公开(公告)号：US08394829B2

公开(公告)日：2013-03-12

申请号：US13103577

申请日：2011-05-09

申请人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Jennifer Alissa Loyer-Drew ,  Stephane Perreault ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk K. Stevens ,  Josh Van Veldhuizen

发明人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Jennifer Alissa Loyer-Drew ,  Stephane Perreault ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk K. Stevens ,  Josh Van Veldhuizen

IPC分类号： C07D215/38 ,  A61K31/04

CPC分类号： C07D215/54 ,  C07D401/12 ,  C07D409/14 ,  C07D413/12

摘要： Provided are compounds of Formula I: wherein X is: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.

摘要翻译： 提供式I的化合物：其中X是：R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，并且所有其它变量如本文所定义，以及它们在治疗肺部炎症中的用途 或支气管收缩剂及其组合物及其制备方法。

公开(公告)号：US20130012504A1

公开(公告)日：2013-01-10

申请号：US13619636

申请日：2012-09-14

申请人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Jennifer Alissa Loyer-Drew ,  Stephane Perreault ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

发明人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Jennifer Alissa Loyer-Drew ,  Stephane Perreault ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

IPC分类号： C07D215/54 ,  C07D401/14 ,  A61K31/496 ,  C07D413/12 ,  A61K31/538 ,  A61K31/4706 ,  C07D409/14 ,  A61P29/00 ,  A61P31/00 ,  A61P37/08 ,  A61P11/00 ,  A61P11/08 ,  A61P11/06 ,  A61P11/10 ,  A61P11/02 ,  A61K31/4709

CPC分类号： C07D215/54 ,  C07D401/12 ,  C07D409/14 ,  C07D413/12

摘要： Provided are compounds of Formula I: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.

摘要翻译： 提供式I化合物：R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，并且所有其它变量如本文所定义，以及它们在治疗肺部炎症或支气管收缩和组合物中的用途 包括及其制备方法。

公开(公告)号：US20110275622A1

公开(公告)日：2011-11-10

申请号：US13103577

申请日：2011-05-09

申请人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Jennifer Alissa Loyer-Drew ,  Stephane Perreault ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

发明人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Jennifer Alissa Loyer-Drew ,  Stephane Perreault ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

IPC分类号： A61K31/4709 ,  C07D401/14 ,  C07D413/12 ,  A61K31/496 ,  A61K31/538 ,  A61P29/00 ,  A61K31/475 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P3/00 ,  C07D215/54 ,  A61K31/4706

CPC分类号： C07D215/54 ,  C07D401/12 ,  C07D409/14 ,  C07D413/12

摘要： Provided are compounds of Formula I: wherein X is: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.

摘要翻译： 提供式I的化合物：其中X是：R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，并且所有其它变量如本文所定义，以及它们在治疗肺部炎症中的用途 或支气管收缩剂及其组合物及其制备方法。

公开(公告)号：US08367829B2

公开(公告)日：2013-02-05

申请号：US13103598

申请日：2011-05-09

申请人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

发明人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

IPC分类号： C07D513/02

CPC分类号： C07D471/04

摘要： This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.

公开(公告)号：US20130018050A1

公开(公告)日：2013-01-17

申请号：US13619792

申请日：2012-09-14

申请人： WILLIAM R. BAKER ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

发明人： WILLIAM R. BAKER ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/536 ,  A61P29/00 ,  A61P11/02 ,  A61P37/08 ,  A61P11/00 ,  A61P11/08 ,  A61P11/06 ,  A61P11/10 ,  A61K31/4709 ,  A61P31/00

CPC分类号： C07D471/04

摘要： This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.

摘要翻译： 本发明提供下式的化合物：其中X是其中R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，所有其它变量如本文所定义，它们在肺部炎症或支气管收缩治疗中的用途，以及 提供了组合物及其制备方法。

公开(公告)号：US08450490B2

公开(公告)日：2013-05-28

申请号：US13619792

申请日：2012-09-14

申请人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

发明人： William R. Baker ,  Shaopei Cai ,  Joshua Aaron Kaplan ,  Musong Kim ,  Gary Phillips ,  Lafe J. Purvis, II ,  Marcin Stasiak ,  Kirk L. Stevens ,  Josh Van Veldhuizen

IPC分类号： C07D513/02

CPC分类号： C07D471/04

摘要： This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.

摘要翻译： 本发明提供下式的化合物：其中X是其中R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，所有其它变量如本文所定义，它们在肺部炎症或支气管收缩治疗中的用途，以及 提供了组合物及其制备方法。

公开(公告)号：US09266878B2

公开(公告)日：2016-02-23

申请号：US14686418

申请日：2015-04-14

申请人： Jerry Evarts ,  Leena Patel ,  Jennifer A. Treiberg ,  Stephane Perreault ,  Arthur Yeung ,  Lafe J. Purvis, II ,  Musong Kim

发明人： Jerry Evarts ,  Leena Patel ,  Jennifer A. Treiberg ,  Stephane Perreault ,  Arthur Yeung ,  Lafe J. Purvis, II ,  Musong Kim

IPC分类号： C07D417/14 ,  C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D471/08

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D471/08

摘要： The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.

公开(公告)号：US20150218154A1

公开(公告)日：2015-08-06

申请号：US14686418

申请日：2015-04-14

申请人： Jerry Evarts ,  Leena Patel ,  Jennifer A. Treiberg ,  Stephane Perreault ,  Arthur Yeung ,  Lafe J. Purvis, II ,  Musong Kim

发明人： Jerry Evarts ,  Leena Patel ,  Jennifer A. Treiberg ,  Stephane Perreault ,  Arthur Yeung ,  Lafe J. Purvis, II ,  Musong Kim

IPC分类号： C07D417/14 ,  C07D403/14 ,  C07D403/12 ,  C07D401/14

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D471/08

摘要： The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.

摘要翻译： 本公开提供式（I）的磷脂酰肌醇3-激酶（PI3K）抑制剂或其药学上可接受的盐，其中R 1，R 2，n，R 3，R 4，R 5和R 6如本文所定义。 这些化合物可用于治疗由一种或多种PI3K异构体如PI3Kδ介导的病症。 本公开进一步提供了包含式（I）化合物或其药学上可接受的盐的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K异构体如PI3Kδ介导的病症的方法。