发明名称 OPTICALLY ACTIVE DIBENZYLAMINE DERIVATIVE, AND METHOD FOR PREPARING THE SAME
摘要 The present invention relates to a substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidine-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}aceitic acid or a pharmaceutically acceptable salt thereof, having the effect of reducing the amount of PCSK9 proteins and increasing the amount of LDL receptors. Disclosed is a medicament for prophylactic and/or treatment of a disease selected from hyper-LDL cholesterolemia, dyslipidemia, arteriosclerosis, atherosclerosis, peripheral vascular diseases, hypercholesterolemia, familial hypercholesterolemia, cardiovascular functional disorders, angina pectoris, ischemia, cardiac ischemia, thrombosis, myocardial infarction, reperfusion disorders, angioplasty restenosis, and hypertension, comprising the above-stated compound or a pharmaceutically acceptable salt thereof as an active ingredient. The invention also relates to a method for preparing (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidine-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}aceitic acid or a pharmaceutically acceptable salt thereof.
申请公布号 EA024241(B1) 申请公布日期 2016.08.31
申请号 EA20120091447 申请日期 2011.06.03
申请人 KOWA COMPANY, LTD. 发明人 OHGIYA TADAAKI;MURAKAMI TAKESHI;MIYOSAWA KATSUTOSHI;SHIBUYA KIMIYUKI;YAMAZAKI KOICHI;KUSAKABE TAICHI
分类号 C07D239/47;A61K31/505;A61P3/06;A61P9/10;A61P13/08;A61P13/12;A61P17/06;A61P19/10;A61P25/28;A61P27/02;A61P29/00;A61P31/12;A61P33/00;A61P35/00;A61P43/00 主分类号 C07D239/47
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