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8 条记录 (耗时 0.063 秒)

    Thrombin inhibitors
    6.
    发明授权
    Thrombin inhibitors 失效
    凝血酶抑制剂

    公开(公告)号：US06376499B1

    公开(公告)日：2002-04-23

    申请号：US09428314

    申请日：1999-10-28

    申请人： Philip E. Sanderson ,  Terry Lyle ,  Bruce Dorsey ,  Matthew G. Stanton ,  Adel M. Naylor-Olsen

    发明人： Philip E. Sanderson ,  Terry Lyle ,  Bruce Dorsey ,  Matthew G. Stanton ,  Adel M. Naylor-Olsen

    IPC分类号： A61K31497

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04

    摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y1 or O; c is CY2 or N; d is CY2; e is CY1 or N; f is CY1 or N; g is CY1 or N; Y1 is hydrogen, C1-4 alkyl, or halogen; Y2 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy; A is  and W, X, Z, R3, R4 and R5 are defined in the specification.

    摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：或其药学上可接受的盐，其中b为N Y1或O; c为CY2或N; d为CY2; e是CY1或N; f是CY1或N; g为CY1或N; Y1是氢，C1-4烷基或卤素; Y 2是氢，C 1-4烷基，C 3-7环烷基，卤素，NH 2，OH或C 1-4烷氧基; A是且W，X，Z，R 3，R 4和R 5在本说明书中定义。

    Anti-cancer agents and uses thereof
    7.
    发明申请
    Anti-cancer agents and uses thereof 失效
    抗癌剂及其用途

    公开(公告)号：US20060270686A1

    公开(公告)日：2006-11-30

    申请号：US10928401

    申请日：2004-08-30

    申请人： Martha Kelly ,  Younghee Lee ,  Bin Liu ,  Ted Fujimoto ,  Joel Freundlich ,  Bruce Dorsey ,  Gary Flynn ,  Arifa Husain

    发明人： Martha Kelly ,  Younghee Lee ,  Bin Liu ,  Ted Fujimoto ,  Joel Freundlich ,  Bruce Dorsey ,  Gary Flynn ,  Arifa Husain

    IPC分类号： A61K31/497 ,  A61K31/44 ,  C07D403/02

    CPC分类号： C07D209/08 ,  C07D213/74 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/10

    摘要： The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3—R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.

    摘要翻译： 本发明涉及新型化合物及其盐，其合成及其作为抗癌剂的用途。 化合物包括式I化合物及其溶剂合物，水合物及其药学上可接受的盐，其中A 1是N或CR 1; N 3或N 3是N或CR 3; A <5>为N或CR 5; 在说明书中定义了R 1，R 3，R 6和L 6; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基，在环部分中具有1-3个氮原子的任选取代的6元杂芳基，任选取代的5元杂芳基具有0 -4个氮原子，并且在环部分中任选具有1个硫原子或1个氧原子，或任选取代的杂芳基，其中6元环稠合到5元环或6元环 其中在每种情况下，1,2,3或4个环原子是独立地选自氮，氧和硫的杂原子。 它们对广泛的癌症尤其是白血病，非小细胞肺和结肠有效。