公开(公告)号：US07960365B2

公开(公告)日：2011-06-14

申请号：US11641524

申请日：2006-12-19

申请人： Niall Morton Hamilton ,  Simon James Anthony Grove ,  Michael John Kiczun ,  John Richard Morphy ,  Brad Sherborne ,  Peter Thomas Albert Littlewood ,  Angus Richard Brown ,  Celia Kingsbury ,  Michael Ohhlmeyer ,  Koc-Kan Ho ,  Steven G. Kultgen

发明人： Niall Morton Hamilton ,  Simon James Anthony Grove ,  Michael John Kiczun ,  John Richard Morphy ,  Brad Sherborne ,  Peter Thomas Albert Littlewood ,  Angus Richard Brown ,  Celia Kingsbury ,  Michael Ohhlmeyer ,  Koc-Kan Ho ,  Steven G. Kultgen

IPC分类号： C07D401/00 ,  A01N57/00

CPC分类号： C07C311/17 ,  C07C311/29 ,  C07D213/61 ,  C07D261/10 ,  C07D307/64 ,  C07D333/34 ,  C07D401/12

摘要： The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.

摘要翻译： 本发明提供具有式I结构的化合物，其中：X是碳原子或氮原子; Ar是苯基或杂芳环; R1是氢，卤素，CN或（1C-4C）烷基; R2是氢，卤素或任选氟化的（1C-3C）烷氧基; 任选卤代（1C-4C）烷氧基，任选卤代芳基（1C-4C）烷氧基，任选卤代（1C-4C）烯基或羟甲基; R4是氢，卤素，任选卤代（1C-4C）烷氧基或任选的卤代芳基（1C-4C）烷氧基; R6是氢，苄基，任选被一个或多个卤素或（1C-4C）烷基取代，或R6任选被卤代（1C-4C）烷基取代; 每个R 7独立地是氢，卤素，任选卤代（1C-4C）烷基或任选卤代（1C-4C）烷氧基及其药学上合适的酸加成盐，用作糖皮质激素受体调节剂，特别是用于治疗中枢神经系统疾病。