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Publication number
JP2017511367A5
JP2017511367A5 JP2016562878A JP2016562878A JP2017511367A5 JP 2017511367 A5 JP2017511367 A5 JP 2017511367A5 JP 2016562878 A JP2016562878 A JP 2016562878A JP 2016562878 A JP2016562878 A JP 2016562878A JP 2017511367 A5 JP2017511367 A5 JP 2017511367A5
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JP
Japan
Prior art keywords
solid form
weight
pharmaceutical composition
dihydropyrazino
pyrazin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2016562878A
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English (en)
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JP2017511367A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2015/025858 external-priority patent/WO2015160880A1/en
Publication of JP2017511367A publication Critical patent/JP2017511367A/ja
Publication of JP2017511367A5 publication Critical patent/JP2017511367A5/ja
Pending legal-status Critical Current

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Claims (14)

  1. (a)1-エチル-7-(2-メチル-6-(1H-1,2,4-トリアゾール-3-イル)ピリジン-3-イル)-3,4-ジヒドロピラジノ[2,3-b]ピラジン-2(1H)-オン;並びに(b)ゲンチジン酸及びニコチンアミドからなる群から選択される共形成物を含む、固体形態。
  2. 前記共形成物がゲンチジン酸である、請求項1記載の固体形態。
  3. 前記共形成物がニコチンアミドである、請求項1記載の固体形態。
  4. 結晶形態の80重量%超である、請求項1記載の固体形態。
  5. 共結晶の80重量%超である、請求項4記載の固体形態。
  6. 共結晶の90重量%超である、請求項5記載の固体形態。
  7. 結晶形態の95重量%超である、請求項6記載の固体形態。
  8. 3重量%未満の1-エチル-7-(2-メチル-6-(1H-1,2,4-トリアゾール-3-イル)ピリジン-3-イル)-3,4-ジヒドロピラジノ[2,3-b]ピラジン-2(1H)-オンの他の固体形態を含有する、請求項7記載の固体形態。
  9. 非晶質の1-エチル-7-(2-メチル-6-(1H-1,2,4-トリアゾール-3-イル)ピリジン-3-イル)-3,4-ジヒドロピラジノ[2,3-b]ピラジン-2(1H)-オンをさらに含む、請求項8記載の固体形態。
  10. 結晶形態の99重量%超である、請求項9記載の固体形態。
  11. 請求項1記載の固体形態を含む、医薬組成物。
  12. 単一単位剤形である、請求項11記載の医薬組成物。
  13. 錠剤である、請求項12記載の医薬組成物。
  14. カプセル剤である、請求項12記載の医薬組成物。
JP2016562878A 2014-04-16 2015-04-15 １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン及び共形成物を含む固体形態、その組成物及び使用方法 Pending JP2017511367A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461980111P 2014-04-16 2014-04-16
US61/980,111 2014-04-16
PCT/US2015/025858 WO2015160880A1 (en) 2014-04-16 2015-04-15 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

Publications (2)

Publication Number Publication Date
JP2017511367A JP2017511367A (ja) 2017-04-20
JP2017511367A5 true JP2017511367A5 (ja) 2018-05-24

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016562878A Pending JP2017511367A (ja) 2014-04-16 2015-04-15 １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン及び共形成物を含む固体形態、その組成物及び使用方法

Country Status (4)

Country Link
US (2) US9512129B2 (ja)
EP (1) EP3131551A4 (ja)
JP (1) JP2017511367A (ja)
WO (1) WO2015160880A1 (ja)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3549940A1 (en) * 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, 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
MY198676A (en) 2017-06-22 2023-09-15 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
CN110403943B (zh) * 2019-08-19 2022-05-17 陕西科技大学 Cc-115在制备抗真菌药物中的应用及其药物组合物

Family Cites Families (128)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4317909A (en) 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4294837A (en) 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4294836A (en) 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4309537A (en) 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk ２−アミノイミダゾ〔４，５−ｂ〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US4963561A (en) 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (ja) 1992-09-26 1996-04-21 Hoechst Ag
DE19601627A1 (de) 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US6031105A (en) 1996-04-09 2000-02-29 Pfizer Inc Substituted pyridines
SK285357B6 (sk) 1997-09-26 2006-11-03 Zentaris Gmbh Zlúčeniny na báze azabenzimidazolu modulujúce funkciu serínovej/treonínovej proteínkinázy
US6800436B1 (en) 1997-11-27 2004-10-05 Chugai Seiyaku Kabushiki Kaisha Diagnostic method, diagnostic reagent and therapeutic preparation for diseases caused by variation in LKB1 gene
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd ２−アリールプリン−９−アセトアミド誘導体
EP1186232A4 (en) 1999-05-31 2004-11-10 Chugai Pharmaceutical Co Ltd 'KNOCKOUT' ANIMALS LACKING THE LKB1 GENE
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 ２−アリール−８−オキソジヒドロプリン誘導体からなる医薬
JP2002100363A (ja) 2000-09-25 2002-04-05 Mitsubishi Chemicals Corp リチウム二次電池用正極材料、リチウム二次電池用正極及びリチウム二次電池
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd ２−（７，８−ジヒドロ−８−オキソ−９ｈ−プリン−９−イル）酢酸誘導体
MXPA03004245A (es) 2000-12-12 2003-09-22 Neurogen Corp Espiro[isobenzofuran-1,4'piperidin]-3-onas y 3h-espiroisobenzofuran-1,4'-piperidinas.
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
EA007062B1 (ru) 2001-09-04 2006-06-30 Бёрингер Ингельхайм Фарма Гмбх Унд Ко. Кг Новые дигидроптеридиноны, способы их получения и их применение в качестве лекарственных средств
US6825184B2 (en) 2001-10-18 2004-11-30 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-Disubstituted benzo-fused urea compounds
TWI314928B (en) 2002-02-28 2009-09-21 Novartis A 5-phenylthiazole derivatives and use as pi3 kinase inhibitors
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
NZ536123A (en) 2002-05-06 2006-09-29 Genelabs Tech Inc Nucleoside derivatives for treating hepatitis C virus infection
WO2004042002A2 (en) 2002-08-05 2004-05-21 University Of Massachusetts Compounds for modulating rna interference
AU2003270701B2 (en) 2002-10-31 2009-11-12 Amgen Inc. Antiinflammation agents
US7423148B2 (en) 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
BRPI0406809A (pt) 2003-01-17 2005-12-27 Warner Lambert Co Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular
JP3876265B2 (ja) 2003-02-26 2007-01-31 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト ジヒドロプテリジノン、その製造方法及び薬物形態での使用
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
PL3521297T3 (pl) 2003-05-30 2022-04-04 Gilead Pharmasset Llc Zmodyfikowane fluorowane analogi nukleozydów
ATE461196T1 (de) 2003-06-26 2010-04-15 Merck Sharp & Dohme Benzodiazepin-cgrp-rezeptor-antagonisten
DK1651673T3 (da) 2003-07-17 2008-08-18 Univ Dundee Fremgangsmåder til anvendelse af et LKB1/STRAD/MO25-kompleks
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
CN101123968A (zh) 2004-06-04 2008-02-13 艾科斯有限公司 肥大细胞病的治疗方法
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
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. ２－アリールプリン誘導体の製造方法
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
US7608622B2 (en) 2004-09-24 2009-10-27 Janssen Pharmaceutica Nv Imidazo[4,5-b]pyrazinone inhibitors of protein kinases
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
CA2577588C (en) 2004-10-29 2013-09-10 Tibotec Pharmaceuticals Ltd. Hiv inhibiting bicyclic pyrimidine derivatives
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New compounds
AU2005316668B2 (en) 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
RU2405780C2 (ru) 2005-02-16 2010-12-10 Астразенека Аб Химические соединения
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
EP1871377A1 (en) 2005-02-25 2008-01-02 Kudos Pharmaceuticals Ltd 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors
US20100130473A1 (en) 2005-02-25 2010-05-27 Marc Geoffrey Hummersone Compounds
KR20080013886A (ko) 2005-04-05 2008-02-13 파마코페이아, 인코포레이티드 면역억제용 퓨린 및 이미다조피리딘 유도체
CA2624965A1 (en) 2005-10-07 2007-04-19 Exelixis, Inc. Pyridopyrimidinone inhibitors of pi3k.alpha.
NZ594630A (en) 2005-10-07 2013-04-26 Exelixis Inc N-(3-amino-quinoxalin-2-yl)-sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
GEP20115304B (en) 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
JP2009511935A (ja) 2005-10-18 2009-03-19 ジョージ メイソン インテレクチュアル プロパティーズ インク． ｍＴＯＲ経路テラノスティック
NZ569050A (en) 2005-11-17 2010-11-26 Osi Pharm Inc Fused bicyclic mTOR inhibitors
WO2007060404A1 (en) 2005-11-22 2007-05-31 Kudos Pharmaceuticals Limited PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
BRPI0706395A2 (pt) 2006-01-11 2011-03-22 Astrazeneca Ab composto, uso do mesmo, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar doença, composição farmacêutica, e, processo para preparar um composto
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
FI3719018T3 (fi) 2006-04-25 2025-10-07 Astex Therapeutics Ltd Puriini- ja deatsapuriinijohdannaisia farmaseuttisina yhdisteinä
PT2024372E (pt) 2006-04-26 2010-09-16 Hoffmann La Roche Derivado de tieno[3,2-d]pirimidina útil como inibidor de pi3k
WO2007129044A1 (en) 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
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
JP2009537621A (ja) 2006-05-22 2009-10-29 アストラゼネカ アクチボラグ インドール誘導体
HUE026571T2 (hu) 2006-08-02 2016-06-28 Cytokinetics Inc Adott kémiai anyagok, készítmények és imidazopiridineket magukba foglaló eljárások
WO2008023161A1 (en) 2006-08-23 2008-02-28 Kudos Pharmaceuticals Limited 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
WO2008030744A2 (en) 2006-09-05 2008-03-13 Board Of Regents, The University Of Texas System Inhibitors of c-met and uses thereof
AU2007338601C1 (en) 2006-09-05 2014-07-24 Emory University Tyrosine kinase inhibitors for prevention or treatment of infection
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
JP2010503648A (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−４−（アゼチジン、ピロリジン、ピペリジン、又はアゼピン）ピリミジン誘導体
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
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
US20090270390A1 (en) 2006-09-14 2009-10-29 Astrazeneca Pyrimidine derivatives
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
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
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
WO2008043031A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc. 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
EP2078016B1 (en) 2006-10-19 2012-02-01 Signal Pharmaceuticals LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
BRPI0717773A2 (pt) 2006-10-19 2013-11-05 Signal Pharm Llc Composto, composição farmacêutica, e, métodos para tratar ou prevenir câncer, uma condição inflamatória, uma condição imunológica ou uma condição metabólica, e para inibir uma quinase em uma célula que expressa a dita quinase
JP5562033B2 (ja) 2006-11-20 2014-07-30 ノバルティス アーゲー ２−メチル−２−［４−（３−メチル−２−オキソ−８−キノリン−３−イル−２，３−ジヒドロ−イミダゾ［４，５−ｃ］キノリン−１−イル）−フェニル］−プロピオニトリルの塩および結晶形態
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
BRPI0814688A2 (pt) 2007-07-09 2017-06-06 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito antiproliferativo em um animal de sangue quente, e para tratar doenças, e, composição farmacêutica
AU2008273892A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009007748A2 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
AP2010005234A0 (en) 2007-10-16 2010-04-30 Wyeth Llc Thienopyrimidine and pyrazolopyrimidline compoundsand their use as MTOR kinase and P13 kinase inhib itors
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
CA2712267A1 (en) 2008-01-15 2009-07-23 Wyeth Llc 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
CA2744498C (en) 2008-11-25 2017-10-24 University Of Rochester Mlk inhibitors and methods of use
EP2477987B1 (en) 2009-09-14 2018-01-10 Gilead Sciences, Inc. Modulators of toll-like receptors
ES2751705T3 (es) 2009-10-26 2020-04-01 Signal Pharm Llc Métodos de síntesis y purificación de compuestos heteroarilo
US8445503B2 (en) 2009-12-23 2013-05-21 Elan Pharmaceuticals, Inc. Inhibitors of polo-like kinase
JP6114554B2 (ja) 2010-02-03 2017-04-12 シグナル ファーマシューティカルズ，エルエルシー 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
US20110318336A1 (en) 2010-03-29 2011-12-29 George Mason Intellectual Properties, Inc. Identification and Treatment of Aggressive Lung Cancer Tumors
US20120028972A1 (en) 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
AU2012290056B2 (en) 2011-08-03 2015-03-19 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for LKB1 status
MX384385B (es) 2011-10-19 2025-03-14 Signal Pharm Llc Tratamiento del cancer con inhibidores de tor cinasa
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
US9375443B2 (en) 2012-02-24 2016-06-28 Signal Pharmaceuticals, Llc Method for treating advanced non-small cell lung cancer (NSCLC) by administering a combination of a TOR kinase inhibitor and azacitidine or erlotinib
AU2013203156C1 (en) 2012-03-15 2016-02-18 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
EA028414B1 (ru) 2012-03-15 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение рака ингибиторами tor киназы
EA028062B1 (ru) 2012-03-15 2017-10-31 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение рака ингибиторами tor киназы
MX360880B (es) 2012-03-15 2018-11-21 Signal Pharm Llc Compuesto 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3il)- 3,4-dihidropirazino [2,3-b]pirazin-2(1h)-ona para usarse en el tratamiento de cancer de mama triple negativo.
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
JP6382949B2 (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 癌を治療するためのｔｏｒキナーゼ阻害剤及び５−置換キナゾリノン化合物を含む組合せ療法
TW201526894A (zh) 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
HK1221150A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用二氢吡嗪并-吡嗪类对癌症的治疗
EP2986319A1 (en) 2013-04-17 2016-02-24 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
EP3549940A1 (en) 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, 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
HK1221148A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 包含tor激酶抑制剂和imid化合物的联合疗法用於治疗癌症
SG11201508223YA (en) 2013-04-17 2015-11-27 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
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
US9782427B2 (en) 2013-04-17 2017-10-10 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy

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