发明申请
US20110002952A1 FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF
有权
GLUCOCORTICOID受体,AP-1和/或NF-κB活性的融合血管调节剂及其用途
- 专利标题: FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF
- 专利标题(中): GLUCOCORTICOID受体,AP-1和/或NF-κB活性的融合血管调节剂及其用途
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申请号: US12866270申请日: 2009-02-05
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公开(公告)号: US20110002952A1公开(公告)日: 2011-01-06
- 发明人: Jingwu Duan , David S. Weinstein , Bin Jiang
- 申请人: Jingwu Duan , David S. Weinstein , Bin Jiang
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 国际申请: PCT/US09/33134 WO 20090205
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; C07D491/147 ; A61K31/4375 ; A61K38/26 ; A61K38/28 ; A61K39/00 ; A61P37/00 ; A61P29/00 ; A61P3/00 ; A61P37/06 ; A61P19/02 ; A61P25/00 ; A61P11/06 ; A61P1/00 ; A61P17/06
摘要:
Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, 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; B1 and B2 rings are pyridyl rings, wherein the B1 and B2 rings are each fused to the A ring and the B1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R1, R2, and R4, and the B2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R3, R7, and R3 71, J2, and J3 are at each occurrence the same or different and are independently -AIQA2-; Q is a bond, O, S, S(0), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3 alkylene, substituted C1-3 alkylene, C24 alkenylene, and substituted C24 alkenylene, 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.
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