JP6382947B2 - 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法 - Google Patents

前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法 Download PDF

Info

Publication number
JP6382947B2
JP6382947B2 JP2016509056A JP2016509056A JP6382947B2 JP 6382947 B2 JP6382947 B2 JP 6382947B2 JP 2016509056 A JP2016509056 A JP 2016509056A JP 2016509056 A JP2016509056 A JP 2016509056A JP 6382947 B2 JP6382947 B2 JP 6382947B2
Authority
JP
Japan
Prior art keywords
dihydropyrazino
compound
pyrazine
androgen receptor
receptor antagonist
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
JP2016509056A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016516819A5 (OSRAM
JP2016516819A (ja
Inventor
ライモン ヘザー
ライモン ヘザー
ツジ トシヤ
ツジ トシヤ
ケー. ナーラ ラマ
ケー. ナーラ ラマ
マエ ヘゲ クリステン
マエ ヘゲ クリステン
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 JP2016516819A publication Critical patent/JP2016516819A/ja
Publication of JP2016516819A5 publication Critical patent/JP2016516819A5/ja
Application granted granted Critical
Publication of JP6382947B2 publication Critical patent/JP6382947B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and 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
    • A61K31/33—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016509056A 2013-04-17 2014-04-16 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法 Active JP6382947B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361813038P 2013-04-17 2013-04-17
US61/813,038 2013-04-17
US201361815509P 2013-04-24 2013-04-24
US61/815,509 2013-04-24
PCT/US2014/034316 WO2014172431A1 (en) 2013-04-17 2014-04-16 Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer

Publications (3)

Publication Number Publication Date
JP2016516819A JP2016516819A (ja) 2016-06-09
JP2016516819A5 JP2016516819A5 (OSRAM) 2017-05-18
JP6382947B2 true JP6382947B2 (ja) 2018-08-29

Family

ID=50736200

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016509056A Active JP6382947B2 (ja) 2013-04-17 2014-04-16 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法

Country Status (22)

Country Link
US (2) US9937169B2 (OSRAM)
EP (1) EP2986320A1 (OSRAM)
JP (1) JP6382947B2 (OSRAM)
KR (1) KR102221005B1 (OSRAM)
CN (1) CN105377299B (OSRAM)
AU (1) AU2014254058B2 (OSRAM)
BR (1) BR112015026257B1 (OSRAM)
CA (1) CA2908957C (OSRAM)
EA (1) EA029072B1 (OSRAM)
HK (1) HK1221149A1 (OSRAM)
IL (1) IL242022B (OSRAM)
MX (1) MX364101B (OSRAM)
MY (1) MY189663A (OSRAM)
NI (1) NI201500151A (OSRAM)
NZ (1) NZ629469A (OSRAM)
PH (1) PH12015502342B1 (OSRAM)
SA (1) SA515370011B1 (OSRAM)
SG (2) SG11201508302PA (OSRAM)
TW (1) TWI674897B (OSRAM)
UA (1) UA115805C2 (OSRAM)
WO (1) WO2014172431A1 (OSRAM)
ZA (1) ZA201507734B (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2908353C (en) 2013-04-17 2021-11-02 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
MX368286B (es) 2013-04-17 2019-09-27 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer.
US9505764B2 (en) 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
EA030726B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ, СПОСОБЫ, ТВЕРДЫЕ ФОРМЫ И СПОСОБЫ ПРИМЕНЕНИЯ, ОТНОСЯЩИЕСЯ К 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1H-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1H)-ОНУ
HK1223286A1 (zh) 2013-05-29 2017-07-28 西格诺药品有限公司 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法
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
JP2017511367A (ja) 2014-04-16 2017-04-20 シグナル ファーマシューティカルズ,エルエルシー 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
WO2016210046A1 (en) * 2015-06-24 2016-12-29 Celgene Corporation Treatment of cancer with dnapk inhibitors
ES2959860T3 (es) 2017-06-22 2024-02-28 Celgene Corp Tratamiento del carcinoma hepatocelular caracterizado por la infección por el virus de la hepatitis B
AU2021382606A1 (en) * 2020-11-18 2023-06-22 Constellation Pharmaceuticals, Inc Ezh2 inhibition therapies for the treatment of androgen receptor mutated prostate cancers

Family Cites Families (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE262026C (OSRAM)
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 (OSRAM) 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
CA2305370C (en) 1997-09-26 2006-11-28 Zentaris Gmbh Azabenzimidazole-based compounds for modulating serine/threonine protein kinase function
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
AU4951300A (en) 1999-05-31 2000-12-18 Chugai Research Institute For Molecular Medicine, Inc. Lkb1 gene knockout animals
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
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
JP2005506350A (ja) 2001-10-18 2005-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害薬としての1,4−二置換ベンゾ−縮合尿素化合物
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
KR20050006221A (ko) 2002-05-06 2005-01-15 제네랩스 테크놀로지스, 인코포레이티드 C형 간염 바이러스 감염 치료용의 뉴클레오시드 유도체
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
ATE527250T1 (de) 2002-11-21 2011-10-15 Novartis Ag 2,4,6-trisubstituierten pyrimidinen als phosphotidylinositol (pi) 3-kinase inhibitoren und deren verwendung zur behandlung von krebs
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
CA2517020C (en) 2003-02-26 2012-06-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, method for the production and use thereof in the form of drugs
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
BRPI0419345B8 (pt) 2003-05-30 2021-05-25 Gilead Pharmasset Llc uso do (2’r)-2’-desoxi-2’-flúor-2’-c-metil nucleosídeo e de uma composição farmacêutica que o compreende
WO2005013894A2 (en) 2003-06-26 2005-02-17 Merck & Co., Inc. 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
WO2005120511A1 (en) 2004-06-04 2005-12-22 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
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
US8153640B2 (en) 2004-10-29 2012-04-10 Tibotec Pharmaceuticals Ltd. HIV inhibiting bicyclic pyrimdine derivatives
US7855205B2 (en) 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New compounds
EP1828186A1 (en) 2004-12-13 2007-09-05 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
PT1853588E (pt) 2005-02-16 2008-08-25 Astrazeneca Ab Compostos químicos
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
JP2008531537A (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 化合物
WO2006108103A1 (en) 2005-04-05 2006-10-12 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
US7709517B2 (en) * 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
AU2006302179C1 (en) 2005-10-07 2013-06-20 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
HRP20130902T1 (hr) 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
WO2007044698A1 (en) 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007047754A2 (en) 2005-10-18 2007-04-26 George Mason Intellectual Properties, Inc. Mtor pathway theranostic
ES2436877T3 (es) 2005-11-17 2014-01-07 OSI Pharmaceuticals, LLC Intermedios para la preparación de inhibidores de mTOR bicíclicos condensados
KR101464384B1 (ko) 2005-11-22 2014-11-21 쿠도스 파마슈티칼스 리미티드 mTOR 억제제로서 피리도피리미딘, 피라조피리미딘 및피리미도피리미딘 유도체
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
KR20080083188A (ko) 2006-01-11 2008-09-16 아스트라제네카 아베 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
JP5606734B2 (ja) 2006-04-25 2014-10-15 アステックス、セラピューティックス、リミテッド 医薬化合物
RU2439074C2 (ru) 2006-04-26 2012-01-10 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНОЕ ТИЕНО[3,2-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (РI3К)
EP2016068A1 (en) 2006-05-03 2009-01-21 AstraZeneca AB Pyrazole derivatives and their use as pi3k inhibitors
WO2007129044A1 (en) 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
US20090306126A1 (en) 2006-05-22 2009-12-10 Astrazeneca Ab Indole Derivatives
DK2069352T5 (en) 2006-08-02 2017-04-03 Cytokinetics Inc SPECIFIC CHEMICAL UNITS, COMPOSITIONS AND PROCEDURES
PT2057156T (pt) 2006-08-23 2017-05-04 Kudos Pharm Ltd Derivados de 2-metilmorfolina pirido-, pirazo- e pirimidopirimidina como inibidores de mtor
US20100144738A1 (en) 2006-09-05 2010-06-10 William Bornmann Inhibitors of c-met and uses thereof
EP2471529A3 (en) 2006-09-05 2012-10-10 Emory University Kinase Inhibitors for Preventing or Treating Pathogen Infection and Method of Use Thereof
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
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
WO2008032027A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
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
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
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
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
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
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
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
CL2007002866A1 (es) 2006-10-04 2008-07-04 Pharmacopeia Inc Compuestos derivados de 6-sustituidos-2-(bencimidazolil) purina y purinona; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento de enfermedades autoinmunes, enfermedad inflamatoria, enfermedad mediada por m
US7981893B2 (en) * 2006-10-19 2011-07-19 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
ES2383370T3 (es) 2006-10-19 2012-06-20 Signal Pharmaceuticals Llc Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa
KR20090080530A (ko) 2006-11-20 2009-07-24 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
US8138183B2 (en) 2007-07-09 2012-03-20 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
BRPI0814818A2 (pt) 2007-07-09 2019-09-10 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica
CA2702838A1 (en) 2007-10-16 2009-04-23 Wyeth Llc Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
MX2010007746A (es) 2008-01-15 2010-08-18 Wyeth Llc Compuestos de 3h-[1,2,3]triazolo[4,5-d]pirimidina, su uso como inhibidores de diana de rapamicina de mamifero quinasa y fosfatidilinositol quinasa y su sintesis.
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
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
EP2349984A1 (en) * 2008-10-17 2011-08-03 Merck & Co. Combination therapy
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
AU2009324894B2 (en) 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use
ES2661850T3 (es) 2009-09-14 2018-04-04 Gilead Sciences, Inc. Moduladores de receptores del tipo toll
NZ618135A (en) 2009-10-26 2015-05-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
CA2783258A1 (en) 2009-12-23 2011-06-30 Elan Pharmaceuticals, Inc. Pteridinones as inhibitors of polo-like kinase
SG183155A1 (en) 2010-02-03 2012-09-27 Signal Pharm 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
JP6158180B2 (ja) * 2011-07-29 2017-07-05 メディベイション プロステイト セラピューティクス, インコーポレイテッド 乳がんの処置
US20130158023A1 (en) 2011-08-03 2013-06-20 Signal Pharmaceuticals, Llc Identification of gene expression as a predictive biomarker for lkb1 status
KR101978537B1 (ko) * 2011-10-19 2019-05-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제를 사용한 암의 치료
US9403829B2 (en) 2011-12-02 2016-08-02 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
JP6114317B2 (ja) 2012-02-24 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キナーゼ阻害剤の組合せ療法を用いて、非小細胞肺がんを処置する方法
AU2013202993B2 (en) 2012-03-15 2015-09-03 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
WO2013138557A1 (en) 2012-03-15 2013-09-19 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
MY198666A (en) 2012-03-15 2023-09-14 Signal Pharm Llc Treatment of cancer with tor kinase inhibitors
CN107137402A (zh) 2012-03-15 2017-09-08 西格诺药品有限公司 用tor激酶抑制剂治疗癌症
TWI673051B (zh) * 2012-09-11 2019-10-01 美商梅維森前列腺療法有限責任公司 恩雜魯它脈(enzalutamide)之調和物
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
AU2014254059B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and a cytidine analog for treating cancer
EA030726B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ, СПОСОБЫ, ТВЕРДЫЕ ФОРМЫ И СПОСОБЫ ПРИМЕНЕНИЯ, ОТНОСЯЩИЕСЯ К 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1H-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1H)-ОНУ
EP2986318A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and an imid compound for treating cancer
HK1221168A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法
TW201526894A (zh) 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
MX368286B (es) 2013-04-17 2019-09-27 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer.
US9505764B2 (en) 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
CA2908353C (en) 2013-04-17 2021-11-02 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines

Also Published As

Publication number Publication date
IL242022B (en) 2020-01-30
EA201591967A1 (ru) 2016-04-29
MX2015014595A (es) 2016-03-03
CN105377299B (zh) 2018-06-12
CA2908957C (en) 2021-05-18
BR112015026257B1 (pt) 2022-12-20
PH12015502342A1 (en) 2016-02-22
US20180185361A1 (en) 2018-07-05
US20140315900A1 (en) 2014-10-23
KR20160004272A (ko) 2016-01-12
US9937169B2 (en) 2018-04-10
JP2016516819A (ja) 2016-06-09
WO2014172431A1 (en) 2014-10-23
NZ629469A (en) 2017-05-26
SG11201508302PA (en) 2015-11-27
UA115805C2 (uk) 2017-12-26
TWI674897B (zh) 2019-10-21
KR102221005B1 (ko) 2021-02-26
AU2014254058B2 (en) 2019-06-06
TW201526896A (zh) 2015-07-16
CA2908957A1 (en) 2014-10-23
MX364101B (es) 2019-04-12
ZA201507734B (en) 2017-05-31
SG10201708111YA (en) 2017-11-29
SA515370011B1 (ar) 2018-07-17
MY189663A (en) 2022-02-23
AU2014254058A1 (en) 2015-11-05
HK1221149A1 (zh) 2017-05-26
CN105377299A (zh) 2016-03-02
PH12015502342B1 (en) 2016-02-22
NI201500151A (es) 2015-11-30
EP2986320A1 (en) 2016-02-24
EA029072B1 (ru) 2018-02-28
US10391092B2 (en) 2019-08-27
BR112015026257A2 (pt) 2017-07-25

Similar Documents

Publication Publication Date Title
ES2894958T3 (es) Tratamiento del cáncer con inhibidores de la quinasa TOR
US10391092B2 (en) Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
JP6838085B2 (ja) Torキナーゼ阻害剤組み合わせ療法を使用して癌を治療する方法
JP6382945B2 (ja) ジヒドロピラジノ−ピラジンによる癌治療
AU2015213353B2 (en) Treatment of cancer with TOR kinase inhibitors
JP2019108368A (ja) Torキナーゼ阻害剤を用いた癌の治療
JP2016522177A (ja) ジヒドロピラジノ−ピラジンによる癌治療
US20160008356A1 (en) Treatment of cancer with tor kinase inhibitors
CN105377260A (zh) 用二氢吡嗪并-吡嗪类对癌症的治疗
JP2017514805A (ja) Torキナーゼ阻害剤組み合わせ療法を使用して癌を治療する方法

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170331

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170331

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20171205

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20180305

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180314

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20180314

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20180717

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20180802

R150 Certificate of patent or registration of utility model

Ref document number: 6382947

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

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250