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    • 6. 发明申请
    • Compounds
    • US20110281812A1
    • 2011-11-17
    • US13146233
    • 2010-01-28
    • Sulejman AlihodzicAntun HutinecSanja KostrunMaja Matanovic SkugorIvana Palej Jakopovic
    • Sulejman AlihodzicAntun HutinecSanja KostrunMaja Matanovic SkugorIvana Palej Jakopovic
    • A61K31/7048A61P11/00A61P11/08A61P17/00A61P19/02A61P1/00A61P9/10A61P29/00C07H17/08A61P11/06
    • C07H17/00
    • 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.