Modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity, and use thereof
申请人:Duan Jingwu
公开号:US20070129400A1
公开(公告)日:2007-06-07
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 an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR
1
or C(R
4
)(R
4a
); K is selected from NR
2
or C(R
5
)(R
5a
); L is selected from NR
3
or C(R
6
)(R
6a
); and A, X, Y, R
1
, R
2
, R
3
, R
4
, R
4a
, R
5
, R
5a
, R
6
, R
6a
, R
8
, R
10
, R
11
, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
提供了非甾体化合物,可用于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,包括肥胖症、糖尿病、炎症和免疫性疾病,其结构为式(I)或其对映异构体、顺异构体、药学上可接受的盐或其水合物,其中J从NR1或C(R4)(R4a)中选择;K从NR2或C(R5)(R5a)中选择;L从NR3或C(R6)(R6a)中选择;A、X、Y、R1、R2、R3、R4、R4a、R5、R5a、R6、R6a、R8、R10、R11和n在此定义。还提供了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,包括所述化合物。