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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：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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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。
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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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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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7.发明授权Pyrimidine compounds, their use as mTOR kinase and Pl3 kinase inhibitors, and their syntheses 有权嘧啶化合物，它们作为mTOR激酶和Pl3激酶抑制剂的用途及其合成公开(公告)号：US08835429B2
公开(公告)日：2014-09-16
申请号：US13264776
申请日：2010-04-15
申请人： Kevin Joseph Curran , Joshua Aaron Kaplan , David James Richard , Jeroen Cunera Verheijen , Arie Zask
发明人： Kevin Joseph Curran , Joshua Aaron Kaplan , David James Richard , Jeroen Cunera Verheijen , Arie Zask
IPC分类号： C07D498/08 , A61K31/5386
CPC分类号： C07D498/08
摘要： The invention relates to pyrimidine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译： 本发明涉及式I的嘧啶化合物或其药学上可接受的盐，其中组成变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。
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公开(公告)号：US08217036B2
公开(公告)日：2012-07-10
申请号：US13218571
申请日：2011-08-26
申请人： Aranapakam Mudumbai Venkatesan , Zecheng Chen , Christoph Martin Dehnhardt , Osvaldo Dos Santos , Efren Guillermo Delos Santos , Arie Zask , Jeroen Cunera Verheijen , Joshua Aaron Kaplan , David James Richard , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Ariamala Gopalsamy , Kevin Joseph Curran , Mengxiao Shi
发明人： Aranapakam Mudumbai Venkatesan , Zecheng Chen , Christoph Martin Dehnhardt , Osvaldo Dos Santos , Efren Guillermo Delos Santos , Arie Zask , Jeroen Cunera Verheijen , Joshua Aaron Kaplan , David James Richard , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Ariamala Gopalsamy , Kevin Joseph Curran , Mengxiao Shi
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D401/12 , A61K31/5377 , A61K45/06 , C07D251/18 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D413/04 , C07D413/14 , C07D451/06 , C07D453/02 , C07D491/113 , C07D498/08
摘要： Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
摘要翻译： 式I的化合物，其中：R1是和R2，R4和R6-9在本文中定义，及其药学上可接受的盐和酯。 这些化合物抑制PI3激酶和mTOR，并可用于治疗PI3激酶和mTOR介导的疾病，如多种癌症。 公开了制备和使用本发明化合物的方法。 还公开了含有本发明化合物的各种组合物。
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公开(公告)号：US20090304692A1
公开(公告)日：2009-12-10
申请号：US12470525
申请日：2009-05-22
申请人： Aranapakam Mudumbai Venkatesan , Zecheng Chen , Christoph Martin Dehnhardt , Osvaldo dos Santos , Efren Guillermo Delos Santos , Arie Zask , Jeroen Cunera Verheijen , Joshua Aaron Kaplan , David James Richard , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Ariamala Gopalsamy , Kevin Joseph Curran , Mengxiao Shi
发明人： Aranapakam Mudumbai Venkatesan , Zecheng Chen , Christoph Martin Dehnhardt , Osvaldo dos Santos , Efren Guillermo Delos Santos , Arie Zask , Jeroen Cunera Verheijen , Joshua Aaron Kaplan , David James Richard , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Ariamala Gopalsamy , Kevin Joseph Curran , Mengxiao Shi
IPC分类号： A61K31/5375 , C07D413/04 , C07D413/14 , C07D405/14 , C07D417/14 , C07D491/08 , C07D498/08 , A61K31/5377 , A61K31/541 , A61K31/7068 , A61K31/675 , A61K33/24 , A61K39/395 , A61P19/00 , A61P35/00
摘要： Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
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公开(公告)号：US20130005723A1
公开(公告)日：2013-01-03
申请号：US13490309
申请日：2012-06-06
申请人： Aranapakam Mudumbai Venkatesan , Zecheng Chen , Christoph Martin Dehnhardt , Osvaldo Dos Santos , Efren Guillermo Delos Santos , Arie Zask , Jeroen Cunera Verheijen , Joshua Aaron Kaplan , David James Richard , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Ariamala Gopalsamy , Kevin Joseph Curran , Mengxiao Shi
发明人： Aranapakam Mudumbai Venkatesan , Zecheng Chen , Christoph Martin Dehnhardt , Osvaldo Dos Santos , Efren Guillermo Delos Santos , Arie Zask , Jeroen Cunera Verheijen , Joshua Aaron Kaplan , David James Richard , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Ariamala Gopalsamy , Kevin Joseph Curran , Mengxiao Shi
IPC分类号： A61K31/5377 , A61P35/00 , C07D491/08
CPC分类号： C07D401/12 , A61K31/5377 , A61K45/06 , C07D251/18 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D413/04 , C07D413/14 , C07D451/06 , C07D453/02 , C07D491/113 , C07D498/08
摘要： Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
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