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    Antiproliferative 1,2,3-thiadiazole compounds
    1.
    发明授权
    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：US06420400B1

    公开(公告)日：2002-07-16

    申请号：US09545237

    申请日：2000-04-07

    申请人： Zaihui Zhang ,  Jun Yan ,  Danny Leung ,  Shisen Wang ,  Penelope C. Costello ,  Jasbinder Sanghera

    发明人： Zaihui Zhang ,  Jun Yan ,  Danny Leung ,  Shisen Wang ,  Penelope C. Costello ,  Jasbinder Sanghera

    IPC分类号： C07D28506

    CPC分类号： C07D285/06

    摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are 1,2,3-thiadiazoles 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.

    摘要翻译： 提供药物组合物和化合物。 本发明化合物具有抗增殖活性，可能促进缺乏细胞周期和死亡正常调节的细胞凋亡。 在本发明的一个实施方案中，提供了与生理上可接受的载体组合的化合物的制剂。 药物制剂可用于治疗过度增殖性疾病，该疾病包括肿瘤生长，淋巴组织增生性疾病，血管生成。 本发明的化合物是具有以下结构的1,2,3-噻二唑：并且包括其立体异构体，溶剂化物和药学上可接受的盐，其中R1，R2，R3和R4各自独立地选自氢，R5，R6和 R7; R5选自烷基，杂烷基，芳基和杂芳基; R6选自（R5）正亚烷基，（R5）正 - 亚杂烷基，（R5）正亚芳基和（R5）n-亚杂芳基; R7选自（R6）正亚烷基，（R6）正 - 亚杂烷基，（R6）n-亚芳基和（R6）n-亚杂芳基; 并且n选自0,1,2,3,4和5，其中R 1和R 2可以一起形成包含它们所连接的氮的杂环结构，并且R 3和R 4可以一起形成包括氮的杂环结构 他们都连在一起; L1和L2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合，亚烷基，杂亚烷基，亚芳基和亚杂芳基。