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公开(公告)号:US20100168430A1
公开(公告)日:2010-07-01
申请号:US11997967
申请日:2006-08-04
申请人: Sawako Ozawa , Nobuhiro Oikawa , Eisaku Mizuguchi , Hirosato Ebiike , Fumio Watanabe , Kenji Morikami , Nobuo Shimma , Nobuya Ishii , Toshiyuki Tsukaguchi , Yasuhiro Tamaki , Hidenori Takahashi
发明人: Sawako Ozawa , Nobuhiro Oikawa , Eisaku Mizuguchi , Hirosato Ebiike , Fumio Watanabe , Kenji Morikami , Nobuo Shimma , Nobuya Ishii , Toshiyuki Tsukaguchi , Yasuhiro Tamaki , Hidenori Takahashi
IPC分类号: C07D471/04
CPC分类号: C07D471/04
摘要: It is intended to provide a compound represented by the formula (1): [wherein Ar is an arylene group to be attached selected from the following formula (2): (wherein * represents a binding site to a nitrogen atom and ** represents a binding site to T); T represents —(O)n—R; R represents a C1-C6 alkyl group or the like; n represents 0 or 1; X represents O or the like; R2, R3 and R4 are independently selected from a hydrogen atom or C1-C3 alkyl; or R2 and R3 may join together with an urea structure containing the nitrogen atoms to which they bind to form a 5- or 6-membered heterocycle; Y represents CH or N], or a pharmaceutically acceptable salt thereof or a prodrug thereof and a pharmaceutical composition containing the same.
摘要翻译: 旨在提供由式(1)表示的化合物:[其中Ar是选自下式(2)中的被连接的亚芳基:(其中*表示与氮原子的结合位点,**表示 结合位点到T); T表示 - (O)n -R; R表示C1-C6烷基等; n表示0或1; X表示O等; R2,R3和R4独立地选自氢原子或C1-C3烷基; 或者R 2和R 3可以与含有它们所结合的氮原子的脲结合物一起形成5-或6-元杂环; Y表示CH或N],或其药学上可接受的盐或其前药,以及含有该化合物的药物组合物。
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公开(公告)号:US08299252B2
公开(公告)日:2012-10-30
申请号:US11997967
申请日:2006-08-04
申请人: Sawako Ozawa , Nobuhiro Oikawa , Eisaku Mizuguchi , Hirosato Ebiike , Fumio Watanabe , Kenji Morikami , Nobuo Shimma , Nobuya Ishii , Toshiyuki Tsukaguchi
发明人: Sawako Ozawa , Nobuhiro Oikawa , Eisaku Mizuguchi , Hirosato Ebiike , Fumio Watanabe , Kenji Morikami , Nobuo Shimma , Nobuya Ishii , Toshiyuki Tsukaguchi
IPC分类号: A61K31/437 , C07D471/04
CPC分类号: C07D471/04
摘要: It is intended to provide a compound represented by the formula (1): [wherein Ar is an arylene group to be attached selected from the following formula (2): (wherein * represents a binding site to a nitrogen atom and ** represents a binding site to T); T represents —(O)n—R; R represents a C1-C6 alkyl group or the like; n represents 0 or 1; X represents O or the like; R2, R3 and R4 are independently selected from a hydrogen atom or C1-C3 alkyl; or R2 and R3 may join together with an urea structure containing the nitrogen atoms to which they bind to form a 5- or 6-membered heterocycle; Y represents CH or N], or a pharmaceutically acceptable salt thereof or a prodrug thereof and a pharmaceutical composition containing the same.
摘要翻译: 旨在提供由式(1)表示的化合物:[其中Ar是选自下式(2)中的被连接的亚芳基:(其中*表示与氮原子的结合位点,**表示 结合位点到T); T表示 - (O)n -R; R表示C1-C6烷基等; n表示0或1; X表示O等; R2,R3和R4独立地选自氢原子或C1-C3烷基; 或者R 2和R 3可以与含有它们所结合的氮原子的脲结合物一起形成5-或6-元杂环; Y表示CH或N],或其药学上可接受的盐或其前药,以及含有该化合物的药物组合物。
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公开(公告)号:US08022205B2
公开(公告)日:2011-09-20
申请号:US12376039
申请日:2007-08-07
申请人: Nobuo Shimma , Hirosato Ebiike , Jun Ohwada , Hatsuo Kawada , Kenji Morikami , Mitsuaki Nakamura , Miyuki Yoshida , Nobuya Ishii , Masami Hasegawa , Shun Yamamoto , Kohei Koyama
发明人: Nobuo Shimma , Hirosato Ebiike , Jun Ohwada , Hatsuo Kawada , Kenji Morikami , Mitsuaki Nakamura , Miyuki Yoshida , Nobuya Ishii , Masami Hasegawa , Shun Yamamoto , Kohei Koyama
IPC分类号: C07D401/04 , C07D401/12 , C07D405/04 , C07D413/12
CPC分类号: C07D487/04
摘要: A drug is provided that is useful as a preventive or therapeutic for cancer as a result of having superior PI3K inhibitory effects as well as superior stability in the body and water-solubility.A compound, or pharmaceutically acceptable salt thereof, represented by formula (I): [wherein, X represents a single bond, etc.; Y represents a single bond, etc. (provided that X and Y are not simultaneously single bonds); Z represents a hydrogen atom, etc.; m represents an integer of 1 or 2; and R1 represents a cyclic substituent].
摘要翻译: 由于具有优异的PI3K抑制作用以及在体内具有优异的稳定性和水溶性,因此提供了可用作癌症的预防或治疗剂的药物。 由式(I)表示的化合物或其药学上可接受的盐:[其中,X表示单键等; Y表示单键等(X和Y不同时为单键)。 Z表示氢原子等; m表示1或2的整数; 并且R 1表示环状取代基]。
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公开(公告)号:US20100069629A1
公开(公告)日:2010-03-18
申请号:US12376039
申请日:2007-08-07
申请人: Nobuo Shimma , Hirosato Ebiike , Jun Ohwada , Hatsuo Kawada , Kenji Morikami , Mitsuaki Nakamura , Miyuki Yoshida , Nobuya Ishii , Masami Hasegawa , Shun Yamamoto , Kohei Koyama
发明人: Nobuo Shimma , Hirosato Ebiike , Jun Ohwada , Hatsuo Kawada , Kenji Morikami , Mitsuaki Nakamura , Miyuki Yoshida , Nobuya Ishii , Masami Hasegawa , Shun Yamamoto , Kohei Koyama
IPC分类号: C07D413/14 , A61P35/00
CPC分类号: C07D487/04
摘要: A drug is provided that is useful as a preventive or therapeutic for cancer as a result of having superior PI3K inhibitory effects as well as superior stability in the body and water-solubility.A compound, or pharmaceutically acceptable salt thereof, represented by formula (I): [wherein, X represents a single bond, etc.; Y represents a single bond, etc. (provided that X and Y are not simultaneously single bonds); Z represents a hydrogen atom, etc.; m represents an integer of 1 or 2; and R1 represents a cyclic substituent].
摘要翻译: 由于具有优异的PI3K抑制作用以及在体内具有优异的稳定性和水溶性,因此提供了可用作癌症的预防或治疗剂的药物。 由式(I)表示的化合物或其药学上可接受的盐:[其中,X表示单键等; Y表示单键等(X和Y不同时为单键)。 Z表示氢原子等; m表示1或2的整数; 并且R 1表示环状取代基]。
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公开(公告)号:US08829199B2
公开(公告)日:2014-09-09
申请号:US13389146
申请日:2010-08-05
申请人: Naoki Taka , Masayuki Ohmori , Kyoko Takami , Masayuki Matsushita , Tadakatsu Hayase , Ikumi Hyodo , Masami Kochi , Hiroki Nishii , Hirosato Ebiike , Yoshito Nakanishi , Toshiyuki Mio , Lisha Wang , Weili Zhao
发明人: Naoki Taka , Masayuki Ohmori , Kyoko Takami , Masayuki Matsushita , Tadakatsu Hayase , Ikumi Hyodo , Masami Kochi , Hiroki Nishii , Hirosato Ebiike , Yoshito Nakanishi , Toshiyuki Mio , Lisha Wang , Weili Zhao
IPC分类号: A61K31/4184 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号: C07F7/0805 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/5377 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/056
摘要: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like ; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.)
摘要翻译: 由式(I)表示的化合物或其药理学上可接受的盐,其可以抑制癌组织中的成纤维细胞生长因子受体(FGFR)家族激酶。 (式中,A表示5〜10元杂芳基或C6-10芳基; R1和R2独立地表示H,OH,X,CN,NO2,C1-4卤代烷基,C1- 6烷基等R 1和R 2一起形成(取代的)3-至10-元杂环基或(取代的)5至10元杂芳基>; R 3表示H,C 1-5烷基 ,C 6-10芳基,C 1-5烷基或C 1-4卤代烷基; R 4表示H,X,C 1-3烷基,C 1-4卤代烷基,OH,CN,NO 2, 等等)
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公开(公告)号:US20100324284A1
公开(公告)日:2010-12-23
申请号:US12735656
申请日:2009-02-06
申请人: Hirosato Ebiike , Jun Ohwada , Kohei Koyama , Takeshi Murata , Woo Sang Hong
发明人: Hirosato Ebiike , Jun Ohwada , Kohei Koyama , Takeshi Murata , Woo Sang Hong
IPC分类号: C07D417/14 , C07D413/14
CPC分类号: C07D487/04
摘要: A preventive or therapeutic agent of a proliferative disease such as cancer, having superior PI3K inhibitory effects, superior cell proliferation inhibitory action as well as superior stability in a body and water solubility, is provided.A compound represented by formula (I): [wherein, Q represents a linking group represented by —X—Y—; X represents a single bond —CO—, —CONH—, —CON(C1-4 alkyl)-, —CS—, —CSNH—, —CSN(C1-4 alkyl)-, or —SO2—; Y represents a single bond, arylene or heteroarylene; provided that X and Y are not simultaneously single bonds; and R1 represents —C0-6 alkylene-(A)m-C1-6 alkyl, or C0-6 alkylene-(A)m-C0-6 alkylene-(heterocycle)] or a pharmaceutically acceptable salt thereof.
摘要翻译: 提供了具有优异的PI3K抑制作用,优异的细胞增殖抑制作用以及优异的身体稳定性和水溶性的癌症等增殖性疾病的预防或治疗剂。 由式(I)表示的化合物:[其中,Q表示由-X-Y-表示的连接基团; X表示单键-CO - , - CONH - , - CON(C 1-4烷基) - , - CS-,-CSNH-,-CSN(C 1-4烷基) - 或-SO 2 - Y表示单键,亚芳基或亚杂芳基; 条件是X和Y不同时为单键; 和R 1表示-C 0-6亚烷基 - (A)m -C 1-6烷基或C 0-6亚烷基 - (A)m -C 0-6亚烷基 - (杂环)]或其药学上可接受的盐。
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公开(公告)号:US06376491B1
公开(公告)日:2002-04-23
申请号:US09464240
申请日:1999-12-15
申请人: Yuhko Aoki , Hirosato Ebiike , Toshihiko Fujii , Kenichi Kawasaki , Pingli Liu , Miyako Masubuchi , Tatsuo Ohtsuka , Shinji Tsujii
发明人: Yuhko Aoki , Hirosato Ebiike , Toshihiko Fujii , Kenichi Kawasaki , Pingli Liu , Miyako Masubuchi , Tatsuo Ohtsuka , Shinji Tsujii
IPC分类号: A61K31535
CPC分类号: C07D307/79 , C07D307/85 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07F9/65517
摘要: The present invention is directed to new bicyclic compounds of the formula [I], and pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, R5, R6, R7, Q1 Q2 and Q3 are as defined in the claims. The compounds have N-myristoyltransferase inhibitory and antifungal activity.
摘要翻译: 本发明涉及式[I]的新的双环化合物及其药学上可接受的盐,其中R1,R2,R3,R4,R5,R6,R7,Q1 Q2和Q3如权利要求中所定义。 该化合物具有N-肉豆蔻酰转移酶抑制和抗真菌活性。
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公开(公告)号:US20120208811A1
公开(公告)日:2012-08-16
申请号:US13389146
申请日:2010-08-05
申请人: Naoki Taka , Masayuki Ohmori , Kyoko Takami , Masayuki Matsushita , Tadakatsu Hayase , Ikumi Hyodo , Masami Kochi , Hiroki Nishii , Hirosato Ebiike , Yoshito Nakanishi , Toshiyuki Mio , Lisha Wang , Weili Zhao
发明人: Naoki Taka , Masayuki Ohmori , Kyoko Takami , Masayuki Matsushita , Tadakatsu Hayase , Ikumi Hyodo , Masami Kochi , Hiroki Nishii , Hirosato Ebiike , Yoshito Nakanishi , Toshiyuki Mio , Lisha Wang , Weili Zhao
IPC分类号: A61K31/4184 , C07D401/14 , A61K31/454 , C07D471/04 , A61P35/02 , A61K31/496 , C07D413/14 , A61K31/5377 , A61P35/00 , C07D403/14 , A61K31/437
CPC分类号: C07F7/0805 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/5377 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/056
摘要: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like ; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.)
摘要翻译: 由式(I)表示的化合物或其药理学上可接受的盐,其可以抑制癌组织中的成纤维细胞生长因子受体(FGFR)家族激酶。 (式中,A表示5〜10元杂芳基或C6-10芳基; R1和R2独立地表示H,OH,X,CN,NO2,C1-4卤代烷基,C1- 6烷基等R 1和R 2一起形成(取代的)3-至10-元杂环基或(取代的)5至10元杂芳基>; R 3表示H,C 1-5烷基 ,C 6-10芳基,C 1-5烷基或C 1-4卤代烷基; R 4表示H,X,C 1-3烷基,C 1-4卤代烷基,OH,CN,NO 2, 等等)
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