2 .beta.-substituted thiomethylpenicillin derivatives and their
preparation and use
    31.
    发明授权
    2 .beta.-substituted thiomethylpenicillin derivatives and their preparation and use 失效
    2β-取代的硫代甲基青霉素衍生物及其制备和用途

    公开(公告)号:US4861768A

    公开(公告)日:1989-08-29

    申请号:US16114

    申请日:1987-02-18

    IPC分类号: C07D499/00 C07D499/86

    CPC分类号: C07D499/00

    摘要: Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.

    摘要翻译: 公开了下式的青霉素衍生物:其中n是0,1或2的整数; Y是氰基,低级酰基,单 - 或二 - 低级烷硫基氨基甲酰基,其中R1是氢原子,低级烷基,苯基,基 - (CH2)m-OR2或 - (CH 2)m COOR 2(m为1〜6的整数,R2为氢原子或青霉素衍生物通常使用的青霉素羧酸酯形成基)或被选自上述的至少一种的苯基 由低级烷基,卤素原子和低级烷氧基组成; 和R是氢原子或青霉素羧酸酯形成基团或其盐。 它们可用作β-内酰胺酶抑制剂。

    Process for the preparation of glyoxal-2-oximes
    35.
    发明授权
    Process for the preparation of glyoxal-2-oximes 失效
    乙二醛2-肟的制备方法

    公开(公告)号:US4224450A

    公开(公告)日:1980-09-23

    申请号:US67888

    申请日:1979-08-20

    CPC分类号: C07D261/08

    摘要: Novel derivatives of glyoxal-2-oxim represented by the chemical formula ##STR1## wherein R is hydrogen or a lower alkyl or phenyl group, are provided in accordance with the present invention. These derivatives are prepared by reacting the corresponding isoxazole-5-carbaldehyde with nitromethane in the presence of a metal alkoxide, or the corresponding 5-acetylisoxazole with a nitrite. They have anti-inflammatory and/or analgesic activities.

    摘要翻译: 根据本发明提供了由化学式 [I]表示的乙二醛-2-肟基的新型衍生物,其中R是氢或低级烷基或苯基。 这些衍生物通过在金属醇盐或相应的5-乙酰异恶唑与亚硝酸盐存在下使相应的异恶唑-5-甲醛与硝基甲烷反应来制备。 它们具有抗炎和/或止痛活性。

    Glyoxal-2-oxim derivatives and a process for relieving pain/or
inflammation therewith
    36.
    发明授权
    Glyoxal-2-oxim derivatives and a process for relieving pain/or inflammation therewith 失效
    乙二醛-2-肟衍生物及其缓解疼痛或炎症的方法

    公开(公告)号:US4212874A

    公开(公告)日:1980-07-15

    申请号:US16821

    申请日:1979-03-02

    CPC分类号: C07D261/08

    摘要: Novel derivatives of glyoxal-2-oxim represented by the chemical formula ##STR1## wherein R is hydrogen or a lower alkyl or phenyl group, are provided in accordance with the present invention. These derivatives are prepared by reacting the corresponding isoxazole-5-carbaldehyde with nitromethane in the presence of a metal alkoxide, or the corresponding 5-acetylisoxazole with a nitrite. They have anti-inflammatory and/or analgesic activities.

    摘要翻译: 根据本发明提供了由化学式 [I]表示的乙二醛-2-肟基的新型衍生物,其中R是氢或低级烷基或苯基。 这些衍生物通过在金属醇盐或相应的5-乙酰异恶唑与亚硝酸盐存在下使相应的异恶唑-5-甲醛与硝基甲烷反应来制备。 它们具有抗炎和/或止痛活性。