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    Phenyl guanidinobenzoate derivatives which have protease inhibitory activity
    26.
    发明授权
    Phenyl guanidinobenzoate derivatives which have protease inhibitory activity 失效
    具有蛋白酶抑制活性的苯胍基苯甲酸酯衍生物

    公开(公告)号：US4746737A

    公开(公告)日：1988-05-24

    申请号：US886046

    申请日：1986-07-16

    申请人： Setsuro Fujii ,  Eizou Hattori ,  Mitsuteru Hirata ,  Koichiro Watanabe ,  Tomio Ohta ,  Nobuo Yokoo ,  Masahiko Nagakura

    发明人： Setsuro Fujii ,  Eizou Hattori ,  Mitsuteru Hirata ,  Koichiro Watanabe ,  Tomio Ohta ,  Nobuo Yokoo ,  Masahiko Nagakura

    IPC分类号： C07C279/18 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D243/08 ,  C07D295/185 ,  C07D265/30

    CPC分类号： C07D207/27 ,  C07C279/18 ,  C07D207/16 ,  C07D243/08 ,  C07D295/185

    摘要： Novel benzoyl esters of the following formula (I), and acid addition salts thereof, ##STR1## in which R.sub.1 and R.sub.2 are the same or different and represent a hydrogen atom or a lower alkoxy group, A represents a single bond, a linear or branched lower alkylene group, a lower alkenylene group, R.sub.3 and R.sub.4 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sub.3 and R.sub.4 join together to form a lower alkylene group, R.sub.5 represents a group of the formula, --X--(CO).sub.n --Y in which X represents a single bond, a linear or branched lower alkylene group or an alkenylene group, n is 0 or 1, Y represents a hydrogen atom, a cycloalkyl group, an aryl group, a hydroxyl group, a lower alkoxy group and the like are prepared by reacting para-nitrobenzoic acid or its derivative with a compound of the general formula (III) or its derivative ##STR2## to obtain a compound of the general formula (IV) ##STR3## followed by reducing the compound of the formula (IX) ##STR4## and subjecting the compound (IX) to guanidylation reaction, or by reaction para-guanidinobenzoic derivative with compound (III) or its derivative.The benzoyl esters have strong anti-trypsin activity, anti-thrombin activity and anticoagulant activity with low toxicity and are useful as a medicine for treatment of pancreatitis and disseminated intravascular coagulation (DIC).

    摘要翻译： 下式（I）的新型苯甲酰基酯及其酸加成盐，其中R 1和R 2相同或不同，表示氢原子或低级烷氧基，A表示单键， 直链或支链低级亚烷基，低级亚烯基，R3和R4相同或不同，表示氢原子或低级烷基，或R3和R4连接在一起形成低级亚烷基，R5表示 其中X表示单键的-X-（CO）nY，直链或支链低级亚烷基或亚烯基，n为0或1，Y表示氢原子，环烷基，芳基， 通过使对硝基苯甲酸或其衍生物与通式（III）的化合物或其衍生物（IMAGE）（III）反应来制备羟基，低级烷氧基等，以获得通式（III）的化合物 （Ⅳ），然后还原式（Ⅸ）化合物（IX）和 使化合物（IX）进行胍基化反应，或通过反应对 - 胍基苯甲酸衍生物与化合物（III）或其衍生物反应。 苯甲酰酯具有很强的抗胰蛋白酶活性，抗凝血酶活性和抗凝血活性，毒性低，可用作治疗胰腺炎和弥散性血管内凝血（DIC）的药物。

    Leucylalany-arginine derivative
    28.
    发明授权
    Leucylalany-arginine derivative 失效
    亮氨酸 - 精氨酸衍生物

    公开(公告)号：US4418012A

    公开(公告)日：1983-11-29

    申请号：US300415

    申请日：1981-09-09

    申请人： Setsuro Fujii ,  Mamoru Sugimoto ,  Takashi Yaegashi

    发明人： Setsuro Fujii ,  Mamoru Sugimoto ,  Takashi Yaegashi

    IPC分类号： C07K5/08 ,  C07K5/083 ,  C12Q1/34 ,  C12Q1/37 ,  C12Q1/56 ,  C07C103/52

    CPC分类号： C07K5/0808 ,  C12Q1/34 ,  C12Q1/56 ,  C12Q2334/30 ,  G01N2333/974 ,  Y02P20/55

    摘要： A leucylalanyarginine derivative represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen or an amino-protecting group; R.sub.2 and R.sub.3 represent hydrogen or guanidino-protecting groups; and R.sub.4 represents naphthyl. The above compound is useful as an excellent substrate for various enzymes, such as trypsin, plasmin, kallikrein, urokinase, Cl-esterase and the like. Accordingly, the activity of enzymes can be measured by use of said compound as a substrate.

    摘要翻译： 由下式表示的亮氨酰基精氨酸衍生物，其中R 1表示氢或氨基保护基; R2和R3表示氢或胍基保护基; 并且R 4表示萘基。 上述化合物可用作各种酶的优异底物，例如胰蛋白酶，纤溶酶，激肽释放酶，尿激酶，C1-酯酶等。 因此，可以通过使用所述化合物作为底物来测量酶的活性。