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25 条记录 (耗时 0.031 秒)

    Method of treating tumors using tetracyclo compounds
    1.
    发明授权
    Method of treating tumors using tetracyclo compounds 失效
    使用四环化合物治疗肿瘤的方法

    公开(公告)号：US4861774A

    公开(公告)日：1989-08-29

    申请号：US947759

    申请日：1986-12-30

    申请人： Masanobu Kohsaka ,  Hiroshi Terano ,  Tadaaki Komori ,  Morita Iwami ,  Michio Yamashita ,  Masashi Hashimoto ,  Itsuo Uchida ,  Shigehiro Takase

    发明人： Masanobu Kohsaka ,  Hiroshi Terano ,  Tadaaki Komori ,  Morita Iwami ,  Michio Yamashita ,  Masashi Hashimoto ,  Itsuo Uchida ,  Shigehiro Takase

    IPC分类号： A61K31/535 ,  A61P31/04 ,  A61P35/00 ,  C07D498/18 ,  C12P17/18 ,  C12R1/465

    CPC分类号： C07D498/18 ,  C12P17/188 ,  C12R1/465 ,  Y02P20/55

    摘要： The invention relates to a method for treatment of carcinoma or sarcoma tumor in mammals which comprises administering to said mammal an effective amount of a tetracyclo compound of the formula: ##STR1## in which R.sup.1 is formyl, protected formyl, hydroxymethyl, protected hydroxymethyl, arylaminomethyl, carboxy, protected carboxy, aryliminomethyl, hydroxyiminomethyl, alkoxyiminomethyl, acyloxyiminomethyl, semicarbazonomethyl or arylsemicarbazonomethyl,R.sup.2 is hydroxy, alkoxy, or protected hydroxy,R.sup.3 is hydrogen and R.sup.4 is methyl, hydroxymethyl or protected hydroxymethyl, orR.sup.3 and R.sup.4 are combined together to form methylene or oxo,R.sup.5 is hydroxy, alkoxy or protected hydroxy, andR.sup.6 is hydrogen, imino-protective group or alkyl,and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及一种治疗哺乳动物癌或肉瘤肿瘤的方法，包括向所述哺乳动物施用有效量的下式的四环化合物：其中R 1为甲酰基，被保护的甲酰基，羟甲基，保护的羟甲基，芳基氨基甲基 羧基，保护的羧基，芳基亚氨基甲基，羟基亚氨基甲基，烷氧基亚氨基甲基，酰氧基亚氨基甲基，氨基甲酰基甲基或芳基氨基丙基甲基，R2是羟基，烷氧基或被保护的羟基，R3是氢，R4是甲基，羟甲基或保护的羟甲基，或R3和R4组合在一起形成 亚甲基或氧代，R 5为羟基，烷氧基或保护的羟基，R 6为氢，亚氨基保护基或烷基，及其药学上可接受的盐。

    N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof
    9.
    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