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公开(公告)号:US08697708B2
公开(公告)日:2014-04-15
申请号:US13232778
申请日:2011-09-14
申请人: Toby Jonathan Blench , Charles Ellwood , Simon Charles Goodacre , Yingjie Lai , Jun Liang , Calum Macleod , Steven R. Magnuson , Vickie H. Tsui , Karen Williams , Birong Zhang
发明人: Toby Jonathan Blench , Charles Ellwood , Simon Charles Goodacre , Yingjie Lai , Jun Liang , Calum Macleod , Steven R. Magnuson , Vickie H. Tsui , Karen Williams , Birong Zhang
IPC分类号: A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00
CPC分类号: A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/519 , C07D513/04
摘要: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
摘要翻译: 提供式I化合物,立体异构体,互变异构体,溶剂合物,前药和药学上可接受的盐,其中A,X,R 1,R 2,R 4和R 5在本文中定义,药物组合物包括式I化合物和药学上可接受的 载体,佐剂或载体,在治疗中使用化合物或组合物的方法,以及制备式I化合物的方法。
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公开(公告)号:US20120202788A1
公开(公告)日:2012-08-09
申请号:US13232778
申请日:2011-09-14
申请人: Toby Jonathan Blench , Charles Ellwood , Simon Charles Goodacre , Yingjie Lai , Jun Liang , Calum Macleod , Steven R. Magnuson , Vickie H. Tsui , Karen Williams , Birong Zhang
发明人: Toby Jonathan Blench , Charles Ellwood , Simon Charles Goodacre , Yingjie Lai , Jun Liang , Calum Macleod , Steven R. Magnuson , Vickie H. Tsui , Karen Williams , Birong Zhang
IPC分类号: A61K31/437 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P29/00 , A61P25/00 , A61P1/00 , A61P1/04 , A61P17/06 , A61P37/08 , A61P17/00 , A61P19/04 , C07D513/04 , A61P11/06
CPC分类号: A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/519 , C07D513/04
摘要: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
摘要翻译: 提供式I化合物,立体异构体,互变异构体,溶剂合物,前药和药学上可接受的盐,其中A,X,R 1,R 2,R 4和R 5在本文中定义,药物组合物包括式I化合物和药学上可接受的 载体,佐剂或载体,在治疗中使用化合物或组合物的方法,以及制备式I化合物的方法。
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公开(公告)号:US08486950B2
公开(公告)日:2013-07-16
申请号:US12813142
申请日:2010-06-10
申请人: Simon Charles Goodacre , Yingjie Lai , Jun Liang , Steven R. Magnuson , Kirk D. Robarge , Mark S. Stanley , Vickie Hsiao-Wei Tsui , Karen Williams , Birong Zhang , Aihe Zhou
发明人: Simon Charles Goodacre , Yingjie Lai , Jun Liang , Steven R. Magnuson , Kirk D. Robarge , Mark S. Stanley , Vickie Hsiao-Wei Tsui , Karen Williams , Birong Zhang , Aihe Zhou
IPC分类号: C07D401/12 , C07D213/75 , A61K31/4439
CPC分类号: C07D213/75 , C07D401/12
摘要: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof.
摘要翻译: 本发明提供式I化合物,其立体异构体或其药学上可接受的盐,其中A,B,D,R 1,R 2,R 4和R 5在本文中定义,药物组合物包括式I化合物及其使用方法。
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公开(公告)号:US20110118230A1
公开(公告)日:2011-05-19
申请号:US12997066
申请日:2009-06-10
申请人: Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum Macleod , Karen Williams
发明人: Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum Macleod , Karen Williams
IPC分类号: A61K31/4375 , C07D471/14 , C07D513/04 , C07D495/04 , C07D491/107 , C07D487/04 , A61K31/496 , A61K31/4545 , A61K31/5377 , A61K31/553 , A61K31/55 , A61K31/541 , A61K31/438 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61P35/00 , A61P35/02
CPC分类号: C07D471/14 , A61K31/4375 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D491/107 , C07D495/04 , C07D513/04 , C07D519/00
摘要: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译: 本发明涉及可用作激酶抑制剂的式(I),(I-a)和(I-b)的1,7-二氮杂咔唑化合物,更具体地用作检查点激酶1(chk1)抑制剂,因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物,更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法,以及将该化合物用于体外,原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。
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公开(公告)号:US08501765B2
公开(公告)日:2013-08-06
申请号:US12997066
申请日:2009-06-10
申请人: Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum MacLeod , Karen Williams
发明人: Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum MacLeod , Karen Williams
IPC分类号: A61K31/437 , C07D471/14
CPC分类号: C07D471/14 , A61K31/4375 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D491/107 , C07D495/04 , C07D513/04 , C07D519/00
摘要: The invention relates to 1,7-diazacarbazole compounds of Formula (I), which are useful as kinase inhibitors, more specifically useful as checkpoint kinase I (chk1) inhibitors, thus useful as cancer therapeutics.
摘要翻译: 本发明涉及式(I)的1,7-二氮杂咔唑化合物,其可用作激酶抑制剂,更具体地用作检查点激酶I(chk1)抑制剂,因此可用作癌症治疗剂。
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公开(公告)号:US20080242655A1
公开(公告)日:2008-10-02
申请号:US11947656
申请日:2007-11-29
申请人: Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
发明人: Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
IPC分类号: A61K31/397 , C07D471/02 , A61K31/4439 , C07D209/04 , A61P35/00 , A61P29/00 , A61K31/404 , C07D237/26 , A61K31/5025
CPC分类号: C07D471/04 , C07D487/04
摘要: The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译: 本发明涉及具有抗癌和/或抗炎活性的具有式I的唑烷基化合物,更具体地涉及抑制MEK激酶活性的唑烷基化合物。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外,原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。
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公开(公告)号:US07855216B2
公开(公告)日:2010-12-21
申请号:US11947656
申请日:2007-11-29
申请人: Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
发明人: Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
IPC分类号: C07D471/04 , A61K31/437 , A61P29/00 , A61P35/00 , C07D487/04 , A61K31/519 , A61K31/5025
CPC分类号: C07D471/04 , C07D487/04
摘要: The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译: 本发明涉及具有抗癌和/或抗炎活性的具有式I的唑烷基化合物,更具体地涉及抑制MEK激酶活性的唑烷基化合物。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外,原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。
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公开(公告)号:US20110124654A1
公开(公告)日:2011-05-26
申请号:US12997069
申请日:2009-06-10
申请人: Huifen Chen , Hazel Joan Dyke , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Joseph Lyssikatos , Calum Macleod , Karen Williams
发明人: Huifen Chen , Hazel Joan Dyke , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Joseph Lyssikatos , Calum Macleod , Karen Williams
IPC分类号: A61K31/519 , C07D403/14 , A61P35/00 , A61P35/02
CPC分类号: C07D471/14
摘要: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译: 本发明涉及有用的式(I),(Ia),(Ib),(Ic),(Id),(Ie),(If),(Ig)和(Ih)的1,5-二氮杂咔唑化合物 作为激酶抑制剂,更具体地用作检查点激酶1(chk1)抑制剂,因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物,更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法,以及将该化合物用于体外,原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。
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公开(公告)号:US09075498B1
公开(公告)日:2015-07-07
申请号:US13335809
申请日:2011-12-22
IPC分类号: G06F3/0481 , G06F17/30
CPC分类号: G06F3/0481 , G06F3/04847 , G06F17/30554 , G06F17/30687
摘要: A computing device determines counts of documents that are similar to a reference document for a set of similarity ratings. Each similarity rating is based on a number of co-occurring terms between the reference document and corresponding similar documents. The computing device present the reference document and a GUI element pertaining to the documents similar to the reference document in a graphical user interface (GUI). Upon a selection of the GUI element, the computing device presents a visual representation of a correlation between the counts of similar documents and the similarity ratings in the GUI. The visual representation is provided prior to displaying at least one of the similar documents.
摘要翻译: 计算设备确定与一组相似性等级的参考文档类似的文档的计数。 每个相似性评级是基于参考文档和相应的类似文档之间的多个共同出现的术语。 计算设备在图形用户界面(GUI)中呈现参考文档和类似于参考文档的文档的GUI元素。 在GUI元素的选择之后,计算设备呈现类似文档的计数与GUI中的相似性等级之间的相关性的视觉表示。 在显示至少一个相似文档之前提供视觉表示。
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公开(公告)号:US07678813B2
公开(公告)日:2010-03-16
申请号:US10596998
申请日:2005-01-10
申请人: Robin D. Clark , Nicholas C. Ray , Paul Blaney , Christopher Hurley , Hazel Hunt , David Clark , Karen Williams
发明人: Robin D. Clark , Nicholas C. Ray , Paul Blaney , Christopher Hurley , Hazel Hunt , David Clark , Karen Williams
IPC分类号: A61K31/47 , C07D217/02 , C07D417/12
CPC分类号: C07D217/04 , C07D217/02 , C07D217/06 , C07D217/08 , C07D401/10 , C07D401/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/10 , C07D513/04 , C07D513/06
摘要: The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
摘要翻译: 本发明提供了一类新颖的氮杂环丁烷化合物和使用该化合物作为糖皮质激素受体调节剂的方法。
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