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    • 6. 发明授权
    • Piperazine-cyclodextrin complexes
    • 哌嗪 - 环糊精复合物
    • US06596706B1
    • 2003-07-22
    • US09530592
    • 2000-05-08
    • Masahiko KikuchiYukihiko NagaseKaneto Uekama
    • Masahiko KikuchiYukihiko NagaseKaneto Uekama
    • A61K31724
    • B82Y5/00A61K47/6951C08B37/0015
    • The present invention relates to a compound represented by formula (1): wherein Q, which may have a substituent, represents an aryl group, a heterocyclic group, a diarylmethyl group, or an aralkyl group; R, which may have a substituent, represents a bicyclic nitrogen-containing heterocyclic group or a phenyl group; and Z represents a C1-C3 alkylene group, a C2-C4 alkenylene group, a C1-C3 alkylene group having one hydroxyl group, a carbonyl moiety, a C1-C2 alkylene group containing one carbonyl moiety at one end or an intermediate position of the carbon chain, or an oxalyl group; or salts thereof and a piperazine-cyclodextrin complex combined with a water-soluble cyclodextrin derivative. The complex exhibits enhanced water solubility, excellent stability, and low topical stimulation and is useful as a therapeutic agent for circulatory diseases and diseases of the brain region.
    • 本发明涉及由式(1)表示的化合物:其中可具有取代基的Q表​​示芳基,杂环基,二芳基甲基或芳烷基; R可以具有取代基,表示双环含氮杂环基或苯基; Z表示C1-C3亚烷基,C2-C4亚链烯基,具有一个羟基的C1-C3亚烷基,羰基部分,在一端或中间位置含有一个羰基部分的C1-C2亚烷基 碳链或草酰基; 或其盐和与水溶性环糊精衍生物组合的哌嗪 - 环糊精复合物。 复合物表现出增强的水溶性,优异的稳定性和低的局部刺激,并且可用作循环系统疾病和脑区疾病的治疗剂。