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公开(公告)号：US07256178B2
公开(公告)日：2007-08-14
申请号：US10522731
申请日：2003-07-31
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Susumu Takeda , Takashi Nakashima , Masashi Yoshida , Toshio Tsuchida , Tomohiro Sameshima
CPC分类号： C07D407/06 , C07D313/00 , C12P17/08 , C12P17/16 , C12P17/162
摘要： Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21′ are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
摘要翻译： 由以下通式（I）表示的化合物，其药学上可接受的盐或其水合物：其中W表示和R 3，R 7，R 7， SUP> 16，R 17，R 20，R 21和R 21'是 相同或不同，各自表示氢等。由于抑制血管生成并抑制VEGF的产生，特别是在缺氧中，化合物（I）可用作固体癌症的补救措施。
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公开(公告)号：US20080275059A1
公开(公告)日：2008-11-06
申请号：US11927542
申请日：2007-10-29
申请人： Yoshihiko KOTAKE , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
发明人： Yoshihiko KOTAKE , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
IPC分类号： A61K31/496 , C07D313/00 , C07D405/12 , A61P19/02 , A61P35/04 , A61P29/00 , A61P35/00 , A61P9/10 , A61K31/365
CPC分类号： A61K31/336 , A61K31/366 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D407/06
摘要： The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
摘要翻译： 本发明涉及由式（I）表示的化合物：其中R 3，R 6，R 7和R 7， SUP> 21个彼此相同或不同，各自表示羟基等），其药理学上可接受的盐或它们的水合物。 本发明的化合物（I）抑制血管生成，特别是在缺氧条件下抑制VEGF的产生，可用作治疗实体癌的治疗剂。
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公开(公告)号：US07619100B2
公开(公告)日：2009-11-17
申请号：US11927542
申请日：2007-10-29
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
IPC分类号： C07D313/00 , C07D313/04
CPC分类号： A61K31/336 , A61K31/366 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D407/06
摘要： The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
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公开(公告)号：US07550503B2
公开(公告)日：2009-06-23
申请号：US11473201
申请日：2006-06-23
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
IPC分类号： A01N43/02 , A61K31/335 , C07D313/00 , C07D313/04
CPC分类号： A61K31/336 , A61K31/366 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D407/06
摘要： The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
摘要翻译： 本发明涉及由式（I）表示的化合物：其中R3，R6，R7和R21彼此相同或不同，各自表示羟基等），其药理学上可接受的盐或 它们的水合物。 本发明的化合物（I）抑制血管生成，特别是在缺氧条件下抑制VEGF的产生，可用作治疗实体癌的治疗剂。
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公开(公告)号：US20080255146A1
公开(公告)日：2008-10-16
申请号：US11927564
申请日：2007-10-29
申请人： Yoshihiko KOTAKE , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
发明人： Yoshihiko KOTAKE , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
IPC分类号： A61K31/496 , C07D313/00 , A61K31/365 , A61P19/02 , A61P29/00 , A61P35/00 , A61P9/10 , C07D405/12
CPC分类号： A61K31/336 , A61K31/366 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D407/06
摘要： The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
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公开(公告)号：US07893068B2
公开(公告)日：2011-02-22
申请号：US11927564
申请日：2007-10-29
申请人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
发明人： Yoshihiko Kotake , Jun Niijima , Yoshio Fukuda , Mitsuo Nagai , Regina Mikie Kanada , Takashi Nakashima , Masahi Yoshida , Toshio Tsuchida
IPC分类号： A61K31/496 , A61K31/365 , C07D313/00 , C07D405/12 , A61P19/02 , A61P29/00 , A61P35/00 , A61P9/10
CPC分类号： A61K31/336 , A61K31/366 , A61K31/4025 , A61K31/4427 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D407/06
摘要： The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
摘要翻译： 本发明涉及由式（I）表示的化合物：其中R3，R6，R7和R21彼此相同或不同，各自表示羟基等），其药理学上可接受的盐或 它们的水合物。 本发明的化合物（I）抑制血管生成，特别是在缺氧条件下抑制VEGF的产生，可用作治疗实体癌的治疗剂。
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公开(公告)号：US07816401B2
公开(公告)日：2010-10-19
申请号：US11580047
申请日：2006-10-13
申请人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： A61K31/335 , A61K31/16
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined herein, characterized by including reacting a compound represented by Formula (12): with a compound represented by Formula (13): in the presence of a catalyst.
摘要翻译： 一种制备由式（11）表示的化合物的方法：其中P1，P7，P8，P9和R1与本文所定义的相同，其特征在于包括使由式（12）表示的化合物与式（12）表示的化合物 13）：在催化剂存在下。
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公开(公告)号：US07884128B2
公开(公告)日：2011-02-08
申请号：US12764336
申请日：2010-04-21
申请人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
发明人： Regina Mikie Kanada , Daisuke Ito , Takashi Sakai , Naoki Asai , Yoshihiko Kotake , Jun Niijima
IPC分类号： A61K31/36
CPC分类号： C07D493/04 , C07D303/12 , C07D303/14 , C07D313/00 , C07D315/00 , C07D405/12 , C07D407/06 , Y02P20/55
摘要： Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.
摘要翻译： 制备式的化合物的方法：其中P2，P3和R2与下文定义相同，其特征在于包括使由式（7）表示的化合物反应：其中P3表示羟基的保护基; 和Het表示1-苯基-1H-四唑-5-基与式（8）表示的化合物：其中P2表示羟基的保护基; 并且R 2表示在碱的存在下可被取代的苯基。
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