Taxoids, their preparation and pharmaceutical compositions containing
them
    1.
    发明授权
    Taxoids, their preparation and pharmaceutical compositions containing them 有权
    紫杉烷类,它们的制备方法和含有它们的药物组合物

    公开(公告)号:US6040466A

    公开(公告)日:2000-03-21

    申请号:US271300

    申请日:1999-03-17

    IPC分类号: C07D305/14

    CPC分类号: C07D305/14

    摘要: New taxoids and methods of preparing new taxoids of general formula (I): ##STR1## in which: R.sub.4 represents an alkanoyloxy radical in which the alkanoyl portion contains 2 to 6 carbon atoms in an unbranched or branched chain, this radical unsubstituted or substituted with one or more halogen atoms, an alkoxy radical containing 1 to 4 carbon atoms, or alternatively R.sub.4 represents a cycloalkanoyloxy radical in which the cycloalkanoyl portion contains 4 to 8 carbon atoms, or alternatively R.sub.4 represents a benzoyloxy radical;R.sub.5 represents an alkoxy radical containing 1 to 4 carbon atoms, substituted by an alkylthio radical containing 1 to 4 carbon atoms; andZ represents a hydrogen atom or a radical of general formula: ##STR2## wherein such new taxoids display noteworthy anti-tumor and anti-leukemic properties.

    摘要翻译: 新的紫杉烷类和通式(I)的新紫杉烷类的制备方法:其中:R4表示烷酰氧基,其中链烷酰基部分在无支链或支链上含有2-6个碳原子,该未取代的基团或被一个或多个 卤原子,含有1至4个碳原子的烷氧基,或者R4表示环烷酰氧基,其中环烷酰基部分含有4至8个碳原子,或者R4表示苯并氧基; R5代表含有1至4个碳原子的烷氧基,被含有1至4个碳原子的烷硫基取代; Z表示氢原子或通式的基团:其中这种新的紫杉醇显示出显着的抗肿瘤和抗白血病性质。

    Transgenic animals overexpressing MDM2
    2.
    发明授权
    Transgenic animals overexpressing MDM2 失效
    转基因动物过表达MDM2

    公开(公告)号:US6028245A

    公开(公告)日:2000-02-22

    申请号:US104497

    申请日:1998-06-25

    IPC分类号: C07K14/47 C12N15/85 C12N15/00

    摘要: The present invention relates to transgenic, non-human animals overexpressing a MDM2 gene. These animals model MDM2 over-expression associated with human tumors, display a major phenotype characterized by the severe skin disorder ichthyosis, and are useful for identifying compounds for the treatment of human disease. Therefore, the invention also relates to methods of using the animals for identifying compounds effective for the treatment of diseases of the skin and respiratory tract, and to the compounds themselves.

    摘要翻译: 本发明涉及过表达MDM2基因的转基因非人动物。 这些动物模型与人肿瘤相关的MDM2过度表达,显示以严重皮肤病鱼鳞病为特征的主要表型,并且可用于鉴定用于治疗人类疾病的化合物。 因此,本发明还涉及使用动物鉴别有效治疗皮肤和呼吸道疾病的化合物的方法以及化合物本身。

    Derivatives of 2-azabicyclo�2.2.1! heptane, their preparation and their
application
    6.
    发明授权
    Derivatives of 2-azabicyclo�2.2.1! heptane, their preparation and their application 失效
    2-氮杂双环[2.2.1]庚烷的衍生物及其制备及应用

    公开(公告)号:US5912365A

    公开(公告)日:1999-06-15

    申请号:US914484

    申请日:1997-08-19

    CPC分类号: C07D209/02 C07D209/52

    摘要: Novel derivatives of 1R- or 1S-2-azabicyclo�2.2.1!heptane with the general formula (I) or (I'), preparation and their application. ##STR1## In the general formulas (I) and (I'), R represents a hydrogen atom or a group with the formula ##STR2## respectively, in which R.sub.1 represents an alkyl group containing 1-4 carbon atoms and Ar represents an optionally substituted phenyl or a- or b-naphthyl group.

    摘要翻译: 具有通式(I)或(I')的1R-或1S-2-氮杂双环[2.2.1]庚烷的新衍生物,其制备及其应用。 在通式(I)和(I')中,R表示氢原子或分别具有式的基团,其中R 1表示含有1-4个碳原子的烷基,Ar表示任选取代的苯基或 - b-萘基。