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公开(公告)号：US08030354B2
公开(公告)日：2011-10-04
申请号：US12287036
申请日：2008-10-03
申请人： Sean P. Brown , Qiong Cao , Paul John Dransfield , Xiaohui Du , Zice Fu , Jonathan Houze , Xian Yun Jiao , Yong-Jae Kim , Todd J. Kohn , SuJen Lai , An-Rong Li , Daniel Lin , Jiwen Liu , Jian Luo , Julio C. Medina , Jeffrey D. Reagan , Vatee Pattaropong , Margrit Schwarz , Wang Shen , Yongli Su , Gayathri Swaminath , Marc Vimolratana , Yingcai Wang , Yumei Xiong , Li Yang , Ming Yu , Jie Zhang , Liusheng Zhu
发明人： Sean P. Brown , Qiong Cao , Paul John Dransfield , Xiaohui Du , Zice Fu , Jonathan Houze , Xian Yun Jiao , Yong-Jae Kim , Todd J. Kohn , SuJen Lai , An-Rong Li , Daniel Lin , Jiwen Liu , Jian Luo , Julio C. Medina , Jeffrey D. Reagan , Vatee Pattaropong , Margrit Schwarz , Wang Shen , Yongli Su , Gayathri Swaminath , Marc Vimolratana , Yingcai Wang , Yumei Xiong , Li Yang , Ming Yu , Jie Zhang , Liusheng Zhu
IPC分类号： A61K31/192 , C07C53/134
CPC分类号： C07C323/62 , C07C59/68 , C07C59/72 , C07C217/54 , C07C217/62 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D213/64 , C07D309/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译： 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式I：其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。
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2.发明申请公开(公告)号：US20100298367A1
公开(公告)日：2010-11-25
申请号：US12863578
申请日：2009-03-04
申请人： Sean P. Brown , Paul J. Dransfield , Jonathan Houze , Todd J. Kohn , Jiwen Liu , Julio Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Ming Yu , Liusheng Zhu
发明人： Sean P. Brown , Paul J. Dransfield , Jonathan Houze , Todd J. Kohn , Jiwen Liu , Julio Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Ming Yu , Liusheng Zhu
IPC分类号： A61K31/216 , A61K31/44 , A61K31/192 , C07D213/63 , C07D213/55 , C07C69/007 , C07C59/62 , A61P9/12 , A61P3/10 , A61P35/04 , A61P13/12 , A61P3/00 , A61P3/06 , A61P9/10 , A61P9/00
CPC分类号： C07C59/72
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译： 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式I或通式III：其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。
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公开(公告)号：US20090137561A1
公开(公告)日：2009-05-28
申请号：US12287036
申请日：2008-10-03
申请人： Sean P. Brown , Qiong Cao , Paul John Dransfield , Xiaohui Du , Jonathan Houze , Xian Yun Jiao , Yong-Jae Kim , Todd J. Kohn , SuJen Lai , An-Rong Li , Daniel Lin , Jian Luo , Julio C. Medina , Jeffrey D. Reagan , Vatee Pattaropong , Margrit Schwarz , Wang Shen , Yongli Su , Gayathri Swaminath , Marc Vimolratana , Xiang Wang , Yumei Xiong , Li Yang , Ming Yu , Jie Zhang , Liusheng Zhu
发明人： Sean P. Brown , Qiong Cao , Paul John Dransfield , Xiaohui Du , Jonathan Houze , Xian Yun Jiao , Yong-Jae Kim , Todd J. Kohn , SuJen Lai , An-Rong Li , Daniel Lin , Jian Luo , Julio C. Medina , Jeffrey D. Reagan , Vatee Pattaropong , Margrit Schwarz , Wang Shen , Yongli Su , Gayathri Swaminath , Marc Vimolratana , Xiang Wang , Yumei Xiong , Li Yang , Ming Yu , Jie Zhang , Liusheng Zhu
IPC分类号： C07C59/48 , A61K31/192 , A61K31/235 , C07C69/76 , C07D309/00 , A61K31/351 , C07D211/20 , A61K31/445 , A61K31/44 , A61K31/55 , C07D223/04 , A61P7/00
CPC分类号： C07C323/62 , C07C59/68 , C07C59/72 , C07C217/54 , C07C217/62 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D213/64 , C07D309/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
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公开(公告)号：US08765940B2
公开(公告)日：2014-07-01
申请号：US13377210
申请日：2010-06-25
申请人： Matthew Brown , Yi Chen , Timothy David Cushing , Felix Gonzalez Lopez De Turiso , Xiao He , Todd J. Kohn , Julia Winslow Lohman , Vatee Pattaropong , Jennifer Seganish , Youngsook Shin , Jillian L. Simard
发明人： Matthew Brown , Yi Chen , Timothy David Cushing , Felix Gonzalez Lopez De Turiso , Xiao He , Todd J. Kohn , Julia Winslow Lohman , Vatee Pattaropong , Jennifer Seganish , Youngsook Shin , Jillian L. Simard
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/107 , C07D491/20 , C07D513/04
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/107 , C07D491/113 , C07D491/20 , C07D495/10 , C07D513/04
摘要： Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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5.发明授权公开(公告)号：US08450522B2
公开(公告)日：2013-05-28
申请号：US12863578
申请日：2009-03-04
申请人： Sean P. Brown , Paul J. Dransfield , Jonathan Houze , Todd J. Kohn , Jiwen Liu , Julio Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Ming Yu , Liusheng Zhu
发明人： Sean P. Brown , Paul J. Dransfield , Jonathan Houze , Todd J. Kohn , Jiwen Liu , Julio Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Ming Yu , Liusheng Zhu
IPC分类号： C07C63/00 , A61K31/185
CPC分类号： C07C59/72
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译： 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式I或通式III：其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。
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公开(公告)号：US20100075974A1
公开(公告)日：2010-03-25
申请号：US12613418
申请日：2009-11-05
申请人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , Xian Yun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
发明人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , Xian Yun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
IPC分类号： A61K31/498 , C07D261/06 , A61K31/42 , C07D277/22 , A61K31/426 , C07D271/06 , A61K31/4245 , C07D413/02 , A61K31/443 , C07D241/36 , A61P3/10 , A61P9/00
CPC分类号： C07D261/08 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译： 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式I：其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。
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公开(公告)号：US06284756B1
公开(公告)日：2001-09-04
申请号：US09423166
申请日：2000-01-21
申请人： Nickolay Y Chirgadze , Richard W Harper , Todd J Kohn , Ho-Shen Lin , Jefferson R McCowan , Alan D Palkowitz , Daniel J Sall , Gerald F Smith , Kumiko Takeuchi , Michael R Wiley , Minsheng Zhang
发明人： Nickolay Y Chirgadze , Richard W Harper , Todd J Kohn , Ho-Shen Lin , Jefferson R McCowan , Alan D Palkowitz , Daniel J Sall , Gerald F Smith , Kumiko Takeuchi , Michael R Wiley , Minsheng Zhang
IPC分类号： A61K314025
CPC分类号： C07D333/58 , C07D333/56 , C07D409/10 , C07D409/12
摘要： This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
摘要翻译： 本申请涉及本文定义的式I（及其药学上可接受的盐）的新型化合物，其制备方法和中间体，包含式I的新型化合物的药物制剂以及式I化合物作为凝血酶抑制剂的用途 。
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公开(公告)号：US08003648B2
公开(公告)日：2011-08-23
申请号：US12613418
申请日：2009-11-05
申请人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , XianYun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
发明人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , XianYun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
IPC分类号： A61K31/498 , A61K31/42 , A61K31/426 , A61K31/4245 , A61K31/443 , C07D261/06 , C07D277/22 , C07D271/06 , C07D413/02 , C07D241/36 , A61P3/10 , A61P9/00
CPC分类号： C07D261/08 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译： 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式I：其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。
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公开(公告)号：US20090111859A1
公开(公告)日：2009-04-30
申请号：US12082645
申请日：2008-04-10
申请人： Sean P. Brown , Paul Dransfield , Zice Fu , Jonathan Houze , Xian Yun Jiao , Todd J. Kohn , Vatee Pattaropong , Marc Vimolratana , Michael J. Schmitt
发明人： Sean P. Brown , Paul Dransfield , Zice Fu , Jonathan Houze , Xian Yun Jiao , Todd J. Kohn , Vatee Pattaropong , Marc Vimolratana , Michael J. Schmitt
IPC分类号： C07C59/68 , C07D261/08 , A61K31/192 , A61K31/42 , C12N5/06 , A61K31/426 , A61K31/155 , A61P35/00 , A61P3/00 , A61P3/10 , A61P9/00
CPC分类号： C07C59/68 , C07C59/72 , C07D261/08
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
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公开(公告)号：US20120094972A1
公开(公告)日：2012-04-19
申请号：US13377210
申请日：2010-06-25
申请人： Matthew Brown , Yi Chen , Timothy David Cushing , Felix Gonzalez Lopez De Turiso , Xiao He , Todd J. Kohn , Julia Winslow Lohman , Vatee Pattaropong , Jennifer Seganish , Youngsook Shin , Jillian L. Simard
发明人： Matthew Brown , Yi Chen , Timothy David Cushing , Felix Gonzalez Lopez De Turiso , Xiao He , Todd J. Kohn , Julia Winslow Lohman , Vatee Pattaropong , Jennifer Seganish , Youngsook Shin , Jillian L. Simard
IPC分类号： A61K31/5415 , C07D491/107 , C07D471/04 , C07D401/14 , C07D491/20 , C07D473/00 , C07D417/14 , C07D513/04 , A61K31/5377 , A61K31/506 , A61K31/4709 , A61K31/52 , A61K31/538 , A61P19/08 , A61P19/02 , A61P27/02 , A61P29/00 , A61P17/06 , A61P1/00 , A61P13/10 , A61P17/00 , A61P35/00 , C07D413/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/107 , C07D491/113 , C07D491/20 , C07D495/10 , C07D513/04
摘要： Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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