Breast cancer resistance protein (BCRP) inhibitor
    3.
    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。

    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。

    Compositions for retarding skin aging
    8.
    发明授权
    Compositions for retarding skin aging 失效
    用于延缓皮肤老化的组合物

    公开(公告)号:US08101211B2

    公开(公告)日:2012-01-24

    申请号:US10450181

    申请日:2001-12-10

    IPC分类号: A61K36/00

    摘要: A composition for retarding skin aging which contains an edible herb medicine or medicines round in Taiwan, in particular a plant extract or extracts having melanin formation-unhibiting, elastase-inhibiting, hyaluronidase-inhibiting, active oxygen-eliminating and/or radical-capturing type antioxidant activities, and a medicinally acceptable base and/or additives for external dermal application. The composition is useful in promoting skin whitening effects, maintaining the tension and elasticity of the skin, facilitating skin moistening and providing the skin with anti-inflammatory and/or anti-allergic properties.

    摘要翻译: 用于延缓在台湾含有食用草药或药物的皮肤老化的组合物,特别是具有黑色素形成抑制,弹性蛋白酶抑制,透明质酸酶抑制,活性氧消除和/或自由基捕获型的植物提取物或提取物 抗氧化剂活性,以及​​用于外部皮肤应用的药学上可接受的碱和/或添加剂。 该组合物可用于促进皮肤美白效果,保持皮肤的张力和弹性,促进皮肤润湿并向皮肤提供抗炎和/或抗过敏性质。

    Pharmaceutical compositions containing camptothecins
    9.
    发明授权
    Pharmaceutical compositions containing camptothecins 失效
    含有喜树碱的药物组合物

    公开(公告)号:US07994186B2

    公开(公告)日:2011-08-09

    申请号:US11107881

    申请日:2005-04-18

    摘要: A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium erythorbate, sodium thioglycolate, sodium pyrosulfite, and α-thioglycerin. The pharmaceutical composition is useful in that, after storage for a long period of time or under light-irradiation conditions, camptothecin or a derivative thereof contained therein undergoes minimum degradation.

    摘要翻译: 一种含喜树碱的药物组合物,其含有:(a)喜树碱或其衍生物,和(b)一种或多种选自抗坏血酸或其盐的化合物,亚硫酸氢钠,亚硫酸钠,焦亚硫酸钾,异硫氰酸钠,钠 巯基乙酸钠,焦亚硫酸钠和α-硫代甘油。 药物组合物的用途在于,长时间储存​​或在光照条件下,喜树碱或其衍生物经受最小的降解。

    Pharmaceutical compositions containing camptothecins
    10.
    发明申请
    Pharmaceutical compositions containing camptothecins 失效
    含有喜树碱的药物组合物

    公开(公告)号:US20060235040A1

    公开(公告)日:2006-10-19

    申请号:US11107881

    申请日:2005-04-18

    摘要: A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium erythorbate, sodium thioglycolate, sodium pyrosulfite, and α-thioglycerin. The pharmaceutical composition is useful in that, after storage for a long period of time or under light-irradiation conditions, camptothecin or a derivative thereof contained therein undergoes minimum degradation.

    摘要翻译: 一种含喜树碱的药物组合物,其含有:(a)喜树碱或其衍生物,和(b)一种或多种选自抗坏血酸或其盐的化合物,亚硫酸氢钠,亚硫酸钠,焦亚硫酸钾,异硫氰酸钠,钠 巯基乙酸盐,焦亚硫酸钠和α-硫代甘油。 药物组合物的用途在于,长时间储存​​或在光照条件下,喜树碱或其衍生物经受最小的降解。