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    N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof
    7.
    发明授权
    N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof 失效
    N-酰基肽，其制备方法及其药物组合物

    公开(公告)号：US4643990A

    公开(公告)日：1987-02-17

    申请号：US452827

    申请日：1982-12-23

    申请人： Kazuyoshi Umehara ,  Keizo Yoshida ,  Hirokazu Tanaka ,  Itsuo Uchida ,  Masanobu Kohsaka ,  Hiroshi Imanaka

    发明人： Kazuyoshi Umehara ,  Keizo Yoshida ,  Hirokazu Tanaka ,  Itsuo Uchida ,  Masanobu Kohsaka ,  Hiroshi Imanaka

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  A61K37/43 ,  C07C67/02 ,  C07C69/52 ,  C07C101/26 ,  C07C101/30 ,  C07C143/12 ,  C07K5/08

    CPC分类号： C07K5/06104 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06086 ,  A61K38/00

    摘要： N-acylpeptides are disclosed of the formula: ##STR1## wherein R.sup.1 is alkanoyloxy or alkenoyloxy; R.sup.2 is alkyl or alkenyl; R.sup.3 and R.sup.4 are each lower alkyl, hydroxy(lower)alkyl, ar(lower)alkyl, esterified carboxy(lower)alkyl, carboxy(lower)alkyl, protected amino(lower)alkyl or amino(lower)alkyl; R.sup.5 is hydrogen, hydroxy(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl; R.sup.6 is carboxy, esterified carboxy or sulfo(lower)alkyl; A.sup.1, A.sup.2 and A.sup.3 are each bond or lower alkylene; and m and n are each an integer of 0 or 1; or its pharmaceutically acceptable salt. These compounds have anti-complementary activity and fibrinolytic activity, and are useful as therapeutic agents for immune-complex diseases or autoimmune diseases such as nephritis, rheumatic diseases, systemic lupus erythematosus, etc. and thrombosis such as cerebral apoplexy, coronary insufficiency, pulmonary embolism, etc.

    摘要翻译： N-酰基肽公开于下式：其中R 1是烷酰氧基或烯酰基氧基; R2是烷基或烯基; R 3和R 4各自为低级烷基，羟基（低级）烷基，芳（低级）烷基，酯化羧基（低级）烷基，羧基（低级）烷基，被保护的氨基（低级）烷基或氨基（低级） R5是氢，羟基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基或酯化羧基（低级）烷基; R6是羧基，酯化的羧基或磺基（低级）烷基; A1，A2和A3各自为键或低级亚烷基; m和n分别为0或1的整数; 或其药学上可接受的盐。 这些化合物具有抗互补活性和纤维蛋白溶解活性，并且可用作免疫复合物疾病或自身免疫性疾病如肾炎，风湿性疾病，系统性红斑狼疮等的治疗剂，以及血栓形成如脑中风，冠状动脉功能不全，肺栓塞 等等