MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
申请人:Dhar T.G. Murali
公开号:US20100113532A1
公开(公告)日:2010-05-06
A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II):
including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C
2-6
alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, R
a
, R
b
, R
c
and R
d
are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
提供了一类新型非甾体化合物,其在治疗与糖皮质激素受体、AP-1和/或NF-κB活性调节相关的疾病中有用,包括肥胖症、糖尿病、炎症和免疫性疾病,其结构为公式(I)或(II):包括其立体异构体、互变异构体、前药或其药学上可接受的盐,其中Q从N、O和S中选择;Y为芳基或杂环芳基;Z为H、C2-6烷基、环烷基、杂环烷基、芳基、杂环芳基、卤素或烷氧基;A、B、R、Ra、Rb、Rc和Rd在此定义。还提供了包含该化合物的制药组合物和治疗肥胖症、糖尿病和炎症或免疫相关疾病的方法。