公开(公告)号：US20150361071A1

公开(公告)日：2015-12-17

申请号：US14736025

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Musong Kim ,  Stephane Perreault ,  Suet Chung Yeung

IPC分类号： C07D403/14 ,  C07D491/048 ,  C07D487/04

CPC分类号： C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, m, R1, R2, R3, R4, and R5 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

摘要翻译： 本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中n，m，R 1，R 2，R 3，R 4和R 5在本文中描述。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

公开(公告)号：US09951065B2

公开(公告)日：2018-04-24

申请号：US15153527

申请日：2016-05-12

申请人： Gilead Sciences, Inc.

发明人： Mark J. Bartlett ,  Julian Andrew Codelli ,  Britton Kenneth Corkey ,  Jennifer Leigh Cosman ,  Kristyna Elbel ,  Jennifer Alissa Loyer-Drew ,  David Sperandio ,  Joshua Van Veldhuizen ,  Hai Yang ,  Suet Chung Yeung

IPC分类号： C07D235/06 ,  C07D235/24 ,  C07D295/125 ,  C07D401/12 ,  C07D471/04 ,  A61K45/06 ,  C07D235/08 ,  A61K31/4184 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/437 ,  A61K31/506 ,  A61K31/497 ,  A61K31/55 ,  A61K31/541 ,  A61K31/439 ,  C07D405/12 ,  C07D405/14 ,  C07D471/08 ,  A61K31/553 ,  C07D235/30 ,  C07D235/14 ,  C07D401/04 ,  C07D235/12 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/438 ,  C07D403/12 ,  A61K31/4439 ,  C07D413/12 ,  A61K31/496 ,  C07D487/04 ,  A61K31/4725 ,  C07D235/28 ,  C07D235/16 ,  C07D409/12

CPC分类号： C07D471/04 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/24 ,  C07D235/28 ,  C07D235/30 ,  C07D295/125 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D471/08 ,  C07D487/04

摘要： The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

公开(公告)号：US20150361095A1

公开(公告)日：2015-12-17

申请号：US14735939

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Zhimin Du ,  Jerry Evarts ,  Joshua Kaplan ,  Musong Kim ,  Devan Naduthambi ,  Leena Patel ,  Stephane Perreault ,  Barton W. Phillips ,  Gary Phillips ,  Kirk L. Stevens ,  Jennifer A. Treiberg ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC分类号： C07D513/04 ,  C07D473/34 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

CPC分类号： C07D513/04 ,  C07D239/91 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D473/34 ,  C07D487/04

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A′, W1, W2, W3, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

摘要翻译： 本申请提供式（J）化合物或其药学上可接受的盐，异构体或其混合物，其中n，m，q，A'，W 1，W 2，W 3，R 1，R 2和R 3在本文中描述。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

公开(公告)号：US20150361054A1

公开(公告)日：2015-12-17

申请号：US14735254

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Shaopei Cai ,  Zhimin Du ,  Joshua Kaplan ,  Jennifer A. Loyer-Drew ,  Devan Naduthambi ,  Barton W. Phillips ,  Gary Phillips ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC分类号： C07D239/90 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D403/14 ,  C07D513/04

CPC分类号： A61K31/496 ,  C07D239/04 ,  C07D239/80 ,  C07D239/90 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D513/04

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

摘要翻译： 本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中W，B，n，m，A'，R 1，R 2和R 3在本文中描述。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

公开(公告)号：US10092563B2

公开(公告)日：2018-10-09

申请号：US14735254

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Shaopei Cai ,  Zhimin Du ,  Joshua Kaplan ,  Jennifer A. Loyer-Drew ,  Devan Naduthambi ,  Barton W. Phillips ,  Gary Phillips ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC分类号： A61K31/496 ,  C07D239/04 ,  C07D239/80 ,  C07D401/14 ,  C07D413/14 ,  C07D407/14 ,  C07D487/04 ,  C07D239/90 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D513/04 ,  C07D403/14 ,  C07D405/14

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

公开(公告)号：US09499523B2

公开(公告)日：2016-11-22

申请号：US14736025

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Musong Kim ,  Stephane Perreault ,  Suet Chung Yeung

IPC分类号： C07D403/14 ,  C07D471/04 ,  C07D491/048 ,  C07D487/04

CPC分类号： C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, m, R1, R2, R3, R4, and R5 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

公开(公告)号：US20150361070A1

公开(公告)日：2015-12-17

申请号：US14735924

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Jerry Evarts ,  Joshua Kaplan ,  Leena Patel ,  Stephane Perreault ,  Barton W. Phillips ,  Gary Phillips ,  Jennifer A. Treiberg ,  Suet Chung Yeung

IPC分类号： C07D403/14 ,  C07D498/04 ,  C07D491/048 ,  C07D471/04 ,  C07D473/34 ,  C07D495/04 ,  C07D513/04 ,  C07D487/04

CPC分类号： C07D403/14 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m′, A′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

摘要翻译： 本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中X，Y，Z，n，m'，A'，R 1，R 2和R 3在本文中描述 。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

公开(公告)号：US11021467B2

公开(公告)日：2021-06-01

申请号：US14735244

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Shaopei Cai ,  Zhimin Du ,  Musong Kim ,  Jennifer A. Loyer-Drew ,  Devan Naduthambi ,  Leena Patel ,  Barton W. Phillips ,  Gary Phillips ,  Kirk L. Stevens ,  Jennifer Anne Treiberg ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D473/34 ,  C07D487/04 ,  C07D513/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, W, A′, B′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

公开(公告)号：US10308639B2

公开(公告)日：2019-06-04

申请号：US14735924

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Jerry Evarts ,  Joshua Kaplan ,  Leena Patel ,  Stephane Perreault ,  Barton W. Phillips ,  Gary Phillips ,  Jennifer A. Treiberg ,  Suet Chung Yeung

IPC分类号： C07D403/14 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D498/04

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m′, A′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

公开(公告)号：US10221197B2

公开(公告)日：2019-03-05

申请号：US14735939

申请日：2015-06-10

申请人： Gilead Sciences, Inc.

发明人： Zhimin Du ,  Jerry Evarts ,  Joshua Kaplan ,  Musong Kim ,  Devan Naduthambi ,  Leena Patel ,  Stephane Perreault ,  Barton W. Phillips ,  Gary Phillips ,  Kirk L. Stevens ,  Jennifer A. Treiberg ,  Joshua Van Veldhuizen ,  William J. Watkins ,  Suet Chung Yeung

IPC分类号： C07D513/04 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D239/91 ,  C07D487/04 ,  C07D401/14 ,  C07D473/34

摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A′, W1, W2, W3, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.