Invention Grant
US07994190B2 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
- Patent Title: 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活性的调节剂及其用途
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Application No.: US12513228Application Date: 2007-10-31
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Publication No.: US07994190B2Publication Date: 2011-08-09
- Inventor: T. G. Murali Dhar , Hai-Yun Xiao , James E. Sheppeck
- Applicant: T. G. Murali Dhar , Hai-Yun Xiao , James E. Sheppeck
- Applicant Address: US NJ Princeton
- Assignee: Bristol-Myers Squibb Company
- Current Assignee: Bristol-Myers Squibb Company
- Current Assignee Address: US NJ Princeton
- Agent Laurelee A. Duncan; Burton Rodney
- International Application: PCT/US2007/083083 WO 20071031
- International Announcement: WO2008/057855 WO 20080515
- Main IPC: A61K31/437
- IPC: A61K31/437 ; C07D401/02

Abstract:
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or 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 the group X is O or (Rx)(Ry); is heterocyclo or heteroaryl; E is —N—, —NR1—, —O—, —C(═O), —S—, —SO2—, or —CR2—; F is —N—, —NR1a, —O—, —C(═O), —S—, —SO2—, or —CR2a—; G is independently N, —NR1b—, —O—, —C(═O), —S—, —SO2— or —CR2b— provided that the heterocyclic ring formed does not contain a S—S or S—O bond and at least one of E, F and G is a hetero atom; and Ma, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, R4, R5a, R6, R7, X, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.
Public/Granted literature
- US20100190820A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF Public/Granted day:2010-07-29
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