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    • 1. 发明申请
    • PIPERAZINE DERIVATIVES AND USE OF THE SAME
    • 哌嗪衍生物及其用途
    • WO1997003060A1
    • 1997-01-30
    • PCT/JP1996001884
    • 1996-07-04
    • SENJU PHARMACEUTICAL CO., LTD.INOUE, JunYOSHIDA, YukaCUI, Ying-SheAZUMA, Mitsuyoshi
    • SENJU PHARMACEUTICAL CO., LTD.
    • C07D303/48
    • C07D303/48
    • Compounds represented by general formula (I) or salts thereof and a process for producing the same wherein R represents carboxy or carboxamide; R represents hydrogen or lower alkyl, or R may be bonded to R or R to thereby form a ring; R and R represent each hydrogen, lower alkyl or sulfide, or R and R may be bonded to each other to thereby form a ring; R represents substituted phenyl or substituted sulfonyl represented by general formula (III): -SO2-R (wherein R represents aryl or amino); and n is 0 or 1. Because of having the effect of inhibiting cysteine protease, the compounds are useful as a preventive or remedy for various diseases in which cysteine protease participates, for example, ischemic diseases, inflammation, muscular dystrophy, immunologic diseases, essential hypertension, Alzheimer's disease, subarachnoidal bleeding, osteoporosis, etc.
    • 由通式(I)表示的化合物或其盐及其制备方法,其中R 1表示羧基或羧酰胺; R 2表示氢或低级烷基,或R 2可以与R 3或R 4键合,从而形成环; R 3和R 4各自代表氢,低级烷基或硫化物,或者R 3和R 4可以彼此键合,从而形成环; R 5表示取代的苯基或由通式(III)表示的取代的磺酰基:-SO 2 -R 7(其中R 7表示芳基或氨基); 并且n为0或1.由于具有抑制半胱氨酸蛋白酶的作用,所述化合物可用作预防或治疗半胱氨酸蛋白酶参与的各种疾病,例如缺血性疾病,炎症,肌营养不良症,免疫疾病,必需的 高血压,阿尔茨海默病,蛛网膜下出血,骨质疏松症等