Compounds
    5.
    发明申请
    Compounds 审中-公开

    公开(公告)号:US20110281812A1

    公开(公告)日:2011-11-17

    申请号:US13146233

    申请日:2010-01-28

    CPC分类号: C07H17/00

    摘要: 2′-O-substituted 14- or 15-membered azalide macrolides of Formula (I) wherein R6 represents (i) —C1-8alkyl, unsubstituted or substituted at the terminal carbon atom by a group selected from hydroxy, —C1-3alkoxy and —C(O)OC1-3alkyl, or when —C1-8alkyl is branched, substitution can alternatively be by a hydroxyl group at each of two terminal carbon atoms, (ii) —CH(NH2)C1-4alkyl, wherein the —C1-4alkyl group may be optionally interrupted by a heteroatom selected from O, S and N, (iii) —CH2N(R7)(R8), wherein R7 and R8 each independently represent H or —C1-3alkyl provided that R7 and R8 cannot both simultaneously represent H, (iv) a 4-6-membered heterocyclic ring containing up to 2 heteroatoms independently selected from O, S and N, wherein the heterocyclic ring is unsubstituted or substituted by —C1-3alkyl, (v) 5-6 membered heteroaromatic ring, unsubstituted or substituted by one to three groups independently selected from halo, hydroxyl, —C1-3alkyl, —C1-3alkoxy, —CF3, —OCF3 and —NH2, (vi) —CH(NH2)CH2-aryl wherein the aryl group may be unsubstituted or substituted by one or two substituents independently selected from —C1-3alkyl, —C1-3alkoxy and hydroxyl, (vii) —C3-7cycloalkyl, or (viii) phenyl unsubstituted or substituted by one or two groups independently selected from halo, hydroxyl, —C1-3alkyl, —C1-3alkoxy, —CF3, —OCF3 and —NH2, or salts thereof, useful in the treatment of neutrophil dominated inflammatory diseases, especially in the treatment of neutrophil dominated inflammatory diseases resulting from neutrophilic infiltration and/or diseases associated with altered cellular functionality of neutrophils, to methods for their preparation, to their use as therapeutic agents, and to salts thereof.

    Novel 14 and 15 membered ring compounds
    7.
    发明申请
    Novel 14 and 15 membered ring compounds 审中-公开
    新型14和15元环化合物

    公开(公告)号:US20070141276A1

    公开(公告)日:2007-06-21

    申请号:US10556706

    申请日:2004-05-11

    IPC分类号: B44C5/00

    CPC分类号: C07H17/08 Y10T428/24157

    摘要: The present invention relates to 14- or 15-membered macrolides substituted at the 4″ position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.

    摘要翻译: 本发明涉及在式(I)的4“位取代的14-或15-元大环内酯及其药学上可接受的衍生物,其制备方法及其在治疗或预防全身或局部微生物感染中的用途 人或动物体。