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11. 发明申请

US20100048576A1 PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS 有权
标题翻译：吡嗪和衍生物作为ALK和c-MET抑制剂
公开(公告)号：US20100048576A1
公开(公告)日：2010-02-25
申请号：US12566362
申请日：2009-09-24
申请人： Bruce D. Dorsey , Karen L. Milkiewicz , Douglas A. Pippin , Jay P. Theroff , Ted Underiner , Linda Weinberg , Craig A. Zificsak
发明人： Bruce D. Dorsey , Karen L. Milkiewicz , Douglas A. Pippin , Jay P. Theroff , Ted Underiner , Linda Weinberg , Craig A. Zificsak
IPC分类号： A61K31/4985 , C07D471/04 , C07D401/14 , C07D403/14
CPC分类号： C07D471/04
摘要： The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐形式，其中A，L 1，R 1，R 2，R 3，R 4，R 5，R 6和X如本文所定义。式I化合物具有ALK和/或c-Met抑制活性，可用于治疗ALK-或c-Met介导的病症或病症。

12. 发明授权

US5866573A Pyrazinone thrombin inhibitors 失效
标题翻译：吡嗪酮凝血酶抑制剂
公开(公告)号：US5866573A
公开(公告)日：1999-02-02
申请号：US837682
申请日：1997-04-21
申请人： Philip E.. Sanderson , Terry A.. Lyle , Bruce D. Dorsey , Richard J. Varsolona
发明人： Philip E.. Sanderson , Terry A.. Lyle , Bruce D. Dorsey , Richard J. Varsolona
IPC分类号： C07D241/20 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/495 , C07D403/12 , C07D413/12
CPC分类号： C07D401/12 , C07D241/20 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##
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：例如：

13. 发明授权

US08471005B2 Pyrrolotriazines as ALK and JAK2 inhibitors 有权
标题翻译：吡咯并三嗪作为ALK和JAK2抑制剂
公开(公告)号：US08471005B2
公开(公告)日：2013-06-25
申请号：US13160890
申请日：2011-06-15
申请人： Henry J. Breslin , Sankar Chatterjee , James L. Diebold , Bruce D. Dorsey , Derek D. Dunn , Diane E. Gingrich , Greg A. Hostetler , Robert L. Hudkins , Rachael Hunter , Kurt A. Josef , Joseph Lisko , Eugen F. Mesaros , Karen L. Milkiewicz , Gregory R. Ott , Babu G. Sundar , Jay P. Theroff , Tho Thieu , Rabindranath Tripathy , Theodore L. Underiner , Linda Weinberg , Gregory J. Wells , Craig A. Zificsak
发明人： Henry J. Breslin , Sankar Chatterjee , James L. Diebold , Bruce D. Dorsey , Derek D. Dunn , Diane E. Gingrich , Greg A. Hostetler , Robert L. Hudkins , Rachael Hunter , Kurt A. Josef , Joseph Lisko , Eugen F. Mesaros , Karen L. Milkiewicz , Gregory R. Ott , Babu G. Sundar , Jay P. Theroff , Tho Thieu , Rabindranath Tripathy , Theodore L. Underiner , Linda Weinberg , Gregory J. Wells , Craig A. Zificsak
IPC分类号： C07D487/04 , C07D403/12 , A61K31/53 , A61K31/5377 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula I or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula I has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I化合物或其盐形式，其中Q 1，Q 2，Q 3和Q 4如本文所定义。式I化合物具有ALK和/或JAK2抑制活性，可用于治疗增殖性疾病。

14. 发明申请

US20120028919A1 PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS 有权
标题翻译：吡咯烷酮作为ALK和JAK2抑制剂
公开(公告)号：US20120028919A1
公开(公告)日：2012-02-02
申请号：US13160890
申请日：2011-06-15
申请人： Henry J. Breslin , Sankar Chatterjee , James L. Diebold , Bruce D. Dorsey , Derek D. Dunn , Diane E. Gingrich , Greg A. Hostetler , Robert L. Hudkins , Rachael Hunter , Kurt A. Josef , Joseph Lisko , Eugen F. Mesaros , Karen L. Milkiewicz , Gregory R. Ott , Babu G. Sundar , Jay P. Theroff , Tho Thieu , Rabindranath Tripathy , Theodore L. Underiner , Linda Weinberg , Gregory J. Wells , Craig A. Zificsak
发明人： Henry J. Breslin , Sankar Chatterjee , James L. Diebold , Bruce D. Dorsey , Derek D. Dunn , Diane E. Gingrich , Greg A. Hostetler , Robert L. Hudkins , Rachael Hunter , Kurt A. Josef , Joseph Lisko , Eugen F. Mesaros , Karen L. Milkiewicz , Gregory R. Ott , Babu G. Sundar , Jay P. Theroff , Tho Thieu , Rabindranath Tripathy , Theodore L. Underiner , Linda Weinberg , Gregory J. Wells , Craig A. Zificsak
IPC分类号： A61K31/5377 , C07D223/16 , A61P35/00 , A61K31/53 , A61K31/695 , C07D487/04 , A61K31/55
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula I or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula I has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I化合物或其盐形式，其中Q 1，Q 2，Q 3和Q 4如本文所定义。式I化合物具有ALK和/或JAK2抑制活性，可用于治疗增殖性疾病。

15. 发明申请

US20080280891A1 Anti-cancer agents and uses thereof 审中-公开
标题翻译：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。

16. 发明授权

US06534510B2 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06534510B2
公开(公告)日：2003-03-18
申请号：US09815404
申请日：2001-03-22
申请人： James C. Barrow , Bruce D. Dorsey , Harold G. Selnick , Phung L. Ngo
发明人： James C. Barrow , Bruce D. Dorsey , Harold G. Selnick , Phung L. Ngo
IPC分类号： C07D40100
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein A is
摘要翻译：本发明的化合物可用于抑制凝血酶和相关的血栓闭塞，并且选自：或其药学上可接受的盐，其中A是

17. 发明授权

US07601716B2 Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors 有权
标题翻译：吡啶并吡嗪及其衍生物作为ALK和c-Met抑制剂
公开(公告)号：US07601716B2
公开(公告)日：2009-10-13
申请号：US11799066
申请日：2007-04-30
申请人： Bruce D. Dorsey , Karen L. Milkiewicz , Douglas A. Pippin , Jay P. Theroff , Ted Underiner , Linda Weinberg , Craig A. Zificsak
发明人： Bruce D. Dorsey , Karen L. Milkiewicz , Douglas A. Pippin , Jay P. Theroff , Ted Underiner , Linda Weinberg , Craig A. Zificsak
IPC分类号： A61K31/4985
CPC分类号： C07D471/04
摘要： The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐形式，其中A，L 1，R 1，R 2，R 3，R 4，R 5，R 6和X如本文所定义。式I化合物具有ALK和/或c-Met抑制活性，可用于治疗ALK-或c-Met介导的病症或病症。

18. 发明授权

US6011038A Pyrazinone thrombin inhibitors 失效
标题翻译：吡嗪酮凝血酶抑制剂
公开(公告)号：US6011038A
公开(公告)日：2000-01-04
申请号：US146650
申请日：1998-09-03
申请人： Bruce D. Dorsey , Philip E. Sanderson , Terry A. Lyle
发明人： Bruce D. Dorsey , Philip E. Sanderson , Terry A. Lyle
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , A61K31/495 , C07D403/12 , C07D413/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##
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闭塞：例如：

19. 发明授权

US5502053A HIV protease inhibitor compounds 失效
标题翻译： HIV蛋白酶抑制剂化合物
公开(公告)号：US5502053A
公开(公告)日：1996-03-26
申请号：US294772
申请日：1994-08-23
申请人： Bruce D. Dorsey , Joel R. Huff , Susan F. Britcher
发明人： Bruce D. Dorsey , Joel R. Huff , Susan F. Britcher
IPC分类号： C07C235/26 , C07C235/36 , C07C235/78 , C07C251/38 , C07D295/092 , C07D307/14 , C07D335/06 , A61K31/395 , C07D265/28
CPC分类号： C07D295/088 , C07C235/26 , C07C235/36 , C07C235/78 , C07C251/38 , C07D307/14 , C07D335/06 , C07C2101/14 , C07C2102/08
摘要： Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：式“IMAGE”的化合物是HIV蛋白酶抑制剂，并通过新的途径合成。这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

20. 发明授权

US07504401B2 Anti-cancer agents and uses thereof 失效
标题翻译：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。

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