申请人:Culic Ognjen
公开号:US20080221046A1
公开(公告)日:2008-09-11
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.
本发明涉及具有抗炎活性的新型半合成大环内酯类化合物。更具体地说,该发明涉及在4″位置取代的14-和15-环大环内酯类化合物,及其药学上可接受的衍生物,用于其制备的工艺和中间体,含有它们的制剂,以及它们在治疗人类和动物的炎症性疾病和症状中的活性和用途,特别是那些与过度分泌TNF-α、IL-1、IL-8、IL-2或IL-5有关的疾病;和/或抑制过度淋巴细胞增殖;和/或过度粒细胞脱颗粒的抑制剂。