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26 条记录 (耗时 0.027 秒)

    Decladinosyl-macrolides with anti-inflammatory activity
    1.
    发明授权
    Decladinosyl-macrolides with anti-inflammatory activity 失效
    具有抗炎活性的宣称大肠杆菌素

    公开(公告)号：US07910559B2

    公开(公告)日：2011-03-22

    申请号：US11813876

    申请日：2006-01-13

    申请人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

    发明人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

    摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地说，本发明涉及在C-3位上缺少被克拉替糖糖化的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用途 特别是与过量分泌TNF-α，IL-1，IL-6，IL-8，IL-2或IL-5相关的那些疾病的治疗中， 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

    New 3-decladinosyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 9a, 11-cyclic carbamates
    10.
    发明申请
    New 3-decladinosyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 9a, 11-cyclic carbamates 失效

    公开(公告)号：US20060154878A1

    公开(公告)日：2006-07-13

    申请号：US10527940

    申请日：2003-09-26

    申请人： Andrea Fajdetic ,  Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Stjepan Mutak

    发明人： Andrea Fajdetic ,  Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Stjepan Mutak

    IPC分类号： A61K31/7048 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.