Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
    5.
    发明授权
    Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa 有权
    胰蛋白酶样丝氨酸蛋白酶抑制剂,它们的制备和用作凝血因子IIa和Xa的选择性抑制剂

    公开(公告)号:US08497245B2

    公开(公告)日:2013-07-30

    申请号:US13332900

    申请日:2011-12-21

    IPC分类号: A61K38/05

    摘要: The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.

    摘要翻译: 本发明提供制备和使用下式的化合物或其药学上可接受的盐的方法: 其中n是1和2之间的整数; m是0和2之间的整数; X选自CH或N; R1选自-CH2NH2,R2选自-H,-OH,-NH2和乙酰基; R3选自-H,苄氧基羰基和苄基磺酰基; 并且R 4选自-OH,其中p是包括0和2的整数,Y选自-O - , - S - , - S(= O) - , - SO 2 - ,亚甲基,-CH(OH) - , - CH(NH 2) - , - CH(CH 2 -OH) - , - CH(CH 2 -NH 2) - 或-N(R 6) - ,R 5选自 -H或简单(C 1 -C 3)烷基,R 6选自-H,简单(C 1 -C 3)烷基或简单(C 1 -C 3)酰基)。 由于它们选择性双重抑制凝血酶和凝血酶原酶,这些化合物可用作抗凝血剂。

    Luminaire
    10.
    发明授权
    Luminaire 失效
    灯具

    公开(公告)号:US06513942B2

    公开(公告)日:2003-02-04

    申请号:US09726711

    申请日:2000-11-30

    IPC分类号: F21V800

    摘要: Luminaire having an optical waveguide plate, which has a first light guiding surface, and having a light reflecting area—arranged opposite the latter—of an opaque reflector, which reflects light back into the optical waveguide plate in such a way that at least part of said light emerges from the second light guiding surface facing away therefrom. The light reflecting area has a very large number of reflecting area regions, which extend obliquely with respect to one another and obliquely with respect to the opposite first light guiding surface of the optical waveguide plate.

    摘要翻译: 具有光波导板的灯具具有第一导光表面,并且具有与后者不透明反射器相对布置的光反射区域,该光反射区域将光反射回到光波导板中,使得至少部分 所述光从第二导光面从背面射出。 光反射区域具有非常多的反射区域,其相对于彼此倾斜地相对于光波导板的相对的第一导光表面倾斜延伸。