公开(公告)号：US20080221046A1

公开(公告)日：2008-09-11

申请号：US11813873

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Dubravko Jelic ,  Sulejman Alihodzic ,  Vanja Vela ,  Zorica Marusic-Istuk ,  Vesna Erakovic ,  Berislav Bosnjak ,  Boska Hrvacic ,  Marija Tomaskovic ,  Vanesa Munic ,  Vanesa Ivetic ,  Antun Hutinec ,  Goran Kragol ,  Marija Leljak

发明人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Dubravko Jelic ,  Sulejman Alihodzic ,  Vanja Vela ,  Zorica Marusic-Istuk ,  Vesna Erakovic ,  Berislav Bosnjak ,  Boska Hrvacic ,  Marija Tomaskovic ,  Vanesa Munic ,  Vanesa Ivetic ,  Antun Hutinec ,  Goran Kragol ,  Marija Leljak

IPC分类号： A61K31/7048 ,  C07H17/00 ,  C12N5/06 ,  A61P29/00 ,  A61P11/06

CPC分类号： C07H17/00 ,  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 substituted at the 4″ 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-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，本发明涉及在4“取代的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在治疗中的活性和用途 特别是与过量分泌TNF-α，IL-1，IL-8，IL-2或IL-5相关的那些疾病; 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。