申请人:Daiichi Sankyo Company, Limited
公开号:US20180170926A1
公开(公告)日:2018-06-21
A crystal of a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R
1
is a hydrogen atom or a hydroxy group, and R is a 2-(trifluoromethyl)pyrimidin-5-yl group or a 5-(trifluoromethyl)pyrazin-2-yl group.
化合物通式为(I)或其药理学上可接受的盐的晶体具有优异的LCAT激活效果,可用作治疗或预防动脉硬化、动脉硬化性心脏病、冠心病(包括心力衰竭、心肌梗死、心绞痛、心脏缺血、心血管紊乱和由血管新生引起的再狭窄)、脑血管疾病(包括中风和脑梗死)、周围血管疾病(包括糖尿病血管并发症)、血脂异常、低HDL胆固醇血症或肾脏疾病的活性成分,特别是抗动脉硬化药物,其中R1是氢原子或羟基,R是2-(三氟甲基)嘧啶-5-基基团或5-(三氟甲基)吡嗪-2-基基团。