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    Production of azacarbazoles
    2.
    发明授权
    Production of azacarbazoles 失效
    生产AZACARBAZOLES

    公开(公告)号：US3560361A

    公开(公告)日：1971-02-02

    申请号：US3560361D

    申请日：1969-03-28

    申请人： GLAXO LAB LTD

    发明人： CLARK VICTOR MALCOLM ,  GREGORY GORDON IAN ,  COCKER JOHN DEREK

    IPC分类号： C07D213/74 ,  C07D471/04 ,  C07D471/14 ,  B01J1/10

    CPC分类号： C07D213/74 ,  C07D471/04 ,  C07D471/14

    摘要： AZACARBAZOLES ARE PREPARED BY THE PHOTOCYCLISATION OF A SECONDARY OR TERTIARY DIARYL AMINE IN WHICH EACH OF THE TWO ARYL GROUPS IS A MONOCYCLIC SIX MEMBERED RING ATTACHED TO THE AMINE NITROGEN ATOM BY A NUCLEAR CARBON ATOM AND AT LEAST ONE OF THE ARYL GROUPS CONTAINS AT LEAST ONE NITROGEN ATOM IN THE NUCLEUS. A HALOGEN ATOM MAY BE SUBSTITUTED IN THE AZACARBAZOLE SO FORMED BY REACTION WITH A PERACID TO FORM AN N-OXIDE DERIVATIBE THEREOF WHICH IS SUBSEQUENTLY REACTED WITH A PHOSPHORUS OXYHALIDE TO INTRODUCE THE HALOGEN ATOM WITH ELIMINATION OF THE N-ATTACHED OXYGEN. THE HALOGEN SUBSTITUTED AZACARBAZOLE MAY BE REACTED WITH A NUCLEPHILE TO REPLACE THE HALOGEN SUBSTITUENT WITH THE RESIDUE OF THE NUCLEOPHILE. THE AZACARBZOLES HAVE ANTIVIRAL ACTIVITY AND/OR MAY BE EMPLOYED AS INTERMEDIATES FOR THE PRODUCTION OF DERIVATIVES HAVING ANTIVIRAL PROPERTIES AND THE 1,6-DIAZOCARBAZOLES AND 1,3,8-TRIAZACARBAZOLES ARE NEW COMPOUNDS.

    Penicillin antibiotics
    3.
    发明授权
    Penicillin antibiotics 失效

    公开(公告)号：US3926957A

    公开(公告)日：1975-12-16

    申请号：US46678074

    申请日：1974-05-03

    申请人： GLAXO LAB LTD

    发明人： GREGSON MICHAEL ,  COOK MARTIN CHRISTOPHER ,  GREGORY GORDON IAN

    IPC分类号： C07C259/02 ,  C07D307/54 ,  C07D333/24 ,  C07D499/70 ,  C07D499/44

    CPC分类号： C07D307/54 ,  C07C259/02 ,  C07D333/24

    摘要： WHERE R is a hydrogen atom or an organic group and Ra is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to Beta -lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

    The invention provides novel antibiotic compounds which are 6 Beta -acylamidopenam-3-carboxylic acids and non-toxic derivatives thereof, characterized in that the acylamido group has the structure