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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.
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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。
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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。
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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。
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5.发明申请Monophosphates as Mutual Prodrugs of Anti-Inflammatory Signal Transduction Modulators (AISTM's) and Beta-Agonists for the Treatment of Pulmonary Inflammation and Bronchoconstriction 审中-公开单磷酸盐作为抗炎信号转导调节剂（AISTM）和β-激动剂的相关前药用于治疗肺部炎症和支气管收缩公开(公告)号：US20100098641A1
公开(公告)日：2010-04-22
申请号：US12519305
申请日：2007-12-12
CPC分类号： C07F9/65038 , C07F9/12 , C07F9/58 , C07F9/65583 , C07F9/65586
摘要： A mutual prodrug of an AISTM and a β-agonist in formulation for delivery by aerosolization to inhibit pulmonary inflammation and bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 μL) dissolved in a quarter normal saline having pH between about 5.0 and 7.0 for the treatment of respiratory tract inflammation and bronchoconstriction by an aerosol having mass median average diameter predominantly between about 1 to 5μ, produced by nebulization or by dry powder inhaler.
摘要翻译： 描述了一种AISTM和一种通过气雾化递送以抑制肺部炎症和支气管收缩的配方的配方的联合前药。 共聚前体药物优选配制成溶解在pH为约5.0至7.0之间的四分之一生理盐水中的小体积溶液（10-500μL），用于治疗呼吸道炎症和气溶胶的支气管收缩，其质量中值平均直径主要在约 1至5μ，通过雾化或干粉吸入器生产。
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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.
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公开(公告)号：US20110275623A1
公开(公告)日：2011-11-10
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： A61K31/437 , C07D413/14 , A61K31/538 , A61P29/00 , A61P11/06 , A61P11/08 , A61P3/00 , C07D471/22 , A61P11/00
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。
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8.发明申请Monophosphates as Mutual Prodrugs of Muscarinic Receptor Antagonists and Beta-Agonists for the Treatment of COPD And Chronic Bronchitis 审中-公开单磷酸盐作为毒蕈碱受体拮抗剂和β-激动剂的相关前药用于治疗COPD和慢性支气管炎公开(公告)号：US20100112061A1
公开(公告)日：2010-05-06
申请号：US12519311
申请日：2007-12-12
IPC分类号： A61K31/661 , A61K9/14 , C07F9/145 , A61K31/675 , A61K31/665 , A61P11/08
CPC分类号： C07F9/65583 , C07F9/5532 , C07F9/572 , C07F9/59 , C07F9/65586 , C07F9/6561
摘要： A mutual prodrug of a MRA and a (β-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 μL) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5μ, produced by nebulization or by dry powder inhaler.
摘要翻译： 描述了MRA和用于通过气雾化递送以抑制肺支气管收缩的制剂的（＆amp; bgr）激素的共同前药，所述共同前药优选配制成溶于四分之一生理盐水的小体积溶液（10-500μL），其具有 5.0至7.0之间的pH值用于通过雾化或干粉吸入器产生的质量中值平均直径主要在1至5μ之间的气溶胶治疗呼吸道支气管收缩。
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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。
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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。
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