| 摘要 |
<p num="1"><br/><br/><br/>The present invention relates to compounds having general Formula (I) or a <br/>pharmaceutically acceptable salt thereof. In this formula R1 is H or (1-<br/>4C)alkyl; R2 is -C(O)R15 or -S(O)2R15; R3 is H, (1-4C)alkyl or -OR16; R4 is H, <br/>(1-4C)alkyl or -OR16; R6 is H or -C(H)NOR16; R7 is H or halogen, cyano; (1-<br/>6C)alkyl, (2-6C)alkenyl or (2- 6C)alkynyl, all three optionally substituted <br/>with OH, halogen or NH2 ;-C(H)NOR16, - OR16, -C(O)R16, or -C(O)OR16; R8 is H, <br/>cyano, halogen, nitro; (1-6C) alkyl, (2- 6C)alkenyl, (2-6C)alkynyl or -O(1-<br/>6C)alkyl, all optionally substituted with amino, hydroxyl or halogen; <br/>(hetero)aryl, optionally substituted with cyano, halogen, (1- 4C)alkyl, (1-<br/>4C)alkoxy, (1-4C)alkoxy(1-4C)alkyl; -C(O)R18, -C(O)OR19, -C(O)NHR17, -<br/>NHC(O)R20, -C(1-4C)alkylNOR21; -C(H)NOR16, or -NHS(O)2R21; R9 is H, halogen, <br/>cyano or (1-4C)alkyl optionally substituted with halogen; R10is H or (1-<br/>4C)alkyl; R11 is H; R12 is H, cyano or (1-4C)alkyl; R13 is H, (1-4C)alkyl, <br/>halogen or formyl; R14 is H, halogen, cyano, (1-4C)alkyl, (2-6C)alkenyl, <br/>C(O)R21 or (hetero)aryl; R15 is H; (1- 6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl,-<br/>O(2-6C)alkyl, -O(2-6C)alkenyl or -O(2- 6C)alkynyl, all optionally substituted <br/>with one or more OH, halogen, cyano or (hetero)aryl, (hetero)aryl, optionally <br/>substituted with (1-4C)alkyl, halogen, cyano, nitro or amino, NH2, (di)(1-<br/>4C)alkylamino, (1-4C)alkyl(1-4C)alkoxyamine, (1- 4C)alkylt hio(1-4C)alkyl or <br/>(1-4C)alkoxy(1-4C)alkyl; R16 is H, (1-6C)alkyl, (2- 6C)alkenyl or (2-<br/>6C)alkynyl; R17 is H, (1-6C)alkyl, optionally substituted with halogen, (1-<br/>4C)alkoxy or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or <br/>(1- 25 4C)alkoxy; (3-6C)cycloalkyl or (hetero)aryl, optio nally substituted <br/>with halogen, (1- 4C)alkyl or (1-4C)alkoxy; R18 is H, NH2, C(O)R21 or (1-<br/>4C)alkyl, optionally substituted with OH, halogen, cyano or -S(1-4C)alkyl; R19 <br/>is H or (1-6C)alkyl, optionally substituted with OH or halogen; R20 is H, (1-<br/>6C)alkyl or (2-6C)alkenyl, both optionally substituted by halogen, O(1-<br/>6C)alkyl, (hetero)aryl, optionally substituted with (1- 4C)alkyl or halogen; <br/>(3-6C)cycloalkyl; (1-6C)alkoxy; (1-6C)alkenyloxy; or (hetero)aryl, optionally <br/>subst ituted with (1-4C)alkyl); NH2, -NH(1-6C)alkyl or -NH(hetero)aryl and R21 <br/>is H or (1-6C)alkyl. The present invention also relates to pharmaceutical <br/>compositions comprising said compounds and the use of these derivatives to <br/>modulate glucocorticoid receptor activity.<br/>
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