Arylpiperidinopropanol and arylpiperazinopropanol derivatives and pharmaceuticals containing the same
申请人:Suntory Limited
公开号:US06407099B1
公开(公告)日:2002-06-18
A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate:
wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
一种具有化学式(I)或其盐、水合物、水合盐或溶剂络合物的化合物:其中R1至R4独立地代表H、卤素、OH、烷氧基、可选择地取代的烷基、芳基或芳基烷基,R5代表H、可选择地取代的烷基、芳基或芳基烷基,E1代表O、S或—NR6,其中R6代表H、可选择地取代的烷基、芳基或芳基烷基,E2代表O、S或—NR7,其中R7代表H、可选择地取代的烷基、芳基或芳基烷基,A代表CH、C(OH)或N,X代表H、卤素、烷氧基或可选择地取代的烷基,Q代表可选择地取代的苯基、苯氧基、苄基苯基或环烷氧基,其中当E1代表O或S时,E2不代表O或S,具有抑制细胞毒性Ca2+超载和脂质过氧化作用,并对缓解和治疗因缺血性疾病等症状而进行的药物制剂具有有效作用。