JP6787791B2 - 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)−オンの固体形態、その組成物、及びそれらの使用方法 - Google Patents

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)−オンの固体形態、その組成物、及びそれらの使用方法 Download PDF

Info

Publication number
JP6787791B2
JP6787791B2 JP2016562778A JP2016562778A JP6787791B2 JP 6787791 B2 JP6787791 B2 JP 6787791B2 JP 2016562778 A JP2016562778 A JP 2016562778A JP 2016562778 A JP2016562778 A JP 2016562778A JP 6787791 B2 JP6787791 B2 JP 6787791B2
Authority
JP
Japan
Prior art keywords
compound
solid
crystal
certain embodiments
solvent
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.)
Active
Application number
JP2016562778A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017511361A (ja
JP2017511361A5 (enExample
Inventor
エクケルト ジェフレイ
エクケルト ジェフレイ
メノン アニル
メノン アニル
ケイ.パリクフ ダルシャン
ケイ.パリクフ ダルシャン
ボエルセン ナサン
ボエルセン ナサン
レエ トーマス
レエ トーマス
Original Assignee
シグナル ファーマシューティカルズ,エルエルシー
シグナル ファーマシューティカルズ,エルエルシー
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by シグナル ファーマシューティカルズ,エルエルシー, シグナル ファーマシューティカルズ,エルエルシー filed Critical シグナル ファーマシューティカルズ,エルエルシー
Publication of JP2017511361A publication Critical patent/JP2017511361A/ja
Publication of JP2017511361A5 publication Critical patent/JP2017511361A5/ja
Application granted granted Critical
Publication of JP6787791B2 publication Critical patent/JP6787791B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2016562778A 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)−オンの固体形態、その組成物、及びそれらの使用方法 Active JP6787791B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461980108P 2014-04-16 2014-04-16
US61/980,108 2014-04-16
US201462003173P 2014-05-27 2014-05-27
US62/003,173 2014-05-27
PCT/US2015/025850 WO2015160875A1 (en) 2014-04-16 2015-04-15 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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2019039173A Division JP2019116491A (ja) 2014-04-16 2019-03-05 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)−オンの固体形態、その組成物、及びそれらの使用方法

Publications (3)

Publication Number Publication Date
JP2017511361A JP2017511361A (ja) 2017-04-20
JP2017511361A5 JP2017511361A5 (enExample) 2018-05-17
JP6787791B2 true JP6787791B2 (ja) 2020-11-18

Family

ID=54321423

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2016562778A Active JP6787791B2 (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)−オンの固体形態、その組成物、及びそれらの使用方法
JP2019039173A Withdrawn JP2019116491A (ja) 2014-04-16 2019-03-05 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)−オンの固体形態、その組成物、及びそれらの使用方法
JP2020208893A Pending JP2021054844A (ja) 2014-04-16 2020-12-17 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)−オンの固体形態、その組成物、及びそれらの使用方法

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2019039173A Withdrawn JP2019116491A (ja) 2014-04-16 2019-03-05 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)−オンの固体形態、その組成物、及びそれらの使用方法
JP2020208893A Pending JP2021054844A (ja) 2014-04-16 2020-12-17 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)−オンの固体形態、その組成物、及びそれらの使用方法

Country Status (8)

Country Link
US (2) US9416134B2 (enExample)
EP (1) EP3131553B1 (enExample)
JP (3) JP6787791B2 (enExample)
CA (2) CA2945960C (enExample)
ES (1) ES2913071T3 (enExample)
MX (2) MX370786B (enExample)
NZ (1) NZ714742A (enExample)
WO (1) WO2015160875A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2909629C (en) * 2013-04-17 2022-12-13 Signal Pharmaceuticals, Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 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
US9505764B2 (en) * 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
TWI787284B (zh) 2017-06-22 2022-12-21 美商西建公司 以b型肝炎病毒感染表徵之肝細胞癌之治療

Family Cites Families (131)

* 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
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
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
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 (enExample) 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
HUP0004024A3 (en) 1997-09-26 2001-10-29 Zentaris Gmbh Azabenzimidazole-based compounds, process for their preparation and pharmaceutical composition thereof
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
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
EP1186232A4 (en) 1999-05-31 2004-11-10 Chugai Pharmaceutical Co Ltd 'KNOCKOUT' ANIMALS LACKING THE LKB1 GENE
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
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
EP1347982B1 (en) 2000-12-12 2005-11-16 Neurogen Corporation Spiro isobenzofuran-1,4'-piperidin]-3-ones and 3h-spiroisobenzofuran-1,4'-piperidines
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
UA76512C2 (en) 2001-09-04 2006-08-15 Boehringer Ingelheim Pharma Dihydropteridinones, a method for producing thereof and use thereof as medicament
EP1438048A1 (en) 2001-10-18 2004-07-21 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
AR038703A1 (es) 2002-02-28 2005-01-26 Novartis Ag Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
US20040063658A1 (en) 2002-05-06 2004-04-01 Roberts Christopher Don Nucleoside derivatives for treating hepatitis C virus infection
AU2003299531A1 (en) 2002-08-05 2004-06-07 University Of Massachusetts Compounds for modulating rna interference
WO2004041285A1 (en) 2002-10-31 2004-05-21 Amgen Inc. Antiinflammation agents
EA013811B1 (ru) 2002-11-21 2010-08-30 Новартис Вэксинес Энд Дайэгностикс, Инк. 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion 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
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
HUE029877T2 (en) 2003-05-30 2017-04-28 Gilead Pharmasset Llc Modified fluorinated nucleoside analogues
EP1641423B1 (en) 2003-06-26 2010-03-17 Merck Sharp & Dohme Corp. Benzodiazepine cgrp receptor antagonists
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
EP1750715A1 (en) 2004-06-04 2007-02-14 Icos Corporation Methods for treating mast cell disorders
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
AU2005289644A1 (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
JP5118972B2 (ja) 2004-10-29 2013-01-16 テイボテク・フアーマシユーチカルズ Hiv阻害性二環式ピリミジン誘導体
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New compounds
US7767687B2 (en) 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
SI1853588T1 (sl) 2005-02-16 2008-10-31 Astrazeneca Ab Kemične spojine
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
JP2008531538A (ja) 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 2,4−ジアミノ−ピリドピリミジン誘導体とmTOR阻害剤としてのその使用
CA2599320A1 (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
JP2008534689A (ja) 2005-04-05 2008-08-28 ファーマコペイア, インコーポレイテッド 免疫抑制のためのプリン及びイミダゾピリジン誘導体
EA016945B1 (ru) 2005-10-07 2012-08-30 Экселиксис, Инк. ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
US7989622B2 (en) 2005-10-07 2011-08-02 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
CN102746298A (zh) 2005-10-07 2012-10-24 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
CA2626456C (en) 2005-10-18 2018-01-09 George Mason Intellectual Properties, Inc. Mtor pathway theranostic
ES2365869T3 (es) 2005-11-17 2011-10-11 OSI Pharmaceuticals, LLC COMPUESTOS BICÍCLICOS FUSIONADOS INHIBIDORES DE LA mTOR.
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
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
EP1979325A1 (en) 2006-01-11 2008-10-15 AstraZeneca AB Morpholino pyrimidine derivatives and their use in therapy
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
DK3421471T3 (da) 2006-04-25 2021-06-14 Astex Therapeutics Ltd Purin- og deazapurinderivater som farmaceutiske forbindelser
WO2007129161A2 (en) 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
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
JP2009535386A (ja) 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ チアゾール誘導体および抗腫瘍剤としてのその使用
WO2007135398A1 (en) 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
PL2069352T3 (pl) 2006-08-02 2014-03-31 Cytokinetics Inc Określone cząstki chemiczne, kompozycje i sposoby
CA2659851C (en) 2006-08-23 2014-02-25 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
US8268809B2 (en) 2006-09-05 2012-09-18 Emory University Kinase inhibitors for preventing or treating pathogen infection and method of use thereof
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
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
EP2064203A1 (en) 2006-09-14 2009-06-03 AstraZeneca AB 2-benzimidaz0lyl-6-m0rph0lin0-4-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
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
CN101595103A (zh) 2006-09-14 2009-12-02 阿斯利康(瑞典)有限公司 嘧啶衍生物
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
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032027A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US7919490B2 (en) 2006-10-04 2011-04-05 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
MX337906B (es) 2006-10-19 2016-03-28 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
CA2666624C (en) 2006-10-19 2015-12-29 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
KR20140091718A (ko) 2006-11-20 2014-07-22 노파르티스 아게 2-메틸-2-[4-(3-메틸-2-옥소-8-퀴놀린-3-일-2,3-디히드로-이미다조[4,5-c]퀴놀린-1-일)-페닐]-프로피오니트릴의 염 및 결정 형태
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
BRPI0814503A2 (pt) 2007-07-09 2017-05-16 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente, e para tratar uma doença, e, composição farmacêutica
AU2008273889B2 (en) 2007-07-09 2012-03-08 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
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
FR2920428B1 (fr) * 2007-08-29 2012-06-15 Univ Rouen Procede de dedoublement de sels de l'omeprazole
EA201000484A1 (ru) 2007-10-16 2010-12-30 ВАЙЕТ ЭлЭлСи Тиенопиримидиновые и пиразолопиримидиновые соединения и их применение в качестве ингибиторов киназы mtor и киназы pi3
WO2009086303A2 (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
WO2010068483A2 (en) 2008-11-25 2010-06-17 University Of Rochester Mlk inhibitors and methods of use
EP2424845A4 (en) * 2009-04-27 2014-03-05 Reddys Lab Ltd Dr PREPARATION OF DECITABIN
CA2772253C (en) 2009-09-14 2018-02-27 Gilead Sciences, Inc. Modulators of toll-like receptors
SG10201500511TA (en) * 2009-10-26 2015-03-30 Signal Pharm Llc Methods Of Synthesis And Purification Of Heteroaryl Compounds
RU2012131124A (ru) 2009-12-23 2014-01-27 Элан Фармасьютикалз, Инк. Птеридиноны как ингибиторы polo-подобных киназ
CA2788678C (en) 2010-02-03 2019-02-26 Signal Pharmaceuticals, Llc Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
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
HK1199068A1 (en) 2011-08-03 2015-06-19 西格诺药品有限公司 Identification of gene expression profile as a predictive biomarker for lkb1 status
PH12014500869A1 (en) 2011-10-19 2014-06-30 Signal Pharm Llc Treatment of cancer with tor kinase inhibitors
KR102040997B1 (ko) 2011-12-02 2019-11-27 시그날 파마소티칼 엘엘씨 7-(6-(2-히드록시프로판-2-일)피리딘-3-일)-1-((트랜스)-4-메톡시시클로헥실)-3,4-디히드로피라지노[2,3-b]피라진-2(1H)-온, 그의 고체 형태의 제약 조성물 및 그의 사용 방법
EP2817029B1 (en) 2012-02-24 2019-07-10 Signal Pharmaceuticals, LLC Methods for treating non-small cell lung cancer using tor kinase inhibitor combination therapy
BR112014022703A2 (pt) 2012-03-15 2021-05-04 Signal Pharmaceuticals, Llc método para o tratamento de carcinoma de células escamosas de cabeça e de pescoço, método para melhorar os critérios de avaliação, método para inibição da fosforilação, método para inibição de dna, método para a medição da inibição da fosforilação, kit
BR112014022700A2 (pt) 2012-03-15 2020-06-30 Signal Pharmaceuticals, Llc uso de uma quantidade eficaz de um inibidor da quinase tor, método para melhorar o critério do grupo de trabalho 2 do antígeno prostático específico (psawg2), método para a inibição da fosforilação de s6rp, 4e-bp1 e/ou de akt, método para a inibição da atividade da proteína quinase dependente do dna (dna-pk), método para a medição da inibição da fosforilação de s6rp, 4e-bp1 ou akt, método para a medição da inibição da fosforilação de dna-pk s2056 e kit
TWI664968B (zh) 2012-03-15 2019-07-11 標誌製藥公司 使用tor激酶抑制劑之癌症治療
MY178012A (en) 2012-03-15 2020-09-29 Signal Pharm Llc Treatment of cancer with tor kinase inhibitors
ES2885769T3 (es) 2012-08-09 2021-12-15 Celgene Corp Una forma sólida de clorhidrato de (s)-3-(4-((4-morpholinometil)bencil)oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona
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
US9630966B2 (en) 2013-04-17 2017-04-25 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
US9505764B2 (en) 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
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
NZ629456A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
CN105377299B (zh) 2013-04-17 2018-06-12 西格诺药品有限公司 用于治疗前列腺癌的包含二氢吡嗪并-吡嗪化合物和雄激素受体拮抗剂的组合疗法
TW201526894A (zh) 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
CA2909629C (en) 2013-04-17 2022-12-13 Signal Pharmaceuticals, Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 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

Also Published As

Publication number Publication date
CA2945960C (en) 2022-08-30
CA3164682A1 (en) 2015-10-22
JP2019116491A (ja) 2019-07-18
NZ714742A (en) 2017-04-28
NZ629877A (en) 2015-12-24
JP2017511361A (ja) 2017-04-20
US9981971B2 (en) 2018-05-29
EP3131553B1 (en) 2022-02-23
US20150299209A1 (en) 2015-10-22
EP3131553A4 (en) 2017-09-06
CA2945960A1 (en) 2015-10-22
EP3131553A1 (en) 2017-02-22
US20160318940A1 (en) 2016-11-03
MX2016013436A (es) 2017-02-15
MX370786B (es) 2020-01-06
JP2021054844A (ja) 2021-04-08
WO2015160875A1 (en) 2015-10-22
US9416134B2 (en) 2016-08-16
MX2019006605A (es) 2019-08-21
ES2913071T3 (es) 2022-05-31

Similar Documents

Publication Publication Date Title
JP6517979B2 (ja) 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)−オンに関する医薬製剤、プロセス、固形形態、及び使用方法
JP2021054844A (ja) 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)−オンの固体形態、その組成物、及びそれらの使用方法
US9975898B2 (en) 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 as tor kinase inhibitors
US9718824B2 (en) 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
NZ629877B (en) 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
HK40015557A (en) 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
NZ629866B (en) 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

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180330

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180330

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20180330

A975 Report on accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A971005

Effective date: 20180619

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180703

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180628

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181002

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181003

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20181002

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20181106

C60 Trial request (containing other claim documents, opposition documents)

Free format text: JAPANESE INTERMEDIATE CODE: C60

Effective date: 20190305

C22 Notice of designation (change) of administrative judge

Free format text: JAPANESE INTERMEDIATE CODE: C22

Effective date: 20190924

C13 Notice of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: C13

Effective date: 20200225

C22 Notice of designation (change) of administrative judge

Free format text: JAPANESE INTERMEDIATE CODE: C22

Effective date: 20200407

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20200521

C302 Record of communication

Free format text: JAPANESE INTERMEDIATE CODE: C302

Effective date: 20200605

C302 Record of communication

Free format text: JAPANESE INTERMEDIATE CODE: C302

Effective date: 20200713

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200720

C302 Record of communication

Free format text: JAPANESE INTERMEDIATE CODE: C302

Effective date: 20200911

C23 Notice of termination of proceedings

Free format text: JAPANESE INTERMEDIATE CODE: C23

Effective date: 20200915

C03 Trial/appeal decision taken

Free format text: JAPANESE INTERMEDIATE CODE: C03

Effective date: 20201013

C30A Notification sent

Free format text: JAPANESE INTERMEDIATE CODE: C3012

Effective date: 20201013

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20201029

R150 Certificate of patent or registration of utility model

Ref document number: 6787791

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250