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    • 26. 发明授权
    • Antiproliferative 1,2,3-thiadiazole compounds
    • 抗增殖性1,2,3-噻二唑化合物
    • US07288556B2
    • 2007-10-30
    • US11218969
    • 2005-09-02
    • Zaihui ZhangGregory B ChopiukTimothy S DaynardShisen Wang
    • Zaihui ZhangGregory B ChopiukTimothy S DaynardShisen Wang
    • C07D285/06A61K31/41
    • A61K31/433C07D285/06
    • 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.
    • 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。
    • 30. 发明授权
    • Heteropolycyclic inhibitors of protein kinases
    • 蛋白激酶的杂多环抑制剂
    • US06514972B2
    • 2003-02-04
    • US09900073
    • 2001-07-06
    • Zaihui ZhangXinyao DuSerguei SviridovGreg Chopiuk
    • Zaihui ZhangXinyao DuSerguei SviridovGreg Chopiuk
    • C07D48704
    • C07D487/04C07D513/04
    • A compound of the formula wherein, independently at each occurrence, v, w, and x are selected from C, N, O, and S, with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R1, R2, R3 and R4 is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.
    • 在每次出现时,v,w和x独立地选自C,N,O和S的化合物,根据需要进行H取代以实现开价值位点; y和z选自N和C,根据需要进行H取代以满足开价值位置,条件是w,v,x,y和z中的每一个不同时为C; 由v,w,x,y和z形成的环可以是饱和或不饱和的; 并且R 1,R 2,R 3和R 4选自氢,烷基,芳基,烷芳基,芳烷基,杂烷基和杂芳基; 其中R 1,R 2,R 3和R 4中的任何相邻的两个可以连接在一起以形成5,6或7-元碳环或杂环,条件是R 1,R 2,R 3和R 4中的每一个不是同时氢。 公开了所述化合物的药物组合物,以及用于治疗包括细胞过度增殖的生物学条件的方法。