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公开(公告)号:US20080287374A1
公开(公告)日:2008-11-20
申请号:US12181957
申请日:2008-07-29
申请人: Ryuta YAMAZAKI , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Sachiko Matsumoto , Ritsuo Aiyama , Oh Yoshida , Masato Nagaoka , Shusuke Hashimoto , Yoshikazu Sugimoto
发明人: Ryuta YAMAZAKI , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Sachiko Matsumoto , Ritsuo Aiyama , Oh Yoshida , Masato Nagaoka , Shusuke Hashimoto , Yoshikazu Sugimoto
IPC分类号: A61K31/352 , A61K31/7048 , A61P35/00
CPC分类号: G01N33/57415 , A61K31/121 , A61K31/352 , C07D311/30 , C07D493/04 , G01N33/5011
摘要: The invention provides a cancer cell useful in screening BCRP-inhibitors, and a BCRP-inhibitor.The BCRP-inhibitor contains, as the active ingredient, a flavonoid represented by any of the following formulae (1), (2), (3), (4), and (5): and glycosides, esters, or salts thereof; and an anticancer agent containing the BCRP-inhibitor together with an anticancer agent available as the substrate of BCRP.
摘要翻译: 本发明提供了可用于筛选BCRP抑制剂和BCRP抑制剂的癌细胞。 BCRP抑制剂含有下列通式(1),(2),(3),(4)和(5)中任一项所示的类黄酮作为活性成分:及其糖苷,酯或其盐; 以及含有BCRP抑制剂的抗癌剂和可用作BCRP底物的抗癌剂。
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公开(公告)号:US07371773B2
公开(公告)日:2008-05-13
申请号:US10544064
申请日:2004-02-03
申请人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
发明人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
IPC分类号: A61K31/415
CPC分类号: C07D211/58 , A61K31/277 , A61K31/7034 , C07C255/37 , C07D317/60
摘要: The invention provides a drug which inhibits BCRP.A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1−7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., —OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
摘要翻译: 本发明提供抑制BCRP的药物。 作为活性成分,含有下述式(1)表示的二苯基丙烯腈衍生物的乳
球癌抗性蛋白质抑制剂:[其中,8个相同或不同的8个R代表氢原子,羟基 基团,硝基,氨基,乙酰氨基(-NHCOCH 3 SO 3); 氰基(-CN基); 甲酰基(-CHO基),-COOR 1(R 1是氢或C 1 -C 4烷基),-O(CH 2) )nOR 2(n = 1-7:R 2是氢或C 1 -C 4烷基),-OOCCH 2 (R 3)是氢,C 1 -C 4烷基,(Z)-2-(3,4-二氯苯基) 二甲氧基 - 苯基)-3-(4-羟基 - 苯基) - 丙烯腈或糖吡喃糖基),C1-C8烷氧基,C1-C4烷基,卤素原子,C1-C4烷氧基C1-C4烷氧基C1- C4烷氧基,C2-C8酰氧基,C2-C8卤代酰氧基,亚甲二氧基,三氟甲基,磷酸基(即-OP(O)(OH)2))或 其盐,硫酸基(即-OSO 3 H)或其盐,糖吡喃糖基或其盐,糖吡喃糖基的磷酸酯或酯的盐, 糖吡喃糖基的硫酸酯或酯的盐或哌啶子基哌啶羰基氧基],其酯或其盐。-
公开(公告)号:US08697742B2
公开(公告)日:2014-04-15
申请号:US11909805
申请日:2006-03-29
申请人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
发明人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
IPC分类号: A01N43/06 , A61K31/38 , A01N43/40 , A61K31/435 , C07D333/02 , C07D487/00
CPC分类号: C07C255/37 , A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/277 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/4164 , A61K31/4184 , A61K31/42 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4409 , A61K31/4525 , A61K31/4535 , A61K31/47 , A61K31/5377 , A61K31/661 , C07C2603/26 , C07D207/337 , C07D209/18 , C07D213/57 , C07D215/14 , C07D215/18 , C07D233/64 , C07D233/84 , C07D235/16 , C07D261/08 , C07D277/30 , C07D277/64 , C07D307/54 , C07D307/56 , C07D307/66 , C07D307/72 , C07D307/79 , C07D307/81 , C07D333/28 , C07D333/36 , C07D333/44 , C07D333/60 , C07D401/04 , C07D401/06 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/06 , C07F9/65586
摘要: A breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative or a salt thereof.
摘要翻译: 乳腺癌抗性蛋白(BCRP / ABCG2)抑制剂。 BCRP抑制剂含有作为活性成分的丙烯腈衍生物或其盐。
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公开(公告)号:US20060135445A1
公开(公告)日:2006-06-22
申请号:US10544062
申请日:2004-02-03
申请人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Sachiko Matsumoto , Ritsuo Aiyama , Oh Yoshida , Masato Nagaoka , Shusuke Hashimoto , Yoshikazu Sugimoto
发明人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Sachiko Matsumoto , Ritsuo Aiyama , Oh Yoshida , Masato Nagaoka , Shusuke Hashimoto , Yoshikazu Sugimoto
IPC分类号: A61K31/7048 , A61K31/353
CPC分类号: G01N33/57415 , A61K31/121 , A61K31/352 , C07D311/30 , C07D493/04 , G01N33/5011
摘要: The invention provides a cancer cell useful in screening BCRP-inhibitors, and a BCRP-inhibitor. The BCRP-inhibitor contains, as the active ingredient, a flavonoid represented by any of the following formulae (1), (2), (3), (4), and (5): and glycosides, esters, or salts thereof; and an anticancer agent containing the BCRP-inhibitor together with an anticancer agent available as the substrate of BCRP.
摘要翻译: 本发明提供了可用于筛选BCRP抑制剂和BCRP抑制剂的癌细胞。 BCRP抑制剂含有下列通式(1),(2),(3),(4)和(5)中任一项所示的类黄酮作为活性成分:及其糖苷,酯或其盐; 以及含有BCRP抑制剂的抗癌剂和可用作BCRP底物的抗癌剂。
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公开(公告)号:US20090253656A1
公开(公告)日:2009-10-08
申请号:US11909805
申请日:2006-03-29
申请人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
发明人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
IPC分类号: A61K31/277 , A61K31/675 , A61K31/5377 , A61K31/496 , A61K31/47 , A61K31/4709 , A61K31/4545 , A61K31/4535 , A61K31/44 , A61K31/426 , A61K31/428 , A61K31/42 , A61K31/4184 , A61K31/4164 , A61K31/403 , A61K31/40 , A61K31/381 , A61K31/343 , A61K31/341 , C07D413/04 , C07F9/576 , C07D215/16 , C07D409/04 , C07D405/04 , C07D213/84 , C07D417/04 , C07D277/62 , C07D277/30 , C07D261/14 , C07D235/16 , C07D233/90 , C07D209/18 , C07D207/337 , C07D333/42 , C07D333/20 , C07D307/82 , C07D307/66 , C07C255/32 , A61P35/00 , C07D333/36 , A61K31/4525
CPC分类号: C07C255/37 , A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/277 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/4164 , A61K31/4184 , A61K31/42 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4409 , A61K31/4525 , A61K31/4535 , A61K31/47 , A61K31/5377 , A61K31/661 , C07C2603/26 , C07D207/337 , C07D209/18 , C07D213/57 , C07D215/14 , C07D215/18 , C07D233/64 , C07D233/84 , C07D235/16 , C07D261/08 , C07D277/30 , C07D277/64 , C07D307/54 , C07D307/56 , C07D307/66 , C07D307/72 , C07D307/79 , C07D307/81 , C07D333/28 , C07D333/36 , C07D333/44 , C07D333/60 , C07D401/04 , C07D401/06 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/06 , C07F9/65586
摘要: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor.The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom;Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
摘要翻译: 本发明涉及一种乳腺癌抗性蛋白(BCRP / ABCG2)抑制剂。 BCRP抑制剂含有式(1)表示的丙烯腈衍生物作为活性成分:其中R1和R2之一表示氰基,另一个表示氢原子; Ar 1表示由式(2)〜(4)表示的基团中的基团,Ar 2表示具有可被卤素原子取代的稠环的芳香族烃基或选自由 下述式(5)〜(15)表示:或其盐。
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公开(公告)号:US20060128636A1
公开(公告)日:2006-06-15
申请号:US10544064
申请日:2004-02-03
申请人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
发明人: Ryuta Yamazaki , Yukiko Nishiyama , Tomio Furuta , Takeshi Matsuzaki , Hiroshi Hatano , Oh Yoshida , Masato Nagaoka , Ritsuo Aiyama , Shusuke Hashimoto , Yoshikazu Sugimoto
IPC分类号: A61K31/7034 , A61K31/277 , A61K31/66
CPC分类号: C07D211/58 , A61K31/277 , A61K31/7034 , C07C255/37 , C07D317/60
摘要: The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1−7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., —OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
摘要翻译: 本发明提供抑制BCRP的药物。 作为活性成分,含有下述式(1)表示的二苯基丙烯腈衍生物的乳
球癌抗性蛋白质抑制剂:[其中,8个相同或不同的8个R代表氢原子,羟基 基团,硝基,氨基,乙酰氨基(-NHCOCH 3 SO 3); 氰基(-CN基); 甲酰基(-CHO基),-COOR 1(R 1是氢或C 1 -C 4烷基),-O(CH 2) )nOR 2(n = 1-7:R 2是氢或C 1 -C 4烷基),-OOCCH 2 (R 3)是氢,C 1 -C 4烷基,(Z)-2-(3,4-二氯苯基) 二甲氧基 - 苯基)-3-(4-羟基 - 苯基) - 丙烯腈或糖吡喃糖基),C1-C8烷氧基,C1-C4烷基,卤素原子,C1-C4烷氧基C1-C4烷氧基C1- C4烷氧基,C2-C8酰氧基,C2-C8卤代酰氧基,亚甲二氧基,三氟甲基,磷酸基(即-OP(O)(OH)2))或 其盐,硫酸基(即-OSO 3 H)或其盐,糖吡喃糖基或其盐,糖吡喃糖基的磷酸酯或酯的盐, 糖吡喃糖基的硫酸酯或酯的盐或哌啶子基哌啶羰基氧基],其酯或其盐。-
公开(公告)号:US5593517A
公开(公告)日:1997-01-14
申请号:US305916
申请日:1994-09-15
申请人: Akiko Saito , Masashi Sahashi , Yoichi Tokai , Akihiko Tsutai , Masami Okamura , Yukiko Nishiyama , Michihiko Inaba
发明人: Akiko Saito , Masashi Sahashi , Yoichi Tokai , Akihiko Tsutai , Masami Okamura , Yukiko Nishiyama , Michihiko Inaba
CPC分类号: B82Y25/00 , F25B9/14 , H01F1/015 , F25B2309/003
摘要: The regenerating material according to the present invention comprises two alloy phases which differ in a content of rare earth elements. Of these alloy phases, a dominant phase in the regenerating material is defined as a main phase, and the other phase is defined as a sub-phase. A plurality of particles, each of which consists of a granular main phase and a sub-phase present on the surface of the main phase, gathers to form an aggregate. Otherwise, a sub-phase present in a main phase in the form of fiber. The refrigerator according to the present invention comprises a regenerator charged with above-mentioned regenerating material, a coolant gas and an expansion means for expanding the coolant gas.
摘要翻译: 根据本发明的再生材料包括稀土元素含量不同的两个合金相。 在这些合金相中,再生材料中的主相被定义为主相,另一相被定义为子相。 多个颗粒,每个颗粒由存在于主相表面上的颗粒状主相和亚相组成,聚集形成聚集体。 否则,以纤维形式存在于主相中的子阶段。 根据本发明的冰箱包括装有上述再生材料的再生器,冷却剂气体和用于膨胀冷却剂气体的膨胀装置。
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