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公开(公告)号：US20110137028A1
公开(公告)日：2011-06-09
申请号：US12910920
申请日：2010-10-25
申请人： Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Gingsee Lee , Garrick Packard , Jingjing Zhao , Patrick Anthony Jokiel , Deborah Mortensen , Jennifer Riggs , Juan Antonio Gamboa , Maria Georges Beauchamps , Matthew Michael Kreilein , Mohit Atul Kothare , Sophie Perrin-Ninkovic , Philip Pye , William Wei-Hwa Leong , Jan Elsner
发明人： Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Gingsee Lee , Garrick Packard , Jingjing Zhao , Patrick Anthony Jokiel , Deborah Mortensen , Jennifer Riggs , Juan Antonio Gamboa , Maria Georges Beauchamps , Matthew Michael Kreilein , Mohit Atul Kothare , Sophie Perrin-Ninkovic , Philip Pye , William Wei-Hwa Leong , Jan Elsner
IPC分类号： C07D487/04 , C07D498/14
CPC分类号： C07D471/04 , C07D241/20 , C07D487/04 , C07D498/14 , C07D519/00
摘要： Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.
摘要翻译： 本文提供了制备具有以下结构的杂芳基化合物的方法：其中R 1 -R 4如本文所定义。 杂芳基化合物可用于治疗或预防癌症，炎症状况，免疫学条件，神经变性疾病，糖尿病，肥胖症，神经障碍，年龄相关疾病或心血管疾病。
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公开(公告)号：US08569494B2
公开(公告)日：2013-10-29
申请号：US12910920
申请日：2010-10-25
申请人： Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Gingsee Lee , Garrick Packard , Jingjing Zhao , Patrick Anthony Jokiel , Deborah Mortensen , Jennifer Riggs , Juan Antonio Gamboa , Marie Georges Beauchamps , Matthew Michael Kreilein , Mohit Atul Kothare , Sophie Perrin-Ninkovic , Philip James Pye , William Wei-Hwa Leong , Jan Elsner , Anusuya Choudhury
发明人： Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Gingsee Lee , Garrick Packard , Jingjing Zhao , Patrick Anthony Jokiel , Deborah Mortensen , Jennifer Riggs , Juan Antonio Gamboa , Marie Georges Beauchamps , Matthew Michael Kreilein , Mohit Atul Kothare , Sophie Perrin-Ninkovic , Philip James Pye , William Wei-Hwa Leong , Jan Elsner , Anusuya Choudhury
IPC分类号： C07D471/00
CPC分类号： C07D471/04 , C07D241/20 , C07D487/04 , C07D498/14 , C07D519/00
摘要： Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.
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![PYRAZINO[2,3-b]PYRAZINE mTOR KINASE INHIBITOR FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY](/abs-image/US/2012/03/22/US20120071658A1/abs.jpg.150x150.jpg)
3.发明申请PYRAZINO[2,3-b]PYRAZINE mTOR KINASE INHIBITOR FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY 有权对于与mTOR / PI3K / AKT PATHWAY相关的肿瘤学指征和疾病的吡嗪并[2,3-b]吡嗪mTOR激酶抑制剂公开(公告)号：US20120071658A1
公开(公告)日：2012-03-22
申请号：US13295533
申请日：2011-11-14
申请人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14 , C07D498/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
摘要翻译： 本文提供具有以下结构的杂芳基化合物：其中R 1 -R 4如本文所定义，包含有效量的杂芳基化合物的组合物以及用于治疗或预防癌症，炎症状况，免疫学条件，神经变性疾病，糖尿病，肥胖症，神经系统疾病 疾病，年龄相关疾病或心血管疾病，包括向有需要的患者施用有效量的杂芳基化合物。
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![Pyrazino[2,3-b]pyrazine mTOR kinase inhibitor for oncology indications and diseases associated with the mTOR/PI3K/AKT pathway](/abs-image/US/2013/08/13/US08507492B2/abs.jpg.150x150.jpg)
4.发明授权Pyrazino[2,3-b]pyrazine mTOR kinase inhibitor for oncology indications and diseases associated with the mTOR/PI3K/AKT pathway 有权吡嗪并[2,3-b]吡嗪mTOR激酶抑制剂与mTOR / PI3K / AKT途径相关的肿瘤适应症和疾病公开(公告)号：US08507492B2
公开(公告)日：2013-08-13
申请号：US13295513
申请日：2011-11-14
申请人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
IPC分类号： A61K31/497
CPC分类号： C07D487/04 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14 , C07D498/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
摘要翻译： 本文提供具有以下结构的杂芳基化合物：其中R 1 -R 4如本文所定义，包含有效量的杂芳基化合物的组合物以及用于治疗或预防癌症，炎症状况，免疫学条件，神经变性疾病，糖尿病，肥胖症，神经系统疾病 疾病，年龄相关疾病或心血管疾病，包括向有需要的患者施用有效量的杂芳基化合物。
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![Pyrazino[2,3-b]pyrazine mTOR kinase inhibitor for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway](/abs-image/US/2013/07/23/US08492381B2/abs.jpg.150x150.jpg)
5.发明授权Pyrazino[2,3-b]pyrazine mTOR kinase inhibitor for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway 有权吡嗪并[2,3-b]吡嗪mTOR激酶抑制剂与mTOR / PI3K / Akt途径相关的肿瘤适应症和疾病公开(公告)号：US08492381B2
公开(公告)日：2013-07-23
申请号：US13295533
申请日：2011-11-14
申请人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
IPC分类号： A61K31/497
CPC分类号： C07D487/04 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14 , C07D498/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
摘要翻译： 本文提供具有以下结构的杂芳基化合物：其中R 1 -R 4如本文所定义，包含有效量的杂芳基化合物的组合物以及用于治疗或预防癌症，炎症状况，免疫学条件，神经变性疾病，糖尿病，肥胖症，神经系统疾病 疾病，年龄相关疾病或心血管疾病，包括向有需要的患者施用有效量的杂芳基化合物。
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![PYRAZINO[2,3-b]PYRAZINE mTOR KINASE INHIBITOR FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY](/abs-image/US/2012/03/08/US20120059164A1/abs.jpg.150x150.jpg)
公开(公告)号：US20120059164A1
公开(公告)日：2012-03-08
申请号：US13295513
申请日：2011-11-14
申请人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14 , C07D498/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
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7.发明申请mTOR KINASE INHIBITORS FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY 有权与mTOR / PI3K / AKT PATHWAY相关的肿瘤学指征和疾病的mTOR激酶抑制剂公开(公告)号：US20100216781A1
公开(公告)日：2010-08-26
申请号：US12605791
申请日：2009-10-26
申请人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
IPC分类号： A61K31/4985 , C07D487/04 , C07D487/10 , C07D498/14 , A61K31/5377 , A61K31/5383 , A61P35/00 , A61P29/00 , A61P37/00 , A61P25/00 , A61P3/10 , A61P3/04 , A61P9/00 , A61P19/02 , A61P11/00 , C12N9/99 , A61P1/00
CPC分类号： C07D487/04 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14 , C07D498/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
摘要翻译： 本文提供具有以下结构的杂芳基化合物：其中R 1 -R 4如本文所定义，包含有效量的杂芳基化合物的组合物以及用于治疗或预防癌症，炎症状况，免疫学条件，神经变性疾病，糖尿病，肥胖症，神经系统疾病 疾病，年龄相关疾病或心血管疾病，包括向有需要的患者施用有效量的杂芳基化合物。
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![Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway](/abs-image/US/2012/02/07/US08110578B2/abs.jpg.150x150.jpg)
8.发明授权Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway 有权吡嗪并[2,3-b]吡嗪mTOR激酶抑制剂用于肿瘤适应症和与mTOR / PI3K / Akt途径相关的疾病公开(公告)号：US08110578B2
公开(公告)日：2012-02-07
申请号：US12605791
申请日：2009-10-26
申请人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Fultz , Rama K. Narla , Sabita Sankar , Jan Elsner
IPC分类号： A61K31/497
CPC分类号： C07D487/04 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14 , C07D498/14
摘要： Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
摘要翻译： 本文提供具有以下结构的杂芳基化合物：其中R 1 -R 4如本文所定义，包含有效量的杂芳基化合物的组合物以及用于治疗或预防癌症，炎症状况，免疫学条件，神经变性疾病，糖尿病，肥胖症，神经系统疾病 疾病，年龄相关疾病或心血管疾病，包括向有需要的患者施用有效量的杂芳基化合物。
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9.发明申请AMINOTRIAZOLOPYRIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH 有权氨基三唑基吡啶类，其组合物及其处理方法公开(公告)号：US20100093698A1
公开(公告)日：2010-04-15
申请号：US12555018
申请日：2009-09-08
申请人： Sogole Bahmanyar , R.J. Bates , Kate Blease , Andrew Antony Calabrese , Thomas Oran Daniel , Mercedes Delgado , Jan Elsner , Paul Erdman , Bruce Fahr , Gregory Ferguson , Branden Lee , Lisa Nadolny , Garrick Packard , Patrick Papa , Veronique Plantevin-Krenitsky , Jennifer Riggs , Patricia Rohane , Sabita Sankar , John Sapienza , Yoshitaka Satoh , Victor Sloan , Randall Stevens , Lida Tehrani , Jayashree Tikhe , Eduardo Torres , Andrew Wallace , Brandon Wade Whitefield , Jingjing Zhao
发明人： Sogole Bahmanyar , R.J. Bates , Kate Blease , Andrew Antony Calabrese , Thomas Oran Daniel , Mercedes Delgado , Jan Elsner , Paul Erdman , Bruce Fahr , Gregory Ferguson , Branden Lee , Lisa Nadolny , Garrick Packard , Patrick Papa , Veronique Plantevin-Krenitsky , Jennifer Riggs , Patricia Rohane , Sabita Sankar , John Sapienza , Yoshitaka Satoh , Victor Sloan , Randall Stevens , Lida Tehrani , Jayashree Tikhe , Eduardo Torres , Andrew Wallace , Brandon Wade Whitefield , Jingjing Zhao
IPC分类号： A61K31/437 , C07D471/02 , A61K31/5377 , A61K31/497 , A61K31/55
CPC分类号： C07D471/04 , C07D519/00
摘要： Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.
摘要翻译： 本文提供了式（I）的杂芳基化合物：其中R 1和R 2如本文所定义，包含有效量的杂芳基化合物的组合物和用于治疗或预防炎性病症或癌症的方法，以及可通过抑制激酶治疗或预防的病症 或激酶途径，其包括向有需要的受试者施用有效量的杂芳基化合物。
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10.发明申请AMINOTRIAZOLOPYRIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH 审中-公开氨基三唑基吡啶类，其组合物及其处理方法公开(公告)号：US20130005707A1
公开(公告)日：2013-01-03
申请号：US13609412
申请日：2012-09-11
申请人： Sogole Bahmanyar , R.J. Bates , Kate Blease , Andrew Antony Calabrese , Thomas Oran Daniel , Mercedes Delgado , Jan Elsner , Paul Erdman , Bruce Fahr , Gregory Ferguson , Branden Lee , Lisa Nadolny , Garrick Packard , Patrick Papa , Veronique Plantevin-Krenitsky , Jennifer Riggs , Patricia Rohane , Sabita Sankar , John Sapienza , Yoshitaka Satoh , Victor Sloan , Randall Stevens , Lida Tehrani , Jayashree Tikhe , Eduardo Torres , Andrew Wallace , Brandon Wade Whitefield , Jingjing Zhao
发明人： Sogole Bahmanyar , R.J. Bates , Kate Blease , Andrew Antony Calabrese , Thomas Oran Daniel , Mercedes Delgado , Jan Elsner , Paul Erdman , Bruce Fahr , Gregory Ferguson , Branden Lee , Lisa Nadolny , Garrick Packard , Patrick Papa , Veronique Plantevin-Krenitsky , Jennifer Riggs , Patricia Rohane , Sabita Sankar , John Sapienza , Yoshitaka Satoh , Victor Sloan , Randall Stevens , Lida Tehrani , Jayashree Tikhe , Eduardo Torres , Andrew Wallace , Brandon Wade Whitefield , Jingjing Zhao
IPC分类号： A61K31/437 , A61K31/5377 , A61K31/506 , A61K31/4545 , A61K31/496 , A61K31/551 , A61P37/00 , A61P37/08 , A61P29/00 , A61P7/02 , A61P35/00 , A61P31/00 , A61P25/28 , A61P9/00 , A61P3/00 , A61P37/06 , A61P19/02 , A61P17/00 , A61P31/12 , A61P3/10 , A61P25/00 , A61P21/04 , A61P1/00 , A61P11/02 , A61P11/00 , A61P17/06 , A61P3/04 , A61P19/06 , A61P9/10 , C12N5/071 , A61K31/4709
CPC分类号： C07D471/04 , C07D519/00
摘要： Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.
摘要翻译： 本文提供了式（I）的杂芳基化合物：其中R 1和R 2如本文所定义，包含有效量的杂芳基化合物的组合物和用于治疗或预防炎性病症或癌症的方法，以及可通过抑制激酶治疗或预防的病症 或激酶途径，其包括向有需要的受试者施用有效量的杂芳基化合物。
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