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公开(公告)号:US20110262368A1
公开(公告)日:2011-10-27
申请号:US12736064
申请日:2008-12-18
申请人: John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Philippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
发明人: John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Philippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
IPC分类号: A61K31/58 , C07J31/00 , A61K31/573 , A61P25/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P11/06 , A61P11/00 , A61P17/00 , A61P17/06 , A61P17/04 , A61P31/12 , A61P31/00 , A61P11/02 , A61P37/06 , A61P37/08 , A61P11/10 , C07J43/00
CPC分类号: C07J43/003 , C07J31/006 , C07J71/0031
摘要: The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
摘要翻译: 本发明提供了具有通式(Ⅶ)的所述化合物和所述11-酮类似物的式(Ⅶ)化合物及其11-酮类似物及其可药用盐,溶剂合物,酯,前体药物,互变异构体和异构体, :其中L,R 1,R 2,R 3,R 4和R 5彼此独立地选择并如本文所定义。 还提供了药物组合物,制备方法和使用这些化合物在治疗和预防广泛范围的免疫,自身免疫和炎性疾病和病症中的方法。 本发明的新型化合物具有有用的药理活性,同时具有意想不到的全身活性。 因此,本发明的化合物代表具有差的副作用特征的已知糖皮质激素的更安全的替代方案。