JP5520831B2 - Ｐｉ３キナーゼの阻害薬 - Google Patents

Ｐｉ３キナーゼの阻害薬 Download PDF

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JP5520831B2
JP5520831B2 JP2010539504A JP2010539504A JP5520831B2 JP 5520831 B2 JP5520831 B2 JP 5520831B2 JP 2010539504 A JP2010539504 A JP 2010539504A JP 2010539504 A JP2010539504 A JP 2010539504A JP 5520831 B2 JP5520831 B2 JP 5520831B2
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pyridin
imidazo
acetamide
pyridazin
mmol
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JP2011507854A5 (enExample
JP2011507854A (ja
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ブツカー，シヨン
キム，テ−ソン
リヤオ・ホンユー
リウ，ロンビン
ノーマン，マーク・エイチ
ピーターソン，エミリー・アン
ステツク，マーキアン
タマヨ，ヌリア・エイ
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アムジエン・インコーポレーテツド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2010539504A 2007-12-19 2008-12-18 Ｐｉ３キナーゼの阻害薬 Expired - Fee Related JP5520831B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US843007P 2007-12-19 2007-12-19
US61/008,430 2007-12-19
PCT/US2008/013940 WO2009085230A1 (en) 2007-12-19 2008-12-18 Inhibitors of pi3 kinase

Publications (3)

Publication Number Publication Date
JP2011507854A JP2011507854A (ja) 2011-03-10
JP2011507854A5 JP2011507854A5 (enExample) 2014-04-17
JP5520831B2 true JP5520831B2 (ja) 2014-06-11

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JP2010539504A Expired - Fee Related JP5520831B2 (ja) 2007-12-19 2008-12-18 Ｐｉ３キナーゼの阻害薬

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US (1) US7820665B2 (enExample)
EP (1) EP2231661A1 (enExample)
JP (1) JP5520831B2 (enExample)
AR (1) AR069862A1 (enExample)
AU (1) AU2008343813B2 (enExample)
CA (1) CA2710194C (enExample)
CL (1) CL2008003798A1 (enExample)
PE (1) PE20091268A1 (enExample)
TW (1) TW200940544A (enExample)
WO (1) WO2009085230A1 (enExample)

Families Citing this family (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2555263A1 (en) * 2004-02-12 2005-09-01 Neurogen Corporation Imidazo-pyridazines, triazolo-pyridazines and related benzodiazepine receptor ligands
EP2188274A4 (en) 2007-08-03 2011-05-25 Boehringer Ingelheim Int VIRAL POLYMERASE HEMMER
US8058274B2 (en) * 2007-08-17 2011-11-15 Icagen, Inc. Heterocycles as potassium channel modulators
US8431608B2 (en) * 2007-08-17 2013-04-30 Icagen Inc. Heterocycles as potassium channel modulators
US8476257B2 (en) 2007-12-19 2013-07-02 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
JPWO2009128520A1 (ja) * 2008-04-18 2011-08-04 塩野義製薬株式会社 Ｐｉ３ｋ阻害活性を有する複素環化合物
AR071523A1 (es) * 2008-04-30 2010-06-23 Merck Serono Sa Compuestos biciclicos fusionados, un proceso para su preparacion, el compuesto para ser utilizado como medicamento en el tratamiento y profilaxis de enfermedades, una composicion farmaceutica y un conjunto que comprende paquetes separados del compuesto y de un ingrediente activo del medicamento
WO2009155121A2 (en) 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
WO2010007099A1 (en) * 2008-07-15 2010-01-21 Cellzome Limited 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
MX2011009796A (es) 2009-03-20 2011-12-14 Amgen Inc Inhibidores de la cinasa pi3.
JP2012526836A (ja) * 2009-05-13 2012-11-01 アムジエン・インコーポレーテツド Ｐｉｋｋ阻害薬としてのヘテロアリール化合物
WO2010130796A1 (en) 2009-05-15 2010-11-18 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors
PE20120493A1 (es) 2009-06-29 2012-05-20 Incyte Corp Pirimidinonas como inhibidores de pi3k
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
CA2787714C (en) 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
AR081823A1 (es) * 2010-04-14 2012-10-24 Incyte Corp DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd
WO2011141713A1 (en) 2010-05-13 2011-11-17 Centro Nacional De Investigaciones Oncologicas (Cnio) New bicyclic compounds as pi3-k and mtor inhibitors
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
WO2012058671A1 (en) 2010-10-31 2012-05-03 Endo Pharmaceuticals Inc. Substituted quinazoline and pyrido-pyrimidine derivatives
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
US20120258967A1 (en) * 2011-03-09 2012-10-11 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
WO2012174312A2 (en) * 2011-06-15 2012-12-20 Glaxosmithkline Llc Benzimidazole derivatives as antiviral agents
KR20230038593A (ko) 2011-09-02 2023-03-20 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
WO2013049250A1 (en) 2011-09-27 2013-04-04 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
US10292390B2 (en) 2011-11-04 2019-05-21 Wisconsin Alumni Research Foundation Inhibition and dispersion of bacterial biofilms with 2-aminobenzimidazole derivatives
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
TWI574962B (zh) * 2012-11-14 2017-03-21 加拓科學公司 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途
CN104837844B (zh) 2012-12-21 2017-08-29 百时美施贵宝公司 作为酪蛋白激酶1 d/e抑制剂的吡唑取代的咪唑并哌嗪
JP6267231B2 (ja) 2012-12-21 2018-01-24 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ カゼインキナーゼ１δ／ε阻害剤としての新規な置換イミダゾール
CN103965199B (zh) * 2013-02-02 2017-07-07 广东东阳光药业有限公司 一种芳杂环化合物、包含它的药物组合物及其用途
EP2958902B1 (en) 2013-02-19 2017-11-15 Amgen Inc. Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer
BR112015018318A2 (pt) * 2013-02-21 2017-08-22 Sunshine Lake Pharma Co Ltd Composto, composição farmacêutica, uso de um composto ou de uma composição farmacêutica, e, métodos para prevenir, gerenciar, tratar ou diminuir a severidade de um distúrbio proliferativo em um paciente e para inibir ou modular a atividade de uma proteína quinase em uma amostra biológica
WO2014151863A1 (en) 2013-03-14 2014-09-25 Amgen Inc. Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
WO2014145852A2 (en) 2013-03-15 2014-09-18 Knopp Biosciences Llc Imidazo(4,5-b) pyridin-2-yl amides as kv7 channel activators
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
PT3068393T (pt) 2013-11-11 2022-06-14 Amgen Inc Terapia de combinação, incluindo um inibidor de mdm2 e um ou mais agentes farmaceuticamente ativos adicionais para o tratamento de cancros
GB201321734D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents
TN2016000270A1 (en) 2014-01-14 2017-10-06 Millennium Pharm Inc Heteroaryls and uses thereof.
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TWI664164B (zh) 2014-02-13 2019-07-01 美商英塞特控股公司 作為ｌｓｄ１抑制劑之環丙胺
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PE20161573A1 (es) 2014-02-13 2017-01-19 Incyte Corp Ciclopropilamina como inhibidor de la lsd1
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015134854A2 (en) * 2014-03-06 2015-09-11 Oyagen, Inc. Small molecule vif dimerization antagonists as anti-hiv agents and for use as hiv/aids therapeutics
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
WO2016040952A2 (en) 2014-09-12 2016-03-17 Knopp Biosciences Llc BENZOIMIDAZOL-1,2-YL AMIDES AS Kv7 CHANNEL ACTIVATORS
CN105503877A (zh) 2014-09-24 2016-04-20 和记黄埔医药（上海）有限公司 咪唑并哒嗪类化合物及其用途
CN104402890A (zh) * 2014-11-10 2015-03-11 常州大学 一种制备五氟磺草胺的方法
CN104447756A (zh) * 2014-11-10 2015-03-25 常州大学 一种五氟磺草胺中间体的制备方法
JP6800158B2 (ja) 2015-02-20 2020-12-16 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｇｄｆ−８阻害剤
PH12017501538B1 (en) 2015-02-27 2024-02-14 Incyte Holdings Corp Salts of p13k inhibitor and processes for their preparation
MY191796A (en) 2015-04-03 2022-07-15 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
TN2017000483A1 (en) 2015-05-20 2019-04-12 Amgen Inc Triazole agonists of the apj receptor.
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
AU2016315881B2 (en) * 2015-09-03 2019-09-19 The Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK1A and uses thereof
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
WO2017192485A1 (en) 2016-05-03 2017-11-09 Amgen Inc. Heterocyclic triazole compounds as agonists of the apj receptor
US10906890B2 (en) 2016-11-16 2021-02-02 Amgen Inc. Triazole phenyl compounds as agonists of the APJ receptor
EP3541792B1 (en) 2016-11-16 2020-12-23 Amgen Inc. Triazole furan compounds as agonists of the apj receptor
MA46827A (fr) 2016-11-16 2019-09-25 Amgen Inc Composés de triazole à substitution cycloalkyle en tant qu'agonistes du récepteur apj
US11191762B2 (en) 2016-11-16 2021-12-07 Amgen Inc. Alkyl substituted triazole compounds as agonists of the APJ Receptor
WO2018093580A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Triazole pyridyl compounds as agonists of the apj receptor
WO2018097945A1 (en) 2016-11-16 2018-05-31 Amgen Inc. Heteroaryl-substituted triazoles as apj receptor agonists
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
WO2019018562A1 (en) 2017-07-19 2019-01-24 Ideaya Biosciences, Inc. AMIDO COMPOUND AS MODULATORS OF AHR
AR112797A1 (es) 2017-09-08 2019-12-11 Amgen Inc Inhibidores de kras g12c y métodos para utilizarlos
MX2020003706A (es) * 2017-10-30 2020-07-22 Bristol Myers Squibb Co Aminoimidazopiridazinas como inhibidores de cinasa.
WO2019089335A1 (en) 2017-11-03 2019-05-09 Amgen Inc. Fused triazole agonists of the apj receptor
WO2019168847A1 (en) 2018-02-27 2019-09-06 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
IL277419B2 (en) 2018-03-19 2024-07-01 Knopp Biosciences Llc Kv7 channel activators compositions and methods of use
WO2019213006A1 (en) 2018-05-01 2019-11-07 Amgen Inc. Substituted pyrimidinones as agonists of the apj receptor
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
CN112469418A (zh) 2018-06-01 2021-03-09 因赛特公司 治疗pi3k相关病症的给药方案
JP7369719B2 (ja) 2018-06-12 2023-10-26 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
JOP20200342A1 (ar) 2018-07-05 2020-12-30 Incyte Corp مشتقات بيرازين مدمجة كمثبطات a2a/a2b
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
MX2021010122A (es) * 2019-02-22 2021-09-23 1St Biotherapeutics Inc Compuestos de imidazopiridinilo y su uso para el tratamiento de trastornos neurodegenerativos.
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CA3225293A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
BR112022002698A2 (pt) 2019-08-14 2022-07-19 Incyte Corp Compostos de imidazolil pirimidinilamina como inibidores de cdk2
AU2020364007A1 (en) 2019-10-11 2022-04-28 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
US20230028414A1 (en) 2019-12-16 2023-01-26 Amgen Inc. Dosing regimen of kras g12c inhibitor
CN112047950B (zh) * 2020-09-14 2023-07-25 华东师范大学 咪唑并吡嗪类衍生物及其合成方法和应用
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH505543A (de) * 1968-11-01 1971-04-15 Ciba Geigy Ag Schädlingsbekämpfungsmittel
AUPP873799A0 (en) * 1999-02-17 1999-03-11 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds
US7091227B2 (en) * 2000-02-07 2006-08-15 Abbott Gmbh & Co. Kg Benzothiazole derivatives
WO2001083456A1 (en) * 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
US7449488B2 (en) * 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
CA2493843C (en) 2002-07-10 2012-04-17 Applied Research Systems Ars Holding N.V. Azolidinone-vinyl fused-benzene derivatives
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
EP1620413A2 (en) * 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
GB0315203D0 (en) 2003-06-28 2003-08-06 Celltech R&D Ltd Chemical compounds
US20050085531A1 (en) * 2003-10-03 2005-04-21 Hodge Carl N. Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
US7470712B2 (en) 2004-01-21 2008-12-30 Bristol-Myers Squibb Company Amino-benzazoles as P2Y1 receptor inhibitors
WO2005080380A1 (en) * 2004-02-03 2005-09-01 Eli Lilly And Company Kinase inhibitors
JP2007520558A (ja) * 2004-02-04 2007-07-26 スミスクライン・ビーチャム・コーポレイション キナーゼ阻害剤として有用なピリミジノン化合物
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
CN101056633A (zh) 2004-10-12 2007-10-17 应用研究系统Ars股份公司 用于贫血治疗的PI3激酶γ抑制剂
HN2005000795A (es) 2004-10-15 2010-08-19 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
US7528138B2 (en) * 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
SE0402735D0 (sv) 2004-11-09 2004-11-09 Astrazeneca Ab Novel compounds
US7473784B2 (en) 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
ES2274712B1 (es) * 2005-10-06 2008-03-01 Laboratorios Almirall S.A. Nuevos derivados imidazopiridina.
US7989461B2 (en) 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
CN101484452A (zh) 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 噻唑衍生物及其作为抗肿瘤药物的用途
US20090118336A1 (en) 2006-05-03 2009-05-07 Laurent David Pyrazole derivatives and their use as pi3k inhibitors
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
US20090306126A1 (en) * 2006-05-22 2009-12-10 Astrazeneca Ab Indole Derivatives
GB0610242D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
FR2903107B1 (fr) * 2006-07-03 2008-08-22 Sanofi Aventis Sa Derives d'imidazopyridine-2-carboxamides, leur preparation et leur application en therapeutique
US20090258882A1 (en) 2006-07-28 2009-10-15 Novartis Ag 2,4-Substituted Quinazolines as Lipid Kinase Inhibitors
EP2058309A4 (en) * 2006-08-04 2010-12-22 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
MX2009002171A (es) 2006-08-30 2009-05-28 Cellzome Ltd Derivados de triazol como inhibidores de cinasas.
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘
EP2079744A1 (en) 2006-10-30 2009-07-22 Novartis AG Imidazopyridazines as pi3k lipid kinase inhibitors
AU2007329352B2 (en) 2006-12-07 2013-01-17 F. Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
EP2114950B1 (en) 2006-12-07 2016-03-09 Genentech, Inc. Phosphoinositide 3-kinase inhibitor compounds and methods of use
EP2118076B1 (en) 2007-02-22 2019-09-04 Merck Serono S.A. Quinoxaline compounds and use thereof
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
US20080233127A1 (en) * 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
WO2008133192A1 (ja) 2007-04-19 2008-11-06 Takeda Pharmaceutical Company Limited 縮合イミダゾール化合物およびその用途
US20100305113A1 (en) 2007-05-09 2010-12-02 Hans-Georg Capraro Substituted Imidazopyridazines as Lipid Kinase Inhibitors
US7592342B2 (en) 2007-05-10 2009-09-22 Smithkline Beecham Corporation Quinoxaline derivatives as PI3 kinase inhibitors
AR067326A1 (es) 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
US8131310B2 (en) 2007-05-18 2012-03-06 Research In Motion Limited Method and system for discontinuous reception de-synchronization detection
JP2010529031A (ja) 2007-05-29 2010-08-26 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害剤としてのナフチリジン誘導体
US7893060B2 (en) 2007-06-12 2011-02-22 F. Hoffmann-La Roche Ag Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
WO2008152387A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Quinazoline derivatives as pi3 kinase inhibitors
UY31137A1 (es) 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
JP5588339B2 (ja) 2007-06-25 2014-09-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規化学化合物
CA2692653A1 (en) 2007-07-11 2009-01-15 Auckland Uniservices Limited Pyrazolo[1,5-.alpha.]pyridines and their use in cancer therapy
AU2008277628B2 (en) * 2007-07-18 2012-03-15 Novartis Ag Bicyclic heteroaryl compounds and their use as kinase inhibitors
ES2401557T3 (es) 2007-08-02 2013-04-22 Amgen, Inc Moduladores de Pl3 cinasas y métodos de uso
JP2011500702A (ja) 2007-10-16 2011-01-06 ワイス・エルエルシー チエノピリミジンおよびピラゾロピリミジン化合物ならびにｍＴＯＲキナーゼおよびＰＩ３キナーゼ阻害剤としてのその使用
JP2011500823A (ja) 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体
WO2009053716A1 (en) 2007-10-26 2009-04-30 F.Hoffmann-La Roche Ag Purine derivatives useful as pi3 kinase inhibitors
GB0721095D0 (en) 2007-10-26 2007-12-05 Piramed Ltd Pharmaceutical compounds
US20090149458A1 (en) 2007-11-27 2009-06-11 Wyeth PYRROLO[3,2-d]PYRIMIDINE COMPOUNDS AND THEIR USE AS PI3 KINASE AND mTOR KINASE INHIBITORS
WO2009068482A1 (en) 2007-11-27 2009-06-04 Cellzome Limited Amino triazoles as pi3k inhibitors
ES2587738T3 (es) 2007-12-21 2016-10-26 Ucb Biopharma Sprl Derivados de quinoxalina y quinolina como inhibidores de quinasa
EA201001017A1 (ru) 2008-01-15 2011-02-28 ВАЙЕТ ЭлЭлСи 3h-[1,2,3]триазоло[4,5-d]пиримидиновые соединения, их применение в качестве ингибиторов киназы mtor и киназы pi3 и их синтезы
US20090192176A1 (en) 2008-01-30 2009-07-30 Wyeth 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
CN101981037B (zh) 2008-01-30 2013-09-04 吉宁特有限公司 吡唑并嘧啶pi3k抑制剂化合物及使用方法

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