申请人:GlaxoSmithKline istrazivacki centar Zagreb d.o.o.
公开号:EP2196469A1
公开(公告)日:2010-06-16
The present invention relates to new compounds represented by Formula I:
wherein M represents a macrolide subunit of the substructure VIII:
L represents the chain of the substructure IX or XIII:
-X1-(CH2)m-Q-(CH2)n-X2- IX
-X1-(CH2)m-V-(CH2)p-Q-(CH2)n-X1- XIII
Z represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity;
The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.
本发明涉及由式 I 表示的新化合物:
其中 M 代表子结构 VIII 的大环内酯亚基:
L 代表子结构 IX 或 XIII 的链:
-X1-(CH2)m-Q-(CH2)n-X2- IX
-X1-(CH2)m-V-(CH2)p-Q-(CH2)n-X1- XIII
Z 代表从具有抗炎活性的类固醇或非类固醇(NSAID)药物中提取的类固醇或非类固醇亚基;
本发明还涉及此类制备的化合物的药学上可接受的盐和溶液、制备它们的工艺和中间体,以及在治疗人类和动物的炎症性疾病和病症中的改进治疗作用和用途。