Camptothecin derivatives
    1.
    发明授权
    Camptothecin derivatives 有权
    喜树碱衍生物

    公开(公告)号:US06310210B1

    公开(公告)日:2001-10-30

    申请号:US09530828

    申请日:2000-05-03

    IPC分类号: C07D47104

    CPC分类号: C07D471/14

    摘要: The present invention relates to new camptothecin derivatives shown by the below formula, which are water-soluble and excellent in an anti-tumor activity, and to salts thereof. In the formula, R1 represents a hydrogen atom or an alkyl group with 1-6 carbon atoms, R2 represents identically or differently 0-4 alkyl groups with 1-6 carbon atoms, a halogen atom, an alkoxyl or hydroxyl group, R3 represents a lower alkylamino, di-lower alkylamino, arylamino, cyclicamino or lower alkoxyl group, and salts thereof.

    摘要翻译: 本发明涉及由下式表示的新的喜树碱衍生物,它是水溶性的,抗肿瘤活性优异的盐及其盐。式中R1表示氢原子或1-6位烷基 碳原子,R2表示相同或不同的具有1-6个碳原子的0-4个烷基,卤素原子,烷氧基或羟基,R3表示低级烷基氨基,二低级烷基氨基,芳基氨基,环氨基或低级烷氧基, 的盐。

    Process for producing camptothecin
    2.
    发明授权
    Process for producing camptothecin 失效
    喜树碱的制备方法

    公开(公告)号:US06743918B2

    公开(公告)日:2004-06-01

    申请号:US10239113

    申请日:2002-11-25

    IPC分类号: C07D49112

    CPC分类号: C07D491/22 A61K31/475

    摘要: Problem: A large scale production of camptothecin, which is a starting compound of irinotecan hydrochloride and various camptothecin derivatives, at a low cost and with ease. Solution: A process for preparing camptothecin, characterized in that it comprises the following steps (a) and (b); (a) the step to hydrolyze 9-methoxycamptothecin or a natural material containing 9-methoxycamptothecin; (b) the step to convert 9-hydroxycamptothecin obtained in the step (a) into camptothecin by 9-O—perfluoro-lower-alkylsulfonylation or 9-O—phenyltetrazolylation, followed by hydrogenolysis.

    摘要翻译: 问题:大量生产喜树碱,它是伊立替康盐酸盐和各种喜树碱衍生物的起始化合物,成本低,易于使用。溶液:一种制备喜树碱的方法,其特征在于它包括以下步骤(a)和 (b);(a)水解9-甲氧基喜树碱或含有9-甲氧基喜树碱的天然物质的步骤;(b)将步骤(a)中得到的9-羟基喜树碱通过9-O-全氟低级 - 烷基磺酰化或9-O-苯基四唑化,然后氢解。

    Taxane derivatives
    4.
    发明授权
    Taxane derivatives 失效
    紫杉烷衍生物

    公开(公告)号:US06268381B1

    公开(公告)日:2001-07-31

    申请号:US09581908

    申请日:2000-06-19

    IPC分类号: A61K31445

    摘要: The present invention relates to taxane derivatives each represented by the following formula (1): [wherein, A1 represents a group (in which R1 represents H or a (substituted) alkyl group) or a group (in which R2 represents an amino group, a mono- or di-alkylamino group, a piperidino group, a pyrrolidino group or a morpholino group), X represents H, an alkoxycarbonyl group or a benzoyl group, Y represents H or a trialkylsilyl group, A2 represents a furyl group, an alkylfuryl group, an alkyl group or a fluorophenyl group, Ac represents an acetyl group, and Bz represents a benzoyl group] or salts thereof; and drugs containing the same as an active ingredient. These compounds have excellent water solubility and antitumor activity.

    摘要翻译: 本发明涉及各种由下式(1)表示的紫杉烷衍生物:[其中,A1表示基团(其中R1表示H或(取代的(alkyl))烷基)或基团(其中R2表示氨基, 一或二烷基氨基,哌啶子基,吡咯烷子基或吗啉代基),X表示H,烷氧基羰基或苯甲酰基,Y表示H或三烷基甲硅烷基,A2表示呋喃基,烷基 基团,烷基或氟苯基,Ac表示乙酰基,Bz表示苯甲酰基]或其盐; 和含有相同活性成分的药物。这些化合物具有优异的水溶性和抗肿瘤活性。

    Structure of electromagnetic relay
    9.
    发明授权
    Structure of electromagnetic relay 失效
    电磁继电器结构

    公开(公告)号:US5903200A

    公开(公告)日:1999-05-11

    申请号:US787103

    申请日:1997-01-22

    摘要: An electromagnetic relay in which an iron core 2 is fixed to a yoke 3, and one end of the yoke 3 is fixed by press-fitting to a base 4. The base 4 is formed with a yoke-receiving groove 4b into which tongue pieces 3e, 3e at one end of the yoke 3 are press-fitted, and a cutout groove 4c into which a head portion 2c of the iron core 2 is received. The yoke 3 is formed with a seal projection 3f disposed by insertion in an opening end of a cutout groove 4c of the base 4. This construction of the electromagnetic relay eliminates poor operation by preventing metal chips produced during assembly from adhering to electrical contacts of the relay.

    摘要翻译: 一种电磁继电器,其中铁芯2固定到磁轭3,并且磁轭3的一端通过压配固定在基座4上。基座4形成有轭接收槽4b,舌片 3e,3e在轭3的一端被压配合,以及切口槽4c,铁芯2的头部2c被容纳在该切口槽4c中。 轭3形成有通过插入基座4的切口槽4c的开口端而设置的密封突起3f。电磁继电器的这种结构通过防止组装期间产生的金属屑粘附到 中继。