JP2013518890A5 - - Google Patents

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JP2013518890A5
JP2013518890A5 JP2012552068A JP2012552068A JP2013518890A5 JP 2013518890 A5 JP2013518890 A5 JP 2013518890A5 JP 2012552068 A JP2012552068 A JP 2012552068A JP 2012552068 A JP2012552068 A JP 2012552068A JP 2013518890 A5 JP2013518890 A5 JP 2013518890A5
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JP
Japan
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pyrazin
dihydropyrazino
pyridin
methyl
triazol
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JP2012552068A
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Japanese (ja)
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JP2013518890A (ja
JP6114554B2 (ja
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Priority claimed from PCT/US2011/023524 external-priority patent/WO2011097333A1/en
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JP2012552068A 2010-02-03 2011-02-03 Torキナーゼ阻害剤に対する感受性についての予測的なバイオマーカーとしてのlkb1変異の同定 Active JP6114554B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30115010P 2010-02-03 2010-02-03
US61/301,150 2010-02-03
US36298210P 2010-07-09 2010-07-09
US61/362,982 2010-07-09
PCT/US2011/023524 WO2011097333A1 (en) 2010-02-03 2011-02-03 Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors

Publications (3)

Publication Number Publication Date
JP2013518890A JP2013518890A (ja) 2013-05-23
JP2013518890A5 true JP2013518890A5 (https=) 2015-06-18
JP6114554B2 JP6114554B2 (ja) 2017-04-12

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JP2012552068A Active JP6114554B2 (ja) 2010-02-03 2011-02-03 Torキナーゼ阻害剤に対する感受性についての予測的なバイオマーカーとしてのlkb1変異の同定

Country Status (24)

Country Link
US (1) US9555033B2 (https=)
EP (2) EP2531194B1 (https=)
JP (1) JP6114554B2 (https=)
KR (2) KR101942212B1 (https=)
CN (1) CN102821767A (https=)
AR (1) AR080643A1 (https=)
AU (1) AU2011212927B2 (https=)
BR (1) BR112012019459A2 (https=)
CA (1) CA2788678C (https=)
CR (1) CR20120406A (https=)
EC (1) ECSP12012080A (https=)
ES (1) ES2670659T3 (https=)
HK (1) HK1221642A1 (https=)
IL (1) IL221282A (https=)
MX (1) MX2012009030A (https=)
NI (1) NI201200128A (https=)
NZ (1) NZ601581A (https=)
PH (2) PH12012501581A1 (https=)
RU (1) RU2565034C2 (https=)
SG (1) SG183155A1 (https=)
TW (1) TWI578989B (https=)
UA (1) UA110697C2 (https=)
WO (1) WO2011097333A1 (https=)
ZA (1) ZA201305379B (https=)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8299248B2 (en) 2006-08-02 2012-10-30 Cytokinetics, Incorporated Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols and methods for their use
CA2843887A1 (en) * 2011-08-03 2013-02-07 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for lkb1 status
KR101978537B1 (ko) * 2011-10-19 2019-05-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제를 사용한 암의 치료
JP6076370B2 (ja) 2011-12-02 2017-02-08 シグナル ファーマシューティカルズ,エルエルシー 7−(6−(2−ヒドロキシプロパン−2−イル)ピリジン−3−イル)−1−((トランス)−4−メトキシシクロヘキシル)−3,4−ジヒドロピラジノ[2,3−b]ピラジン−2(1H)−オンの薬剤組成物、その固体形態、およびその使用方法
WO2013103836A2 (en) * 2012-01-05 2013-07-11 Dana-Farber Cancer Institute, Inc. Methods of treating cancer
TWI615143B (zh) * 2012-02-24 2018-02-21 標誌製藥公司 使用tor激酶抑制劑組合療法以治療癌症之方法
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
EP2945636B1 (en) 2013-01-16 2017-06-28 Signal Pharmaceuticals, LLC Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
TW201521725A (zh) 2013-04-17 2015-06-16 Signal Pharm Llc 使用tor激酶抑制劑組合療法以治療癌症之方法
BR112015026292B1 (pt) 2013-04-17 2022-04-12 Signal Pharmaceuticals, Llc Uso de 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino [2,3-b]pirazin-2(1h)- ona e métodos in vitro
US9782427B2 (en) 2013-04-17 2017-10-10 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
BR112015026297B1 (pt) 2013-04-17 2022-08-23 Signal Pharmaceuticals, Llc Uso de um inibidor da quinase tor e quinazolinona 5-substituída, composição farmacêutica que os compreende, e kit
AU2014254052B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
US9937169B2 (en) 2013-04-17 2018-04-10 Signal Pharmaceuticals, Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
TW201527300A (zh) 2013-04-17 2015-07-16 Signal Pharm Llc 關於1-乙基-7-(2-甲基-6-(1H-1,2,4-三唑-3-基)吡啶-3-基)-3,4-二氫吡并[2,3-b]吡-2(1H)-酮之醫藥調配物、方法、固態型式及使用方法
EP3003313A1 (en) 2013-05-29 2016-04-13 Signal Pharmaceuticals, LLC Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
KR101602532B1 (ko) 2013-08-29 2016-03-11 경북대학교 산학협력단 위암의 재발 가능성 예측을 위한 정보제공 방법
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
US9512129B2 (en) 2014-04-16 2016-12-06 Signal Pharmaceuticals, Llc Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
EA201790189A1 (ru) 2014-07-14 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе
KR101765335B1 (ko) * 2014-09-26 2017-08-22 서울대학교산학협력단 암 세포 조영용 mri 조영제 조성물
KR101720046B1 (ko) * 2014-09-26 2017-03-29 서울대학교산학협력단 광역학 치료용 자기조립형 약학 조성물
US10189841B2 (en) 2015-11-20 2019-01-29 Forma Therapeutics, Inc. Purinones as ubiquitin-specific protease 1 inhibitors
SMT202100225T1 (it) 2016-12-20 2021-05-07 Astrazeneca Ab Composti di ammino-triazolopiridina e loro uso nel trattamento del cancro
EP3641772B1 (en) 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
RU2646513C1 (ru) * 2017-08-30 2018-03-05 Федеральное государственное бюджетное учреждение "Ростовский научно-исследовательский онкологический институт" Министерства здравоохранения Российской Федерации Способ лечения местно-распространенного рака легкого iiв-iiiа стадии
CN109298102B (zh) * 2018-12-03 2021-09-21 瑞德肝脏疾病研究(上海)有限公司 一种药物肺部代谢特征的体外评价方法

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW274550B (https=) * 1992-09-26 1996-04-21 Hoechst Ag
CA2311414A1 (en) 1997-11-27 1999-06-10 Chugai Research Institute For Molecular Medicine, Inc. Diagnostic method, diagnostic reagent and therapeutic preparation for diseases caused by variation in lkb1 gene
EP1186232A4 (en) 1999-05-31 2004-11-10 Chugai Pharmaceutical Co Ltd 'KNOCKOUT' ANIMALS LACKING THE LKB1 GENE
TWI314928B (en) 2002-02-28 2009-09-21 Novartis A 5-phenylthiazole derivatives and use as pi3 kinase inhibitors
US7423148B2 (en) 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
DE602004013160T2 (de) 2003-07-17 2009-07-02 University Of Dundee, Dundee Verfahren zur anwendung eines an lkb1/strad/mo25-komplexes
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
US20080194019A1 (en) 2003-09-09 2008-08-14 Beth Israel Deaconess Medical Center, Inc. Tumor Suppressor Lkb1 Kinase Directly Activates Amp-Activated Kinase
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
US20060058311A1 (en) * 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
WO2006036883A2 (en) 2004-09-24 2006-04-06 Janssen Pharmaceutica, N.V. Imidazo{4,5-b}pyrazinone inhibitors of protein kinases
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
AU2005316668B2 (en) * 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
AU2006217744A1 (en) 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited 2,4-diamino-pyridopyrimidine derivatives and their use as MTOR inhibitors
AU2006217742A1 (en) 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited Hydrazinomethyl, HYDR zonomethyl and 5-membered heterocylic compounds which act as MTOR inhibitors and their use as anti cancer agents
CN101395155A (zh) 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
US8247408B2 (en) 2005-10-07 2012-08-21 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer
BRPI0617162B8 (pt) 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
EP2385053B1 (en) 2005-11-17 2013-10-02 OSI Pharmaceuticals, Inc. Intermediates for the preparation of fused bicyclic mTOR inhibitors
PL1954699T3 (pl) 2005-11-22 2013-01-31 Kudos Pharm Ltd Pochodne pirydo-, pirazo- i pirymidopirymidyny jako inhibitory mTOR
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525081D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
JP2009523161A (ja) 2006-01-11 2009-06-18 アストラゼネカ アクチボラグ モルホリノピリミジン誘導体と療法におけるその使用
WO2007125321A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
MX2008013578A (es) 2006-04-26 2009-03-23 Hoffmann La Roche Derivados de tieno [3,2-d]pirimidina utiles como inhibidores de fosfatidilinositol 3-cinasa(p13k).
EP2016075A1 (en) 2006-05-03 2009-01-21 AstraZeneca AB Thiazole derivatives and their use as anti-tumour agents
US20090118336A1 (en) 2006-05-03 2009-05-07 Laurent David Pyrazole derivatives and their use as pi3k inhibitors
WO2007135398A1 (en) 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
KR101438245B1 (ko) * 2006-08-23 2014-09-04 쿠도스 파마슈티칼스 리미티드 Mtor 억제제로서의 2-메틸모르폴린 피리도-, 피라조- 및 피리미도-피리미딘 유도체
CN101595103A (zh) 2006-09-14 2009-12-02 阿斯利康(瑞典)有限公司 嘧啶衍生物
JP2010503651A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性障害の治療用のPI3K及びmTOR阻害剤としての2−ベンゾイミダゾリル−6−モルホリノ−フェニルピリミジン誘導体
EP2069330A1 (en) 2006-09-14 2009-06-17 AstraZeneca AB 2 -benzimidazolyl- 6 -morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032036A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 6-benzimidaz0lyl-2-m0rph0lin0-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032060A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperazinylpyrimidine derivatives as p13k and mtor inhibitors for the treatment of proliferative disorders
WO2008032091A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032027A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032072A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 2-benzimidaz0lyl-6-m0rph0lin0-4-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032089A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
ATE543819T1 (de) 2006-10-19 2012-02-15 Signal Pharm Llc Heteroarylverbindungen, zusammensetzungen daraus und behandlungsverfahren damit
US7968556B2 (en) * 2006-10-19 2011-06-28 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
RS53335B (sr) 2006-11-20 2014-10-31 Novartis Ag Kristalna monotozilatna so 2-metil-2-[4-(3-metil-2-okso-8-hinolin-3-il-2,3-dihidro-imidazo[4,5-c]hinolin-1-il)-fenil]-propionitrila
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
EP2178563A2 (en) * 2007-07-06 2010-04-28 OSI Pharmaceuticals, Inc. Combination anti-cancer therapy comprising an inhibitor of both mtorc1 and mtorc2
WO2009007751A2 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
CA2692945A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Compounds - 945
CN101809002B (zh) 2007-07-09 2013-03-27 阿斯利康(瑞典)有限公司 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物
EP2178866A2 (en) 2007-07-09 2010-04-28 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
US8129371B2 (en) 2007-10-16 2012-03-06 Wyeth Llc Thienopyrimidine and pyrazolopyrimidine compounds and their use as mTOR kinase and PI3 kinase inhibitors
WO2009091788A1 (en) 2008-01-15 2009-07-23 Wyeth 3h-[1,2,3]triazolo[4,5-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
US20110091574A1 (en) 2008-02-15 2011-04-21 Catholic Healthcare West Treatment of adenocarcinoma expressing lkb1 with mtor inhibitor in combination with cox2 inhibitor
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
US8110578B2 (en) * 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
NO2477987T3 (https=) * 2009-09-14 2018-06-09
US8541418B2 (en) 2009-12-23 2013-09-24 Elan Pharmaceutical, Inc. Inhibitors of polo-like kinase
US20110318336A1 (en) 2010-03-29 2011-12-29 George Mason Intellectual Properties, Inc. Identification and Treatment of Aggressive Lung Cancer Tumors

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