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公开(公告)号：US20140088085A1
公开(公告)日：2014-03-27
申请号：US13979634
申请日：2012-01-12
申请人： Laurence E. Burgess , George A. Doherty , C. Todd Eary , Robert D. Groneberg , Zachary Jones , James Jeffry Howbert , Robert Hershberg , Joseph P. Lyssikatos , Hong Woon Yang
发明人： Laurence E. Burgess , George A. Doherty , C. Todd Eary , Robert D. Groneberg , Zachary Jones , James Jeffry Howbert , Robert Hershberg , Joseph P. Lyssikatos , Hong Woon Yang
IPC分类号： C07D223/16 , C07D243/14 , C07D487/04 , C07D401/12
CPC分类号： C07D223/16 , C07D243/14 , C07D401/12 , C07D487/04
摘要： Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.
摘要翻译： 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，纤维化疾病，心血管疾病，感染性疾病，炎症性疾病，移植排斥反应或移植物抗宿主病。
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公开(公告)号：US20110092485A1
公开(公告)日：2011-04-21
申请号：US12859178
申请日：2010-08-18
申请人： James Jeffry Howbert , Gregory Dietsch , Robert Hershberg , Laurence E. Burgess , Joseph P. Lyssikatos , Brad Newhouse , Hong Woon Yang
发明人： James Jeffry Howbert , Gregory Dietsch , Robert Hershberg , Laurence E. Burgess , Joseph P. Lyssikatos , Brad Newhouse , Hong Woon Yang
IPC分类号： A61K31/55 , C07D223/16 , A61P11/06 , A61P37/02 , A61P35/00
CPC分类号： A61K31/55 , C07D223/14 , C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/04 , C07D405/10
摘要： Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
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公开(公告)号：US08691809B2
公开(公告)日：2014-04-08
申请号：US12859178
申请日：2010-08-18
申请人： James Jeffry Howbert , Gregory Dietsch , Robert Hershberg , Laurence E. Burgess , Joseph P. Lyssikatos , Brad Newhouse , Hong Woon Yang
发明人： James Jeffry Howbert , Gregory Dietsch , Robert Hershberg , Laurence E. Burgess , Joseph P. Lyssikatos , Brad Newhouse , Hong Woon Yang
IPC分类号： A61K31/55 , C07D223/16 , A61P11/06 , A61P37/02 , A61P35/00
CPC分类号： A61K31/55 , C07D223/14 , C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/04 , C07D405/10
摘要： Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
摘要翻译： 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，感染性疾病，炎性疾病，移植物排斥反应和移植物宿主病。
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公开(公告)号：US07893065B2
公开(公告)日：2011-02-22
申请号：US12186202
申请日：2008-08-05
申请人： Allison L. Marlow , Eli M. Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli M. Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： C07D237/20 , A61K31/50 , A61P29/00 , A61P35/00
CPC分类号： C07D213/80 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/5025 , A61K31/5377 , A61K45/06 , C07D209/46 , 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 , A61K2300/00
摘要： Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and W are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative and inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译： 公开了式I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8，R9和W如说明书中所定义。 这些化合物是MEK抑制剂，并且可用于治疗过度增殖性疾病，例如癌症和炎症，以及哺乳动物中的炎性病症。 还公开了使用这些化合物治疗哺乳动物中过度增生和炎性疾病的方法和含有这些化合物的药物组合物。
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公开(公告)号：US20100063053A1
公开(公告)日：2010-03-11
申请号：US12577312
申请日：2009-10-12
申请人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： A61K31/50 , C07D213/72 , A61K31/44 , C07D237/02 , A61P35/00 , A61P29/00
CPC分类号： C07D213/78 , 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 Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y 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I和V的化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8和R9，W，X和Y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性疾病的方法和含有这些化合物的药物组合物。
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公开(公告)号：US07598383B2
公开(公告)日：2009-10-06
申请号：US10992612
申请日：2004-11-18
申请人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： C07D487/04 , A61K31/44
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 I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specifications. 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I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8和R9，W，X和Y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性疾病的方法和含有这些化合物的药物组合物。
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公开(公告)号：US20090215834A1
公开(公告)日：2009-08-27
申请号：US12186273
申请日：2008-08-05
申请人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： A61K31/4412 , C07D213/78 , A61P29/00 , A61P35/04
CPC分类号： C07D213/80 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/5025 , A61K31/5377 , A61K45/06 , C07D209/46 , 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 , A61K2300/00
摘要： Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.
摘要翻译： 公开了式V的化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8和R9以及W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，如癌症和炎症以及炎性病症。 还公开了使用这些化合物治疗哺乳动物的过度增殖性疾病和炎性病症的方法以及含有这些化合物的药物组合物。
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公开(公告)号：US08431574B2
公开(公告)日：2013-04-30
申请号：US12356441
申请日：2009-01-20
IPC分类号： A01N43/58 , A61K31/50 , C07D237/00
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 Formulas III and IV and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and R10 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III和IV的化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 7，R 8，R 9和R 10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性疾病的方法和含有这些化合物的药物组合物。
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9.发明授权Crystalline forms of 2-(2-flouro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide 失效2-（2-氟-4-碘苯基氨基）-N-（2-羟基乙氧基）-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-甲酰胺的结晶形式公开(公告)号：US08299076B2
公开(公告)日：2012-10-30
申请号：US11914433
申请日：2006-05-17
申请人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , Jim Blake , Richard Anthony Storey , Rebecca Jane Booth , John David Pittam , John Leonard , Mark Richard Fielding
发明人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , Jim Blake , Richard Anthony Storey , Rebecca Jane Booth , John David Pittam , John Leonard , Mark Richard Fielding
IPC分类号： A01N43/58 , A01N43/54 , A01N43/40 , C07D401/00 , C07D239/02 , C07D487/00 , A61P35/00 , A61P29/00
CPC分类号： C07D237/24 , C07D213/80 , C07D213/82 , C07D213/84 , C07D213/85
摘要： Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide 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： 公开了可用于治疗过度增殖的2-（2-氟-4-碘苯基氨基）-N-（2-羟基乙氧基）-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-甲酰胺的结晶形式 疾病，如癌症和炎症，哺乳动物和炎症病症。 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和含有这些化合物的药物组合物。
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10.发明申请Combinations Comprising Heterocyclic Inhibitors of MEK and Methods of Use Thereof 审中-公开包含MEK的杂环抑制剂的组合及其使用方法公开(公告)号：US20120263679A1
公开(公告)日：2012-10-18
申请号：US13484093
申请日：2012-05-30
申请人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： A61K31/4412 , A61K31/7088 , A61K39/395 , A61K31/4704 , A61K38/17 , A61P35/00 , A61P31/04 , A61P9/00 , A61P5/28 , A61P37/00 , A61K38/21 , A61K48/00
CPC分类号： C07D213/80 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/5025 , A61K31/5377 , A61K45/06 , C07D209/46 , 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 , A61K2300/00
摘要： Disclosed are combinations comprising (a) a compound of the Formula: wherein R1, R2, R7, R8, R9 and W are as defined in the specification, and (b) at least one additional therapeutic agent. Such combinations are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such combinations in the treatment of hyperproliferative diseases and inflammatory conditions in mammals.
摘要翻译： 公开了包含（a）下式化合物的组合：其中R 1，R 2，R 7，R 8，R 9和W如说明书中所定义，和（b）至少一种另外的治疗剂。 这样的组合可用于治疗过度增生性疾病，例如癌症和炎症，以及哺乳动物中的炎性病症。 还公开了使用这些组合来治疗哺乳动物中过度增殖性疾病和炎性病症的方法。
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