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公开(公告)号：US08637526B2
公开(公告)日：2014-01-28
申请号：US13099179
申请日：2011-05-02
申请人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
发明人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
摘要翻译： 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号：US08623895B2
公开(公告)日：2014-01-07
申请号：US13538698
申请日：2012-06-29
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Joseph P. Lyssikatos , Thomas D. Aicher , Ellen R Laird , John Robinson , Shelley Allen
IPC分类号： A61K31/433 , A61K31/4439 , C07D417/12 , C07D285/12
CPC分类号： C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要翻译： 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。
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公开(公告)号：US08580828B2
公开(公告)日：2013-11-12
申请号：US13586355
申请日：2012-08-15
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtil
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtil
IPC分类号： A61K31/41 , C07D417/04
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
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94.发明申请Methods of Treating a Hyperproliferative Disorder or Inhibiting Cell Growth in a Mammal 有权治疗过度增生性疾病或抑制哺乳动物细胞生长的方法公开(公告)号：US20120277277A1
公开(公告)日：2012-11-01
申请号：US13463487
申请日：2012-05-03
IPC分类号： A61K31/4184 , A61P17/00 , A61P35/00
CPC分类号： C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumour agent or in combination with radiation therapy.
摘要翻译： 公开了抑制哺乳动物异常细胞生长或治疗过度增殖性疾病的方法，包括向哺乳动物施用包含6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑的药物组合物 -5-羧酸（2-羟基 - 乙氧基） - 酰胺或其药学上可接受的盐与有效量的抗肿瘤剂组合或与放射治疗组合。
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公开(公告)号：US08211921B2
公开(公告)日：2012-07-03
申请号：US12356428
申请日：2009-01-20
申请人： James F. Blake , Joseph P. Lyssikatos , Allison L. Marlow , Jeongbeob Seo , Eli M. Wallace , Hong-Woon Yang
发明人： James F. Blake , Joseph P. Lyssikatos , Allison L. Marlow , Jeongbeob Seo , Eli M. Wallace , Hong-Woon Yang
IPC分类号： A61K31/4412 , C07D213/80 , C07D213/82 , A61K31/4965 , C07D241/28
CPC分类号： C07D209/46 , C07D213/80 , C07D213/82 , C07D215/48 , C07D231/56 , C07D237/24 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/04 , C07D401/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, and X are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译： 公开了式及其药学上可接受的盐和前药的化合物，其中R1，R2，R7，R8，R9，W和X如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。 还公开了使用这些化合物治疗哺乳动物中过度增殖疾病的方法和含有这些化合物的药物组合物。
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96.发明授权Compositions comprising N3 alkylated benzimidazole derivatives as MEK inhibitors and methods of use thereof 有权包含N 3烷基化苯并咪唑衍生物作为MEK抑制剂的组合物及其使用方法公开(公告)号：US08193231B2
公开(公告)日：2012-06-05
申请号：US12826158
申请日：2010-06-29
IPC分类号： A61K31/4184
CPC分类号： C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Disclosed are pharmaceutical compositions comprising 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.
摘要翻译： 公开了包含6-（4-溴-2-氯 - 苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基 - 乙氧基） - 酰胺或其药学上可接受的盐 其中。 还公开了使用这种组合物抑制哺乳动物异常细胞生长或治疗过度增殖性疾病的方法。
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97.发明授权Method of treatment using N3 alkylated benzimidazole derivatives as MEK inhibitors 有权使用N 3烷基化苯并咪唑衍生物作为MEK抑制剂的处理方法公开(公告)号：US08193229B2
公开(公告)日：2012-06-05
申请号：US12824521
申请日：2010-06-28
IPC分类号： A61K31/4184
CPC分类号： C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Disclosed are methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula or a pharmaceutically accepted salt thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals.
摘要翻译： 公开了治疗哺乳动物中过度增殖性疾病或与血管发生或血管发生相关的疾病的方法，包括向所述哺乳动物施用有效量的下式化合物或其药学上可接受的盐，其中A，R 1，R 2，R 7， R8和R9如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物中的过度增生性疾病，例如癌症和炎症。
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公开(公告)号：US08178693B2
公开(公告)日：2012-05-15
申请号：US12824559
申请日：2010-06-28
IPC分类号： A61K31/4184 , C07D235/06
CPC分类号： C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
摘要翻译： 公开了式及其药学上可接受的盐和前药的化合物，其中A，R 1，R 2，R 7，R 8和R 9如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物中的过度增生性疾病，例如癌症和炎症。 还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法，以及含有这些化合物的药物组合物。
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![Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors](/abs-image/US/2012/03/20/US08138181B2/abs.jpg.150x150.jpg)
99.发明授权Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors 有权咪唑并[1,2-a]吡啶化合物作为受体酪氨酸激酶抑制剂公开(公告)号：US08138181B2
公开(公告)日：2012-03-20
申请号：US12593879
申请日：2008-03-27
申请人： Shelley Allen , Julie Marie Greschuk , Nicholas C. Kallan , Fredrik P. Marmsäter , Mark C. Munson , James P. Rizzi , John E. Robinson , Stephen T. Schlachter , George T. Topalov , Qian Zhao , Joseph P. Lyssikatos
发明人： Shelley Allen , Julie Marie Greschuk , Nicholas C. Kallan , Fredrik P. Marmsäter , Mark C. Munson , James P. Rizzi , John E. Robinson , Stephen T. Schlachter , George T. Topalov , Qian Zhao , Joseph P. Lyssikatos
IPC分类号： A61K31/5386 , A61K31/437 , A61K31/506 , C07D471/02 , C07D401/14 , C07D498/08 , A61P35/04
CPC分类号： C07D471/04
摘要： Compounds of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5 R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.
摘要翻译： 式I化合物：其中A，B，R 1，R 1a，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有说明书中给出的含义，是受体酪氨酸抑制剂，其可用于治疗由3类和 5类受体酪氨酸激酶。 本发明的具体化合物也被发现是Pim-1的抑制剂。
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公开(公告)号：US20120022043A1
公开(公告)日：2012-01-26
申请号：US13099179
申请日：2011-05-02
申请人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
发明人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
IPC分类号： A61K31/519 , A61K31/5377 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06 , A61P17/00 , A61P25/00 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04
摘要： The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
摘要翻译： 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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