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    Compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation
    1.
    发明授权
    Compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation 有权
    可用于补体，凝固酶和激肽释放酶途径的化合物及其制备方法

    公开(公告)号：US06653340B1

    公开(公告)日：2003-11-25

    申请号：US09647154

    申请日：2000-09-27

    申请人： Yarlagadda S. Babu ,  J. Claude Bennett ,  Shri Niwas ,  R. Scott Rowland

    发明人： Yarlagadda S. Babu ,  J. Claude Bennett ,  Shri Niwas ,  R. Scott Rowland

    IPC分类号： A61K31343

    CPC分类号： C07D277/68 ,  C07D307/84 ,  C07D333/70 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

    摘要： The present invention is concerned with new compounds, and particularly those having a fused bicyclic ring substituted with an amidine moiety. These compounds are each potent inhibitors of Factor D of the alternate pathway of complement, C1s of the classical pathway of complement, Factors Xa, XIIa, VIIa and thrombin of the coagulation pathway, plasmin in the fibrinolytic pathway, and kallikrein and high molecular weight kininogen in the inflammatory pathways. These proteases, which have serine in their active site, are called serine proteases and they are pivotal to most of the processes of inflammation and coagulation. In fact, these various systems are interactive with one another and it is difficult to activate one pathway without it influencing the others.

    摘要翻译： 本发明涉及新化合物，特别是具有被脒部分取代的稠合双环的化合物。 这些化合物各自是补体交替途径因子D的功能抑制剂，补体经典途径的C1s，凝血途径的因子Xa，XIIa，VIIa和凝血酶，纤维蛋白溶解途径中的纤溶酶，激肽释放酶和高分子量激肽原 在炎症通路中。 这些在其活性位点具有丝氨酸的蛋白酶被称为丝氨酸蛋白酶，它们对炎症和凝血的大多数过程是至关重要的。 事实上，这些各种系统是相互交互的，并且难以激活一个路径而不影响其他路径。

    Amide and carbamate derivatives of N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c] quinolin-1-Yl]-1,1-dimethylethyl}methanesulfonamide and methods
    6.
    发明授权
    Amide and carbamate derivatives of N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c] quinolin-1-Yl]-1,1-dimethylethyl}methanesulfonamide and methods 失效
    N- {2- [4-氨基-2-（乙氧基甲基）-1H-咪唑并[4,5-c]喹啉-1-基] -1,1-二甲基乙基}甲磺酰胺的酰胺和氨基甲酸酯衍生物和方法

    公开(公告)号：US08476292B2

    公开(公告)日：2013-07-02

    申请号：US11991663

    申请日：2006-09-08

    申请人： Tushar A. Kshirsagar ,  Shri Niwas ,  Bryon A. Merrill

    发明人： Tushar A. Kshirsagar ,  Shri Niwas ,  Bryon A. Merrill

    IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D471/06

    CPC分类号： C07D471/04

    摘要： Amide and carbamate derivatives N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-1,1-dimethylethyl}methanesulfonamide, pharmaceutical compositions containing these compounds, methods of making the compounds, and methods of use of these compounds in modulating the immune system, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.

    摘要翻译： 酰胺和氨基甲酸酯衍生物N- {2- [4-氨基-2-（乙氧基甲基）-1H-咪唑并[4,5-c]喹啉-1-基] -1,1-二甲基乙基}甲磺酰胺，含有这些化合物的药物组合物 公开了制备化合物的方法，以及这些化合物在调节免疫系统中的用途，用于在动物中诱导细胞因子生物合成和治疗包括病毒和肿瘤疾病的疾病的方法。