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    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

    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。

    Breast cancer resistance protein (bcrp) inhibitor
    7.
    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

    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。

    Phenanthroindolizidine compound and NFκB inhibitor containing same as active ingredient
    10.
    发明授权
    Phenanthroindolizidine compound and NFκB inhibitor containing same as active ingredient 有权
    菲并吲哚哩啶化合物和含有与活性成分相同的NF＆kgr B抑制剂

    公开(公告)号：US09174979B2

    公开(公告)日：2015-11-03

    申请号：US13125698

    申请日：2009-10-23

    申请人： Takashi Ikeda ,  Seigo Sawada ,  Takashi Yaegashi ,  Takeshi Matsuzaki ,  Shusuke Hashimoto ,  Ryuta Yamazaki

    发明人： Takashi Ikeda ,  Seigo Sawada ,  Takashi Yaegashi ,  Takeshi Matsuzaki ,  Shusuke Hashimoto ,  Ryuta Yamazaki

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P35/00 ,  C07D491/147

    CPC分类号： C07D471/04 ,  C07D491/147

    摘要： A novel compound having an excellent NFκB inhibitory effect is provided and specifically disclosed is a compound represented by the following formula (1) or a salt thereof:wherein, R1 represents a hydrogen atom, a lower alkyl group, a lower alkyloxy group, or a halogen atom;R2 represents a hydroxyl group, or a lower alkyloxy group;R3 represents a hydrogen atom, a lower alkyl group, or a halogen atom;R4 represents a hydrogen atom or a lower alkyloxy group;R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6;R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5;R7 represents a hydrogen atom or a lower alkyl group; andR8 represents a hydrogen atom, a hydroxyl group, an amino group, or a lower alkylcarbonyloxy group (excluding the case where R1, R3, R4 and R7 are hydrogen atoms, R2 and R8 are hydroxyl groups, and R5 and R6 are methoxy groups).

    摘要翻译： 提供了具有优异的NF＆Kgr B抑制效果的新化合物，具体公开了下式（1）表示的化合物或其盐：其中，R1表示氢原子，低级烷基，低级烷氧基， 或卤素原子; R2表示羟基或低级烷氧基; R3表示氢原子，低级烷基或卤素原子; R4表示氢原子或低级烷氧基; R5表示与R6一起形成的与R6或异丙烯二氧基一起形成的氢原子，低级烷氧基，卤素原子，羟基或亚甲二氧基; R6表示与R5一起形成的氢原子，低级烷氧基或亚甲二氧基，或与R5形成的异丙烯二氧基; R7表示氢原子或低级烷基; 并且R 8表示氢原子，羟基，氨基或低级烷基羰基氧基（R 1，R 3，R 4和R 7为氢原子的情况除外，R 2和R 8为羟基，R 5和R 6为甲氧基 ）。