| 摘要 |
This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings:-R1 is-H or-(1-4C)alkyl;-R2 is-C(O)R15 or-S(O)2R15;-R3 is-H,-(1-4C)alkyl or-OR16;-R4 is-H,-(1-4C)alkyl or-OR16;-R6 is-H or-C(R16)NOR16;-R7 is-H,-halogen,-cyano;-(1-6C)alkyl,-(2-6C)alkenyl or-(2-6C)alkynyl, all optionally substituted with-amino,-hydroxyl or-halogen;-R8 is-H,-cyano,-halogen,-nitro;-(1-6C)alkyl,-(2-6C)alkenyl,-(2-6C)alkynyl or-O(l-6C)alkyl, all optionally substituted with-amino,-hydroxyl or-halogen;-(hetero)aryl, optionally substituted with-cyano,-halogen,-(1-4C)alkyl,-(1-4C)alkoxy,-(l-4C)alkoxy(l-4C)alkyl or-(hetero)aryl;-C(R16)NOR16;-C(O)N(R17)2;-C(O)R18,-C(O)OR19,-NHC(O)R20, or-NHS(O)2R21;-R9 is-H,-halogen,-cyano, or-(1-4C)alkyl, optionally substituted with-halogen;-R10 is-H or-(1-4C)alkyl;-R11 is-H;-R12 is-H,-cyano or-(1-4C)alkyl;-R13 is-H,-(1-4C)alkyl,-halogen or-formyl;-R14 is-H,-halogen,-cyano,-(1-4C)a!kyl or-(hetero)aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used for treating inflammatory diseases.
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