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31. 发明授权

US08455495B2 Pyridazino-pyridinone compounds and methods of use 失效
标题翻译：哒嗪 - 吡啶酮化合物及其使用方法
公开(公告)号：US08455495B2
公开(公告)日：2013-06-04
申请号：US13060663
申请日：2009-08-26
申请人： Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
发明人： Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
IPC分类号： A01N43/58 , A61K31/50 , C07D237/26
CPC分类号： C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, R1, R2, R3, R4, R5, R6, X and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式I，其中A，R 1，R 2，R 3，R 4，R 5，R 6，X和n如本文所定义。本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗p38地图激酶介导的疾病包括类风湿性关节炎，银屑病，慢性阻塞性肺病，疼痛和其它炎性疾病以及中间体和可用于制备式I化合物的方法。

32. 发明授权

US08435987B2 Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof 失效
标题翻译：吡唑并吡啶酮和吡唑并吡嗪酮化合物作为P38调节剂及其使用方法
公开(公告)号：US08435987B2
公开(公告)日：2013-05-07
申请号：US13197322
申请日：2011-08-03
申请人： Liping H. Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
发明人： Liping H. Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
IPC分类号： A61K31/437 , A61K31/4985 , A61K31/5377 , C07D487/04 , C07D471/04 , A61P19/02 , A61P29/00 , A61P19/08 , A61P19/10 , A61P35/00 , A61P1/00 , A61P17/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。该化合物具有通式I，其中A1，A2，B，R1，R2，R4，R5，R6和Z如本文所定义。本发明还包括药物组合物，其包含一种或多种式I化合物，用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣，慢性阻塞性肺病，疼痛和其它炎症性疾病）的这些化合物和组合物的用途以及中间体和可用于制备式I化合物的方法。

33. 发明授权

US08367671B2 Pyrazolo[3.4-B]pyrazine compounds as p38 modulators and methods of use as anti-inflamatory agents 有权
标题翻译：吡唑并[3,4-B]吡嗪化合物作为p38调节剂和用作抗炎剂的方法
公开(公告)号：US08367671B2
公开(公告)日：2013-02-05
申请号：US12933406
申请日：2009-03-19
申请人： Andrew Tasker , Liping H. Pettus , Ryan Wurz
发明人： Andrew Tasker , Liping H. Pettus , Ryan Wurz
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, B, R1, R2, R3, R4, R5 and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式I，其中A1，B，R1，R2，R3，R4，R5和n如本文所定义。本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗p38地图激酶介导的疾病包括类风湿性关节炎，银屑病，慢性阻塞性肺病，疼痛和其它炎性疾病以及中间体和可用于制备式I化合物的方法。

34. 发明申请

US20110275629A1 Pyridazino-pyridinone Compounds and Methods of Use 失效
标题翻译：哒嗪 - 吡啶酮化合物和使用方法
公开(公告)号：US20110275629A1
公开(公告)日：2011-11-10
申请号：US13060663
申请日：2009-08-26
申请人： Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
发明人： Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
IPC分类号： A61K31/5025 , C07D413/14 , A61K31/5377 , A61P19/08 , A61P19/10 , A61P35/00 , A61P27/02 , A61P35/02 , A61P5/48 , A61P19/02 , A61P29/00 , A61P19/06 , A61P11/00 , A61P1/00 , A61P37/08 , A61P25/00 , A61P17/00 , A61P11/06 , A61P21/00 , A61P3/10 , A61P37/06 , A61P25/28 , A61P9/10 , A61P31/00 , A61P31/18 , A61P31/16 , A61P31/14 , A61P31/22 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, R1, R2, R3, R4, R5, R6, X and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式I，其中A，R 1，R 2，R 3，R 4，R 5，R 6，X和n如本文所定义。本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗p38地图激酶介导的疾病包括类风湿性关节炎，银屑病，慢性阻塞性肺病，疼痛和其它炎性疾病以及中间体和可用于制备式I化合物的方法。

35. 发明授权

US07846944B2 Pyrazolo-pyridinone compounds and methods of use thereof 有权
标题翻译：吡唑并吡啶酮化合物及其使用方法
公开(公告)号：US07846944B2
公开(公告)日：2010-12-07
申请号：US12151478
申请日：2008-05-06
申请人： Liping Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
发明人： Liping Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
IPC分类号： C07D487/04 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, B, R1, R2, R3, R4 and R5 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式I，其中A1，A2，A3，A4，B，R1，R2，R3，R4和R5如本文所定义。本发明还包括药物组合物，其包含一种或多种式I化合物，用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣，慢性阻塞性肺病，疼痛和其它炎症性疾病）的这些化合物和组合物的用途以及中间体和可用于制备式I化合物的方法。

36. 发明授权

US07700593B2 Imidazo- and triazolo-pyridine compounds and methods of use thereof 失效
标题翻译：咪唑并 - 三唑并吡啶化合物及其使用方法
公开(公告)号：US07700593B2
公开(公告)日：2010-04-20
申请号：US11973076
申请日：2007-10-05
申请人： Dawei Zhang , Andrew Tasker , Kelvin K. C. Sham , Partha Pratim Chakrabarti , James Richard Falsey , Bradley J. Herberich , Liping H. Pettus , Robert M. Rzasa
发明人： Dawei Zhang , Andrew Tasker , Kelvin K. C. Sham , Partha Pratim Chakrabarti , James Richard Falsey , Bradley J. Herberich , Liping H. Pettus , Robert M. Rzasa
IPC分类号： A61K31/5377 , C07D221/02 , A61K31/496 , A61P29/00 , C07D295/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。该化合物具有通式I，其中A，B，R 1，R 2，R 3和R 4在本文中定义。本发明还包括包含一种或多种式I化合物的药物组合物，这些化合物和组合物用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣和其他炎症疾病）的用途，以及可用于制备式Ⅰ的化合物。

37. 发明授权

US07687643B2 Process for preparing 3,3-dimethylindolines 失效
标题翻译：制备3,3-二甲基吲哚的方法
公开(公告)号：US07687643B2
公开(公告)日：2010-03-30
申请号：US11014184
申请日：2004-12-15
申请人： Andrew Tasker , Shawn Eisenberg , Yuelie Lu
发明人： Andrew Tasker , Shawn Eisenberg , Yuelie Lu
IPC分类号： C07D209/40
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Selected amines 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：选择的胺对于预防和治疗疾病如血管生成介导的疾病是有效的。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。

38. 发明授权

US07652009B2 Substituted heterocycles and methods of use 有权
标题翻译：取代的杂环和使用方法
公开(公告)号：US07652009B2
公开(公告)日：2010-01-26
申请号：US11289659
申请日：2005-11-29
申请人： Tae-Seong Kim , Steven Bellon , Shon Booker , Noel D'Angelo , Celia Dominguez , Ingrid Fellows , Matthew Lee , Longbin Liu , Elizabeth Rainbeau , Aaron C. Siegmund , Andrew Tasker , Ning Xi , Yuan Cheng
发明人： Tae-Seong Kim , Steven Bellon , Shon Booker , Noel D'Angelo , Celia Dominguez , Ingrid Fellows , Matthew Lee , Longbin Liu , Elizabeth Rainbeau , Aaron C. Siegmund , Andrew Tasker , Ning Xi , Yuan Cheng
IPC分类号： A61K31/506 , C07D401/02 , C07D239/22
CPC分类号： C07D401/14 , C07D215/233 , C07D401/12 , C07D409/14 , C07D413/12
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF 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HGF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。

39. 发明申请

US20080249090A1 Substituted pyridone compounds and methods of use 失效
标题翻译：取代的吡啶酮化合物和使用方法
公开(公告)号：US20080249090A1
公开(公告)日：2008-10-09
申请号：US11879830
申请日：2007-07-18
申请人： Essa Hu , Jason Brooks Human , Roxanne Kunz , Andrew Tasker , Ryan White
发明人： Essa Hu , Jason Brooks Human , Roxanne Kunz , Andrew Tasker , Ryan White
IPC分类号： A61K31/5377 , A61K31/517 , C07D471/04 , A61P35/04 , A61P35/00 , C07D403/02
CPC分类号： C07D471/04 , C07D401/04
摘要： The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括能够调节c-kit受体的新一类化合物，因此可用于治疗c-kit介导的疾病，包括各种炎性，纤维化和/或肥大细胞介导的疾病如肥大细胞增多症。这些化合物具有通式I，其中A 0-3和R 6-16在本文中定义。本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

40. 发明申请

US20080161346A1 Compounds and methods of use 失效
标题翻译：化合物和使用方法
公开(公告)号：US20080161346A1
公开(公告)日：2008-07-03
申请号：US12004156
申请日：2007-12-19
申请人： Yuan Cheng , Deborah Choquette , Jean-Christophe Harmange , Andrew Tasker
发明人： Yuan Cheng , Deborah Choquette , Jean-Christophe Harmange , Andrew Tasker
IPC分类号： A61K31/4725 , C07D217/00 , A61K31/47 , A61P29/00
CPC分类号： C07D401/06 , C07D401/14 , C07D417/14
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF 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：选择的化合物对于预防和治疗诸如VEGF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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