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    Decladinosyl-macrolides with anti-inflammatory activity
    3.
    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。

    Compounds
    7.
    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

    申请人： Sulejman Alihodzic ,  Antun Hutinec ,  Sanja Kostrun ,  Maja Matanovic Skugor ,  Ivana Palej Jakopovic

    发明人： Sulejman Alihodzic ,  Antun Hutinec ,  Sanja Kostrun ,  Maja Matanovic Skugor ,  Ivana Palej Jakopovic

    IPC分类号： A61K31/7048 ,  A61P11/00 ,  A61P11/08 ,  A61P17/00 ,  A61P19/02 ,  A61P1/00 ,  A61P9/10 ,  A61P29/00 ,  C07H17/08 ,  A61P11/06

    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.