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    1,4-dihydropyridine-4-aryl-2,6-dimethyl-3,5-dicarboxylates useful as agents against drug resistant tumor cells
    1.
    发明授权
    1,4-dihydropyridine-4-aryl-2,6-dimethyl-3,5-dicarboxylates useful as agents against drug resistant tumor cells 失效
    可用作抗药性肿瘤细胞的药剂的1,4-二氢吡啶-4-芳基-2,6-二甲基-3,5-二羧酸盐

    公开(公告)号：US5216172A

    公开(公告)日：1993-06-01

    申请号：US647192

    申请日：1991-01-28

    申请人： Kouzou Toyota ,  Hisashi Shinkai ,  Hirozumi Eto ,  Akira Kamimura ,  Chikahiko Eguchi ,  Koji Ohsumi ,  Takashi Tsuruo

    发明人： Kouzou Toyota ,  Hisashi Shinkai ,  Hirozumi Eto ,  Akira Kamimura ,  Chikahiko Eguchi ,  Koji Ohsumi ,  Takashi Tsuruo

    IPC分类号： C07D211/90 ,  C07D405/04 ,  C07D405/06

    CPC分类号： C07D405/04 ,  C07D211/90 ,  C07D405/06

    摘要： Agents against drug-resistant tumor cells comprising a 1,4-dihydropyridine derivative represented by the following formula (I): ##STR1## wherein R.sup.1 is an aryl group which may be substituted;R.sup.2 and R.sup.3, which may be the same or different, each is a member selected from the group consisting of an alkyl group, an alkyloxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group, an aminocarbonyl group, a hydroxycarbonyl group, a formyl group, and a cyano group, each of which may be substituted;R.sup.4 and R.sup.5 is a hydrogen atom or a member selected from the group consisting of a lower alkyl group, a hydroxymethyl group, a cyano group, an amino group, a formyl group, and a halogen atom; andR.sup.6 is a member selected from the group consisting of an alkyl group, an aralkyl group, an alkoxycarbonyl group and an aralkyloxycarbonyl group, each of which may be substituted and the alkyl moiety in each may also contain a double bond, a triple bond or a hetero atom and combinations thereof with anti-cancer agents.

    摘要翻译： 包含由下式（I）表示的1,4-二氢吡啶衍生物的抗药性肿瘤细胞的药剂：其中R 1为可被取代的芳基; R 2和R 3可以相同或不同，各自为选自烷基，烷氧基羰基，芳氧基羰基，芳烷氧基羰基，氨基羰基，羟基羰基，甲酰基， 和氰基，其各自可以被取代; R4和R5是氢原子或选自低级烷基，羟甲基，氰基，氨基，甲酰基和卤素原子的成员; 并且R 6是选自烷基，芳烷基，烷氧基羰基和芳烷氧基羰基的基团，其各自可以被取代，并且各自的烷基部分也可以含有双键，三键或 杂原子及其与抗癌剂的组合。

    Prophylactic/Therapeutic Agent for Cancer
    5.
    发明申请
    Prophylactic/Therapeutic Agent for Cancer 审中-公开
    预防/治疗癌症治疗剂

    公开(公告)号：US20090202569A1

    公开(公告)日：2009-08-13

    申请号：US12225882

    申请日：2007-04-06

    申请人： Tetsuo Mashima ,  Takashi Tsuruo ,  Hideaki Tojo ,  Hiroyuki Sumi

    发明人： Tetsuo Mashima ,  Takashi Tsuruo ,  Hideaki Tojo ,  Hiroyuki Sumi

    IPC分类号： A61K39/395 ,  C07K16/18 ,  C07H21/02 ,  A61K31/7088 ,  C12N5/06

    CPC分类号： A61K45/06 ,  A61K31/7088 ,  A61K39/395 ,  A61K2300/00

    摘要： The present invention provides a preventative/therapeutic agent for cancer capable of selectively and effectively killing cancer cells. A medicament of the present invention prepared by combining at least one selected from a substance that inhibits the activity of an enzyme belonging to the acyl-CoA synthase family and a substance that inhibits expression of a gene for an enzyme belonging to the acyl-CoA synthase family, with at least one selected from a substance that inhibits the activity of fatty acid synthase and a substance that inhibits expression of a fatty acid synthase gene and the like can be used as a preventative/therapeutic agent for cancer capable of selectively and effectively killing cancer cells.

    摘要翻译： 本发明提供了能够选择性且有效地杀死癌细胞的癌症预防/治疗剂。 通过组合选自抑制属于酰基辅酶A合成酶家族的酶的活性的物质和抑制属于酰基辅酶A合成酶的酶的基因表达的物质中的至少一种而制备的本发明的药物 可以使用选自抑制脂肪酸合酶活性的物质中的至少一种和抑制脂肪酸合酶基因表达的物质等作为能够选择性有效杀死的癌症的预防/治疗剂 癌细胞。

    Agent for enhancing antitumor activity of antitumor agent
    6.
    发明授权
    Agent for enhancing antitumor activity of antitumor agent 失效
    用于增强抗肿瘤剂抗肿瘤活性的药剂

    公开(公告)号：US4628047A

    公开(公告)日：1986-12-09

    申请号：US498639

    申请日：1983-05-27

    申请人： Yoshio Sakurai ,  Takashi Tsuruo

    发明人： Yoshio Sakurai ,  Takashi Tsuruo

    IPC分类号： C07D281/10 ,  A61K31/55 ,  A61K31/554 ,  A61P35/00 ,  A61P43/00 ,  A61K31/70 ,  A61K31/44

    CPC分类号： A61K31/55

    摘要： An agent for enhancing antitumor activity of antitumor agents comprising as the active ingredient diltiazem or a pharmaceutically acceptable acid addition salt thereof, an antitumor composition comprising the diltiazem or an acid addition salt thereof and a conventional antitumor agent, and further a method for treating tumors by administering diltiazem or an acid addition salt thereof together with a conventional antitumor agent in oral or parenteral route to patients suffering from various tumors. Said active diltiazem or a salt thereof is effective for enhancing the antitumor activity of antitumor agents because it can enhance sensitivity of tumor cells to antitumor agents regardless the tumor cells have resistance to the antitumor agents or not.

    摘要翻译： 包含作为活性成分的地尔硫卓或其药学上可接受的酸加成盐的抗肿瘤剂的抗肿瘤活性的药剂，包含地尔硫卓或其酸加成盐的抗肿瘤组合物和常规的抗肿瘤剂，以及进一步的治疗肿瘤的方法 将经口服或肠胃外途径的地尔硫卓或其酸加成盐与常规抗肿瘤药物一起给予患有各种肿瘤的患者。 所述活性地尔硫卓或其盐对于提高抗肿瘤剂的抗肿瘤活性是有效的，因为它可以增强肿瘤细胞对抗肿瘤剂的敏感性，而不管肿瘤细胞对抗肿瘤剂具有抗性。

    Method for judging sensibility to imatinib
    7.
    发明申请
    Method for judging sensibility to imatinib 审中-公开
    判断伊马替尼敏感性的方法

    公开(公告)号：US20060246436A1

    公开(公告)日：2006-11-02

    申请号：US10515051

    申请日：2003-05-21

    申请人： Ryuzo Ohno ,  Takashi Tsuruo ,  Yusuke Nakamura

    发明人： Ryuzo Ohno ,  Takashi Tsuruo ,  Yusuke Nakamura

    IPC分类号： C12Q1/68

    CPC分类号： C07K14/47 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158

    摘要： A method of judging whether a patient is sensitive to imatinib or not, in case where the patient is suffering from a disease such as CML to be treated by administration of imatinib, that is, a method for judging whether the administration of imatinib is effective for the therapy of the disease or not, is disclosed. Amounts of a plurality of genes selected from the group consisting of the specific 77 genes in sample cells separated from body are measured; and the measured amounts are compared with those of responders and non-responders to imatinib or a derivative thereof or a pharmaceutically acceptable salt thereof:

    摘要翻译： 判断患者是否对伊马替尼敏感的方法，在患者患有如待治疗伊马替尼治疗的CML等疾病的情况下，即判断伊马替尼的给药是否有效的方法 公开了该疾病的治疗。 测定从与身体分离的样品细胞中的特异性77个基因中选出的多个基因的量; 并将测量的量与伊马替尼或其衍生物或其药学上可接受的盐的应答者和无应答者的量进行比较：

    Cancer remedy comprising anthranilic acid derivatives as active ingredient
    8.
    发明申请
    Cancer remedy comprising anthranilic acid derivatives as active ingredient 审中-公开
    包括邻氨基苯甲酸衍生物作为活性成分的癌症治疗

    公开(公告)号：US20050027008A1

    公开(公告)日：2005-02-03

    申请号：US10923875

    申请日：2004-08-24

    申请人： Naoki Tsuchiya ,  Takumi Takeyasu ,  Takashi Kawamura ,  Takao Yamori ,  Takashi Tsuruo

    发明人： Naoki Tsuchiya ,  Takumi Takeyasu ,  Takashi Kawamura ,  Takao Yamori ,  Takashi Tsuruo

    IPC分类号： A61K31/167 ,  A61K31/18 ,  A61K31/192 ,  A61K31/235 ,  A61K31/24 ,  A61K31/277 ,  A61K31/41 ,  A61P35/00 ,  C07C235/38 ,  C07D257/04 ,  A61K31/195 ,  A61K31/165

    CPC分类号： C07D257/04 ,  A61K31/167 ,  A61K31/18 ,  A61K31/192 ,  A61K31/235 ,  A61K31/24 ,  A61K31/277 ,  A61K31/41 ,  C07C235/38

    摘要： A cancer remedy comprising a compound represented by the following formula as an active ingredient: wherein, X represents a group represented by either of the following formulae: wherein, R1 and R2 represent each a hydrogen atom, a hydroxy group, a trihalomethyl group, a C1-C12 alkoxy group or alkylthio group, a (substituted) C7-C11 aralkyloxy group or a (substituted) C3-C10 alkenyloxy group; R4 and R5 represent each a hydrogen atom, a halogen atom, a C1-C4 alkyl group or a C1-C4 alkoxy group; A represents —O—, —S—, —S(═O)—, —S(═O)2—, —CH2—, —OCH2—, —SCH2, —C(═O)— or —CH(OR6)—; Y represents a hydrogen atom, a halogen atom, a nitro group, a nitrile group, an amino group, —COOR7, —NHCOR8 or —NHSO2R9−; E represents —C(═O)—, —CR10R11C(═O)—, —CH2CH2C(═O)— or —CH═CHC(═O)—; G represents a hydrogen atom, a hydroxy group, —SO2NH2, —COOR3, —CN or a tetrazol-5-yl group; and Z represents a hydrogen atom, a halogen atom, a nitro group or a methyl group.

    摘要翻译： 包含由下式表示的化合物作为活性成分的癌症治疗剂：其中，X表示由下式表示的基团：其中，R 1和R 2各自表示氢原子，羟基 ，三卤代甲基，C1-C12烷氧基或烷硫基，（取代）C7-C11芳烷氧基或（取代）C3-C10烯氧基; R 4和R 5各自表示氢原子，卤素原子，C 1 -C 4烷基或C 1 -C 4烷氧基; A表示-O - ， - S - ， - S（= O） - ， - S（= O）2 - ， - CH 2 - ， - OCH 2 - ，-SCH 2，-C（= O） - 或-CH <6>） - ; Y表示氢原子，卤素原子，硝基，腈基，氨基，-COOR 7，-NHCOR 8或-NHSO 2 R 9。 E表示-C（= O） - ，-CR 10 R 11（= O） - ， - CH 2 CH 2 C（= O） - 或-CH = CHC（= O） - ; G表示氢原子，羟基，-SO 2 NH 2，-COOR 3，-CN或四唑-5-基; Z表示氢原子，卤素原子，硝基或甲基。

    Novel tetronic acid derivative
    9.
    发明申请
    Novel tetronic acid derivative 失效
    新型四氢酸衍生物

    公开(公告)号：US20050014232A1

    公开(公告)日：2005-01-20

    申请号：US10852766

    申请日：2004-05-21

    申请人： Kazuo Shinya ,  Takashi Tsuruo ,  Akihiro Tomida ,  Hae-Ryong Park

    发明人： Kazuo Shinya ,  Takashi Tsuruo ,  Akihiro Tomida ,  Hae-Ryong Park

    IPC分类号： A61K31/7048 ,  A61P35/00 ,  A61P43/00 ,  C07H17/08 ,  C12P19/62 ,  C12P19/60

    CPC分类号： C07H17/08 ,  A61K31/7048 ,  C12P19/62 ,  C12R1/465

    摘要： The present inventors intended to search for substances that can regulate the expression of a molecular chaperone, GRP78, using the expression of GRP78 as an indicator. As a result, a novel tetronic acid derivative, versipelostatin compound (also known as JL68) shown in formula (I) having the activity of suppressing GRP78 expression was isolated from the metabolite of Streptomyces versipellis strain 4083-SVS6. Versipelostatin can be obtained from the culture supernatant by culturing the above-mentioned Streptomyces versipellis strain 4083-SVS6.

    摘要翻译： 本发明人意图使用GRP78的表达作为指标来搜索可以调节分子伴侣GRP78表达的物质。 结果，从Streptomyces versipellis株4083-SVS6的代谢物中分离出具有抑制GRP78表达活性的式（I）所示的新型tetronic酸衍生物（也称为JL68）。 通过培养上述的链霉菌菌株4083-SVS6可以从培养上清液中获得多糖嵌合抑制素。

    Prophylactic/therapeutic agent for cancer
    10.
    发明申请
    Prophylactic/therapeutic agent for cancer 审中-公开
    癌症预防/治疗剂

    公开(公告)号：US20090155241A1

    公开(公告)日：2009-06-18

    申请号：US11988995

    申请日：2005-07-22

    申请人： Tetsuo Mashima ,  Takashi Tsuruo

    发明人： Tetsuo Mashima ,  Takashi Tsuruo

    IPC分类号： A61K39/395 ,  C07H21/02 ,  C07K16/18 ,  G01N33/53 ,  C12Q1/68 ,  C12Q1/00 ,  A61K31/7088 ,  C12N9/96 ,  C07C245/00

    CPC分类号： G01N33/573 ,  A61K38/00 ,  A61K49/0008 ,  C12N9/93 ,  C12Y602/01003 ,  G01N33/574 ,  G01N2333/91051 ,  G01N2800/52

    摘要： A compound or its salt that inhibits the activity of a protein having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1; a compound or its salt that inhibits the expression of a gene for the protein; an antisense polynucleotide comprising a nucleotide sequence complementary or substantially complementary to the nucleotide sequence of a polynucleotide encoding the protein or a partial peptide thereof or a part of the nucleotide sequence; an antibody against the protein; etc. are useful as preventive/therapeutic agents for cancer, apoptosis promoters for cancer cells, or the like.

    摘要翻译： 抑制与SEQ ID NO：1所示的氨基酸序列具有相同或基本相同的氨基酸序列的蛋白质的活性的化合物或其盐; 抑制蛋白质基因表达的化合物或其盐; 反义多核苷酸，其包含与编码所述蛋白质或其部分肽或所述核苷酸序列的一部分的多核苷酸的核苷酸序列互补或基本互补的核苷酸序列; 抗蛋白的抗体; 等可用作癌症的预防/治疗剂，癌细胞的凋亡启动子等。