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    Antiproliferative 1,2,3-thiadiazole compounds
    6.
    发明授权
    Antiproliferative 1,2,3-thiadiazole compounds 失效

    公开(公告)号：US07022702B2

    公开(公告)日：2006-04-04

    申请号：US10144203

    申请日：2002-05-10

    申请人： Zaihui Zhang ,  Gregory B. Chopiuk ,  Timothy S. Daynard ,  Shisen Wang

    发明人： Zaihui Zhang ,  Gregory B. Chopiuk ,  Timothy S. Daynard ,  Shisen Wang

    IPC分类号： A61K31/433 ,  C07D285/06

    CPC分类号： A61K31/433 ,  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, R22 , R3 and R4 is independently selected from hydrogen, R5R6, 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 Al, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene.

    Antiproliferative 1,2,3-thiadiazole compounds
    9.
    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：US07288556B2

    公开(公告)日：2007-10-30

    申请号：US11218969

    申请日：2005-09-02

    申请人： Zaihui Zhang ,  Gregory B Chopiuk ,  Timothy S Daynard ,  Shisen Wang

    发明人： Zaihui Zhang ,  Gregory B Chopiuk ,  Timothy S Daynard ,  Shisen Wang

    IPC分类号： C07D285/06 ,  A61K31/41

    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。