MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-?B ACTIVITY AND USE THEREOF

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-?B 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-, -NR<SUB>1</SUB>-, -O-, -S-, -SO<SUB>2</SUB>- or -CR<SUB>2</SUB>-; F is -N-, -NR<SUB>1a</SUB>-, -O-, -S-, SO<SUB>2</SUB>- or -CR<SUB>2a</SUB>-; G is N, -NR<SUB>1b</SUB>-, -O-, -S-, SO<SUB>2</SUB>- or -CR<SUB>2b</SUB>-, 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, J<SUB>a</SUB>, M, M<SUB>a</SUB>, Q, R<SUB>x</SUB>, R<SUB>y</SUB>, R<SUB>1</SUB>, R<SUB>1a</SUB>, R<SUB>1b</SUB>, R<SUB>2</SUB>, R<SUB>2a</SUB>, R<SUB>2b</SUB>, and R<SUB>3</SUB> to R<SUB>21</SUB>, Z, Z<SUB>a</SUB>, Z<SUB>b</SUB>, and Z<SUB>c</SUB> are as defined above.