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公开(公告)号：US07858626B2
公开(公告)日：2010-12-28
申请号：US11830024
申请日：2007-07-30
申请人： Amogh Boloor , Mui Cheung , Ronda Gayle Davis-Ward , Philip Anthony Harris , Kevin Hinkle , Christopher P. Lauderman , Robert Anthony Mook, Jr. , Jeffery Alan Stafford , James Marvin Veal
发明人： Amogh Boloor , Mui Cheung , Ronda Gayle Davis-Ward , Philip Anthony Harris , Kevin Hinkle , Christopher P. Lauderman , Robert Anthony Mook, Jr. , Jeffery Alan Stafford , James Marvin Veal
IPC分类号： C07D403/04 , A61K31/53 , A61P35/00
CPC分类号： C07D239/30 , C07D231/56 , C07D235/08 , C07D403/12 , C07D413/14
摘要： Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译： 本文描述了可用作VEGFR2抑制剂的嘧啶衍生物。 所述的发明还包括制备此类嘧啶衍生物的方法以及使用该嘧啶衍生物的方法来治疗过度增殖性疾病。
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公开(公告)号：US20100105712A1
公开(公告)日：2010-04-29
申请号：US12609398
申请日：2009-10-30
申请人： Amogh Boloor , Mui Cheung , Philip Anthony Harris , Kevin Hinkle , Jeffery Alan Stafford , James Marvin Veal
发明人： Amogh Boloor , Mui Cheung , Philip Anthony Harris , Kevin Hinkle , Jeffery Alan Stafford , James Marvin Veal
IPC分类号： A61K31/506 , A61P7/00 , A61P27/10 , C07D403/12
CPC分类号： C07D239/30 , C07D231/56 , C07D235/08 , C07D403/12 , C07D413/14
摘要： Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译： 本文描述了可用作VEGFR2抑制剂的嘧啶衍生物。 所述的发明还包括制备此类嘧啶衍生物的方法以及使用该嘧啶衍生物的方法来治疗过度增殖性疾病。
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公开(公告)号：US07262203B2
公开(公告)日：2007-08-28
申请号：US11383229
申请日：2006-05-15
申请人： Amogh Boloor , Mui Cheung , Ronda Davis , Philip Anthony Harris , Kevin Hinkle , Robert Anthony Mook, Jr. , Jeffery Alan Stafford , James Marvin Veal
发明人： Amogh Boloor , Mui Cheung , Ronda Davis , Philip Anthony Harris , Kevin Hinkle , Robert Anthony Mook, Jr. , Jeffery Alan Stafford , James Marvin Veal
IPC分类号： C07D239/48 , C07D403/04 , A61K31/506 , A61P27/02
CPC分类号： C07D239/30 , C07D231/56 , C07D235/08 , C07D403/12 , C07D413/14
摘要： Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译： 本文描述了可用作VEGFR2抑制剂的嘧啶衍生物。 所述的发明还包括制备此类嘧啶衍生物的方法以及使用该嘧啶衍生物的方法来治疗过度增殖性疾病。
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公开(公告)号：US06964977B2
公开(公告)日：2005-11-15
申请号：US10362739
申请日：2001-08-23
申请人： Philip Anthony Harris , Robert N Hunter , Robert Walton McNutt, Jr. , Lee Frederick Kuyper , Karen Elizabeth Lackey , Michael Robert Peel , Edgar Raymond Wood, III
发明人： Philip Anthony Harris , Robert N Hunter , Robert Walton McNutt, Jr. , Lee Frederick Kuyper , Karen Elizabeth Lackey , Michael Robert Peel , Edgar Raymond Wood, III
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/454 , A61K31/53 , A61P7/02 , A61P9/10 , A61P29/00 , A61P29/02 , A61P35/00 , A61P43/00 , C07D209/14 , C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D487/04 , A61K31/415
CPC分类号： C07D401/12 , A61K31/4045 , A61K31/405 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/454 , A61K31/53 , C07D209/14 , C07D209/34 , C07D403/12 , C07D405/12 , C07D487/04
摘要： The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
摘要翻译： 本发明涉及结构（I）的羟吲哚衍生物，含有它们的组合物及其使用和制造方法。 这些化合物通常在药理学上作为通常通过改变促分裂原活化的信号通路而减轻的疾病状态中的药物有用，特别是在病理学上涉及异常细胞增殖的蛋白激酶的抑制或拮抗作用中。 这种疾病状态包括肿瘤生长，再狭窄，动脉粥样硬化，疼痛和血栓形成。 特别地，本发明涉及一系列取代的羟吲哚化合物，其表现出Trk家族蛋白酪氨酸激酶抑制，并且其可用于癌症治疗和慢性疼痛适应症。
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公开(公告)号：US07105530B2
公开(公告)日：2006-09-12
申请号：US10451305
申请日：2001-12-19
申请人： Amogh Boloor , Mui Cheung , Ronda Davis , Philip Anthony Harris , Kevin Hinkle , Robert Anthony Mook, Jr. , Jeffery Alan Stafford , James Marvin Veal
发明人： Amogh Boloor , Mui Cheung , Ronda Davis , Philip Anthony Harris , Kevin Hinkle , Robert Anthony Mook, Jr. , Jeffery Alan Stafford , James Marvin Veal
IPC分类号： C07D239/48 , A61K31/506 , A61P27/02
CPC分类号： C07D239/30 , C07D231/56 , C07D235/08 , C07D403/12 , C07D413/14
摘要： Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also Includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译： 本文描述了可用作VEGFR2抑制剂的嘧啶衍生物。 所述的发明还包括制备此类嘧啶衍生物的方法以及使用该嘧啶衍生物的方法来治疗过度增殖性疾病。
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16.发明授权Substituted oxidole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors 失效取代的氧化物衍生物作为蛋白质酪氨酸和蛋白质丝氨酸/苏氨酸激酶抑制剂公开(公告)号：US06369086B1
公开(公告)日：2002-04-09
申请号：US09262351
申请日：1999-03-04
申请人： Stephen Thomas Davis , Scott Howard Dickerson , Philip Anthony Harris , Robert Neil Hunter, III , Lee Frederick Kuyper , Karen Elizabeth Lackey , Michael Joseph Luzzio , James Marvin Veal , Duncan Herrick Walker
发明人： Stephen Thomas Davis , Scott Howard Dickerson , Philip Anthony Harris , Robert Neil Hunter, III , Lee Frederick Kuyper , Karen Elizabeth Lackey , Michael Joseph Luzzio , James Marvin Veal , Duncan Herrick Walker
IPC分类号： A61K314439
CPC分类号： C07D231/12 , C07D209/34 , C07D209/40 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/04 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04
摘要： The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of such kinases as well as protecting a patient undergoing chemotherapy from chemotherapy induced alopecia.
摘要翻译： 本发明一般涉及新型取代的羟基吲哚化合物和组合物。 这样的化合物和组合物可用作治疗通过抑制或拮抗蛋白激酶激活的信号通路而减轻的疾病或病症的药理学作用。 特别地，本发明涉及一系列取代的羟吲哚化合物，其表现出蛋白质酪氨酸激酶和蛋白质丝氨酸/苏氨酸激酶抑制，并且其可用于通过抑制这种激酶抑制肿瘤生长以及保护接受化疗的患者 化疗引起秃发。
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公开(公告)号：US20130053375A1
公开(公告)日：2013-02-28
申请号：US13696603
申请日：2011-05-06
申请人： Michael Jonathan Bury , Linda N. Casillas , Adam Kenneth Charnley , Michael P. DeMartino , Xiaoyang Dong , Patrick Eidam , Pamela A. Haile , Philip Anthony Harris , Ami Lakdawala Shah , Bryan W. King , Robert W. Marquis, JR. , John F. Mehlmann , Joseph J. Romano , Clark A. Sehon
发明人： Michael Jonathan Bury , Linda N. Casillas , Adam Kenneth Charnley , Michael P. DeMartino , Xiaoyang Dong , Patrick Eidam , Pamela A. Haile , Philip Anthony Harris , Ami Lakdawala Shah , Bryan W. King , Robert W. Marquis, JR. , John F. Mehlmann , Joseph J. Romano , Clark A. Sehon
IPC分类号： A61K31/4706 , A61K31/4709 , C12N9/99 , C07D215/44 , C07D401/12 , C07D405/12 , C07D411/12 , C07D413/12 , C07D471/04 , C07D417/14 , C07D513/04 , C07D215/42 , A61K31/506 , C07D405/14 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/541 , A61K31/496 , A61P29/00 , A61P11/06 , A61P17/00 , A61P1/00 , C07D417/12
CPC分类号： C07D215/42 , A61K31/47 , C07D215/44 , C07D215/48 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D411/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Disclosed are quinoline compounds having the formula: wherein R1, R2 and A are as defined herein, and methods of making and using the same.
摘要翻译： 公开了具有下式的喹啉化合物：其中R1，R2和A如本文所定义，以及制备和使用它们的方法。
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公开(公告)号：US07812022B2
公开(公告)日：2010-10-12
申请号：US11721504
申请日：2005-12-06
申请人： David Edward Uehling , Kirk Lawrence Stevens , Scott Howard Dickerson , Alex Gregory Waterson , Philip Anthony Harris , Douglas McCord Sammond , Robert Dale Hubbard , Holly Kathleen Emerson , Joseph W. Wilson
发明人： David Edward Uehling , Kirk Lawrence Stevens , Scott Howard Dickerson , Alex Gregory Waterson , Philip Anthony Harris , Douglas McCord Sammond , Robert Dale Hubbard , Holly Kathleen Emerson , Joseph W. Wilson
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
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公开(公告)号：US06815439B2
公开(公告)日：2004-11-09
申请号：US10669400
申请日：2003-09-23
IPC分类号： A61K3133
CPC分类号： C07D471/04 , C07D471/14 , C07D513/04 , C07D513/14 , C40B40/00
摘要： Substituted aza-oxindole derivatives useful as cyclin dependent kinase II inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.
摘要翻译： 用作细胞周期蛋白依赖性激酶II抑制剂的取代的氮杂 - 羟吲哚衍生物，用于预防/降低接受这种治疗的患者中化学疗法和/或放射治疗引起的上皮细胞毒性副作用（例如，脱发，足底 - 手掌综合征，粘膜炎）的严重性 治疗。
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公开(公告)号：US20110190280A1
公开(公告)日：2011-08-04
申请号：US12674016
申请日：2008-08-27
申请人： George Adjabeng , Neil Bifulco , Ronda G. Davis-Ward , Scott Howard Dickerson , Kelly Horne Donaldson , Philip Anthony Harris , Keith Hornberger , Kimberly Petrov , Tara Renae Rheault , Gregory Schaaf , John Stellwagen , David Edward Uehling , Alex Gregory Waterson
发明人： George Adjabeng , Neil Bifulco , Ronda G. Davis-Ward , Scott Howard Dickerson , Kelly Horne Donaldson , Philip Anthony Harris , Keith Hornberger , Kimberly Petrov , Tara Renae Rheault , Gregory Schaaf , John Stellwagen , David Edward Uehling , Alex Gregory Waterson
IPC分类号： A61K31/541 , C07D403/14 , A61K31/506 , C07D413/14 , A61K31/5377 , C07D417/14 , C07D498/04 , A61K31/5365 , A61P35/00
CPC分类号： C07D417/04 , C07D413/04 , C07D413/14 , C07D417/14
摘要： The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
摘要翻译： 本发明提供噻唑和恶唑化合物，含有它们的组合物，以及制备方法及其用作药剂的方法。
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