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公开(公告)号：US20110190257A1
公开(公告)日：2011-08-04
申请号：US12999003
申请日：2009-07-01
申请人： Robert Andrew Heald , Philip Jackson , Joseph P. Lyssikatos , Stephen Price , Pascal Pierre Alexandre Savy
发明人： Robert Andrew Heald , Philip Jackson , Joseph P. Lyssikatos , Stephen Price , Pascal Pierre Alexandre Savy
IPC分类号： A61K31/397 , C07D471/02 , C07D231/56 , C07D277/62 , C07D275/06 , A61K31/437 , A61K31/416 , A61K31/428 , A61P35/00
CPC分类号： C07D231/56 , C07D275/04 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, 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： 本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。 本发明提供了可用于抑制异常细胞生长，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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2.发明授权公开(公告)号：US08492427B2
公开(公告)日：2013-07-23
申请号：US12998000
申请日：2009-07-01
IPC分类号： A61K31/437 , A61K31/4035 , A61K31/416 , A61K31/4985 , C07D231/54 , C07D241/00 , C07D221/00 , C07D209/44
CPC分类号： C07D209/46
摘要： The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, 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）的异吲哚酮，更具体地涉及MEK激酶抑制活性。 本发明提供了可用于抑制异常细胞生长，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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3.发明申请ISOINDOLONES DERIVATIVES AS MEK KINASE INHIBITORS AND METHODS OF USE 失效ISOINDOLONES衍生物作为MEK激酶抑制剂和使用方法公开(公告)号：US20110124622A1
公开(公告)日：2011-05-26
申请号：US12998000
申请日：2009-07-01
IPC分类号： A61K31/4035 , C07D209/46 , C07D405/10 , C07D471/04 , C07D487/04 , C07D209/96 , C07D413/10 , A61K31/437 , A61K31/4985 , A61K31/4245 , A61P35/00 , A61P29/00
CPC分类号： C07D209/46
摘要： The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, 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）的异吲哚酮，更具体地涉及MEK激酶抑制活性。 本发明提供了可用于抑制异常细胞生长，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：US08691826B2
公开(公告)日：2014-04-08
申请号：US13613952
申请日：2012-09-13
申请人： Toby Jonathan Blench , Christine Edwards , Robert Andrew Heald , Janusz Jozef Kulagowski , Jonathan Mark Sutton , Carmelida Capaldi
发明人： Toby Jonathan Blench , Christine Edwards , Robert Andrew Heald , Janusz Jozef Kulagowski , Jonathan Mark Sutton , Carmelida Capaldi
IPC分类号： A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
摘要翻译： 式（I）化合物：可用作人中性粒细胞弹性蛋白酶的抑制剂。
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公开(公告)号：US08883799B2
公开(公告)日：2014-11-11
申请号：US13326524
申请日：2011-12-15
申请人： Jennafer Dotson , Robert Andrew Heald , Timothy Heffron , Graham Elgin Jones , Sussie Lerche Krintel , Neville James McLean , Chudi Ndubaku , Alan G. Olivero , Laurent Salphati , Lan Wang , BinQing Wei
发明人： Jennafer Dotson , Robert Andrew Heald , Timothy Heffron , Graham Elgin Jones , Sussie Lerche Krintel , Neville James McLean , Chudi Ndubaku , Alan G. Olivero , Laurent Salphati , Lan Wang , BinQing Wei
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04 , C07D413/00 , C07D265/00 , C07D498/00 , A61K31/535 , C07D498/14 , C07D491/14 , C07D495/14 , C07D487/14
CPC分类号： C07D498/22 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K39/3955 , A61K2039/505 , C07D471/14 , C07D471/22 , C07D487/14 , C07D491/14 , C07D491/147 , C07D495/14 , C07D498/14 , C07D498/20 , C07K16/22 , C07K2317/24
摘要： Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
摘要翻译： 描述了具有抗癌活性，抗炎活性或免疫调节特性，更具体地与PI3激酶调节或抑制活性的式I的三环PI3k抑制剂化合物。 描述了使用式I的三环PI3K抑制剂化合物用于体外，原位和体内诊断或治疗哺乳动物细胞，生物体或相关病理条件的方法。 式I化合物包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐。 虚线表示可选的双键，至少一条虚线是双键。 取代基如所述。
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公开(公告)号：US20120171199A1
公开(公告)日：2012-07-05
申请号：US13326524
申请日：2011-12-15
申请人： Jennafer Dotson , Robert Andrew Heald , Timothy Heffron , Graham Elgin Jones , Sussie Lerche Krintel , Neville James McLean , Chudi Ndubaku , Alan G. Olivero , Laurent Salphati , Lan Wang , BinQing Wei
发明人： Jennafer Dotson , Robert Andrew Heald , Timothy Heffron , Graham Elgin Jones , Sussie Lerche Krintel , Neville James McLean , Chudi Ndubaku , Alan G. Olivero , Laurent Salphati , Lan Wang , BinQing Wei
IPC分类号： A61K31/5383 , C07D491/147 , C07D498/14 , C07D487/14 , C07D498/22 , A61K31/5386 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P37/02 , A61P25/00 , A61P9/00 , A61P1/16 , A61P31/12 , A61P7/00 , A61P3/10 , A61P37/04 , A61P35/02 , C07D471/14 , C07D495/14 , A61K39/395
CPC分类号： C07D498/22 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K39/3955 , A61K2039/505 , C07D471/14 , C07D471/22 , C07D487/14 , C07D491/14 , C07D491/147 , C07D495/14 , C07D498/14 , C07D498/20 , C07K16/22 , C07K2317/24
摘要： Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
摘要翻译： 描述了具有抗癌活性，抗炎活性或免疫调节特性，更具体地与PI3激酶调节或抑制活性的式I的三环PI3k抑制剂化合物。 描述了使用式I的三环PI3K抑制剂化合物用于体外，原位和体内诊断或治疗哺乳动物细胞，生物体或相关病理条件的方法。 式I化合物包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐。 虚线表示可选的双键，至少一条虚线是双键。 取代基如所述。
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公开(公告)号：US20130065913A1
公开(公告)日：2013-03-14
申请号：US13613952
申请日：2012-09-13
申请人： Toby Jonathan Blench , Christine Edwards , Robert Andrew Heald , Janusz Jozef Kulagowski , Jonathan Mark Sutton , Carmelida Capaldi
发明人： Toby Jonathan Blench , Christine Edwards , Robert Andrew Heald , Janusz Jozef Kulagowski , Jonathan Mark Sutton , Carmelida Capaldi
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
摘要翻译： 式（I）化合物：可用作人中性粒细胞弹性蛋白酶的抑制剂。
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公开(公告)号：US20090227579A1
公开(公告)日：2009-09-10
申请号：US12305404
申请日：2007-06-20
IPC分类号： A61K31/5377 , C07D475/06 , A61K31/4985 , A61P19/02 , A61P19/10 , A61P35/00 , A61P35/04 , C07D401/14 , C07D413/14
CPC分类号： C07D475/06
摘要： The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin K.
摘要翻译： 本发明涉及用于治疗与半胱氨酸蛋白酶活性相关的疾病的化合物和组合物。 这些化合物是半胱氨酸蛋白酶S，K，F，L和B的可逆抑制剂。特别感兴趣的是与组织蛋白酶K.
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