EA034512B1 - Лечение злокачественной опухоли ингибиторами tor-киназы - Google Patents

Лечение злокачественной опухоли ингибиторами tor-киназы Download PDF

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Publication number
EA034512B1
EA034512B1 EA201890768A EA201890768A EA034512B1 EA 034512 B1 EA034512 B1 EA 034512B1 EA 201890768 A EA201890768 A EA 201890768A EA 201890768 A EA201890768 A EA 201890768A EA 034512 B1 EA034512 B1 EA 034512B1
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EA
Eurasian Patent Office
Prior art keywords
tumor
solid tumor
tor kinase
patient
kinase inhibitor
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EA201890768A
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English (en)
Russian (ru)
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EA201890768A2 (ru
EA201890768A3 (ru
Inventor
Шуйчань Сюй
Кристен Мей Хедж
Антония Лопес-Хирона
Хитер Рэймон
Рама К. Нарла
Раджеш Чопра
Original Assignee
СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи
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Publication of EA201890768A2 publication Critical patent/EA201890768A2/ru
Publication of EA201890768A3 publication Critical patent/EA201890768A3/ru
Publication of EA034512B1 publication Critical patent/EA034512B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41661,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201890768A 2011-10-19 2012-10-18 Лечение злокачественной опухоли ингибиторами tor-киназы EA034512B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161549034P 2011-10-19 2011-10-19
US201261591401P 2012-01-27 2012-01-27
US201261647233P 2012-05-15 2012-05-15
US201261653436P 2012-05-31 2012-05-31

Publications (3)

Publication Number Publication Date
EA201890768A2 EA201890768A2 (ru) 2018-08-31
EA201890768A3 EA201890768A3 (ru) 2018-12-28
EA034512B1 true EA034512B1 (ru) 2020-02-14

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EA201490814A EA030664B1 (ru) 2011-10-19 2012-10-18 Лечение злокачественной опухоли ингибиторами tor-киназы
EA201890768A EA034512B1 (ru) 2011-10-19 2012-10-18 Лечение злокачественной опухоли ингибиторами tor-киназы

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EA201490814A EA030664B1 (ru) 2011-10-19 2012-10-18 Лечение злокачественной опухоли ингибиторами tor-киназы

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US (4) US9493466B2 (enExample)
EP (3) EP3659599B1 (enExample)
JP (5) JP2014530861A (enExample)
KR (1) KR101978537B1 (enExample)
CN (2) CN107157990B (enExample)
BR (1) BR112014009755B1 (enExample)
CA (1) CA2852921C (enExample)
EA (2) EA030664B1 (enExample)
ES (2) ES2894958T3 (enExample)
IL (3) IL232128B (enExample)
IN (1) IN2014CN02887A (enExample)
MX (4) MX348566B (enExample)
MY (1) MY183661A (enExample)
PH (1) PH12014500869A1 (enExample)
SG (3) SG10201505102WA (enExample)
TW (4) TWI629983B (enExample)
UA (1) UA115319C2 (enExample)
WO (1) WO2013059396A2 (enExample)
ZA (2) ZA201402771B (enExample)

Families Citing this family (32)

* 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
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
CN105188704B (zh) 2013-01-16 2017-09-19 西格诺药品有限公司 被取代的吡咯并嘧啶化合物、其组合物和使用其的治疗方法
US20160008356A1 (en) * 2013-02-28 2016-01-14 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
NZ631082A (en) * 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
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
UA115805C2 (uk) * 2013-04-17 2017-12-26 Сігнал Фармасьютікалз, Елелсі Комбінована терапія, яка включає сполуку дигідропіразинопіразину й антагоніст рецептора андрогену, для лікування раку простати
EA037683B1 (ru) 2013-04-17 2021-04-29 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
KR102223060B1 (ko) * 2013-04-17 2021-03-05 시그날 파마소티칼 엘엘씨 암 치료를 위한 TOR 키나제 억제제 및 IMiD 화합물을 포함하는 조합요법
US9358232B2 (en) 2013-04-17 2016-06-07 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
PH12021552945B1 (en) 2013-04-17 2024-02-28 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
CN105407892B (zh) 2013-05-29 2019-05-07 西格诺药品有限公司 一种化合物的药物组合物、其固体形式及它们的使用方法
WO2015051251A1 (en) * 2013-10-04 2015-04-09 Signal Pharmaceuticals, Llc A tor kinase inhibitor in the prevention or treatment of cancer characterized by gene mutations
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
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
WO2015160868A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc Methods for treating cancer using tor kinase inhibitor combination therapy
WO2015160880A1 (en) 2014-04-16 2015-10-22 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
CA2955009A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
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
BR112018010216B1 (pt) 2015-11-20 2024-02-15 Forma Therapeutics, Inc Purinonas como inibidores da protease específica da ubiquitina 1 e composição farmacêutica compreendendo os referidos compostos
US10765681B2 (en) 2016-02-05 2020-09-08 Academia Sinica Purine compounds possessing anticancer activity
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
AU2017384388B2 (en) 2016-12-20 2020-09-17 Astrazeneca Ab Amino-triazolopyridine compounds and their use in treating cancer
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
AU2018360801A1 (en) * 2017-11-01 2020-05-14 Celgene Corporation Process for producing a T cell composition
RS66798B1 (sr) 2018-03-09 2025-06-30 Recurium Ip Holdings Llc Supstituisani 1,2-dihidro-3h-pirazolo[3,4-d]pirimidin-3-oni
CN110526907B (zh) * 2018-05-23 2021-04-23 四川大学 苯并噁嗪酮类衍生物及其应用
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
US11535621B2 (en) 2019-07-31 2022-12-27 Ribon Therapeutics, Inc. Heterobicyclic amides as inhibitors of CD38
EP4063371A1 (en) * 2019-11-22 2022-09-28 Medshine Discovery Inc. Pyrimidopyrrole spiro compounds and derivatives thereof as dna-pk inhibitors
CA3159290A1 (en) * 2019-11-25 2021-06-03 Kevin X Chen Pyrimidoimidazole compounds used as dna-pk inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010062571A1 (en) * 2008-10-27 2010-06-03 Signal Pharmaceuticals, Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway
RU2009118623A (ru) * 2006-10-19 2010-11-27 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи (US) Гетероарильные соединения, содержащие их композиции и способы лечения с применением этих соединений

Family Cites Families (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE262026C (enExample)
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
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
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
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
SK285357B6 (sk) 1997-09-26 2006-11-03 Zentaris Gmbh Zlúčeniny na báze azabenzimidazolu modulujúce funkciu serínovej/treonínovej proteínkinázy
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
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
ATE310004T1 (de) 2000-12-12 2005-12-15 Neurogen Corp Spiro(isobenzofuran-1,4'-piperidin)-3-one und 3h- spiroisobenzofuran-1,4'-piperidine
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
CA2458699C (en) 2001-09-04 2010-10-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
US6825184B2 (en) 2001-10-18 2004-11-30 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-Disubstituted benzo-fused urea compounds
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
CA2484921A1 (en) 2002-05-06 2003-11-13 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection
AU2003299531A1 (en) 2002-08-05 2004-06-07 University Of Massachusetts Compounds for modulating rna interference
EP1556053A4 (en) 2002-10-31 2006-04-19 Amgen Inc ANTI-INFLAMMATORY AGENTS
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
DK1599478T3 (da) 2003-02-26 2007-09-17 Boehringer Ingelheim Pharma Dihydropteridinoner, fremgangsmåde til fremstilling af disse og anvendelse af disse som lægemiddel
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
MXPA05011248A (es) * 2003-04-23 2005-12-14 Wyeth Corp Derivados de wortmanina solubles en agua.
EP2345659A1 (en) 2003-05-30 2011-07-20 Pharmasset, Inc. Modified fluorinated nucleoside analogues
CA2529196A1 (en) 2003-06-26 2005-02-17 Merck & Co., Inc. Benzodiazepine cgrp receptor antagonists
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
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
EP1796467A4 (en) * 2004-09-24 2009-07-01 Janssen Pharmaceutica Nv INHIBITORS IMIDAZO {4,5-B} PYRAZINONE PROTEIN KINASES
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
KR20070085286A (ko) 2004-10-29 2007-08-27 티보텍 파마슈티칼즈 리미티드 Hiv를 저해하는 바이사이클릭 피리미딘 유도체
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New 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
PL1853588T3 (pl) 2005-02-16 2008-11-28 Astrazeneca Ab Związki chemiczne
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
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
EP2275103B1 (en) 2005-11-21 2014-04-23 Novartis AG mTOR inhibitors in the treatment of endocrine tumors
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
EA017925B1 (ru) * 2006-08-02 2013-04-30 Цитокинетикс, Инкорпорэйтед ПРОИЗВОДНЫЕ 1Н-ИМИДАЗО[4,5-b]ПИРАЗИНА
JP5600004B2 (ja) 2006-09-05 2014-10-01 エモリー ユニバーシティー 感染の予防または治療のためのチロシンキナーゼ阻害剤
WO2008030744A2 (en) 2006-09-05 2008-03-13 Board Of Regents, The University Of Texas System Inhibitors of c-met and uses thereof
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
CN101679432B (zh) 2006-10-19 2015-04-22 西格诺药品有限公司 杂芳基化合物、其组合物及其作为蛋白激酶抑制剂的用途
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP5590040B2 (ja) * 2008-11-12 2014-09-17 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのピラジノピラジンおよび誘導体
AU2009324894B2 (en) * 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use
NZ599549A (en) * 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
ES2670659T3 (es) * 2010-02-03 2018-05-31 Signal Pharmaceuticals, Llc Identificación de mutación en LKB1 como un biomarcador predictivo para la sensibilidad a inhibidores de la quinasa TOR
US20120028972A1 (en) * 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
WO2013019927A1 (en) 2011-08-03 2013-02-07 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for lkb1 status
CN104093398B (zh) 2011-12-02 2017-03-15 西格诺药品有限公司 7‑(6‑(2‑羟基丙烷‑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、其固体形式的药物组合物及其使用方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2009118623A (ru) * 2006-10-19 2010-11-27 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи (US) Гетероарильные соединения, содержащие их композиции и способы лечения с применением этих соединений
WO2010062571A1 (en) * 2008-10-27 2010-06-03 Signal Pharmaceuticals, Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway

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