Epoxysuccinic acid derivatives
    1.
    发明授权
    Epoxysuccinic acid derivatives 失效
    环氧琥珀酸衍生物

    公开(公告)号:US4393228A

    公开(公告)日:1983-07-12

    申请号:US880180

    申请日:1978-02-22

    CPC分类号: C07D303/48

    摘要: The epoxysuccinic acid derivatives of this invention are prepared by esterification of an epoxysuccinic acid or a halide thereof, by partial hydrolysis of an epoxysuccinic acid diester, by amidation of an epoxysuccinic acid monoester, or by hydrolysis of an epoxysuccinic acid amide monoester. These epoxysuccinic acid derivatives have excellent thiol protease inhibitory activity and anti-inflammatory activity without the acceleration of vascular permeability.

    摘要翻译: 本发明的环氧琥珀酸衍生物通过环氧琥珀酸或其卤化物的酯化,环氧琥珀酸二酯的部分水解,环氧琥珀酸单酯的酰胺化,或通过环氧琥珀酸酰胺单酯的水解而制得。 这些环氧琥珀酸衍生物具有优异的硫醇蛋白酶抑制活性和抗炎活性,而不加速血管通透性。

    Epoxysuccinyl amino acid derivatives
    3.
    发明授权
    Epoxysuccinyl amino acid derivatives 失效
    环氧琥珀酰氨基酸衍生物

    公开(公告)号:US4474800A

    公开(公告)日:1984-10-02

    申请号:US149312

    申请日:1980-05-13

    IPC分类号: C07D303/48 A61K31/335

    CPC分类号: C07D303/48

    摘要: An epoxysuccinyl amino acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, benzyl or cycloalkyl having 5 to 6 carbon atoms, R.sup.2 is alkyl having 3 to 4 carbon atoms, R.sup.3 is hydrogen, benzyloxycarbonyl, acetyl or benzoyl, and n is an integer of 2 to 7. The subject compounds exhibit inhibitory activity towards thiol protease, especially, calcium-activated neutral thiol protease which exists in excess in muscle tissues of mammals afflicted with muscular dystrophy.

    摘要翻译: 式中,R 1为氢,碱金属,苄基或碳原子数5〜6的环烷氧基烷基氨基酸衍生物,R2为碳原子数3〜4的烷基,R3为氢,苄氧羰基,乙酰基或苯甲酰基, n是2至7的整数。本发明化合物对于硫酸蛋白酶,特别是对于患有肌营养不良的哺乳动物的肌肉组织中存在过量的钙激活的中性硫醇蛋白酶表现出抑制活性。