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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。
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公开(公告)号:US20090093479A1
公开(公告)日:2009-04-09
申请号:US12336857
申请日:2008-12-17
申请人: Martha KELLY , Younghee LEE , Bin LIU , Ted FUJIMOTO , Joel FREUNDLICH , Bruce D. DORSEY , Gary A. FLYNN , Arifa HUSAIN
发明人: Martha KELLY , Younghee LEE , Bin LIU , Ted FUJIMOTO , Joel FREUNDLICH , Bruce D. DORSEY , Gary A. FLYNN , Arifa HUSAIN
IPC分类号: A61K31/5377 , C07D401/02 , C07D211/80 , C07D409/02 , C07D401/14 , C07D405/02 , A61K31/497 , A61K31/506 , A61P35/00 , A61K31/422 , A61K31/4709 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/44 , C07D413/02
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。
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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。
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