/00 , C07D209/32 , A61K31/4035 , C07D265/02 , A61K31/535 , C07D273/01
CPC分类号： C07C259/10 , C07C317/18 , C07C323/12 , C07D207/27 , C07D211/76 , C07D239/10 , C07D261/04 , C07D263/22 , C07D265/02 , C07D265/32 , C07D273/00
摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
摘要翻译： 本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。
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