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    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：US4382889A

    公开(公告)日：1983-05-10

    申请号：US335700

    申请日：1981-12-30

    申请人： Masahuru Tamai ,  Takashi Adachi ,  Shigeo Morimoto ,  Kiyoshi Oguma ,  Kazunori Hanada ,  Sadafumi Omura

    发明人： Masahuru Tamai ,  Takashi Adachi ,  Shigeo Morimoto ,  Kiyoshi Oguma ,  Kazunori Hanada ,  Sadafumi Omura

    IPC分类号： C07D303/48 ,  A61K31/335 ,  A61K31/336 ,  A61K38/00 ,  A61P43/00 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K14/81 ,  C07C103/52

    CPC分类号： C07K5/06078 ,  C07K5/06043 ,  A61K38/00

    摘要： An epoxysuccinic acid derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, alkali metal, alkyl having 1-2 carbon atoms, cycloalkyl having 5-6 carbon atoms or benzyl, R.sup.2 is alkyl having 3-4 carbon atoms or benzyl, R.sup.3 is hydrogen or methyl, and R.sup.4 is alkyl having 1-10 carbon atoms, phenyl, benzyl, phenethyl, cycloalkyl having 3-6 carbon atoms or a group of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl having 1-4 carbon atoms or said alkyl substituted with hydroxy, methylmercapto, phenyl, hydroxyphenyl, indolyl, an optionally protected carboxy, an optionally protected amino or an optionally protected guanidino, and R.sup.6 is hydroxy, alkalimetaloxy, alkoxy having 1-2 carbon atoms, benzyloxy, amino or dimethylamino, or R.sup.3 and R.sup.4 taken together with the nitrogen atom to which they are attached form a 5-6 membered heterocyclic ring, or said heterocyclic ring substituted with a protected carboxy.

    摘要翻译： 其中R 1为氢，碱金属，具有1-2个碳原子的烷基，具有5-6个碳原子的环烷基或苄基，R2为具有3-4个碳原子的烷基或苄基，R3表示下式的环氧琥珀酸衍生物 氢或甲基，R 4是具有1-10个碳原子的烷基，苯基，苄基，苯乙基，具有3-6个碳原子的环烷基或下式的基团：其中R5是氢，具有1-4个碳原子的烷基或 所述烷基被羟基，甲基巯基，苯基，羟基苯基，吲哚基，任选保护的羧基，任选保护的氨基或任选被保护的胍基取代，R 6是羟基，碱金属氧基，具有1-2个碳原子的烷氧基，苄氧基，氨基或二甲基氨基， 或者R 3和R 4与它们所连接的氮原子一起形成5-6元杂环，或被被保护的羧基取代的所述杂环。

    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

    申请人： Masaharu Tamai ,  Shigeo Morimoto ,  Takashi Adachi ,  Kiyoshi Oguma ,  Kazunori Hanada ,  Sadafumi Omura

    发明人： Masaharu Tamai ,  Shigeo Morimoto ,  Takashi Adachi ,  Kiyoshi Oguma ,  Kazunori Hanada ,  Sadafumi Omura

    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。