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258 条记录 (耗时 0.029 秒)

    11Beta-long-chain-substituted 19-nor-17alpha-pregna-1,3,5(10)-trien-17beta-ols with a 21,16alpha-lactone ring
    82.
    发明申请
    11Beta-long-chain-substituted 19-nor-17alpha-pregna-1,3,5(10)-trien-17beta-ols with a 21,16alpha-lactone ring 失效
    具有21,16α-内酯环的11β-长链取代的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-

    公开(公告)号：US20030229059A1

    公开(公告)日：2003-12-11

    申请号：US10397854

    申请日：2003-03-27

    申请人： Schering AG

    发明人： Gerd Mueller ,  Jens Hoffmann ,  Karl-Heinrich Fritzemeier ,  Alexander Hillisch

    IPC分类号： A61K031/585 ,  C07J017/00

    CPC分类号： C07J17/00

    摘要： This invention relates to new 19-nor-17null-pregna-1,3,5(10)-trien-17null-ols with a 21,16null-lactone ring with a long-chain substituent in 11null-position of general formula II 1 in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

    摘要翻译： 本发明涉及具有21,16α-内酯环的新的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-环，其通式II在11b位具有长链取代基 其中R 11表示具有6至17个碳原子的直链烷基，R 3和R 13具有在说明书中更详细说明的含义。 化合物以组织选择性的方式作为纯抗雌激素起作用，并且由于这些性质而适用于制药。

    Histone deacetylase inhibitor and use thereof
    83.
    发明申请
    Histone deacetylase inhibitor and use thereof 审中-公开
    组蛋白脱乙酰酶抑制剂及其用途

    公开(公告)号：US20030216345A1

    公开(公告)日：2003-11-20

    申请号：US10438075

    申请日：2003-05-15

    申请人： Schering AG

    发明人： Osamu Nakanishi ,  Takayuki Tatamiya

    IPC分类号： A61K048/00 ,  C07H021/04

    CPC分类号： C12N15/1137 ,  A61K38/00 ,  C12N9/16 ,  C12N2310/315 ,  G01N2333/4703 ,  G01N2510/00

    摘要： To provide a novel apoptosis inducer, and a method of screening an apoptosis inducer. For example, an apoptosis inducer comprising inhibiting HDAC6 such as an antisense oligonucleotide to the gene of histone deacetylase 6 (HDAC6), and anti-cancer agent comprising this apoptosis inducer, and the present invention also provides a method of screening an apoptosis inducer that inhibits HDAC6, and more specifically a method of screening an apoptosis inducer said method comprising the steps of (1) determining whether or not a test substance inhibits histone deacetylase 6 (HDAC6) by using deacetylation of an acetylated substance that can be a substrate for histone deacetylase 6 (HDAC6) or decrease in the expression of histone deacetylase 6 (HDAC6) as an index; and (2) confirming, when inhibition is present, whether it induces apoptosis of the cell in vitro and/or in vivo.

    摘要翻译： 提供新的细胞凋亡诱导剂，以及筛选细胞凋亡诱导剂的方法。 例如，包含抑制HDAC6如组蛋白脱乙酰酶6（HDAC6）基因的反义寡核苷酸的细胞凋亡诱导剂和包含该凋亡诱导剂的抗癌剂，本发明还提供一种筛选抑制 HDAC6，更具体地是筛选凋亡诱导剂的方法，所述方法包括以下步骤：（1）通过使用可以作为组蛋白脱乙酰酶底物的乙酰化物质的脱乙酰化来确定测试物质是否抑制组蛋白脱乙酰酶6（HDAC6） 6（HDAC6）或组蛋白脱乙酰酶6（HDAC6）表达的降低作为指标; 和（2）当存在抑制时确认其是否在体外和/或体内诱导细胞凋亡。

    Near infrared fluorescent contrast agent and fluorescence imaging
    85.
    发明申请
    Near infrared fluorescent contrast agent and fluorescence imaging 审中-公开

    公开(公告)号：US20030180221A1

    公开(公告)日：2003-09-25

    申请号：US10324010

    申请日：2002-12-20

    申请人： Schering AG

    发明人： Naoto Miwa ,  Michihito Inagaki ,  Hiroaki Eguchi ,  Masafumi Okumura ,  Yoshio Inagaki ,  Toru Harada

    IPC分类号： A61K049/00 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02 ,  C07D41/02

    CPC分类号： A61K49/0021 ,  A61K49/0032

    摘要： A near infrared fluorescent contrast agent comprising a compound having three or more sulfonic acid groups in a molecule, and a method of fluorescence imaging comprising introducing the near infrared fluorescent contrast agent of the present invention into a living body, exposing the body to an excitation light, and detecting near infrared fluorescence from the contrast agent. The near infrared fluorescent contrast agent of the present invention is excited by an excitation light and emits near infrared fluorescence. This infrared fluorescence is superior in transmission through biological tissues. Thus, detection of lesions in the deep part of a living body has been made possible. In addition, the inventive contrast agent is superior in water solubility and low toxic, and therefore, it can be used safely.