Antibacterial agents and process for producing the same
    1.
    发明申请
    Antibacterial agents and process for producing the same 失效
    抗菌剂及其制造方法

    公开(公告)号:US20050130934A1

    公开(公告)日:2005-06-16

    申请号:US11049423

    申请日:2005-02-02

    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。

    Antibacterial agents and process for producing the same
    2.
    发明授权
    Antibacterial agents and process for producing the same 失效
    抗菌剂及其制造方法

    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

    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。

    Oligosaccharide derivatives and process for producing the same
    4.
    发明授权
    Oligosaccharide derivatives and process for producing the same 失效
    寡糖衍生物及其制备方法

    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。

    Breast cancer resistance protein (bcrp) inhibitor
    6.
    发明申请
    Breast cancer resistance protein (bcrp) inhibitor 失效
    乳腺癌抗性蛋白(bcrp)抑制剂

    公开(公告)号:US20060128636A1

    公开(公告)日:2006-06-15

    申请号:US10544064

    申请日:2004-02-03

    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。

    Breast cancer resistance protein (BCRP) inhibitor
    10.
    发明授权
    Breast cancer resistance protein (BCRP) inhibitor 失效
    乳腺癌抗性蛋白(BCRP)抑制剂

    公开(公告)号:US07371773B2

    公开(公告)日:2008-05-13

    申请号:US10544064

    申请日:2004-02-03

    IPC分类号: A61K31/415

    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。