7-acylamino-3-heteroarylthio-3-cephem carboxylic acid antibiotics and prodrugs thereof
    84.
    发明授权
    7-acylamino-3-heteroarylthio-3-cephem carboxylic acid antibiotics and prodrugs thereof 失效
    7-酰基氨基-3-杂芳硫基-3-头孢烯羧酸抗生素及其前体药物

    公开(公告)号:US06723716B1

    公开(公告)日:2004-04-20

    申请号:US09668722

    申请日:2000-09-21

    IPC分类号: C07D50159

    摘要: The present invention relates to a cephem prodrug having formula III or formula IV: or a pharmaceutically acceptable salt thereof, wherein R′1 is selected from the group consisting of hydrogen and —C(O)CH(NH2)CH3 and R′2 is selected from the group consisting of hydrogen and an acyl group that is cleaved by an enzyme found in mammals, with the proviso that, when either R′1 or R′2 is hydrogen, the other is not. A, B, L, G, E, and J are each independently nitrogen or carbon such that the respective rings are selected from the group consisting of provided that the group —CH2—S—CH2CH2NHR′2 is attached only to a carbon atom of said heterocyclic group, and Q is selected from the group consisting of nitrogen and —CX, wherein X is selected from the group consisting of hydrogen and chlorine.

    摘要翻译: 本发明涉及具有式III或式IV的头孢烯前药或其药学上可接受的盐,其中R'1选自氢和-C(O)CH(NH 2)CH 3和R' <2>选自氢和由哺乳动物中发现的酶切割的酰基,条件是当R'1或R'2都是氢时,另一个不是 。 A,B,L,G,E和J各自独立地为氮或碳,使得各个环选自提供基团-CH 2 -S-CH 2 CH 2 NHR'2仅与碳原子连接 的所述杂环基,Q选自氮和-CX,其中X选自氢和氯。