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。

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。

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.

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.

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。

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。

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。

公开(公告)号：US20090181963A1

公开(公告)日：2009-07-16

申请号：US12354027

申请日：2009-01-15

申请人： Christoph Martin Dehnhardt ,  Aranapakam Mudumbai Venkatesan ,  Efren Guillermo Delos Santos ,  Zecheng Chen ,  Osvaldo Dos Santos ,  Natasja Brooijmans ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Semiramis Ayral-Kaloustian

发明人： Christoph Martin Dehnhardt ,  Aranapakam Mudumbai Venkatesan ,  Efren Guillermo Delos Santos ,  Zecheng Chen ,  Osvaldo Dos Santos ,  Natasja Brooijmans ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Semiramis Ayral-Kaloustian

IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The invention relates to 3H-[1,2,3]triazolo[4,5-d]pyrimidine compounds of the Formula 1: 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1的3H- [1,2,3]三唑并[4,5-d]嘧啶化合物或其药学上可接受的盐，其中组分变量如本文所定义，包含该化合物的组合物和 制备和使用化合物的方法。

公开(公告)号：US20080233127A1

公开(公告)日：2008-09-25

申请号：US12044500

申请日：2008-03-07

申请人： Matthew Gregory Bursavich ,  Aranapakam Mudumbai Venkatesan ,  Pawel Wojciech Nowak ,  Sabrina Lombardi ,  Adam Matthew Gilbert ,  Christoph Martin Denhardt ,  Osvaldo Dos Santos ,  Efren Guillermo Delos Santos ,  Natasja Brooijmans ,  Semiramis Ayral-Kaloustian ,  Zecheng Chen ,  Jeroen Cunera Verheijen ,  Joshua Kaplan ,  Arie Zask

发明人： Matthew Gregory Bursavich ,  Aranapakam Mudumbai Venkatesan ,  Pawel Wojciech Nowak ,  Sabrina Lombardi ,  Adam Matthew Gilbert ,  Christoph Martin Denhardt ,  Osvaldo Dos Santos ,  Efren Guillermo Delos Santos ,  Natasja Brooijmans ,  Semiramis Ayral-Kaloustian ,  Zecheng Chen ,  Jeroen Cunera Verheijen ,  Joshua Kaplan ,  Arie Zask

IPC分类号： A61K39/395 ,  C07D473/00 ,  A61K31/5377 ,  A61P35/04 ,  A61P3/00 ,  A61P1/00 ,  A61P29/00 ,  A61P19/00 ,  A61K31/52

CPC分类号： C07D473/34

摘要： The present invention relates to Imidazolopyrimidine Analogs, methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods for treating or preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog. The invention also relates to methods for treating or preventing mTOR-related disorders comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog.

摘要翻译： 本发明涉及咪唑并嘧啶类似物，制备咪唑并嘧啶类似物的方法，包含咪唑并嘧啶类似物的组合物，以及用于治疗或预防PI3K相关病症的方法，其包括向有需要的受试者施用有效量的咪唑并嘧啶类似物。 本发明还涉及治疗或预防mTOR相关病症的方法，包括向有需要的受试者施用有效量的咪唑并嘧啶类似物。

公开(公告)号：US20100003250A1

公开(公告)日：2010-01-07

申请号：US12496675

申请日：2009-07-02

申请人： Zecheng Chen ,  Aranapakam Mudumbai Venkatesan ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Kevin Joseph Curran

发明人： Zecheng Chen ,  Aranapakam Mudumbai Venkatesan ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Kevin Joseph Curran

IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K39/395 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The invention relates to 2-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine 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2-芳基-7H-吡咯并[2,3-d]嘧啶-4-基）吗啉化合物或其药学上可接受的盐，其中组分变量如本文所定义，组合物包含 化合物，以及制备和使用该化合物的方法。