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![Substituted pyrazino[2,3-b]pyrazines as mTOR kinase inhibitors](/abs-image/US/2014/12/09/US08907087B2/abs.jpg.150x150.jpg)
1.发明授权公开(公告)号：US08907087B2
公开(公告)日：2014-12-09
申请号：US13927255
申请日：2013-06-26
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella I. Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Jan Elsner
IPC分类号： C07D241/38 , C07D498/14 , 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. Furthermore, provided are methods of preparing a compound of formula (III), Furthermore, provided are methods of preparing a compound of formula (VI),
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。 此外，提供制备式（III）化合物的方法。此外，提供制备式（VI）化合物的方法，
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2.发明申请INHIBITION OF PHOSPHORYLATION OF PRAS40, GSK3-BETA OR P70S6K1 AS A MARKER FOR TOR KINASE INHIBITORY ACTIVITY 有权PRAS40，GSK3-BETA或P70S6K1的磷酸化抑制作为诱导剂抑制活性的标记公开(公告)号：US20140113905A1
公开(公告)日：2014-04-24
申请号：US14055995
申请日：2013-10-17
IPC分类号： A61K31/4985 , G01N33/574 , G01N33/50
CPC分类号： G01N33/6842 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/522 , C12Q1/485 , G01N33/5011 , G01N2333/9121 , G01N2800/52 , G01N2800/7028
摘要： Provided herein are methods for treating a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3β or p70S6K1, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3β or p70S6K1.
摘要翻译： 本文提供了通过抑制PRAS40，GSK3和bgr的磷酸化来治疗可治疗癌症的方法。 或p70S6K1，包括向具有通过抑制PRAS40，GSK3和bgr的磷酸化可治疗的癌症的患者施用有效量的TOR激酶抑制剂; 或p70S6K1。
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3.发明授权公开(公告)号：US09783505B2
公开(公告)日：2017-10-10
申请号：US15241232
申请日：2016-08-19
发明人： Patrick Papa , Brian Edwin Cathers , Andrew Antony Calabrese , Brandon Wade Whitefield , Brydon Bennett , Daniel Cashion , Deborah Mortensen , Dehua Huang , Eduardo Torres , Jason Parnes , John Sapienza , Joshua Hansen , Katerina Leftheris , Matthew Correa , Maria Mercedes Delgado , Raj K. Raheja , Sogole Bahmanyar , Sayee Hegde , Stephen Norris , Veronique Plantevin-Krenitsky
IPC分类号： A61K31/505 , C07D239/48 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D405/12 , C07D471/04 , C07D405/14 , A61K31/506 , C07D417/12 , A61K31/5377
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.
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![Substituted pyrazino[2,3-b]pyrazines as mTOR kinase inhibitors](/abs-image/US/2017/09/26/US09771371B2/abs.jpg.150x150.jpg)
公开(公告)号：US09771371B2
公开(公告)日：2017-09-26
申请号：US14874524
申请日：2015-10-05
发明人： Jan Elsner , Roy L. Harris , Branden Gingsee Lee , Deborah Mortensen , Garrick K. Packard , Patrick Papa , Jason Parnes , Sophie Perrin-Ninkovic , Jennifer Riggs , John Sapienza , Graziella I. Shevlin , Lida Tehrani , Jingjing Zhao
IPC分类号： C07D487/04 , C07D498/14 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14
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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公开(公告)号：US09079900B2
公开(公告)日：2015-07-14
申请号：US14174896
申请日：2014-02-07
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 Pye , William Wei-Hwa Leong , Jan Elsner , Anusuya Choudhury
IPC分类号： A61K31/497 , C07D241/00 , C07D471/04 , C07D487/04 , C07D498/14 , C07D519/00
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.
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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![Substituted pyrazino[2,3-b]pyrazines as mTOR kinase inhibitors](/abs-image/US/2022/04/05/US11292796B2/abs.jpg.150x150.jpg)
公开(公告)号：US11292796B2
公开(公告)日：2022-04-05
申请号：US16865512
申请日：2020-05-04
发明人： Jan Elsner , Roy L. Harris , Branden Gingsee Lee , Deborah Mortensen , Garrick K. Packard , Patrick Papa , Jason Parnes , Sophie Perrin-Ninkovic , Jennifer Riggs , John Sapienza , Graziella I. Shevlin , Lida Tehrani , Jingjing Zhao
IPC分类号： C07D487/04 , C07D498/14 , C07D241/20 , C07D471/04 , C07D471/14 , C07D487/10 , C07D487/14
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. Further provided herein are methods for preparing a compound of formula (I), the method comprising contacting a compound of formula (III) with a compound of the following formula: R1-Y, in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R1-R4, Y, the palladium catalyst and the base are as defined herein.
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7.发明授权Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for tor kinase inhibitory activity 有权抑制PRAS40，GSK3-β或P70S6K1作为激酶抑制活性的标志物的磷酸化公开(公告)号：US09557338B2
公开(公告)日：2017-01-31
申请号：US14835817
申请日：2015-08-26
IPC分类号： G01N33/68 , A61K31/4985 , G01N33/50 , C12Q1/48 , A61K31/437 , A61K31/519 , A61K31/522
CPC分类号： G01N33/6842 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/522 , C12Q1/485 , G01N33/5011 , G01N2333/9121 , G01N2800/52 , G01N2800/7028
摘要： Provided herein are methods for treating a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3β or p70S6K1, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a cancer treatable by inhibition of phosphorylation of PRAS40, GSK3β or p70S6K1.
摘要翻译： 本文提供治疗通过抑制PRAS40，GSK3β或p70S6K1的磷酸化可治疗的癌症的方法，包括通过抑制PRAS40，GSK3β或p70S6K1的磷酸化可治疗癌症的患者施用有效量的TOR激酶抑制剂。
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8.发明授权Substituted diaminopyrimidyl compounds, compositions thereof, and methods of treatment therewith 有权取代的二氨基嘧啶基化合物，其组合物及其处理方法公开(公告)号：US09556126B2
公开(公告)日：2017-01-31
申请号：US14576197
申请日：2014-12-19
发明人： Patrick Papa , Brian Edwin Cathers , Andrew Antony Calabrese , Brandon Wade Whitefield , Brydon Bennett , Daniel Cashion , Deborah Mortensen , Dehua Huang , Eduardo Torres , Jason Parnes , John Sapienza , Joshua Hansen , Katerina Leftheris , Matthew Correa , Maria Mercedes Delgado , Raj K. Raheja , Sogole Bahmanyar , Sayee Hegde , Stephen Norris , Veronique Plantevin-Krenitsky
IPC分类号： C07D403/12 , A61K31/505 , C07D239/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D405/12 , C07D471/04 , C07D405/14 , A61K31/506 , C07D417/12
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.
摘要翻译： 本文提供具有以下结构的二氨基嘧啶化合物：其中X，L，R 1和R 2如本文所定义，包含有效量的二氨基嘧啶基化合物的组合物，以及用于治疗或预防PKC-θ介导的病症的方法或病症 可通过抑制激酶例如PKC-θ治疗或预防。
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公开(公告)号：US20140113904A1
公开(公告)日：2014-04-24
申请号：US14055985
申请日：2013-10-17
发明人： Deborah Mortensen , Heather Raymon , Rama K. Narla , Kristen Mae Hege , Kimberly Elizabeth Fultz , Toshiya Tsuji
IPC分类号： A61K31/4985 , G01N33/50
CPC分类号： A61K31/4985 , G01N33/5041
摘要： Provided herein are methods for treating or preventing prostate cancer, comprising administering an effective amount of a TOR kinase inhibitor to a patient having prostate cancer.
摘要翻译： 本文提供了治疗或预防前列腺癌的方法，包括向具有前列腺癌的患者施用有效量的TOR激酶抑制剂。
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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/2013/10/31/US20130289271A1/abs.jpg.150x150.jpg)
公开(公告)号：US20130289271A1
公开(公告)日：2013-10-31
申请号：US13927255
申请日：2013-06-26
发明人： Sophie Perrin-Ninkovic , Roy L. Harris , John Sapienza , Graziella I. Shevlin , Patrick Papa , Branden Lee , Garrick Packard , Lida Tehrani , Jingjing Zhao , Jennifer Riggs , Jason Parnes , Deborah Mortensen , Weiming Xu , Loui Madakamutil , Kimberly Elizabeth Fultz , Rama Narla , Sabita Sankar , Jan Elsner
IPC分类号： C07D487/04 , C07D498/14
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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