| 摘要 |
The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ wherein R1 and R2 are independently selected from the group consisting of H, CF3, halo, C1-3alkyl and C1-3-alkoxy; R3 and R4 are independently selected from the group consisting of H, CF3, halo, CH3 and OCH3; R5 is selected from the group consisting of H, CF3, halo, OH, CH2OH, C1-4alkyl, CH2-cyclopropyl and C1-4alkoxy, wherein C1-4alkyl and C1-4alkoxy, may be optionally substituted with one or two OH substituents; R6 is selected from the group consisting of C3-5alkyl and —CH2—C3-4cycloalkyl; R7 is selected from the group consisting of R8 is selected from the group consisting of C1-3alkyl, C1-3alkoxy, CH2CN, CH2OH, OH, CN and halo; R9 is the group —(CHR10)s—(X)t—(CHR10)u—R11; each R10 is independently selected from the group consisting of H, OH or CH2OH; R11 is an isoxazole, —C(O)OH, or a 5- or 6-membered heteroaryl group, wherein the isoxazole or the 5- or 6-membered heteroaryl group may be optionally substituted with one or two halo, NH2 or CH3 substituents; X is CH2, NH, O; r is 0, 1 or 2; s is 0, 1 or 2; t is 0 or 1;/ u is 0, 1 or 2; with the proviso that no more than two R10 groups represent OH or CH2OH. |
