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公开(公告)号:US20050130934A1
公开(公告)日:2005-06-16
申请号:US11049423
申请日:2005-02-02
IPC分类号: A61K31/731 , A61K31/737 , C08B37/00
CPC分类号: A61K31/702 , A61K31/731 , A61K31/737
摘要: An antibacterial agent showing a high affinity for Helicobactor pyroli and having an antibacterial effect specific to H. Pyroli. The agent has a chemical structure wherein an antibacterial substance is bonded to a sulfated polysaccharide or an oligosaccharide prepared by partial decomposition of the sulfated polysaccharide. Preferable embodiments are those having the chemical structure represented by Y—OCH(AH2NHR)n or Y—BH2NHR, wherein Y represents a sulfated polysaccharide or an oligosaccharide prepared by partial decomposition of the sulfated polysaccharide; A a carbon derived from aldehyde group occurring through the reduction of the reduced end sugar of Y and subsequent oxidation of the resulting product with an oxidant; B a carbon derived from the aldehyde group at the reduced end sugar of Y; R an antibacterial substance with a primary amino group or with an amino group introduced therein or represents an antibacterial substance derivative prepared by bonding an antibacterial substance through a spacer to the carbon A or the carbon B; and n=1 or 2.
摘要翻译: 对Helicobactor pyroli具有高亲和力并具有对H. Pyroli特异性的抗菌作用的抗菌剂。 该药剂具有抗菌物质与通过硫酸化多糖的部分分解制备的硫酸化多糖或寡糖结合的化学结构。 优选的实施方案是具有由Y-OCH(AHN 2 NHR)n或Y-BH 2 NHR表示的化学结构的那些,其中Y表示 通过硫酸化多糖的部分分解制备的硫酸化多糖或寡糖; 衍生自醛基的碳通过还原末端糖的Y而发生,随后用氧化剂氧化所得产物; B是衍生自Y的还原末端糖的醛基的碳; R是具有伯氨基或在其中引入氨基的抗菌物质,或代表通过间隔剂将抗菌物质与碳A或碳B结合而制备的抗菌物质衍生物; n = 1或2。
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公开(公告)号:US07498317B2
公开(公告)日:2009-03-03
申请号:US11049423
申请日:2005-02-02
IPC分类号: A61K31/731 , A61K31/737
CPC分类号: A61K31/702 , A61K31/731 , A61K31/737
摘要: An antibacterial agent showing a high affinity for Helicobactor pyroli and having an antibacterial effect specific to H. Pyroli. The agent has a chemical structure wherein an antibacterial substance is bonded to a sulfated polysaccharide or an oligosaccharide prepared by partial decomposition of the sulfated polysaccharide. Preferable embodiments are those having the chemical structure represented by Y—OCH(AH2NHR)n or Y—BH2NHR, wherein Y represents a sulfated polysaccharide or an oligosaccharide prepared by partial decomposition of the sulfated polysaccharide; A a carbon derived from aldehyde group occurring through the reduction of the reduced end sugar of Y and subsequent oxidation of the resulting product with an oxidant; B a carbon derived from the aldehyde group at the reduced end sugar of Y; R an antibacterial substance with a primary amino group or with an amino group introduced therein or represents an antibacterial substance derivative prepared by bonding an antibacterial substance through a spacer to the carbon A or the carbon B; and n=1 or 2.
摘要翻译: 对Helicobactor pyroli具有高亲和力并具有对H. Pyroli特异性的抗菌作用的抗菌剂。 该药剂具有抗菌物质与通过硫酸化多糖的部分分解制备的硫酸化多糖或寡糖结合的化学结构。 优选的实施方案是具有由Y-OCH(AH2NHR)n或Y-BH2NHR表示的化学结构的那些,其中Y表示硫酸化多糖或通过硫酸化多糖的部分分解制备的寡糖; 衍生自醛基的碳通过还原末端糖的Y而发生,随后用氧化剂氧化所得产物; B是衍生自Y的还原末端糖的醛基的碳; R是具有伯氨基或在其中引入氨基的抗菌物质,或代表通过间隔剂将抗菌物质与碳A或碳B结合而制备的抗菌物质衍生物; n = 1或2。
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公开(公告)号:US06645940B2
公开(公告)日:2003-11-11
申请号:US10313466
申请日:2002-12-06
IPC分类号: A61K3170
CPC分类号: C07H15/04
摘要: An oligosaccharide derivative, at higher homogeneity than fucose polysaccharide and rhamnose polysaccharide and with greater antiulcer effects, which is represented by the following general formula: Y—OCH(CH2NHR)2 wherein, Y represents an oligofucose or oligorhamnose at a polymerization number of 2 to 20, where the hydroxyl groups may or may not be partially modified in the form of sulfate ester, and R represents phenyl group, a higher alkylphenyl group, a higher alkyl group or —(CH2)n—NHX wherein n is an integer of 1 to 10 and X represents a higher alkanoyl group or an alkylamino group.
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公开(公告)号:US06518249B1
公开(公告)日:2003-02-11
申请号:US09485978
申请日:2000-02-18
IPC分类号: A61K3170
CPC分类号: C07H15/04
摘要: An oligosaccharide derivative, at higher homogeneity than fucose polysaccharide and rhamnose polysaccharide and with greater antiulcer effects, which is represented by the following general formula: Y—OCH(CH2NHR)2 wherein, Y represents an oligofucose or oligorhamnose at a polymerization number of 2 to 20, where the hydroxyl groups may or may not be partially modified in the form of sulfate ester, and R represents phenyl group, a higher alkylphenyl group, a higher alkyl group or —(CH2)n—NHX wherein n is an integer of 1 to 10 and X represents a higher alkanoyl group or an alkylamino group.
摘要翻译: 一种低聚糖衍生物,其比岩藻糖多糖和鼠李糖多糖具有更高的均一性,并且具有较大的抗溃疡作用,其由以下通式表示:其中Y表示聚合数为2至20的寡聚核糖或寡鼠李糖,其中羟基可以 或可以不以硫酸酯的形式部分修饰,R代表苯基,高级烷基苯基,高级烷基或 - (CH2)n-NHX,其中n为1至10的整数,X表示较高的 烷酰基或烷基氨基。
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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: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: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。
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