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公开(公告)号：US07196104B2
公开(公告)日：2007-03-27
申请号：US10631423
申请日：2003-07-30
申请人： Benny C. Askew, Jr. , Frenel F. De Morin , Andrew Hague , Ellen Laber , Aiwen Li , Gang Liu , Patricia Lopez , Rana Nomak , Vincent Santora , Christopher Tegley , Kevin Yang
发明人： Benny C. Askew, Jr. , Frenel F. De Morin , Andrew Hague , Ellen Laber , Aiwen Li , Gang Liu , Patricia Lopez , Rana Nomak , Vincent Santora , Christopher Tegley , Kevin Yang
IPC分类号： A61K31/44 , C07D417/12
CPC分类号： C07D213/75 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/06 , C07D471/04 , C07D491/10
摘要： Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译： 所选择的新型尿素化合物对于预防和治疗诸如细胞增殖或细胞凋亡介导的疾病的疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及stoke，癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号：US20150158903A1
公开(公告)日：2015-06-11
申请号：US14343603
申请日：2012-09-07
申请人： Ravindra B. Upasani , Boyd L. Harrison , Benny C. Askew, Jr. , Jean-Cosme Dodart , Francesco G. Salituro , Albert J. Robichaud
发明人： Ravindra B. Upasani , Boyd L. Harrison , Benny C. Askew, Jr. , Jean-Cosme Dodart , Francesco G. Salituro , Albert J. Robichaud
CPC分类号： C07J41/00 , C07J1/00 , C07J1/0029 , C07J3/00 , C07J7/007 , C07J9/00 , C07J9/005 , C07J31/003 , C07J31/006 , C07J41/0005 , C07J41/0011 , C07J41/0055 , C07J43/003
摘要： Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L1, L2, L3, X1, X2, Y, Rz4, Rz5, Rz6, n, R1, R2, R3a, R3b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R14, R17, R19, R20, R23a, R23b, and R24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
摘要翻译： 根据式（I）和其药学上可接受的盐提供化合物，其中Z是式（i），（ii），（iii），（iv）或（v）的基团，其中L 1， L3，X1，X2，Y，Rz4，Rz5，Rz6，n，R1，R2，R3a，R3b，R4a，R4b，R6a，R6b，R7a，R7b，R11a，R11b，R14，R17，R19，R20， R23b和R24如本文所定义，及其药物组合物。 本发明的化合物可用于预防和治疗哺乳动物中各种CNS相关病症。
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公开(公告)号：US08853391B2
公开(公告)日：2014-10-07
申请号：US13140357
申请日：2009-12-03
申请人： Bayard R. Huck , Amanda E. Sutton , Benny C. Askew, Jr. , Christopher Charles Victor Jones , Garry R. Smith , Nadia Brugger
发明人： Bayard R. Huck , Amanda E. Sutton , Benny C. Askew, Jr. , Christopher Charles Victor Jones , Garry R. Smith , Nadia Brugger
IPC分类号： C07D401/14 , C07D413/14 , C07D471/14 , C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.
摘要翻译： 公开了联吡啶基 - 吡咯衍生物化合物及其类似物，包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗适于蛋白激酶信号转导抑制，调节和/或调节的疾病。
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14.发明申请公开(公告)号：US20110294801A1
公开(公告)日：2011-12-01
申请号：US13062413
申请日：2009-09-03
申请人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
发明人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
IPC分类号： A61K31/519 , C07D487/06 , C07D487/16 , A61P31/00 , A61K31/5377 , A61P35/00 , A61P37/00 , A61P29/00 , C07D498/06 , C07D498/16
CPC分类号： C07D498/08 , C07D487/08 , C07D487/18 , C07D498/18 , C07D513/08 , C07D513/18 , C07D515/08
摘要： Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
摘要翻译： 公开了抑制蛋白激酶的大环衍生物化合物以及包含这些化合物的药物组合物及其合成方法。 这些化合物可用于治疗由不稳定和/或受干扰的激酶活性如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。
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公开(公告)号：US07772233B2
公开(公告)日：2010-08-10
申请号：US11788028
申请日：2007-04-18
申请人： Andreas Goutopoulos , Benny C. Askew, Jr. , Nhut Kiet Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
发明人： Andreas Goutopoulos , Benny C. Askew, Jr. , Nhut Kiet Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
IPC分类号： C07D237/12 , C07D413/04 , A61K31/50 , A61K31/5355 , A61P35/00 , A61P29/00 , C07D213/74 , C07D405/12 , C07D213/57
CPC分类号： C07D213/84 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D237/24 , C07D405/12
摘要： The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
摘要翻译： 本发明提供式（I）的新的芳基氨基N-杂芳基MEK抑制剂：这些化合物是可用于治疗过度增殖性疾病如癌症和炎症的MEK抑制剂。 还公开了哺乳动物中过度增殖性疾病的治疗，以及含有这些化合物的药物组合物。
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公开(公告)号：US07531553B2
公开(公告)日：2009-05-12
申请号：US10804915
申请日：2004-03-19
申请人： Lucian V. Di Pietro , Jean-Christophe Harmange , Benny C. Askew, Jr. , Daniel Elbaum , Julie Germain , Gregory J. Habgood , Joseph L. Kim , Vinod F. Patel , Michele Potashman , Simon van der Plas
发明人： Lucian V. Di Pietro , Jean-Christophe Harmange , Benny C. Askew, Jr. , Daniel Elbaum , Julie Germain , Gregory J. Habgood , Joseph L. Kim , Vinod F. Patel , Michele Potashman , Simon van der Plas
IPC分类号： A61K31/47 , C07D215/00
CPC分类号： C07D401/12 , C07D235/30 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译： 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号：US08889719B2
公开(公告)日：2014-11-18
申请号：US13785120
申请日：2013-03-05
IPC分类号： A61K31/455 , C07D213/46 , C07D213/82 , C07D213/79 , C07D213/81
CPC分类号： C07D213/82 , C07D213/79 , C07D213/81
摘要： The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
摘要翻译： 本发明提供根据式（I）的新化合物，其用于治疗过度增生性疾病如癌症，再狭窄和炎症的制备和用途。
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公开(公告)号：US08404725B2
公开(公告)日：2013-03-26
申请号：US13057052
申请日：2009-07-27
IPC分类号： A61K31/455 , C07D213/46
CPC分类号： C07D213/82 , C07D213/79 , C07D213/81
摘要： The invention provides novel substituted phenylamino isonicotinamide compounds (I), pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined in the specification. Said compounds are MEK inhibitors useful in the treatment of hyperproliferative diseases related to the hyperactivity of MEK, such as restenosis, as well as diseases modulated by the MEK cascade, such as cancer and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
摘要翻译： 本发明提供新的取代的苯基氨基异烟酰胺化合物（I），其药学上可接受的盐，溶剂合物或前药，其中X，R 1，R 2，R 3，R 4，R 5和R 6如说明书中所定义。 所述化合物是可用于治疗与MEK的多动症相关的过度增生性疾病的MEK抑制剂，例如再狭窄，以及由MEK级联调节的疾病，例如癌症和炎症。 还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。
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公开(公告)号：US20110184032A1
公开(公告)日：2011-07-28
申请号：US13057052
申请日：2009-07-27
IPC分类号： A61K31/44 , C07D213/74 , A61P35/00 , A61P29/00 , A61P1/18 , A61P13/12 , A61P9/00 , A61P17/06 , A61P17/00 , A61P3/10 , A61P27/02 , A61P35/02
CPC分类号： C07D213/82 , C07D213/79 , C07D213/81
摘要： The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
摘要翻译： 本发明提供根据式（I）的新化合物，其用于治疗过度增生性疾病如癌症，再狭窄和炎症的制备和用途。
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20.发明授权Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use 有权取代的2,3-二氢-1,5-异吲哚-1-酮衍生物及其使用方法公开(公告)号：US07320992B2
公开(公告)日：2008-01-22
申请号：US10926238
申请日：2004-08-24
申请人： Christopher Tegley , Jeffrey A. Adams , Benny C. Askew, Jr. , Michael Croghan , Daniel Elbaum , Julie Germain , Gregory J. Habgood , Scott Harried , Aiwen Li , Nobuko Nishimura , Rana Nomak , Andrew Tasker , Kevin Yang
发明人： Christopher Tegley , Jeffrey A. Adams , Benny C. Askew, Jr. , Michael Croghan , Daniel Elbaum , Julie Germain , Gregory J. Habgood , Scott Harried , Aiwen Li , Nobuko Nishimura , Rana Nomak , Andrew Tasker , Kevin Yang
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译： 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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