申请人:Dehmlow Henrietta
公开号:US20100216833A1
公开(公告)日:2010-08-26
The present invention relates to compounds of the formula (I)
wherein R
1
, R
2
, R
3
, R
4
, R
5
, X
1
, X
2
, X
3
, X
4
, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXRα and/or LXRβ agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
本发明涉及式(I)的化合物,其中R1、R2、R3、R4、R5、X1、X2、X3、X4、n和k在说明书和权利要求书中定义,并且其药学上可接受的盐和/或药学上可接受的酯。该化合物用于治疗和预防LXRα和/或LXRβ激动剂调节的疾病,包括增加的脂质和
胆固醇水平,特别是低HDL
胆固醇,高LDL
胆固醇,动脉粥样硬化疾病,糖尿病,特别是非
胰岛素依赖性糖尿病,代谢综合征,血脂异常,阿尔茨海默病,败血症,炎症性疾病,如结肠炎,胰腺炎,肝胆瘤/纤维化以及有炎症成分的疾病,例如阿尔茨海默病或受损/可改善的认知功能。