abstract |
REFERS TO 1,2,3,4,10,14-HEXAHYDRO-DIBENZO [c, f] PYRID [1,2-a] AZEPIN-2-IL COMPOUNDS OF FORMULA (I), WHERE R1 IS HO ALKYL ( C1-C4); R2 IS -C (O) R15 O -S (O) 2R15; R3 AND R4 ARE INDEPENDENTLY H, (C1-C4) ALKYL, O -OR16; R6 IS H O -C (R16) NOR16; R7 IS H, HALOGEN, CYANE, ALKYL (C1-C6), AMONG OTHERS; R8 IS H, CYANE, HALOGEN, NITRO, ALKYL (C1-C6), -OR-ALKYL (C1-C6), AMONG OTHERS OPTIONALLY SUBSTITUTED; R9 IS H, HALOGEN, CYANE OR ALKYL (C1-C4) OPTIONALLY SUBSTITUTED; R10 IS H O ALKYL (C1-C4); R11 IS H; R12 IS H, CYANE, OR ALKYL (C1-C4); R13 IS H, (C1-C4) ALKYL, HALOGEN, OR FORMIL; R14 IS H, HALOGEN, CYANE, ALKYL (C1-C4) OR HETEROARYL. THE PREFERRED ARE: REL-N - [(2R, 10R, 14bR) -8-BROMO-1,2,3,4,10,14b-HEXAHYDRO-10-METHYLDIBENZO [c, f] PYRID [1,2-a] AZEPIN-2-IL] -2,2,2-TRIFLUOROACETAMIDE, REL-2,2-DICHLORO-N - [(2R, 10R, 14bR) -8-BROMO-1,2,3,4,10,14b- HEXAHYDRO-10-METHYLDIBENZO [c, f] PYRID [1,2-a] AZEPIN-2-IL] -2,2,2-TRIFLUOROACETAMIDE, AMONG OTHERS. THESE COMPOUNDS ARE MODULATORS OF THE GLUCOCORTICOID RECEPTOR SO THEY ARE USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES |