发明申请
US20090075995A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
有权
GLUCOCORTICOID受体的调节剂,AP-1和/或NF-kB活性及其用途
- 专利标题: MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
- 专利标题(中): GLUCOCORTICOID受体的调节剂,AP-1和/或NF-kB活性及其用途
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申请号: US11835438申请日: 2007-08-08
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公开(公告)号: US20090075995A1公开(公告)日: 2009-03-19
- 发明人: David S. Weinstein , Ping Chen , T.G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
- 申请人: David S. Weinstein , Ping Chen , T.G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; A61K31/436 ; C07D491/052 ; A61P31/12 ; A61K31/427 ; C07D417/12
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, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
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