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1.发明申请PYRAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS 审中-公开吡唑并嘧啶类似物及其作为MTOR激酶和PI3激酶抑制剂的用途公开(公告)号：US20080234262A1
公开(公告)日：2008-09-25
申请号：US12050445
申请日：2008-03-18
申请人： Arie Zask , Pawel Wojciech Nowak , Jeroen Cunera Verheijen , Kevin J. Curran , Joshua Kaplan , David Malwitz , Matthew Gregory Bursavich , Derek Cecil Cole , Semiramis Ayral-Kaloustian , Ker Yu , David James Richard , Mark Lefever
发明人： Arie Zask , Pawel Wojciech Nowak , Jeroen Cunera Verheijen , Kevin J. Curran , Joshua Kaplan , David Malwitz , Matthew Gregory Bursavich , Derek Cecil Cole , Semiramis Ayral-Kaloustian , Ker Yu , David James Richard , Mark Lefever
IPC分类号： A61K31/5377 , A61K31/519 , A61P35/00 , C07D413/14 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to Pyrazolopyrimidine Analogs, methods of making Pyrazolopyrimidine Analogs, compositions comprising a Pyrazolopyrimidine Analog, and methods for treating mTOR-related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. The invention also relates to treating PI3K-related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog.
摘要翻译： 本发明涉及吡唑并嘧啶类似物，制备吡唑并嘧啶类似物的方法，包含吡唑并嘧啶类似物的组合物和用于治疗mTOR相关病症的方法，其包括向有需要的受试者施用有效量的吡唑并嘧啶类似物。 本发明还涉及治疗PI3K相关疾病，包括向有需要的受试者施用有效量的吡唑并嘧啶类似物。
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2.发明授权Thienopyrimidine and pyrazolopyrimidine compounds and their use as mTOR kinase and PI3 kinase inhibitors 失效噻吩并嘧啶和吡唑并嘧啶化合物及其作为mTOR激酶和PI3激酶抑制剂的用途公开(公告)号：US08129371B2
公开(公告)日：2012-03-06
申请号：US12251712
申请日：2008-10-15
申请人： Arie Zask , Joshua Aaron Kaplan , Jeroen Cunera Verheijen , Kevin J. Curran , David James Richard , Semiramis Ayral-Kaloustian
发明人： Arie Zask , Joshua Aaron Kaplan , Jeroen Cunera Verheijen , Kevin J. Curran , David James Richard , Semiramis Ayral-Kaloustian
IPC分类号： C07D265/36 , C07D265/28 , A61K31/537 , A61P37/06 , A61P35/00 , C07D487/04 , C07D495/04
CPC分类号： C07D519/00
摘要： The invention relates to thienopyrimidine and pyrazolopyrimidine compounds of the Formulas (Ia) and (IIa), 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（Ia）和（IIa）的噻吩并嘧啶和吡唑并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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3.发明申请THIENOPYRIMIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS 失效三硝基嘧啶和吡唑并嘧啶化合物及其作为MTOR激酶和PI3激酶抑制剂的用途公开(公告)号：US20090098086A1
公开(公告)日：2009-04-16
申请号：US12251712
申请日：2008-10-15
申请人： Arie Zask , Joshua Aaron Kaplan , Jeroen Cunera Verheijen , Kevin J. Curran , David James Richard , Semiramis Ayral-Kaloustian
发明人： Arie Zask , Joshua Aaron Kaplan , Jeroen Cunera Verheijen , Kevin J. Curran , David James Richard , Semiramis Ayral-Kaloustian
IPC分类号： A61K38/21 , C07D487/04 , C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/5383 , C07D493/08
CPC分类号： C07D519/00
摘要： The invention relates to thienopyrimidine and pyrazolopyrimidine compounds of the Formulas (Ia) and (IIa), 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（Ia）和（IIa）的噻吩并嘧啶和吡唑并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：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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公开(公告)号：US08039469B2
公开(公告)日：2011-10-18
申请号：US12470521
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： A61K31/535 , 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：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：US20110312955A1
公开(公告)日：2011-12-22
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： A61K31/5377 , A61P35/02 , A61P35/00
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：US20090291079A1
公开(公告)日：2009-11-26
申请号：US12470521
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： A61K31/5377 , C07D413/14 , A61K31/7068 , A61K31/675 , A61K33/24 , A61K31/7048 , A61K31/704 , A61K39/395 , A61P19/00 , A61P29/00 , A61P37/00 , A61P35/00
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：US08445486B2
公开(公告)日：2013-05-21
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： A61K31/535 , 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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