公开(公告)号：US20080255060A1

公开(公告)日：2008-10-16

申请号：US11568562

申请日：2005-05-02

申请人： Sulejman Alihodzic ,  Stjepan Mutak ,  Drazen Pavlovic ,  Ivana Palej ,  Vlado Stimac ,  Samra Kapic ,  Adrijana Vinter ,  Maja Matanovic Skugor

发明人： Sulejman Alihodzic ,  Stjepan Mutak ,  Drazen Pavlovic ,  Ivana Palej ,  Vlado Stimac ,  Samra Kapic ,  Adrijana Vinter ,  Maja Matanovic Skugor

IPC分类号： A61K31/7048 ,  C07H17/08 ,  A61P31/00

CPC分类号： C07H17/08

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。

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.