发明授权
US08198311B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
有权
糖皮质激素受体,AP-1和/或NF-κB活性的调节剂及其用途
- 专利标题: Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
- 专利标题(中): 糖皮质激素受体,AP-1和/或NF-κB活性的调节剂及其用途
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申请号: US12513232申请日: 2007-10-31
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公开(公告)号: US08198311B2公开(公告)日: 2012-06-12
- 发明人: James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
- 申请人: James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
- 申请人地址: US NJ Princeton
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 当前专利权人地址: US NJ Princeton
- 代理商 Burton Rodney
- 国际申请: PCT/US2007/083085 WO 20071031
- 国际公布: WO2008/057857 WO 20080515
- 主分类号: A61K31/416
- IPC分类号: A61K31/416 ; C07D231/56
摘要:
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 inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, provided that the E-F-G containing heterocyclic ring formed does not contain a S—S or S—O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.
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