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    Anti-cancer agents and uses thereof
    2.
    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。

    Anti-cancer agents and uses thereof
    6.
    发明授权
    Anti-cancer agents and uses thereof 失效
    抗癌剂及其用途

    公开(公告)号：US07504401B2

    公开(公告)日：2009-03-17

    申请号：US10928401

    申请日：2004-08-30

    申请人： Martha Kelly ,  Bruce D. Dorsey ,  Gary A. Flynn

    发明人： Martha Kelly ,  Bruce D. Dorsey ,  Gary A. Flynn

    IPC分类号： A61K31/497 ,  A61K31/4439 ,  A61K31/421 ,  A61K31/404 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

    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A1为N或CR1; A3是N或CR3; A5为N或CR5; R1，R3-R6和L在说明书中定义; 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。

    Anti-cancer agents and uses thereof
    9.
    发明申请
    Anti-cancer agents and uses thereof 审中-公开
    抗癌剂及其用途

    公开(公告)号：US20080280891A1

    公开(公告)日：2008-11-13

    申请号：US11819494

    申请日：2007-06-27

    申请人： Martha Kelly ,  Younghee Lee ,  Bin Liu ,  Ted Fujimoto ,  Joel Freundlich ,  Bruce D. Dorsey ,  Gary A. Flynn ,  Arifa Husain ,  William R. Moore, Jr.

    发明人： Martha Kelly ,  Younghee Lee ,  Bin Liu ,  Ted Fujimoto ,  Joel Freundlich ,  Bruce D. Dorsey ,  Gary A. Flynn ,  Arifa Husain ,  William R. Moore, Jr.

    IPC分类号： A61K31/541 ,  A61K31/404 ,  C07D209/42 ,  C07D401/02 ,  C07D417/14 ,  A61K31/44 ,  A61P35/00 ,  A61K31/4439 ,  A61K31/5377 ,  C07D413/14

    CPC分类号： A61K31/404 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/541 ,  C07D213/74 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D413/12 ,  C07D498/04

    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, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.

    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，前列腺，非小细胞肺和结肠有效。 它们还可用于治疗增殖性视网膜病变，例如糖尿病性神经病变和黄斑变性。