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    Antiproliferative 1,2,3-thiadiazole compounds
    2.
    发明申请
    Antiproliferative 1,2,3-thiadiazole compounds 有权
    抗增殖性1,2,3-噻二唑化合物

    公开(公告)号：US20060009500A1

    公开(公告)日：2006-01-12

    申请号：US11218969

    申请日：2005-09-02

    申请人： Zalhui Zhang ,  Gregory Chopiuk ,  Timothy Daynard ,  Shisen Wang

    发明人： Zalhui Zhang ,  Gregory Chopiuk ,  Timothy Daynard ,  Shisen Wang

    IPC分类号： A61K31/433

    CPC分类号： A61K31/433 ,  C07D285/06

    摘要： This invention is directed to methods of using compounds having the structure: and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3 and R4 is independently selected from hydrogen, R5, R6, and R7; R5 is selected from alkyl, heteroalkyl, aryl and heteroaryl; R6 is selected from (R5)n-alkylene, (R5)n-heteroalkylene, (R5)n-arylene and (R5)n-heteroarylene; R7 is selected from (R6)n-alkylene, (R6)n-heteroalkylene, (R6)n-arylene, and (R6)n-heteroarylene; and n is selected from 0, 1, 2, 3, 4 and 5, where R1 and R2 may together form a heterocyclic structure including the nitrogen to which they are both attached, and R3 and R4 may together form a heterocyclic structure including the nitrogen to which they are both attached; and each of L1 and L2 is independently selected from -A1-A2-A3- where each of A1, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene. These compounds are useful in treating hyperproliferative disorders and inducing apoptosis.

    摘要翻译： 本发明涉及使用具有以下结构的化合物的方法：其包括立体异构体，溶剂化物和药学上可接受的盐，其中R 1，R 2，R 2， SO 3和R 4独立地选自氢，R 5，R 6和R 7， / SUP>; R 5选自烷基，杂烷基，芳基和杂芳基; R 6选自（R 5）N 1 - 亚烷基，（R 5） 亚磺酰基，（R 5） - 亚芳基和（R 5）5 - 亚杂芳基。 R 7选自（R 6）N - 亚烷基，（R 6） 亚磺酰基，（R 6） - 亚芳基和（R 6） - 亚 - 亚芳基 ; 并且n选自0,1,2,3,4和5，其中R 1和R 2可以一起形成杂环结构，包括它们是氮的杂环结构 两个连接的R 3和R 4可以一起形成包括它们都连接的氮的杂环结构; 并且L 1和L 2各自独立地选自-A1-A2-A3-，其中A1，A2和A3各自独立地选自直接键， 亚烷基，杂亚烷基，亚芳基和亚杂芳基。 这些化合物可用于治疗过度增殖性疾病和诱导凋亡。

    Compositions and methods for inhibiting the enzymatic activity of PTP-1B
    7.
    发明申请
    Compositions and methods for inhibiting the enzymatic activity of PTP-1B 审中-公开
    抑制PTP-1B酶活性的组合物和方法

    公开(公告)号：US20060070135A1

    公开(公告)日：2006-03-30

    申请号：US11127934

    申请日：2005-05-12

    申请人： Michel Tremblay ,  Dan Leung ,  Timothy Daynard

    发明人： Michel Tremblay ,  Dan Leung ,  Timothy Daynard

    IPC分类号： A01K67/027 ,  C12Q1/54 ,  C12Q1/37

    CPC分类号： C12Q1/42 ,  C12N15/8509 ,  G01N2500/04

    摘要： The present invention provides mice that have had their PTP-1B genes disrupted by targeted homologous recombination. The mice have no detectable PTP-1B protein, yet appear to be physiologically normal. However, in the fed state on a normal diet, the mice have half the level of circulating insulin as their wild-type littermates. In glucose and insulin tolerance tests, the mice show an increased insulin sensitivity. When fed a high fat, high carbohydrate diet, the mice show a resistance to weight gain as compared to their wild-type littermates. Methods of making the mice and cell lines derived from the mice are also provided. The present invention also provides methods of identifying inhibitors of the enzymatic activity of PTP-1B as well as inhibitors identified by such methods.

    摘要翻译： 本发明提供了通过靶向同源重组破坏其PTP-1B基因的小鼠。 小鼠没有可检测的PTP-1B蛋白，但似乎在生理上正常。 然而，在正常饮食中的喂养状态下，小鼠具有作为野生型同窝出生物循环胰岛素水平的一半水平。 在葡萄糖和胰岛素耐量测试中，小鼠显示胰岛素敏感性增加。 当饲喂高脂肪，高碳水化合物饮食时，与野生型同窝仔相比，小鼠显示出对体重增加的抵抗力。 还提供了制备来自小鼠的小鼠和细胞系的方法。 本发明还提供鉴定PTP-1B的酶活性抑制剂以及通过这些方法鉴定的抑制剂的方法。