公开(公告)号：US20080242694A1

公开(公告)日：2008-10-02

申请号：US11901598

申请日：2007-09-17

申请人： Neil R. D'Sidocky ,  Roy L. Harris ,  Sayee G. Hegde ,  Robert Hilgraf ,  Margaret A. McCarrick ,  Jeffrey A. McKie ,  Deborah S. Mortensen ,  Lisa Nadolny ,  Sophie M. Perin-Ninkovic ,  John J. Sapienza ,  Jonathan L. Wright

发明人： Neil R. D'Sidocky ,  Roy L. Harris ,  Sayee G. Hegde ,  Robert Hilgraf ,  Margaret A. McCarrick ,  Jeffrey A. McKie ,  Deborah S. Mortensen ,  Lisa Nadolny ,  Sophie M. Perin-Ninkovic ,  John J. Sapienza ,  Jonathan L. Wright

IPC分类号： A61K31/4375 ,  C07D417/04 ,  A61P35/00 ,  A61K31/4725

CPC分类号： C07D417/04 ,  C07D285/135 ,  C07D403/04 ,  C07D417/14

摘要： Provided herein are Heterocyclic Compounds having the following structure: wherein R1, R2, X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.

摘要翻译： 本文提供具有以下结构的杂环化合物：其中R 1，R 2，X，Y和Z如本文所定义，组合物包含有效量的杂环化合物 以及用于治疗或预防癌症，炎性病症，免疫学条件，代谢条件和通过抑制激酶途径可治疗或可预防的病症的方法，包括向有需要的患者施用有效量的杂环化合物。

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。

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.

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。

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。

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.

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。

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。

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。