2-(heteroaryl)-benzoxazole compounds and derivatives, compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
申请人:Foldrx Pharmaceuticals, Inc.
公开号:EP2314584A1
公开(公告)日:2011-04-27
Compounds (I), compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases.
formula I:
wherein:
Y is COOH, COOR5, CONR7R8, tetrazolyl, CONHOH, B(OH)2, CONHSO2Ar, CONHCH(R6)COOH, OH, CH2OH or -(CH2)n-C(R6)(NH2)-COOH;
X is O;
Het is heteroaryl, optionally substituted with halo, OR, alkyl or haloalkyl;
Ar, R, R5 - R8 and n are as described herein.
化合物 (I)、组合物和方法可用于稳定转甲状腺素并治疗、预防或改善转甲状腺素介导的疾病的一种或多种症状。
式 I:
其中
Y 是 COOH、COOR5、CONR7R8、四唑基、CONHOH、B(OH)2、CONHSO2Ar、CONHCH(R6)COOH、OH、CH2OH 或 -(CH2)n-C(R6)(NH2)-COOH;
X 是 O;
Het 是杂芳基,可选择被卤素、OR、烷基或卤代烷基取代;
Ar、R、R5 - R8 和 n 如本文所述。