[EN] CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 BASED ON THE 1,3 -OXAZINAN- 2 -ONE STRUCTURE<br/>[FR] INHIBITEURS CYCLIQUES DE LA 11-BÊTA-HYDROXYSTÉROÏDE DÉSHYDROGÉNASE 1 BASÉE SUR LA STRUCTURE 1,3-OXAZINAN-2-ONE
申请人:VITAE PHARMACEUTICALS INC
公开号:WO2011011123A1
公开(公告)日:2011-01-27
This invention relates to substitued 1, 3-oxazin-2-one compounds of the Formula (I), (II), (IIA), (IIB), (IIC), (II D), (IIE), (III), (III A), (III B), (IV), (IV A), (IV B), (IV C), (IV D), (V), (V A), (V B), (VI), (VI A), (VI B), (VII), (VII A), (VII B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
这项发明涉及Formula (I), (II), (IIA), (IIB), (IIC), (II D), (IIE), (III), (III A), (III B), (IV), (IV A), (IV B), (IV C), (IV D), (V), (V A), (V B), (VI), (VI A), (VI B), (VII), (VII A), (VII B)的取代1,3-噁唑-2-酮化合物,以及其药学上可接受的盐和药物组合物,用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病。该发明还涉及这些新化合物的药物组合物和它们在细胞中减少或控制皮质醇的产生或抑制皮质醇酮转化为皮质醇的方法的用途。