申请人:TAISHO PHARMACEUTICAL CO., LTD
公开号:EP1291343A1
公开(公告)日:2003-03-12
Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula:
wherein R1 represents a group represented by the formula: R2-(CH2)m- (wherein R2 represents a C3-8 cycloalkyl group, a C2-6 alkoxycarbonyl group, a C2-10 alkenyl group, a C2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R3-A- (wherein R3 represents a hydrogen atom, a C1-6 alkoxy group, a C3-8 cycloalkoxy group, or the like, and A represents a straight-chain C2-10 alkylene group which may be substituted with a C1-6 alkyl group or a trifluoromethyl group), or a C3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom,
or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.
本发明提供了抑制 20-HETE 生成的药物制剂,20-HETE 参与肾脏和脑血管等主要器官微血管的收缩或扩张,或参与引起细胞增殖。本发明涉及由式表示的羟基脒化合物:
其中 R1 代表由式表示的基团:R2-(CH2)m-(其中 R2 代表 C3-8 环烷基、C2-6 烷氧羰基、C2-10 烯基、C2-6 炔基、取代或非取代芳基或类似基团,且 m 是 1 至 8 的整数)、由式表示的基团:R3-A-(其中 R3 代表氢原子、C1-6 烷氧基、C3-8 环烷氧基或类似基团,A 代表可被 C1-6 烷基或三氟甲基取代的直链 C2-10 烯基),或 C3-8 环烷基,X 代表氧原子或硫原子、
或其药学上可接受的盐类,并涉及将其作为活性成分的药物。