Invention Grant
US08304539B2 Fused heteroaryl 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活性的融合杂芳基调节剂及其用途
- Patent Title: Fused heteroaryl modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
- Patent Title (中): 糖皮质激素受体,AP-1和/或NF-κB活性的融合杂芳基调节剂及其用途
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Application No.: US12866270Application Date: 2009-02-05
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Publication No.: US08304539B2Publication Date: 2012-11-06
- Inventor: Jingwu Duan , David S. Weinstein , Bin Jiang
- Applicant: Jingwu Duan , David S. Weinstein , Bin Jiang
- Applicant Address: US NJ Princeton
- Assignee: Bristol-Myers Squibb Company
- Current Assignee: Bristol-Myers Squibb Company
- Current Assignee Address: US NJ Princeton
- Agent Burton Rodney; Laurelee A. Duncan
- International Application: PCT/US2009/033134 WO 20090205
- International Announcement: WO2009/100171 WO 20090813
- Main IPC: C07D491/147
- IPC: C07D491/147 ; C07D413/00

Abstract:
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 taυtomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; •A is a S- to 8-membered carbocyclic ring or a S- 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 R5, R7, and R3 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, C1-3 alkylene, substituted C1-3 alkylene, C2-4 alkenylene, and substituted C2-4 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.
Public/Granted literature
- US20110002952A1 FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF Public/Granted day:2011-01-06
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