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1. 发明申请

WO2010030967A1 4-ARYLOXYQUINOLIN-2(1H)-ONES AS MTOR KINASE AND PI3 KINASE INHIBITORS, FOR USE AS ANTI-CANCER AGENTS 审中-公开
标题翻译： 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：WO2010030967A1
公开(公告)日：2010-03-18
申请号：PCT/US2009/056783
申请日：2009-09-14
申请人： WYETH LLC , TSOU, Hwei-Ru , BIRNBERG, Gary, Harold , MAC EWAN, Gloria, Jean , OTTENG, Mercy, Adufa , NOWAK, Pawel, Wojciech , AYRAL-KALOUSTIAN, Semiramis , MANSOUR, Tarek, Suhayl , ZASK, Arie , YU, Ker
发明人： TSOU, Hwei-Ru , BIRNBERG, Gary, Harold , MAC EWAN, Gloria, Jean , OTTENG, Mercy, Adufa , NOWAK, Pawel, Wojciech , AYRAL-KALOUSTIAN, Semiramis , MANSOUR, Tarek, Suhayl , ZASK, Arie , YU, Ker
IPC分类号： C07D215/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , A61K31/4704 , A61P35/00
CPC分类号： C07D215/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12
摘要： 4-aryloxyquinolin-2(1H)-ones as mtor kinase and PI3 kinase inhibitors, for use as anti-cancer agents. Compounds of the formula I and pharmaceutically acceptable salts thereof, wherein A, B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 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：作为mTOR激酶和PI3激酶抑制剂的4-芳氧基喹啉-2（1H） - 酮用作抗癌剂。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如本文所述定义。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。

2. 发明申请

WO2009091788A1 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： 3H- [1,2,3]三唑[4,5-D]吡嗪化合物，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：WO2009091788A1
公开(公告)日：2009-07-23
申请号：PCT/US2009/030939
申请日：2009-01-14
申请人： WYETH , DEHNHARDT, Christoph, Martin , VENKATESAN, Aranapakam, Mudumbai , DELOS SANTOS, Efren, Guillermo , CHEN, Zecheng , DOS SANTOS, Osvaldo , BROOIJMANS, Natasja , ZASK, Arie , VERHEIJEN, Jeroen Cunera , AYRAL-KALOUSTIAN, Semiramis
发明人： DEHNHARDT, Christoph, Martin , VENKATESAN, Aranapakam, Mudumbai , DELOS SANTOS, Efren, Guillermo , CHEN, Zecheng , DOS SANTOS, Osvaldo , BROOIJMANS, Natasja , ZASK, Arie , VERHEIJEN, Jeroen Cunera , AYRAL-KALOUSTIAN, Semiramis
IPC分类号： A61K31/519 , A61P35/00 , C07D487/04
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方法用于制造和使用这些化合物。

3. 发明申请

WO2008116129A3 IMIDAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS PI3 KINASE AND MTOR INHIBITORS 审中-公开
标题翻译：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：WO2008116129A3
公开(公告)日：2009-02-12
申请号：PCT/US2008057771
申请日：2008-03-21
申请人： WYETH CORP , BURSAVICH MATTHEW GREGORY , VENKATESAN ARANAPAKAM MUDUMBAI , NOWAK PAWEL WOJCIECH , LOMBARDI SABRINA , GILBERT ADAM MATTHEW , DEHNHARDT CHRISTOPH MARTIN , DOS SANTOS OSVALDO , DELOS SANTOS EFREN GUILLERMO , BROOIJMANS NATASJA , AYRAL-KALOUSTIAN SEMIRAMIS , CHEN ZECHENG , VERHEIJEN JEROEN CUNERA , KAPLAN JOSHUA , ZASK ARIE
发明人： BURSAVICH MATTHEW GREGORY , VENKATESAN ARANAPAKAM MUDUMBAI , NOWAK PAWEL WOJCIECH , LOMBARDI SABRINA , GILBERT ADAM MATTHEW , DEHNHARDT CHRISTOPH MARTIN , DOS SANTOS OSVALDO , DELOS SANTOS EFREN GUILLERMO , BROOIJMANS NATASJA , AYRAL-KALOUSTIAN SEMIRAMIS , CHEN ZECHENG , VERHEIJEN JEROEN CUNERA , KAPLAN JOSHUA , ZASK ARIE
IPC分类号： C07D473/34 , A61K31/52 , A61P35/00
CPC分类号： C07D473/34
摘要： The present invention relates to Imidazolopyrimidine Analogs, of Formula Ib methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods fot treating ot 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：本发明涉及咪唑并吡啶类似物，式Ib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，以及不能预防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。本发明还涉及用于治疗或预防mTOR相关疾病的方法，包括向有需要的受试者施用有效量的咪唑并嘧啶类似物。

4. 发明申请

WO2008086462A2 AMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS INHIBITORS OF ß-CANTENIN/TCF-4 PATHWAY AND CANCER TREATMENT AGENTS 审中-公开
标题翻译：氨基取代的喹唑啉衍生物作为β-CANTENIN / TCF-4途径和癌症治疗剂的抑制剂
公开(公告)号：WO2008086462A2
公开(公告)日：2008-07-17
申请号：PCT/US2008050728
申请日：2008-01-10
申请人： WYETH CORP , VENKATESAN ARANAPAKAM M , DEHNHARDT CHRISTOPH , CHEN ZECHENG , SANTOS OSVALDO DOS , SANTOS EFREN DELOS , CURRAN KEVIN , AYRAL-KALOUSTIAN SEMIRAMIS , CHEN LEI
发明人： VENKATESAN ARANAPAKAM M , DEHNHARDT CHRISTOPH , CHEN ZECHENG , SANTOS OSVALDO DOS , SANTOS EFREN DELOS , CURRAN KEVIN , AYRAL-KALOUSTIAN SEMIRAMIS , CHEN LEI
IPC分类号： C07D239/95 , A61K31/517 , A61P35/00 , C07D401/12 , C07D401/14 , C07D403/12
CPC分类号： C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present invention relates to amino-substituted quinazoline derivatives as inhibitors of ß-catenin/tcf-4 pathway, which can be useful in the treatment of cancer; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.
摘要翻译：本发明涉及作为β-连环蛋白/ tcf-4途径抑制剂的氨基取代的喹唑啉衍生物，其可用于治疗癌症; 为他们的准备过程; 包含它们的药物组合物; 以及使用它们的方法。

5. 发明申请

WO2005030775A1 6-[(SUBSTITUTED)PHENYL]TRIAZOLOPYRIMIDINES AS ANTICANCER AGENTS 审中-公开
标题翻译： 6 - [（取代的）苯基]三唑并嘧啶作为反应剂
公开(公告)号：WO2005030775A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/030515
申请日：2004-09-17
申请人： WYETH HOLDINGS CORPORATION , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , WU, Yanzhong , TONG, Wei
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , WU, Yanzhong , TONG, Wei
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及某些6 - [（取代的）苯基]三唑并嘧啶化合物或其药学上可接受的盐，以及含有所述化合物或其药学上可接受的盐的组合物，其中所述化合物是可用于治疗哺乳动物癌症的抗癌剂。本发明还涉及治疗或抑制哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，并进一步提供了治疗或预防表达多重耐药性（MDR）或耐多药耐药性的癌性肿瘤的方法在有需要的哺乳动物中，所述方法包括向所述哺乳动物施用有效量的所述化合物或其药学上可接受的盐。本发明涉及通过促进微管聚合来治疗或抑制有需要的哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，其包括对所述哺乳动物施用有效量的所述化合物及其药学上可接受的盐。

6. 发明申请

WO2010120994A3 UREIDOARYL-AND CARBAMOYLARYL-MORPHOLINO- PYRIMIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS 审中-公开
标题翻译：尿嘧啶和卡巴酰-L-吗啉 - 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：WO2010120994A3
公开(公告)日：2013-08-01
申请号：PCT/US2010031183
申请日：2010-04-15
申请人： WYETH LLC , VERHEIJEN JEROEN CUNERA , ZASK ARIE , AYRAL-KALOUSTIAN SEMIRAMIS , DEHNHARDT CHRISTOPH MARTIN , ZHANG NAN , VENKATESAN ARANAPAKAM MUDUMBAI , NGUYEN THAI HIEP , CURRAN KEVIN JOSEPH , KAPLAN JOSHUA AARON
发明人： VERHEIJEN JEROEN CUNERA , ZASK ARIE , AYRAL-KALOUSTIAN SEMIRAMIS , DEHNHARDT CHRISTOPH MARTIN , ZHANG NAN , VENKATESAN ARANAPAKAM MUDUMBAI , NGUYEN THAI HIEP , CURRAN KEVIN JOSEPH , KAPLAN JOSHUA AARON
IPC分类号： C07D239/42 , C07D239/38 , C07D401/12 , C07D405/04 , C07D471/04 , C07D487/04 , C07D491/147 , C07D495/04
CPC分类号： C07D495/04 , C07D239/42 , C07D239/48 , C07D401/12 , C07D405/04 , C07D405/14 , C07D471/04 , C07D487/04 , C07D491/052 , C07D491/147
摘要： The invention relates to ureidophenyl-morpholino pyrimidine and guanidinophenyl-morpholino pyrimidine compounds of formula, and to methods for making and using the compounds.
摘要翻译：本发明涉及式I的脲基苯基 - 吗啉代嘧啶和胍基苯基 - 吗啉代嘧啶化合物，以及制备和使用该化合物的方法。

7. 发明申请

WO2010120987A1 RING FUSED, UREIDOARYL- AND CARBAMOYLARYL-BRIDGED MORPHOLINO-PYRIMIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： RING FUSED，UREIDOARYL-和CARBAMOYLARYL-BRIDGED MORPHOLINO-PYRIMININE COMPOUNDS，THEAR Use as MTOR KINASE and PI3 KINASE INHIBITORS AND AND THE SYNTHESES
公开(公告)号：WO2010120987A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/031175
申请日：2010-04-15
申请人： WYETH LLC , ZASK, Arie , VERHEIJEN, Jeroen Cunera , KAPLAN, Joshua Aaron , CURRAN, Kevin Joseph , AYRAL-KALOUSTIAN, Semiramis , RICHARD, David James
发明人： ZASK, Arie , VERHEIJEN, Jeroen Cunera , KAPLAN, Joshua Aaron , CURRAN, Kevin Joseph , AYRAL-KALOUSTIAN, Semiramis , RICHARD, David James
IPC分类号： C07D413/04 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D491/147 , A61K31/517 , A61K31/519 , A61P35/00
CPC分类号： C07D413/04 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/147 , C07D495/04
摘要： The invention relates to ring fused, bridged 4-morpholino-pyhmidine compounds of Formula (I), their ring homologues and methods for making and using the compounds.
摘要翻译：本发明涉及式（I）的环稠合的桥连的4-吗啉代 - 嘧啶化合物，它们的环同系物以及制备和使用该化合物的方法。

8. 发明申请

WO2010011620A1 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
标题翻译： 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：WO2010011620A1
公开(公告)日：2010-01-28
申请号：PCT/US2009/051202
申请日：2009-07-21
申请人： WYETH , BURSAVICH, Matthew, G. , NOWAK, Pawel, W. , MALWITZ, David , LOMBARDI, Sabrina , GILBERT, Adam, M. , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , ANDERSON, James, Thomas , BROOIJMANS, Natasja
发明人： BURSAVICH, Matthew, G. , NOWAK, Pawel, W. , MALWITZ, David , LOMBARDI, Sabrina , GILBERT, Adam, M. , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , ANDERSON, James, Thomas , BROOIJMANS, Natasja
IPC分类号： C07D487/04 , A61K31/4188 , 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- （I）的芳基-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。

9. 发明申请

WO2007075783A3 SUBSTITUTED ISOQUINOLINE-1,3(2H,4H)-DIONES, 1-THIOXO-1,4-DIHYDRO-2H-ISOQUINOLINE-3-ONES AND 1,4-DIHYDRO-3(2H)-ISOQUINOLONES AND USE THEREOF AS KINASE INHIBITOR 审中-公开
公开(公告)号：WO2007075783A3
公开(公告)日：2007-07-05
申请号：PCT/US2006/048603
申请日：2006-12-20
申请人： WYETH , TSOU, Hwei-Ru , AYRAL-KALOUSTIAN, Semiramis , BIRNBERG, Gary, Harold , FLOYD, Middleton, Brawner , KAPLAN, Joshua , KUTTERER, Kristina, M.K. , LIU, Xiaoxiang , NILAKANTAN, Ramaswamy , OTTENG, Mercy, Adufa , TANG, Zhilian , ZASK, Arie , REICH, Marvin , TRAN, Tritan
发明人： TSOU, Hwei-Ru , AYRAL-KALOUSTIAN, Semiramis , BIRNBERG, Gary, Harold , FLOYD, Middleton, Brawner , KAPLAN, Joshua , KUTTERER, Kristina, M.K. , LIU, Xiaoxiang , NILAKANTAN, Ramaswamy , OTTENG, Mercy, Adufa , TANG, Zhilian , ZASK, Arie , REICH, Marvin , TRAN, Tritan
IPC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
摘要： This invention provides compounds of Formula (I), having the structure where G 1 , G 2 , G 3 , G 4 , A 1 , A 2 , Y 1 , Y 2 , L 1 , Z, e and f are defined herein, or a pharmaceutically acceptable salt thereof, which are useful for treating or preventing cancer.

10. 发明申请

WO2004026293A2 METHOD OF TREATING RESISTANT TUMORS 审中-公开
标题翻译：治疗抵抗性肿瘤的方法
公开(公告)号：WO2004026293A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/029832
申请日：2003-09-18
申请人： WYETH HOLDINGS CORPORATION , GREENBERGER, Lee, Martin , LOGANZO, Frank, Jr. , DISCAFANI-MARRO, Carolyn, Mary , ZASK, Arie , AYRAL-KALOUSTIAN, Semiramis
发明人： GREENBERGER, Lee, Martin , LOGANZO, Frank, Jr. , DISCAFANI-MARRO, Carolyn, Mary , ZASK, Arie , AYRAL-KALOUSTIAN, Semiramis
IPC分类号： A61K31/191
CPC分类号： A61K31/194 , A61K31/191 , A61K31/192 , A61K31/195
摘要： The invention provides a method of treating or inhibiting the growth of or eradicating a tumor in a mammal in need thereof wherein said tumor is resistant to at least one chemotherapeutic agents which method comprises providing to said mammal an effective amount of a compound of Formula II or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了治疗或抑制有需要的哺乳动物肿瘤生长或根除肿瘤的方法，其中所述肿瘤对至少一种化学治疗剂具有抗性，该方法包括向所述哺乳动物提供有效量的式II化合物或其药学上可接受的盐。

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