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1.发明申请3-SUBSTITUTED-1H-INDOLE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开3-取代的1H-吲哚化合物，它们作为MTOR激酶和PI3激酶抑制剂使用，以及它们的合成公开(公告)号：US20090311217A1
公开(公告)日：2009-12-17
申请号：US12473605
申请日：2009-05-28
申请人： Matthew Gregory Bursavich , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Thai Hiep Nguyen , Sabrina Lombardi , David Malwitz , Natasja Brooijmans , Derek Cecil Cole , Adam Matthew Gilbert , Pawel Wojciech Nowak , Kaapjoo Park , Sasmita Das , Hwei-Ru Tsou , Aranapakam Mudumbai Venkatesan , Mercy Adufa Otteng , Gary Harold Birnberg , Gloria Jean MacEwan
发明人： Matthew Gregory Bursavich , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Thai Hiep Nguyen , Sabrina Lombardi , David Malwitz , Natasja Brooijmans , Derek Cecil Cole , Adam Matthew Gilbert , Pawel Wojciech Nowak , Kaapjoo Park , Sasmita Das , Hwei-Ru Tsou , Aranapakam Mudumbai Venkatesan , Mercy Adufa Otteng , Gary Harold Birnberg , Gloria Jean MacEwan
IPC分类号： A61K31/404 , C07D405/02 , C07D403/14 , C07D413/02 , A61K31/496 , A61K31/5377 , A61K38/21 , A61K39/395 , A61P35/00
CPC分类号： C07D405/14 , C07D405/06
摘要： The invention relates to 3-substituted-1H-indole 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3-取代-1H-吲哚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，以及制备和使用该化合物的方法。
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![3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES](/abs-image/US/2009/12/03/US20090298820A1/abs.jpg.150x150.jpg)
2.发明申请3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开3-取代的1H-吡咯并[2,3-b]吡啶和3-取代的1H-吡咯[3,2-B]吡啶化合物，它们作为MTOR激酶和PI3激酶抑制剂使用，以及它们的合成公开(公告)号：US20090298820A1
公开(公告)日：2009-12-03
申请号：US12473658
申请日：2009-05-28
申请人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Semiramis Ayral-Kaloustian , Matthew Gregory Bursavich , Sabrina Lombardi , Nan Zhang , Adam Matthew Gilbert , George Theordore Grosu , Natasja Brooijmans , Thai Hiep Nguyen
发明人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Semiramis Ayral-Kaloustian , Matthew Gregory Bursavich , Sabrina Lombardi , Nan Zhang , Adam Matthew Gilbert , George Theordore Grosu , Natasja Brooijmans , Thai Hiep Nguyen
IPC分类号： A61K31/437 , A61K31/5375 , A61K31/5377 , A61K31/496 , C07D471/04 , A61P35/00 , C07D498/08 , A61P29/00 , A61P17/00 , A61P19/00
CPC分类号： C07D471/04 , C07D498/08
摘要： The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine 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3-取代-1H-吡咯并[2,3-b]吡啶和3-取代-1H-吡咯并[3,2-b]吡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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![4-PHENOXY-6-ARYL-1H-PYRAZOLO[3,4-D]PYRIMIDINE AND N-ARYL-6-ARYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES](/abs-image/US/2010/01/21/US20100015141A1/abs.jpg.150x150.jpg)
3.发明申请4-PHENOXY-6-ARYL-1H-PYRAZOLO[3,4-D]PYRIMIDINE AND N-ARYL-6-ARYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开4-苯基-6-芳基-1H-吡唑并[3,4-D]吡嗪和N-芳基-6-芳基-1H-吡唑并[3,4-D]嘧啶-4-胺化合物，它们作为MTOR KINASE 和PI3激酶抑制剂及其合成公开(公告)号：US20100015141A1
公开(公告)日：2010-01-21
申请号：US12506291
申请日：2009-07-21
申请人： Matthew Gregory Bursavich , Pawel Wojciech Nowak , David Malwitz , Sabrina Lombardi , Adam Matthew Gilbert , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Natasja Brooijmans
发明人： Matthew Gregory Bursavich , Pawel Wojciech Nowak , David Malwitz , Sabrina Lombardi , Adam Matthew Gilbert , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Natasja Brooijmans
IPC分类号： A61K31/519 , C07D487/04 , A61K39/395 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to 4,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine compounds, including 4-phenoxy-6-aryl-1H-pyrazolo[3,4-d]pyrimidine and N-aryl-6-aryl-1H-pyrazolo[3,4-d]pyrimidin-4-amine 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4,6-二取代-1H-吡唑并[3,4-d]嘧啶-4-胺化合物，包括4-苯氧基-6-芳基-1H-吡唑并[3,4-d]嘧啶和N- 芳基-6-芳基-1H-吡唑并[3,4-d]嘧啶-4-胺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和方法 用于制造和使用这些化合物。
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4.发明申请IMIDAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS PI3 KINASE AND MTOR INHIBITORS 审中-公开咪唑吡嗪类似物及其作为PI3激酶和MT抑制剂的用途公开(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。
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5.发明申请4-ARYLOXYQUINOLIN-2(1H)-ONES AS MTOR KINASE AND PI3 KINASE INHIBITORS, FOR USE AS ANTI-CANCER AGENTS 审中-公开4-ARYLOXYQUINOLIN-2（1H） - 作为MTOR激酶和PI3激酶抑制剂，用作抗癌剂公开(公告)号：US20100068204A1
公开(公告)日：2010-03-18
申请号：US12558661
申请日：2009-09-14
申请人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Mercy Adufa Otteng , Pawel Wojciech Nowak , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Arie Zask , Ker Yu
发明人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Mercy Adufa Otteng , Pawel Wojciech Nowak , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Arie Zask , Ker Yu
IPC分类号： A61K39/395 , C07D215/00 , A61K31/47
CPC分类号： C07D215/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12
摘要： Compounds of the formula I and pharmaceutically acceptable salts thereof, wherein A, B, R1, R2, R3, R4, R5, R6, and R7 are defined as set forth herein are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds of the invention and a pharmaceutically acceptable carrier, methods of making the compounds of the invention and methods of using the compounds for inhibiting mTOR and PI3 kinases and for treating cancers.
摘要翻译： 公开了式I化合物及其药学上可接受的盐，其中A，B，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。 还公开了包含本发明化合物和药学上可接受的载体的药物组合物，制备本发明化合物的方法和使用该化合物抑制mTOR和PI3激酶和治疗癌症的方法。
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6.发明授权Substituted isoquinoline-1,3(2H,4H)-diones, 1-thioxo,1,4-dihydro-2H-isoquinoline-3-ones and 1,4-dihyro-3 (2H)-isoquinolones and methods of use thereof 失效取代的异喹啉-1,3（2H，4H） - 二酮，1-硫代，1,4-二氢-2H-异喹啉-3-酮和1,4-二羟基-3（2H） - 异喹诺酮及其使用方法公开(公告)号：US07713994B2
公开(公告)日：2010-05-11
申请号：US11728897
申请日：2007-03-26
申请人： Hwei-Ru Tsou , Semiramis Ayral-Kaloustian , Gary Harold Birnberg , Middleton Brawner Floyd , Joshua Kaplan , Kristina M. Kutterer , Xiaoxiang Liu , Ramaswamy Nilakantan , Mercy Adufa Otteng , Zhilian Tang , Arie Zask , Tritin Tran , Scott Christian Mayer , Annette L. Banker , Marvin Reich
发明人： Hwei-Ru Tsou , Semiramis Ayral-Kaloustian , Gary Harold Birnberg , Middleton Brawner Floyd , Joshua Kaplan , Kristina M. Kutterer , Xiaoxiang Liu , Ramaswamy Nilakantan , Mercy Adufa Otteng , Zhilian Tang , Arie Zask , Tritin Tran , Scott Christian Mayer , Annette L. Banker , Marvin Reich
IPC分类号： A61K31/47 , C07D217/08
CPC分类号： C07D217/24 , C07D237/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D487/04
摘要： This invention provides compounds of Formula (I), having the structure where G1, G2, G3, G4, A1, A2, Y1, Y2, L1, Z, e and f are defined herein, or a pharmaceutically acceptable salt thereof, which are useful for treating or preventing cancer.
摘要翻译： 本发明提供具有本文定义的G1，G2，G3，G4，A1，A2，Y1，Y2，L1，Z，e和f的结构的式（I）化合物或其药学上可接受的盐， 可用于治疗或预防癌症。
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7.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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![[a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES](/abs-image/US/2009/07/30/US20090192147A1/abs.jpg.150x150.jpg)
8.发明申请[a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开[a] - 兴奋剂化合物，它们作为mTOR激酶和PI3激酶抑制剂使用，以及它们的合成公开(公告)号：US20090192147A1
公开(公告)日：2009-07-30
申请号：US12363013
申请日：2009-01-30
申请人： Semiramis Ayral-Kaloustian , Nan Zhang , Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Thai Hiep Nguyen , James Thomas Anderson
发明人： Semiramis Ayral-Kaloustian , Nan Zhang , Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Thai Hiep Nguyen , James Thomas Anderson
IPC分类号： A61K31/5383 , C07D471/00 , A61K31/437 , C07D487/00 , A61K31/4985
CPC分类号： C07D498/04 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D491/04 , C07D491/14 , C07D498/14 , C07D513/04 , C07D513/14
摘要： The invention relates to [a]-fused indole compounds of the Formula II, or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein. The invention also relates to compositions comprising the compounds of Formula II, and methods for making and using the compounds.
摘要翻译： 本发明涉及式[II]的[a] - 吲哚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。 本发明还涉及包含式II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-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES](/abs-image/US/2010/03/11/US20100061982A1/abs.jpg.150x150.jpg)
9.发明申请3-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开3-取代的1H-吲哚，3-取代的1H-吡咯并[2,3-b]吡啶和3-取代的1H-吡咯[3,2-B]吡啶化合物，它们作为MTOR激酶和PI3激酶抑制剂 ，和他们的合成公开(公告)号：US20100061982A1
公开(公告)日：2010-03-11
申请号：US12556833
申请日：2009-09-10
申请人： Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Hwei-Ru Tsou , Nan Zhang , Aranapakam Mudumbai Venkatesan , Li Di , Edward Harvel Kerns
发明人： Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Hwei-Ru Tsou , Nan Zhang , Aranapakam Mudumbai Venkatesan , Li Di , Edward Harvel Kerns
IPC分类号： A61K39/395 , C07D405/06 , A61K31/40 , C07D403/06 , A61K31/497 , C07D498/02 , A61K31/5386
CPC分类号： C07D407/06 , C07D471/04
摘要： The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine 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3-取代-1H-吲哚，3-取代-1H-吡咯并[2,3-b]吡啶和3-取代-1H-吡咯并[3,2-b]吡啶化合物： 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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10.发明申请2-Aryl- and 2-Heteroarylthiazolyl Compounds, Methods for Their Preparation and Use Thereof 审中-公开2-芳基和2-杂芳基噻唑化合物，其制备方法及用途公开(公告)号：US20090270363A1
公开(公告)日：2009-10-29
申请号：US12412506
申请日：2009-03-27
申请人： Nan Zhang , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Thai Hiep Nguyen , Chuansheng Niu , Edward Christian Rosfjord , Ronald Suayan , Hwei-Ru Tsou
发明人： Nan Zhang , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Thai Hiep Nguyen , Chuansheng Niu , Edward Christian Rosfjord , Ronald Suayan , Hwei-Ru Tsou
IPC分类号： A61K31/428 , C07D277/66 , C07D417/10 , A61K31/506 , A61K31/397 , A61P35/00
CPC分类号： C07D277/66 , C07D277/60 , C07D417/04 , C07D417/10 , C07D417/12
摘要： The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin, including elevated securin levels.
摘要翻译： 本发明公开了稠合双环2-芳基 - 或2-杂芳基噻唑基化合物及其药学上可接受的盐和酯，其可用于抑制癌细胞的生长，特别是抑制人乳腺癌肿瘤生长，并且治疗相关的疾病或病症 与Securin，包括提高的Securin水平。
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