KR101942212B1 - Ｔｏｒ 키나제 억제자에 대한 민감성 예측 바이오마커로서 ｌｋｂ1 돌연변이의 동정 - Google Patents

Ｔｏｒ 키나제 억제자에 대한 민감성 예측 바이오마커로서 ｌｋｂ1 돌연변이의 동정 Download PDF

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KR101942212B1
KR101942212B1 KR1020177027392A KR20177027392A KR101942212B1 KR 101942212 B1 KR101942212 B1 KR 101942212B1 KR 1020177027392 A KR1020177027392 A KR 1020177027392A KR 20177027392 A KR20177027392 A KR 20177027392A KR 101942212 B1 KR101942212 B1 KR 101942212B1
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substituted
pyrazin
unsubstituted
dihydropyrazino
tor kinase
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KR20170116201A (ko
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사비타 산카르
라제쉬 초프라
웨이밍 수
유홍 닝
슈이찬 수
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시그날 파마소티칼 엘엘씨
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers
    • G01N33/57411—Specifically defined cancers of cervix
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers
    • G01N33/57423—Specifically defined cancers of lung
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020177027392A 2010-02-03 2011-02-03 Ｔｏｒ 키나제 억제자에 대한 민감성 예측 바이오마커로서 ｌｋｂ1 돌연변이의 동정 Active KR101942212B1 (ko)

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

Related Parent Applications (1)

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KR1020127022877A Division KR20120123513A (ko) 2010-02-03 2011-02-03 Ｔｏｒ 키나제 억제자에 대한 민감성 예측 바이오마커로서 ｌｋｂ1 돌연변이의 동정

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KR20170116201A KR20170116201A (ko) 2017-10-18
KR101942212B1 true KR101942212B1 (ko) 2019-01-24

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KR1020127022877A Ceased KR20120123513A (ko) 2010-02-03 2011-02-03 Ｔｏｒ 키나제 억제자에 대한 민감성 예측 바이오마커로서 ｌｋｂ1 돌연변이의 동정
KR1020177027392A Active KR101942212B1 (ko) 2010-02-03 2011-02-03 Ｔｏｒ 키나제 억제자에 대한 민감성 예측 바이오마커로서 ｌｋｂ1 돌연변이의 동정

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US (1) US9555033B2 (enExample)
EP (2) EP2992878A1 (enExample)
JP (1) JP6114554B2 (enExample)
KR (2) KR20120123513A (enExample)
CN (1) CN102821767A (enExample)
AR (1) AR080643A1 (enExample)
AU (1) AU2011212927B2 (enExample)
BR (1) BR112012019459A2 (enExample)
CA (1) CA2788678C (enExample)
CR (1) CR20120406A (enExample)
EC (1) ECSP12012080A (enExample)
ES (1) ES2670659T3 (enExample)
HK (1) HK1221642A1 (enExample)
IL (1) IL221282A (enExample)
MX (1) MX2012009030A (enExample)
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SG (1) SG183155A1 (enExample)
TW (1) TWI578989B (enExample)
UA (1) UA110697C2 (enExample)
WO (1) WO2011097333A1 (enExample)
ZA (1) ZA201305379B (enExample)

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
AU2012290056B2 (en) * 2011-08-03 2015-03-19 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for LKB1 status
WO2013059396A2 (en) * 2011-10-19 2013-04-25 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
MX363034B (es) 2011-12-02 2019-03-06 Signal Pharm Llc Composiciones farmaceuticas de 7-(6-(2-hidroxipropan-2-il)piridin- 3-il)-1-((trans)-4-metoxiciclohexil)-3,4-dihidropirazino[2,3-b]pi razin-2(1h)-ona, una forma solida de las mismas y metodos de su uso.
CA2860665A1 (en) * 2012-01-05 2013-07-11 Dana-Farber Cancer Institute, Inc. Methods of treating cancer
EA028462B1 (ru) * 2012-02-24 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения немелкоклеточного рака легких на поздних стадиях c применением комбинированного лечения с ингибитором киназы tor
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
ES2638179T3 (es) 2013-01-16 2017-10-19 Signal Pharmaceuticals, Llc Compuestos de pirrolopirimidina sustituidos, composiciones de los mismos, y métodos de tratamiento con los mismos
WO2014172432A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
JP6382945B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
KR102459285B1 (ko) 2013-04-17 2022-10-27 시그날 파마소티칼 엘엘씨 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법
CA2909579A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
WO2014172431A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
TWI654979B (zh) 2013-04-17 2019-04-01 美商標誌製藥公司 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法
CN113831345A (zh) 2013-05-29 2021-12-24 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
KR101602532B1 (ko) 2013-08-29 2016-03-11 경북대학교 산학협력단 위암의 재발 가능성 예측을 위한 정보제공 방법
EP3131551A4 (en) 2014-04-16 2017-09-20 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, COMPOSITIONS AND METHODS OF USE THEREOF
WO2015160868A1 (en) 2014-04-16 2015-10-22 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
WO2015160882A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 7-(6-(2-HYDROXYPROPAN-2YL) 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
JP2017520603A (ja) 2014-07-14 2017-07-27 シグナル ファーマシューティカルズ，エルエルシー 置換ピロロピリミジン化合物を使用するがんの治療方法及びその組成物
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
KR101720046B1 (ko) * 2014-09-26 2017-03-29 서울대학교산학협력단 광역학 치료용 자기조립형 약학 조성물
KR101765335B1 (ko) * 2014-09-26 2017-08-22 서울대학교산학협력단 암 세포 조영용 ｍｒｉ 조영제 조성물
KR102708936B1 (ko) 2015-11-20 2024-09-25 포르마 세라퓨틱스 인크. 유비퀴틴-특이적 프로테아제 1 억제제로서의 퓨리논
KR102220971B1 (ko) 2016-12-20 2021-02-25 아스트라제네카 아베 아미노-트리아졸로피리딘 화합물 및 암 치료에서의 이의 용도
SG11201912403SA (en) 2017-06-22 2020-01-30 Celgene Corp 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080194019A1 (en) 2003-09-09 2008-08-14 Beth Israel Deaconess Medical Center, Inc. Tumor Suppressor Lkb1 Kinase Directly Activates Amp-Activated Kinase

Family Cites Families (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW274550B (enExample) 1992-09-26 1996-04-21 Hoechst Ag
WO1999028459A1 (fr) 1997-11-27 1999-06-10 Chugai Research Institute For Molecular Medicine, Inc. Technique d'examen, reactif pour examen et medicament relatif a des affections provoquees par des modifications survenues dans le gene lkb1
WO2000072670A1 (en) 1999-05-31 2000-12-07 Chugai Research Institute For Molecular Medicine, Inc. Lkb1 gene knockout animals
AR038703A1 (es) 2002-02-28 2005-01-26 Novartis Ag Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
MXPA05005477A (es) 2002-11-21 2005-07-25 Chiron Corp Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer.
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
WO2005010174A2 (en) 2003-07-17 2005-02-03 University Of Dundee Methods for use of an lkb1/strad7mo25 complex
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
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
CN101065016A (zh) 2004-09-24 2007-10-31 詹森药业有限公司 蛋白激酶的抑制剂咪唑并[4,5－b]吡嗪酮
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
JP5111113B2 (ja) 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
EP1877388A2 (en) 2005-02-25 2008-01-16 Kudos Pharmaceuticals Ltd Hydrazinomethyl, hydrazonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents
KR20070113252A (ko) 2005-02-25 2007-11-28 쿠도스 파마슈티칼스 리미티드 2,4-디아미노-피리도피리미딘 유도체 및 이의 ｍＴＯＲ억제제로서의 용도
HRP20130902T1 (hr) 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
JP5480503B2 (ja) 2005-10-07 2014-04-23 エクセリクシス， インク． ＰＩ３Ｋαのピリドピリミジノン型阻害剤
EP2364974A1 (en) 2005-10-07 2011-09-14 Exelixis, Inc. N-(3-Phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
KR20080078668A (ko) 2005-11-17 2008-08-27 오에스아이 파마슈티컬스, 인코포레이티드 융합된 바이사이클릭 ｍＴＯＲ 억제자
JP5161102B2 (ja) 2005-11-22 2013-03-13 クドス ファーマシューティカルズ リミテッド ｍＴＯＲ阻害剤としてのピリドピリミジン、ピラゾピリミジンおよびピリミドピリミジン誘導体
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525081D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
US20110034454A1 (en) 2006-01-11 2011-02-10 Allan Paul Dishington Morpholino pyrimidine derivatives and their use in therapy
DK3421471T3 (da) * 2006-04-25 2021-06-14 Astex Therapeutics Ltd Purin- og deazapurinderivater som farmaceutiske forbindelser
PT2024372E (pt) 2006-04-26 2010-09-16 Hoffmann La Roche Derivado de tieno[3,2-d]pirimidina útil como inibidor de pi3k
JP2009535388A (ja) 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ ピラゾール誘導体、及びそのｐｉ３ｋ阻害薬としての使用
WO2007129044A1 (en) 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
EP2029593A1 (en) 2006-05-22 2009-03-04 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
JP2010503649A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ ピリミジン誘導体
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
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
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
JP2010503650A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性疾患の治療のための、ｐｉ３ｋおよびｍｔｏｒ阻害剤としての２−ベンズイミダゾリル−６−モルホリノ−４−ピペリジン−４−イルピリミジン誘導体
WO2008032027A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032028A1 (en) 2006-09-14 2008-03-20 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
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
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
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
KR20140104060A (ko) * 2006-10-19 2014-08-27 시그날 파마소티칼 엘엘씨 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도
ZA200902384B (en) * 2006-10-19 2010-07-28 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
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
JP2010532756A (ja) * 2007-07-06 2010-10-14 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド ｍＴＯＲＣ１及びｍＴＯＲＣ２の両方の阻害剤を含む組み合わせ抗癌療法
EP2178866A2 (en) 2007-07-09 2010-04-28 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
EP2176238B1 (en) 2007-07-09 2012-04-18 AstraZeneca AB Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k
AU2008273892A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
AU2008273889B2 (en) 2007-07-09 2012-03-08 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009052145A1 (en) 2007-10-16 2009-04-23 Wyeth 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
WO2009102986A1 (en) 2008-02-15 2009-08-20 Catholic Healthcare West (D/B/A St. Joseph's Hospital And Medical Center) Treatment of adenocarcinoma expressing lkb1 with mtor inhibitor in combination with cox1 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
PT2477987T (pt) 2009-09-14 2018-03-13 Gilead Sciences Inc Moduladores de recetores do tipo toll
CA2783258A1 (en) 2009-12-23 2011-06-30 Elan Pharmaceuticals, Inc. Pteridinones as 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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080194019A1 (en) 2003-09-09 2008-08-14 Beth Israel Deaconess Medical Center, Inc. Tumor Suppressor Lkb1 Kinase Directly Activates Amp-Activated Kinase

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