公开(公告)号：US08907087B2

公开(公告)日：2014-12-09

申请号：US13927255

申请日：2013-06-26

申请人： Signal Pharmaceuticals, LLC

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，

公开(公告)号：US09771371B2

公开(公告)日：2017-09-26

申请号：US14874524

申请日：2015-10-05

申请人： SIGNAL PHARMACEUTICALS, LLC

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.

公开(公告)号：US09079900B2

公开(公告)日：2015-07-14

申请号：US14174896

申请日：2014-02-07

申请人： SIGNAL PHARMACEUTICALS, LLC

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。

公开(公告)号：US10683298B2

公开(公告)日：2020-06-16

申请号：US16186883

申请日：2018-11-12

申请人： SIGNAL PHARMACEUTICALS, LLC

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 the preparation of substituted pyrazino[2,3-b]pyrazines of formula (II): the method comprising contacting a compound of formula (VI): the method further comprising cyclizing a compound of formula (VII) in a second solvent, in the presence of a second base, or an acid, wherein said cyclization occurs under conditions suitable to provide a compound of formula (VI), with R1-Y in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R1-R3, Y, the palladium catalyst and the base are as defined herein.

公开(公告)号：US09193692B2

公开(公告)日：2015-11-24

申请号：US14529261

申请日：2014-10-31

申请人： SIGNAL PHARMACEUTICALS, LLC

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： C07D241/16 ,  C07D241/20 ,  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. Furthermore, provided herein are compounds having the following formulas (IV), (V), (VII) and (VIII): wherein R, R2, R3, R4, Hal and Hal2 are as defined herein, for preparation of the Heteroaryl Compounds.

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，本文提供了具有下式（IV），（V），（VII）和（VIII）的化合物：其中R，R2，R3，R4，Hal和Hal2如本文所定义，用于制备杂芳基化合物。

公开(公告)号：US20150051397A1

公开(公告)日：2015-02-19

申请号：US14529261

申请日：2014-10-31

申请人： SIGNAL PHARMACEUTICALS, LLC

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 ,  Jan Elsner

IPC分类号： C07D241/20

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：US20140155593A1

公开(公告)日：2014-06-05

申请号：US14174896

申请日：2014-02-07

申请人： SIGNAL PHARMACEUTICALS, LLC

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： C07D498/14 ,  C07D487/04

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。

公开(公告)号：US11292796B2

公开(公告)日：2022-04-05

申请号：US16865512

申请日：2020-05-04

申请人： SIGNAL PHARMACEUTICALS, LLC

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.

公开(公告)号：US20130289271A1

公开(公告)日：2013-10-31

申请号：US13927255

申请日：2013-06-26

申请人： SIGNAL PHARMACEUTICALS, LLC

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.

公开(公告)号：US20230158035A1

公开(公告)日：2023-05-25

申请号：US18095670

申请日：2023-01-11

申请人： Signal Pharmaceuticals, LLC

发明人： Matthew Alexander ,  Sogole Bahmanyar ,  John Frederick Boylan ,  Joshua Hansen ,  Dehua Huang ,  Robert Hubbard ,  Brandon Jeffy ,  Jim Leisten ,  Mehran Moghaddam ,  Raj K. Raheja ,  Heather Raymon ,  Kimberly Schwarz ,  Marianne Sloss ,  Eduardo Torres ,  Tam Minh Tran ,  Shuichan Xu ,  Jingjing Zhao

IPC分类号： A61K31/52 ,  C07D473/32 ,  A61P35/00 ,  A61K31/5377

CPC分类号： A61K31/52 ,  C07D473/32 ,  A61P35/00 ,  A61K31/5377

摘要： Provided herein are Aminopurine Compounds having the following structures:






wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.