917494-83-8Relevant articles and documents
5-Functionalized indazoles as glucocorticoid receptor agonists
Bai, Mei,Carr, Grant,DeOrazio, Russell J.,Friedrich, Thomas D.,Dobritsa, Svetlana,Fitzpatrick, Kevin,Guzzo, Peter R.,Kitchen, Douglas B.,Lynch, Michael A.,Peace, Denise,Sajad, Mohammed,Usyatinsky, Alexander,Wolf, Mark A.
scheme or table, p. 3017 - 3020 (2010/06/20)
An indazole based series of glucocorticoid receptor agonists is reported. The SAR exploration of this scaffold yielded compounds with nanomolar affinity for the glucocorticoid receptor with indications of selectivity for the preferred transrepression mech
MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF
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Page/Page column 87, (2008/12/05)
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.