LU92508I2 - Cabozantinib et toutes les formes thérapeutiquement équivalentes qui en dérivent telles que protégées par le brevet de base, y compris les sels pharmacetuiquement acceptables - Google Patents

Cabozantinib et toutes les formes thérapeutiquement équivalentes qui en dérivent telles que protégées par le brevet de base, y compris les sels pharmacetuiquement acceptables Download PDF

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Publication number
LU92508I2
LU92508I2 LU92508C LU92508C LU92508I2 LU 92508 I2 LU92508 I2 LU 92508I2 LU 92508 C LU92508 C LU 92508C LU 92508 C LU92508 C LU 92508C LU 92508 I2 LU92508 I2 LU 92508I2
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Luxembourg
Prior art keywords
compounds
pharmacetually
cabozantinib
protected
acceptable salts
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LU92508C
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English (en)
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Exelixis Inc
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Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of LU92508I2 publication Critical patent/LU92508I2/fr

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Families Citing this family (284)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3366959B2 (ja) 1998-06-19 2003-01-14 三洋昭和パネルシステム株式会社 高さ調整自在な幅木
EP1415987B1 (fr) 2000-10-20 2007-02-28 Eisai R&D Management Co., Ltd. Composes heteroaromatiques azotes pour le traitement des maladies de cancer
EP1604665B1 (fr) 2003-03-10 2011-05-11 Eisai R&D Management Co., Ltd. Inhibiteur de kinase c-kit
MXPA06003113A (es) 2003-09-19 2006-06-20 Astrazeneca Ab Derivados de quinazolina.
CA2744997A1 (fr) * 2003-09-26 2005-04-07 Exelixis, Inc. Modulateurs de c-met et procede d'utilisation
WO2005044788A1 (fr) 2003-11-11 2005-05-19 Eisai Co., Ltd. Derive d'uree et son procede de production
US20050267182A1 (en) * 2003-11-13 2005-12-01 Ambit Biosciences Corporation Urea derivatives as FLT-3 modulators
CA2553433A1 (fr) * 2004-01-23 2005-08-11 Amgen Inc. Composes de quinoleine, de quinazoline, de pyridine et de pyrimidine et utilisations connexes pour traiter l'inflammation, l'angiogenese et le cancer
EP1719762B1 (fr) * 2004-02-27 2012-06-27 Eisai R&D Management Co., Ltd. Nouveau derive de la pyridine et derive de la pyrimidine (1)
US7456176B2 (en) 2004-04-08 2008-11-25 Targegen, Inc. Benzotriazine inhibitors of kinases
US7459562B2 (en) 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
US7439246B2 (en) 2004-06-28 2008-10-21 Bristol-Myers Squibb Company Fused heterocyclic kinase inhibitors
US7432373B2 (en) 2004-06-28 2008-10-07 Bristol-Meyers Squibb Company Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
US20050288290A1 (en) 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
US7652051B2 (en) 2004-08-25 2010-01-26 Targegen, Inc. Heterocyclic compounds and methods of use
ATE428421T1 (de) 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
EP2289510A1 (fr) 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Dérivés hétérocycliques pour le traitement des maladies induites par des enzymes stearoyl-coa desaturase
EP1799667B1 (fr) 2004-09-20 2013-03-20 Xenon Pharmaceuticals Inc. Derives heterocycliques et leur utilisation comme agents therapeutiques
EP2269610A3 (fr) 2004-09-20 2011-03-09 Xenon Pharmaceuticals Inc. Dérivés hétérocycliques et leur utilisation en tant qu'inhibiteurs de la stearoyl-coa desaturase
MX2007003332A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de estearoil-coa-desaturasa.
MX2007003319A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
JP4958786B2 (ja) 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体および治療薬としてのそれらの使用
MX2007003327A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa.
CA2581516C (fr) 2004-10-12 2013-06-11 Astrazeneca Ab Derives de quinazoline
US7652009B2 (en) 2004-11-30 2010-01-26 Amgem Inc. Substituted heterocycles and methods of use
EP1674466A1 (fr) * 2004-12-27 2006-06-28 4Sc Ag Derives benzazoles 2,5- et 2-6-disubstitues utiles comme des inhibiteurs de la proteine kinase
US7576090B2 (en) * 2004-12-27 2009-08-18 4Sc Ag Benzazole analogues and uses thereof
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
JP5148499B2 (ja) * 2005-05-20 2013-02-20 メチルジーン インコーポレイテッド Ｖｅｇｆ受容体およびｈｇｆ受容体シグナル伝達の阻害剤
KR20080026562A (ko) * 2005-06-02 2008-03-25 갤럭시 바이오테크, 엘엘씨 항체를 이용한 뇌종양 치료 방법
BRPI0611187A2 (pt) 2005-06-03 2010-08-24 Xenon Pharmaceuticals Inc derivados aminotiazàis como inibidores da estearoil-coa desaturase humana
EP1925676A4 (fr) 2005-08-02 2010-11-10 Eisai R&D Man Co Ltd Procédé d'analyse de l' effet d 'un inhibiteur de vascularisation
PL1889836T3 (pl) 2005-08-24 2013-10-31 Eisai R&D Man Co Ltd Nowa pochodna pirydyny i pochodna pirymidyny (3)
TW200804345A (en) 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
US7732613B2 (en) 2005-09-14 2010-06-08 Bristol-Myers Squibb Company Met kinase inhibitors
WO2007061127A1 (fr) * 2005-11-22 2007-05-31 Eisai R & D Management Co., Ltd. Agent antitumeur pour myelomes multiples
AR059246A1 (es) * 2006-01-30 2008-03-19 Array Biopharma Inc Compuestos heterobiciclicos de tiofeno y metodos de uso
UY30183A1 (es) 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
MX2008011220A (es) 2006-03-07 2008-09-11 Array Biopharma Inc Compuestos de pirazol heterobiciclicos y metodos de uso.
AR059922A1 (es) * 2006-04-01 2008-05-07 Galaxy Biotech Llc Anticuerpos monoclonales humanizados para el factor de crecimiento de hepatocitos
DK2010528T3 (en) 2006-04-19 2018-01-15 Novartis Ag 6-O-Substituted Benzoxazole and Benzothiazole Compounds and Methods for Inhibiting CSF-1R Signaling
WO2007136103A1 (fr) 2006-05-18 2007-11-29 Eisai R & D Management Co., Ltd. Agent antitumoral destiné au cancer de la thyroïde
RS52062B (sr) 2006-05-19 2012-06-30 Abbott Laboratories Cns aktivni azabiciklični alkanski derivati koji su supstituisani spojenim bicikloheterociklom
US20080004273A1 (en) * 2006-05-30 2008-01-03 Stephane Raeppel Inhibitors of protein tyrosine kinase activity
US20110053931A1 (en) * 2006-06-08 2011-03-03 John Gaudino Quinoline compounds and methods of use
JP2010500365A (ja) 2006-08-07 2010-01-07 インサイト・コーポレイション キナーゼ阻害剤としてのトリアゾロトリアジン
CN101454311B (zh) 2006-08-23 2013-03-27 卫材R&D管理有限公司 苯氧基吡啶衍生物的盐和其结晶及其制备方法
KR101472600B1 (ko) 2006-08-28 2014-12-15 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암에 대한 항종양제
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
WO2008049855A2 (fr) * 2006-10-27 2008-05-02 Glaxo Group Limited Nouveaux composés
ES2560435T3 (es) 2006-11-22 2016-02-19 Incyte Holdings Corporation Imidazotriazinas e imidazopirimidinas como inhibidores de la quinasa
WO2008079291A2 (fr) * 2006-12-20 2008-07-03 Amgen Inc. Hétérocycles substitués et leurs méthodes d'utilisation
US7915287B2 (en) * 2006-12-20 2011-03-29 Amgen Inc. Substituted heterocycles and methods of use
JP2010516680A (ja) * 2007-01-19 2010-05-20 エックスカバリー，インコーポレイテッド キナーゼ阻害薬化合物
EP2119707B1 (fr) 2007-01-29 2015-01-14 Eisai R&D Management Co., Ltd. Composition destinée au traitement d'un cancer de l'estomac de type indifférencié
BRPI0812159A2 (pt) * 2007-05-21 2017-05-02 Novartis Ag inibidores de csf-1r, composições e métodos de uso
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
EP2185542A2 (fr) 2007-08-15 2010-05-19 Glaxo Group Limited Composés
EP2183254B1 (fr) 2007-08-29 2017-06-21 MethylGene Inc. Inhibiteurs de l'activité protéine tyrosine kinase
CN101848895B (zh) 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
JP2009132660A (ja) 2007-11-30 2009-06-18 Eisai R & D Management Co Ltd 食道癌治療用組成物
US8558000B2 (en) 2008-01-23 2013-10-15 Bristol-Myers Squibb Company 4-pyridinone compounds and their use for cancer
PL2947072T3 (pl) 2008-03-17 2017-05-31 Ambit Biosciences Corporation 1-(3-(6,7-dimetoksychinazolin-4-yloksy)fenylo)-3-(5-(1,1,1-trifluoro-2-metylopropan-2-ylo)izoksazol-3-ilo)mocznik jako modulator kinazy RAF w leczeniu chorób nowotworowych
RU2503664C2 (ru) 2008-04-10 2014-01-10 Тайхо Фармасьютикал Ко., Лтд. Производное ацилтиомочевины или его соль, и его применение
JP5746015B2 (ja) * 2008-04-16 2015-07-08 マックス プランク ゲゼルシャフト ツゥアー フェデルゥン デル ヴィッセンシャフテン エー フォー Ａｘｌキナーゼ阻害剤としてのキノリン誘導体
UY31800A (es) * 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
MX393622B (es) 2008-05-21 2025-03-24 Incyte Corp Sales de 2-fluoro-n-metil-4-[7-(quinolin-6-il-metil)-imidazo[1,2-b][1,2,4]triazin-2-il]benzamida y procesos relacionados con la preparacion de las mismas.
CA2728228A1 (fr) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Composes inhibiteurs de l'oxindolyle
AU2009271003A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Imidazolylpyrimidine compounds as HDAC and/or CDK inhibitors
NZ602832A (en) 2008-07-14 2014-04-30 Gilead Sciences Inc Fused heterocyclic hdac inhibitor compounds
EP2149565A1 (fr) * 2008-07-24 2010-02-03 Bayer Schering Pharma AG Dérivés de chinazoline substitués par du sulfonamide en tant que modulateurs d'immunité pour le traitement de inflammations et allergies
AU2009276699A1 (en) 2008-07-28 2010-02-04 Gilead Sciences, Inc. Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds
AR075084A1 (es) * 2008-09-26 2011-03-09 Smithkline Beecham Corp Metodo de preparacion de quinolinil -oxidifenil - ciclopropanodicarboxamidas e intermediarios correspondientes
CA2740746A1 (fr) * 2008-10-14 2010-04-22 Ning Xi Composes comprenant un cycle spiro et methodes d'utilisation
CN102256493A (zh) * 2008-10-29 2011-11-23 迪赛孚尔制药有限公司 表现出抗癌活性和抗增殖活性的环丙烷酰胺及其类似物
CA2743416A1 (fr) * 2008-11-13 2010-05-20 Exelixis Inc. Procedes de preparation de derives de quinoline
EP2367795A1 (fr) * 2008-12-04 2011-09-28 Exelixis, Inc. Procédés de préparation de dérivés de quinoléine
DE102009003975A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
EA038195B1 (ru) 2009-01-16 2021-07-22 Экселиксис, Инк. Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее применение для лечения рака почек и печени
EP2210891A1 (fr) * 2009-01-26 2010-07-28 Domain Therapeutics Nouveaux ligands du récepteur de l'adénosine et leurs utilisations
EP2408300B1 (fr) * 2009-03-21 2016-05-11 Sunshine Lake Pharma Co., Ltd. Dérivés d'ester d'amino, sels de ceux-ci et procédés d'utilisation
KR20120061063A (ko) 2009-06-05 2012-06-12 화이자 인코포레이티드 Ｇｐｒ 119 조절제로서의 ｌ-(피페리딘-4-일)-피라졸 유도체
ES2463826T3 (es) 2009-06-08 2014-05-29 Gilead Sciences, Inc. Compuestos inhibidores de HDAC de cicloalquilcarbamato benzamida anilina
KR20120031170A (ko) 2009-06-08 2012-03-30 길리애드 사이언시즈, 인코포레이티드 알카노일아미노 벤즈아미드 아닐린 ｈｄａｃ 저해제 화합물
EP2454238A1 (fr) 2009-07-17 2012-05-23 Exelixis, Inc. Formes cristallines du n [3 fluoro-4-({méthyloxy)-7-[(3-morpholin-4-yl- propyl)oxy]quinoléin-4-yl}oxy)phényl]-n'-(4-fluorophényl)cyclopropane- 1,1-dicarboxamide
UA108618C2 (uk) * 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
BR112012003592B8 (pt) 2009-08-19 2021-05-25 Eisai R&D Man Co Ltd composição farmacêutica contendo derivado de quinolina
CN102030705B (zh) * 2009-09-30 2012-12-19 上海睿智化学研究有限公司 7-苄氧基-6-甲氧基-4-羟基喹啉的合成方法
EP2311809A1 (fr) * 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinolinyloxyphenylsulfonamides
EP2501233B1 (fr) 2009-11-03 2014-09-24 GlaxoSmithKline LLC Composés de quinazoline
US20110129463A1 (en) * 2009-11-27 2011-06-02 Proteologics, Ltd. Quinazolin-4(3A)-One Derivatives and Methods of Use Thereof
DE102009056886A1 (de) 2009-12-03 2011-06-09 Bayer Schering Pharma Aktiengesellschaft cMet-Inhibitoren zur Behandlung der Endometriose
CN102086211B (zh) * 2009-12-08 2013-09-11 广东东阳光药业有限公司 作为蛋白激酶抑制剂的芳杂环化合物
JP5714030B2 (ja) 2010-02-03 2015-05-07 インサイト コーポレーションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｃ−Ｍｅｔ阻害剤としてのイミダゾ［１，２−ｂ］［１，２，４］トリアジン
EP2545038A1 (fr) * 2010-03-12 2013-01-16 Exelixis, Inc. Forme cristaline hydratée du n-[3-fluoro-4-({6-(méthyloxy)-7-[(3- morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phényl]-n'-(4-fluorophényl)cyclopropane-1,1-dicarboxamide
EP2553641A4 (fr) * 2010-03-26 2015-01-07 EastNets Système informatique de paiement mobile et procédé
CN102212062B (zh) * 2010-04-02 2015-04-29 广东东阳光药业有限公司 氨基酯类衍生物及其盐和使用方法
US20120070368A1 (en) * 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
EP2560488B1 (fr) 2010-04-23 2015-10-28 Cytokinetics, Inc. Aminopyridines et aminotriazines, leurs compositions et leurs procédés d'utilisation
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
US8569319B2 (en) 2010-04-29 2013-10-29 Deciphera Pharmaceuticals, LLS Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities
EP3450432A1 (fr) 2010-05-17 2019-03-06 Incozen Therapeutics Pvt. Ltd. Nouveaux composés 3,5 disubstitués-3h-imidazo[4,5-b] pyridine et 3,5-disubstitués-3h-[1,2,3]triazolo[4,5-b] pyridine utilisés comme modulateurs de kinases de protéine
CA2802644C (fr) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Agent anticancereux utilisant des composes ayant un effet inhibiteur de kinase en combinaison
JP2013532627A (ja) 2010-07-01 2013-08-19 武田薬品工業株式会社 ｃＭＥＴ阻害剤とＨＧＦおよび／またはｃＭＥＴに対する抗体との組み合わせ
WO2012009722A1 (fr) * 2010-07-16 2012-01-19 Exelixis, Inc. Compositions pharmaceutiques modulatrices de c-met
US20140186407A9 (en) 2010-07-16 2014-07-03 Exelixis Inc. C-Met Modulator Pharmaceutical Compositions
EP2423208A1 (fr) 2010-08-28 2012-02-29 Lead Discovery Center GmbH Composants actifs pharmaceutiquement en tant qu'inhibiteurs Axl
US8664244B2 (en) * 2010-09-12 2014-03-04 Advenchen Pharmaceuticals, LLC Compounds as c-Met kinase inhibitors
CN103391773A (zh) * 2010-09-27 2013-11-13 埃克塞里艾克西斯公司 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂
JP2013540759A (ja) * 2010-09-27 2013-11-07 エクセリクシス， インク． 去勢抵抗性前立腺癌および造骨性転移の治療のためのｍｅｔおよびｖｅｇｆの二元阻害薬
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
WO2012042421A1 (fr) 2010-09-29 2012-04-05 Pfizer Inc. Procédé de traitement de la croissance cellulaire anormale
JP2013543011A (ja) * 2010-11-22 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド 癌の治療法
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
TWI640509B (zh) 2011-02-10 2018-11-11 艾克塞里克斯公司 製造喹啉化合物之方法及包含該化合物之醫藥組合物
WO2012122011A2 (fr) 2011-03-04 2012-09-13 Glaxosmithkline Llc Amino-quinoléines en tant qu'inhibiteurs de kinase
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
EP2700403B1 (fr) 2011-04-18 2015-11-25 Eisai R&D Management Co., Ltd. Agent thérapeutique pour les tumeurs
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
TWI610918B (zh) * 2011-05-02 2018-01-11 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
WO2012166899A2 (fr) 2011-06-03 2012-12-06 Eisai R&D Management Co., Ltd. Biomarqueurs pour la prédiction et l'estimation de la sensibilité de sujets atteints d'un cancer de la thyroïde et du rein vis-à-vis de composés lenvatinib
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
CA2845933C (fr) 2011-09-06 2020-06-09 New York Blood Center, Inc. Inhibiteurs du vih
CN102408411B (zh) * 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
EP2768796B1 (fr) 2011-10-20 2019-11-20 Exelixis, Inc. Procédé de préparation de dérivés de quinoléine
US8843421B2 (en) 2011-11-01 2014-09-23 Accenture Global Services Limited Identification of entities likely to engage in a behavior
EP2775921A1 (fr) 2011-11-08 2014-09-17 Exelixis, Inc. Méthode de quantification d'un traitement anti-cancéreux
EP2776033A1 (fr) 2011-11-08 2014-09-17 Exelixis, Inc. Double inhibiteur de met et vegf pour le traitement du cancer
TWI577671B (zh) 2011-11-14 2017-04-11 Sunshine Lake Pharma Co Ltd Aminoquinazoline derivatives and salts thereof and methods of use thereof
US9546179B2 (en) * 2011-12-20 2017-01-17 Wei Qian Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof
CN102643268B (zh) * 2011-12-30 2014-05-21 沈阳药科大学 喹啉类及噌啉类化合物及其应用
EP2620869B1 (fr) 2012-01-27 2017-11-01 Optim Corporation Terminal portable, procédé et programme de changement d'interface utilisateur
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
AP3908A (en) 2012-03-30 2016-11-24 Rhizen Pharmaceuticals Sa Novel 3,5-disubstituted-3H-imidazo[4,5-B]pyridine and 3,5-disubstituted-3H-[1,2,3]triazolo [4,5-B] pyridine compounds as modulators of C-met protein kinases
WO2013152252A1 (fr) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Polythérapie antinéoplasique
WO2013166296A1 (fr) 2012-05-02 2013-11-07 Exelixis, Inc. Double modulateur met-vegf pour traiter des métastases osseuses ostéolytiques
WO2013180128A1 (fr) * 2012-05-28 2013-12-05 協和発酵キリン株式会社 Dérivé de 4-[4-(hétérocyclique aromatique à 5 chaînons carbonyl uréide)phényloxy]quinoléine
CN103509024B (zh) * 2012-06-28 2015-10-28 上海医药工业研究院 嘧啶并苯并氮杂卓类化合物及其作为抗肿瘤药物的应用
CN103626761B (zh) * 2012-08-24 2015-07-29 上海医药工业研究院 苯并吡啶氮杂卓类化合物及其作为抗肿瘤药物的应用
CN103626762B (zh) * 2012-08-24 2015-07-29 上海医药工业研究院 苯并吡啶氮杂卓类化合物及其应用
TW201425307A (zh) 2012-09-13 2014-07-01 Glaxosmithkline Llc 作為激酶抑制劑之胺基－喹啉類
TWI592417B (zh) 2012-09-13 2017-07-21 葛蘭素史克智慧財產發展有限公司 胺基喹唑啉激酶抑制劑之前藥
CN103664776B (zh) * 2012-09-26 2016-05-04 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
CN103705521A (zh) * 2012-09-28 2014-04-09 韩冰 一类治疗脑梗塞的化合物及其用途
CN103804305A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
CN103804382A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
CN102977014B (zh) * 2012-11-05 2015-01-07 沈阳药科大学 新的喹啉类化合物及其用途
CN103804381A (zh) * 2012-11-06 2014-05-21 韩冰 一类治疗缺血性脑损伤的化合物及其用途
CN103800328A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804290A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804361A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804291A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103800340A (zh) * 2012-11-09 2014-05-21 韩冰 一类治疗青光眼的化合物及其用途
CN103804298A (zh) * 2012-11-09 2014-05-21 韩冰 一类治疗青光眼的化合物及其用途
CN103804362A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
CN103804306A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
CN103804363A (zh) * 2012-11-14 2014-05-21 韩冰 一类具有神经保护作用的化合物及其用途
CN102964308B (zh) * 2012-11-30 2015-03-18 中国药科大学 新型嘧啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
AU2013364953A1 (en) 2012-12-21 2015-04-30 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same
CN103965104B (zh) * 2013-01-29 2017-09-29 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
TWI630203B (zh) 2013-02-21 2018-07-21 葛蘭素史克智慧財產發展有限公司 做為激酶抑制劑的喹唑啉類
BR112015023571A2 (pt) * 2013-03-15 2017-07-18 Hoffmann La Roche derivados de sulfamato e sulfamida de arila como moduladores rorc
CA2907334C (fr) * 2013-03-15 2021-12-07 Exelixis, Inc. Metabolites de n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
WO2014145693A1 (fr) * 2013-03-15 2014-09-18 Exelixis, Inc. Métabolites de n-[3-fluoro-4-({ 6-(méthyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phényl]-n'-(4-fluorophényl)cyclopropane-1,1-dicarboxamide
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
KR20150138268A (ko) 2013-04-04 2015-12-09 엑셀리시스, 인코포레이티드 암을 치료하기 위한 약물 병용요법
CN104109124B (zh) * 2013-04-19 2016-08-31 正大天晴药业集团股份有限公司 卡博替尼·0.5苹果酸盐的晶体
CN104109128B (zh) * 2013-04-19 2016-10-05 连云港润众制药有限公司 卡博替尼苹果酸盐及其制备方法
CN105264380B (zh) 2013-05-14 2017-09-05 卫材R&D管理有限公司 用于预测和评价子宫内膜癌受试者对乐伐替尼化合物响应性的生物标志
CN104370811B (zh) * 2013-08-15 2019-02-12 广东东阳光药业有限公司 一种喹啉化合物的新晶型及其制备方法
JP6612232B2 (ja) 2013-08-28 2019-11-27 クラウン バイオサイエンス インコーポレイテッド（タイカン） 対象のマルチキナーゼ阻害剤に対する応答性を予測する遺伝子発現シグネチャ、及びその使用
CN104628657A (zh) * 2013-11-06 2015-05-20 韩冰 一类治疗缺血性脑损伤的化合物及其用途
AU2015218236B2 (en) 2014-02-14 2019-06-13 Exelixis, Inc. Crystalline solid forms of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl) cyclopropane-1, 1-dicarboxamide, processes for making, and methods of use
TWI672141B (zh) 2014-02-20 2019-09-21 美商醫科泰生技 投予ｒｏｓ１突變癌細胞之分子
EP3112343B1 (fr) * 2014-02-28 2023-03-29 Tohoku University Derives amides
US10159666B2 (en) 2014-03-17 2018-12-25 Exelixis, Inc. Dosing of cabozantinib formulations
MX2016012285A (es) 2014-03-24 2017-01-23 Genentech Inc Tratamiento de cáncer con antagonista de c-met y correlación de estos con la expresión de hgf.
EP3906921A1 (fr) 2014-04-25 2021-11-10 Exelixis, Inc. Procédé de traitement de l'adénocarcinome pulmonaire
WO2015177758A1 (fr) 2014-05-23 2015-11-26 Mylan Laboratories Ltd Nouveaux polymorphes de (s)-malate de cabozantinib et cabozantinib sous forme de base libre
CN104788372B (zh) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体
CN106715397B (zh) * 2014-07-31 2021-07-23 埃克塞里艾克西斯公司 制备氟-18标记的卡博替尼及其类似物的方法
BR112017002318A2 (pt) * 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
CA2957005C (fr) 2014-08-28 2021-10-12 Eisai R&D Management Co., Ltd. Derive de quinoline de purete elevee et son procede de fabrication
ES2764440T3 (es) 2014-09-19 2020-06-03 New York Blood Center Inc Fenilpirrolcarboxamidas sustituidas con actividad terapéutica en VIH
KR102595599B1 (ko) 2014-12-02 2023-11-02 이그니타, 인코포레이티드 신경모세포종의 치료를 위한 병용
EP3229836B1 (fr) 2014-12-09 2019-11-13 Institut National de la Sante et de la Recherche Medicale (INSERM) Anticoprs monoclonaux contre 'axl'
SG11201706630UA (en) 2015-02-25 2017-09-28 Eisai R&D Man Co Ltd Method for suppressing bitterness of quinoline derivative
WO2016135041A1 (fr) 2015-02-26 2016-09-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Protéines de fusion et anticorps les contenant pour favoriser l'apoptose
WO2016140717A1 (fr) 2015-03-04 2016-09-09 Merck Sharp & Dohme Corp. Association d'un antagoniste de pd-1 et d'un inhibiteur des tyrosines kinases vegfr/fgfr/ret pour traiter le cancer
WO2016150966A1 (fr) 2015-03-25 2016-09-29 Sandoz Ag Formes cristallines de phosphate et de chlorhydrate de cabozantinib
CN106279147A (zh) * 2015-05-21 2017-01-04 中国科学院上海药物研究所 一种吡啶并氮杂环化合物及其制备方法和用途
BR112017027227B1 (pt) 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
US20170020856A1 (en) * 2015-06-29 2017-01-26 Ontogenesis, Llc N-Acylalkyl Prodrugs of Multi-Tyrosine Kinase Inhibitors and Methods of Use
CN107646030A (zh) * 2015-08-19 2018-01-30 桑多斯股份公司 丙二酸酯衍生物的不对称双酰胺化
JP6553726B2 (ja) 2015-08-20 2019-07-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
CN105218445B (zh) * 2015-08-25 2018-05-22 江苏中邦制药有限公司 一种酪氨酸激酶抑制剂Foretinib的制备方法
CN106543143B (zh) * 2015-09-22 2019-03-22 合肥中科普瑞昇生物医药科技有限公司 一类新型的flt3激酶抑制剂及其用途
CN108697661A (zh) 2015-12-18 2018-10-23 亚尼塔公司 用于治疗癌症的组合
CN105541798B (zh) * 2016-02-03 2018-01-23 中国人民解放军第二军医大学 具有抗肿瘤活性的喹啉类多靶点激酶抑制剂及其制备方法
CN107129465B (zh) * 2016-02-26 2020-06-19 中国科学院上海药物研究所 芳基胍类化合物及其制备方法和用途
EP3436462A1 (fr) * 2016-03-31 2019-02-06 Merck Patent GmbH Composés inhibiteurs de cyclophilines et leurs utilisations
CN109069499A (zh) 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法
CN105906568A (zh) * 2016-04-28 2016-08-31 西安交通大学 一种具有抗肿瘤活性的环丙二酰胺化合物及其制备方法和应用
CN106083715A (zh) * 2016-06-01 2016-11-09 谢阳 一种喹啉、喹唑啉类化合物及其药物组合物和应用
CN106008371A (zh) * 2016-06-24 2016-10-12 谢阳 1-芳基脲基环烷基-1-甲酰胺类化合物及其药物组合物和应用
CN107556238A (zh) * 2016-06-30 2018-01-09 深圳万乐药业有限公司 一种卡博替尼的合成方法
WO2018026877A1 (fr) 2016-08-05 2018-02-08 Calitor Sciences, Llc Méthode de préparation de composés de quinoléine-4-ol substitués
US10980792B2 (en) * 2016-09-12 2021-04-20 Zhuhai Beihai Biotech Co., Ltd. Formulations of Cabozantinib
CN107235896B (zh) * 2016-09-13 2019-11-05 上海翔锦生物科技有限公司 酪氨酸激酶抑制剂及其应用
JP2019529476A (ja) 2016-09-27 2019-10-17 ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ Ｎ−（４−（６，７−ジメトキシキノリン−４−イルオキシ）フェニル）−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドを用いた尿路上皮癌及び他の尿生殖器悪性腫瘍の治療方法
CA3040788C (fr) * 2016-10-18 2022-01-11 Beijing Konruns Pharmaceutical Co., Ltd. Compose d'acide carboxylique a substitution quinolinyle ou sel pharmaceutiquement acceptable de celui-ci, composition pharmaceutique et utilisation associees
JP7105774B2 (ja) 2016-12-01 2022-07-25 イグナイタ インコーポレイテッド がん治療のための方法
CN106632028B (zh) * 2016-12-22 2019-01-22 上海再启生物技术有限公司 一种卡博替尼的制备方法
CN108329298A (zh) * 2017-01-17 2018-07-27 南昌弘益药业有限公司 一类喹啉类新化合物制备方法
BR112019015011A2 (pt) 2017-01-20 2020-04-28 Exelixis Inc combinações de cabozantinibe e atezolizumabe para tratar câncer
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
MX2021007061A (es) 2017-02-15 2022-10-07 Taiho Pharmaceutical Co Ltd Composición farmacéutica que comprende 4-(2-fluoro-4-(3-(2- fenilacetil)tioureido)fenoxi)-7-metoxi-n-metilquinolina-6-carboxa mida e hidroxipropil-b-ciclodextrina.
CN108503650B (zh) * 2017-02-27 2021-02-12 北京赛特明强医药科技有限公司 二噁烷并喹唑啉类化合物或其药用盐或其水合物及其作为酪氨酸激酶抑制剂的应用
CA3059660A1 (fr) * 2017-04-27 2018-11-01 Astrazeneca Ab Composes de phenoxyquinalzoline et leur utilisation en traitement d'un cancer
BR112019023064A2 (pt) 2017-05-16 2020-06-09 Eisai R&D Man Co Ltd tratamento de carcinoma hepatocelular
IL270780B2 (en) 2017-05-26 2025-04-01 Exelixis Inc Crystalline solid forms of salts of N–{4–[(7,6–dimethoxyquinolin–4–yl)oxy]phenyl}–N'–(4–fluorophenyl)cyclopropane–1,1–dicarboxamide, processes for preparation and methods of use
AU2018279834B2 (en) 2017-06-09 2024-05-23 Exelixis, Inc. Liquid dosage forms to treat cancer
AU2018300980A1 (en) 2017-07-12 2020-01-02 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
US11344543B2 (en) * 2017-07-14 2022-05-31 Innate Tumor Immunity, Inc. NLRP3 modulators
EP3654952A1 (fr) 2017-07-19 2020-05-27 Ignyta, Inc. Compositions pharmaceutiques contenant de l'entrectinib
US10180422B1 (en) 2017-08-22 2019-01-15 Scripps Health Methods of treating a neuroendocrine tumor
KR20200047627A (ko) * 2017-08-31 2020-05-07 애브비 인코포레이티드 엑토뉴클레오티드 피로포스파타아제-포스포디에스테라아제 1(enpp-1) 저해제 및 그의 용도
WO2019049956A1 (fr) 2017-09-08 2019-03-14 大鵬薬品工業株式会社 Agent antitumoral et potentialisateur d'effet antitumoral
JP7311498B2 (ja) 2017-10-17 2023-07-19 イグナイタ インコーポレイテッド 薬学的組成物および剤形
ES3064093T3 (en) * 2017-10-20 2026-04-22 Univ Vanderbilt Antagonists of the muscarinic acetylcholine receptor m4
AU2018360581A1 (en) 2017-10-31 2020-06-11 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
CN109824587A (zh) * 2017-11-23 2019-05-31 上海翔锦生物科技有限公司 酪氨酸激酶抑制剂xjf007及其中间体的制备方法
CN109896997A (zh) * 2017-12-08 2019-06-18 中国药科大学 N－酰基苯胺类c－Met激酶抑制剂的制备方法及其用途
CA3086522A1 (fr) 2017-12-20 2019-06-27 Angex Pharmaceutical, Inc. Composes de carbamate et d'uree utilises comme inhibiteurs de multikinases
US20190262330A1 (en) * 2017-12-21 2019-08-29 Exelixis, Inc. Method of Treating Hepatocellular Carcinoma Using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate
GEAP202415420A (en) * 2018-01-26 2024-12-25 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
CN111936487B (zh) * 2018-01-26 2024-07-09 埃克塞里艾克西斯公司 用于治疗激酶依赖性病症的化合物
IL276028B2 (en) * 2018-01-26 2025-02-01 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
US11414406B2 (en) 2018-02-02 2022-08-16 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
CN108264482A (zh) * 2018-02-05 2018-07-10 南京法恩化学有限公司 一种卡博替尼的制备方法
KR102433023B1 (ko) 2018-02-11 2022-08-16 베이징 사이텍-엠큐 파마슈티컬즈 리미티드 디옥시노퀴놀린 화합물, 이의 제조방법 및 용도
WO2019180141A1 (fr) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinaisons de rogaratinib
US11498902B2 (en) 2018-06-05 2022-11-15 Natco Pharma Limited Process for the preparation of Cabozantinib and its pharmaceutically acceptable salts thereof
CN120305263A (zh) 2018-06-15 2025-07-15 汉达癌症医药责任有限公司 卡博替尼的盐类于制备治疗癌症的剂型的用途
SG11202101060WA (en) * 2018-08-01 2021-02-25 Agency Science Tech & Res Bicyclic compounds as kinase modulators, methods and uses thereof
WO2020042972A1 (fr) * 2018-08-27 2020-03-05 北京赛特明强医药科技有限公司 Composé de dioxane et de quinazoline ou de quinoléine lié à un cycle aromatique substitué par urée, composition et utilisation associée
WO2020075196A1 (fr) 2018-10-11 2020-04-16 Cipla Limited Polymorphes de n-(4-(6,7-diméthoxyquinolin-4-yloxy) phényl)-n'-(4-fluorophényl)cyclopropane-1, 1-dicarboxamide, (s)-malate, leurs procédés de production et leurs utilisations pharmaceutiques
CN111303024B (zh) * 2018-12-12 2023-03-28 安徽中科拓苒药物科学研究有限公司 一种喹啉结构的pan-KIT激酶抑制剂及其用途
EP4631505A3 (fr) * 2018-12-13 2025-12-10 Exelixis, Inc. Formes cristallines et formes salines d'un inhibiteur de kinase
CA3124330A1 (fr) 2018-12-21 2020-06-25 Daiichi Sankyo Company, Limited Combinaison d'un conjugue anticorps-medicament et d'un inhibiteur de kinase
CA3126721A1 (fr) * 2019-01-25 2020-07-30 Exelixis, Inc. Composes pour le traitement de troubles dependant de la kinase
CN109776432B (zh) * 2019-03-21 2020-07-24 广州六顺生物科技股份有限公司 一种多靶点激酶抑制剂、药物组合物及多靶点激酶抑制剂的制备方法和应用
KR102913995B1 (ko) * 2019-04-12 2026-01-16 내셔날 헬스 리서치 인스티튜트 치료 용도를 위한 키나제 억제제로서의 헤테로사이클릭 화합물
CN111825609A (zh) * 2019-04-22 2020-10-27 北京康辰药业股份有限公司 化合物晶型、其制备方法、药物组合物以及应用
SG11202111978VA (en) * 2019-06-03 2021-11-29 Exelixis Inc Crystalline salt forms of a kinase inhibitor
AR119069A1 (es) 2019-06-04 2021-11-24 Exelixis Inc Compuestos para el tratamiento de trastornos dependientes de quinasas
CN110117254B (zh) * 2019-06-20 2022-05-13 江苏君若药业有限公司 卡博替尼的制备方法
CN112390749B (zh) * 2019-08-19 2024-12-03 鲁南制药集团股份有限公司 一种卡博替尼及其中间体的合成方法
CN112778217B (zh) * 2019-11-08 2024-01-26 沈阳化工研究院有限公司 一种喹唑啉类化合物及其应用
CN111393363B (zh) * 2020-04-27 2022-12-20 威海海洋生物医药产业技术研究院有限公司 4-苯氧基喹啉并n-磺酰脒类化合物及其制备方法和用途
CN113577066B (zh) * 2020-04-30 2022-12-16 中国科学院上海药物研究所 芳基胍化合物或其药学上可接受的盐的用途
IT202000027678A1 (it) 2020-11-18 2022-05-18 Indena Spa Dispersioni solide amorfe di cabozantinib-(s)-malato e processi per la loro preparazione
CA3202761A1 (fr) 2020-11-25 2022-06-02 Nanocopoeia, Llc Particules de cabozantinib amorphes et utilisations associees
EP4263535A1 (fr) * 2020-12-17 2023-10-25 Astrazeneca AB N-(2-(4-cyanothiazolidin-3-yl)-2-oxoéthyl)-quinoléine-4-carboxamides
KR20240006021A (ko) * 2021-03-24 2024-01-12 바이오콘 리미티드 카보잔티닙의 제조방법
KR20240115979A (ko) 2021-11-08 2024-07-26 프로젠토스 테라퓨틱스, 인크. 혈소판-유래 성장 인자 수용체(pdgfr) 알파 억제제 및 이의 용도
CN118339144A (zh) * 2021-12-03 2024-07-12 湖南湘源美东医药科技有限公司 卡博替尼共晶及制备方法以及作为药物或在药物制剂中的应用
CN114605391B (zh) * 2022-02-21 2024-01-26 广州六顺生物科技股份有限公司 喹喔啉类衍生物及其制备方法和应用
WO2023165948A1 (fr) 2022-03-01 2023-09-07 Synthon B.V. Sel de cabozantinib à l'acide l (+) tartrique et ses formes solides
WO2023222946A1 (fr) 2022-05-18 2023-11-23 Fermion Oy Procédé de préparation de cabozantinib
JP2025517908A (ja) 2022-05-24 2025-06-12 第一三共株式会社 抗ｃｄｈ６抗体－薬物コンジュゲートの投薬量レジメン
EP4551226A1 (fr) 2022-07-08 2025-05-14 Astrazeneca AB Inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique en combinaison avec des inhibiteurs du récepteur hgf pour le traitement du cancer
EP4622961A1 (fr) 2022-11-25 2025-10-01 Synthon B.V. Procédé de préparation de cabozantinib ou de tivozanib
WO2024114710A1 (fr) * 2022-12-01 2024-06-06 江苏奥赛康药业有限公司 Procédé de préparation de cabozantinib et d'un intermédiaire de celui-ci
AU2024215796A1 (en) 2023-01-31 2025-05-15 Handa Oncology, Llc Improved cabozantinib compositions and methods of use
CN116751161A (zh) * 2023-06-28 2023-09-15 中国人民解放军军事科学院军事医学研究院 喹啉类化合物及其制备方法、药物组合物及医药用途
IL316197A (en) * 2023-10-17 2025-05-01 Great Novel Therapeutics Biotech & Medicals Corp Tyrosine kinase inhibitors and their uses
CN117843713A (zh) * 2023-12-18 2024-04-09 上海亲合力生物医药科技股份有限公司 基于肿瘤微环境激活的激酶抑制剂、组合物及应用
WO2025253311A1 (fr) 2024-06-04 2025-12-11 Hetero Labs Limited Composés 1,2-dicarboxamide utilisés en tant qu'inhibiteurs de kinase
WO2026074526A1 (fr) 2024-10-04 2026-04-09 Hetero Labs Limited Composés 1,2-dicarboxamide utilisés en tant qu'inhibiteurs de kinase

Family Cites Families (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US506181A (en) 1893-10-03 Folding crate
GB2160201B (en) * 1984-06-14 1988-05-11 Wyeth John & Brother Ltd Quinazoline and cinnoline derivatives
US5123951A (en) * 1986-03-31 1992-06-23 Rhone-Poulenc Nederland B.V. Synergistic plant growth regulator compositions
JPS646261A (en) * 1987-03-31 1989-01-10 Nisshin Flour Milling Co 4-thioquinazoline derivative, its production and antiulcer agent containing said derivative as active component
US5143854A (en) * 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5034393A (en) * 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5238951A (en) 1991-02-01 1993-08-24 E. R. Squibb & Sons, Inc. Heterocyclic amido prostaglandin analogs
DE4114733A1 (de) * 1991-05-06 1992-11-12 Huels Chemische Werke Ag Verfahren zur herstellung von substituierten malonesteraniliden und malonsaeure-monoaniliden
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5358941A (en) 1992-12-02 1994-10-25 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids with lactose
US6498144B1 (en) 1993-10-18 2002-12-24 North Shore - Long Island Jewish Research Institute Use of scatter factor to enhance angiogenesis
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
GB9510757D0 (en) 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
TW321649B (fr) 1994-11-12 1997-12-01 Zeneca Ltd
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
DE69618587T2 (de) 1995-06-07 2002-08-29 Sugen, Inc. Chinazoline und pharmazeutische zusammensetzungen
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
NZ311000A (en) 1995-06-07 1999-04-29 Smithkline Beecham Biolog Vaccine comprising a polysaccharide antigen-carrier protein conjugate and a free carrier protein
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
WO1997017329A1 (fr) * 1995-11-07 1997-05-15 Kirin Beer Kabushiki Kaisha Derives de quinoline et derives de quinazoline inhibant l'autophosphorylation d'un recepteur de facteur de croissance originaire de plaquettes, et compositions pharmaceutiques les contenant
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
NZ325248A (en) 1995-12-23 1999-09-29 Pfizer Res & Dev Quinoline and quinazoline compounds useful in therapy
WO1997030035A1 (fr) 1996-02-13 1997-08-21 Zeneca Limited Derives de la quinazoline utilises comme inhibiteurs du vegf
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
ES2169355T3 (es) 1996-03-05 2002-07-01 Astrazeneca Ab Derivados de 4-anilinoquinazolina.
JP2000506880A (ja) 1996-03-15 2000-06-06 ゼネカ・リミテッド シンノリン誘導体及びその使用
US6107300A (en) 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
JP3370340B2 (ja) 1996-04-12 2003-01-27 ワーナー―ランバート・コンパニー チロシンキナーゼの不可逆的阻害剤
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
DE69716916T2 (de) 1996-07-13 2003-07-03 Glaxo Group Ltd., Greenford Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
AU733551B2 (en) 1996-09-25 2001-05-17 Astrazeneca Ab Qinoline derivatives inhibiting the effect of growth factors such as VEGF
CA2239227C (fr) 1996-10-01 2007-10-30 Kyowa Hakko Kirin Co., Ltd. Composes heterocycliques azotes
GB9700504D0 (en) 1997-01-11 1997-02-26 Pfizer Ltd Pharmaceutical compounds
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
DE69816080T2 (de) 1997-04-18 2004-04-15 Kirin Beer K.K. Verfahren zur herstellung von chinolinderivaten
ES2207834T3 (es) 1997-04-22 2004-06-01 Janssen Pharmaceutica N.V. Quino- y quinazolinas antagonistas del crf.
GB9708917D0 (en) 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
ATE368665T1 (de) 1997-08-22 2007-08-15 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
JP4194678B2 (ja) * 1997-11-28 2008-12-10 キリンファーマ株式会社 キノリン誘導体およびそれを含む医薬組成物
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
AU4317399A (en) 1998-05-28 1999-12-13 Parker Hughes Institute Quinazolines for treating brain tumor
EP1107964B8 (fr) 1998-08-11 2010-04-07 Novartis AG Derives d'isoquinoline possedant une activite d'inhibition de l'angiogenese
EP1105378B1 (fr) 1998-08-21 2005-03-30 Parker Hughes Institute Derives de quinazoline
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
CA2343284C (fr) 1998-09-10 2008-11-18 Ipr-Institute For Pharmaceutical Research Ag Produits pour l'application locale
US6288082B1 (en) * 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
HUP0103520A3 (en) 1998-09-29 2003-01-28 Wyeth Holdings Corp Madison Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors and pharmaceutical compositions containing them
DK1117653T3 (da) 1998-10-01 2003-05-26 Astrazeneca Ab Quinolin- og quinazolinderivater og deres anvendelse som inhibitorer af cykokin-merierede sygdomme
EP1119567B1 (fr) 1998-10-08 2005-05-04 AstraZeneca AB Derives de quinazoline
ES2188254T3 (es) 1998-11-19 2003-06-16 Warner Lambert Co N-(4-(3-chloro-4-fluoro-fenilamino)-7-(3-morfolin-4-il-propoxi)-quin azolin-6-il)-acrilamada, un inhibidor irreversible de tirosina quinasas.
CA2361057C (fr) * 1999-01-22 2010-04-06 Kazuo Kubo Derives de quinoline et derives de quinazoline
BRPI0017548B8 (pt) 1999-02-10 2023-05-02 Astrazeneca Ab Composto
GB9904103D0 (en) 1999-02-24 1999-04-14 Zeneca Ltd Quinoline derivatives
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6258820B1 (en) 1999-03-19 2001-07-10 Parker Hughes Institute Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
AU3630100A (en) 1999-03-19 2000-10-09 Parker Hughes Institute Quinazoline formulations and therapeutic use thereof
RS49836B (sr) 1999-03-31 2008-08-07 Pfizer Products Inc., Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
GB9910580D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
US6126917A (en) 1999-06-01 2000-10-03 Hadasit Medical Research Services And Development Ltd. Epidermal growth factor receptor binding compounds for positron emission tomography
YU90901A (sh) 1999-06-21 2004-07-15 Boehringer Ingelheim Pharma Gmbh. & Co.Kg. Biciklični heterocikli, lekovi koji sadrže ta jedinjenja, njihova primena i postupci za njihovo pripremanje
GB9922171D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
SK3822002A3 (en) * 1999-09-21 2002-10-08 Astrazeneca Ab Quinazoline derivatives, process for the preparation thereof and their use
US6759410B1 (en) 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
WO2001045641A2 (fr) 1999-11-30 2001-06-28 Parker Hughes Institute Inhibiteurs d'agregation de plaquettes induite par thrombine
US20020002169A1 (en) 1999-12-08 2002-01-03 Griffin John H. Protein kinase inhibitors
US7135466B2 (en) * 1999-12-24 2006-11-14 Kirin Beer Kabushiki Kaisha Quinoline and quinazoline derivatives and drugs containing the same
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
JP2003520855A (ja) * 2000-01-28 2003-07-08 アストラゼネカ アクチボラグ 化学的化合物
US6664390B2 (en) 2000-02-02 2003-12-16 Warner-Lambert Company Llc Method for the simplified production of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazoline-4-yl]-amine or (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazoline-4-yl]-amine
WO2001057008A1 (fr) 2000-02-07 2001-08-09 Abbott Gesellschaft Mit Beschrankter Haftung & Company Kommanditgesellschaft Derives de 2-benzothiazolyle uree et leur utilisation en tant qu'inhibiteurs de proteine kinase
IL151249A0 (en) 2000-03-13 2003-04-10 American Cyanamid Co Use of cyanoquinolines for treating or inhibiting colonic polyps
US6608048B2 (en) 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
US6521618B2 (en) 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
US6627634B2 (en) 2000-04-08 2003-09-30 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
NZ522568A (en) 2000-06-22 2004-12-24 Pfizer Prod Inc Substituted bicyclic derivatives for the treatment of abnormal cell growth
EP1174118A1 (fr) 2000-06-28 2002-01-23 Cognis France S.A. Utilisation de l'inuline et de dérivés de celui-ci
NZ522696A (en) 2000-06-28 2004-08-27 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
FR2811658B1 (fr) 2000-07-17 2004-07-02 Cfpi Nufarm Reacteur biologique a lit fixe immerge et procede de traitement d'effluents liquides
JP2002030083A (ja) * 2000-07-18 2002-01-29 Kirin Brewery Co Ltd Ｎ−（２−クロロ−４−｛［６−メトキシ−７−（３−ピリジルメトキシ）−４−キノリル］オキシ｝フェニル）−ｎ’−プロピルウレアの二塩酸塩
CA2417500C (fr) * 2000-07-28 2008-11-18 Georgetown University Medical Center Inhibiteur de l'erbb-2 kinase selectif de petites molecules
US7115615B2 (en) 2000-08-21 2006-10-03 Astrazeneca Quinazoline derivatives
US6740651B2 (en) 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6653305B2 (en) 2000-08-26 2003-11-25 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
DE10042058A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6617329B2 (en) 2000-08-26 2003-09-09 Boehringer Ingelheim Pharma Kg Aminoquinazolines and their use as medicaments
US6403580B1 (en) 2000-08-26 2002-06-11 Boehringer Ingelheim Pharma Kg Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them
US6656946B2 (en) 2000-08-26 2003-12-02 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
AU2001292137A1 (en) 2000-10-13 2002-04-22 Astrazeneca Ab Quinazoline derivatives
AU2001292138A1 (en) 2000-10-13 2002-04-22 Astrazeneca Ab Quinazoline derivatives with anti-tumour activity
EP1415987B1 (fr) * 2000-10-20 2007-02-28 Eisai R&D Management Co., Ltd. Composes heteroaromatiques azotes pour le traitement des maladies de cancer
US20040063733A1 (en) 2000-10-25 2004-04-01 Lambert Christine Marie Paul Quinazoline derivatives
AU2002210714A1 (en) 2000-11-02 2002-06-11 Astrazeneca Ab Substituted quinolines as antitumor agents
AU2001295791A1 (en) 2000-11-02 2002-05-15 Astrazeneca Ab 4-substituted quinolines as antitumor agents
JPWO2002036577A1 (ja) 2000-11-02 2004-03-11 日本新薬株式会社 キナゾリン誘導体及び医薬
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
US6900220B2 (en) 2001-01-02 2005-05-31 Syntex (U.S.A.) Llc Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists
WO2002085895A1 (fr) 2001-04-19 2002-10-31 Astrazeneca Ab Derives quinazoline
DE60208364T2 (de) 2001-04-27 2006-09-28 Kirin Beer K.K. Chinolinderivate mit einer azolylgruppe und chinazolinderivate
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
WO2002092577A1 (fr) 2001-05-14 2002-11-21 Astrazeneca Ab Derives quinazoliniques
WO2002092578A1 (fr) 2001-05-14 2002-11-21 Astrazeneca Ab Derives de quinazoline
WO2002092579A1 (fr) 2001-05-14 2002-11-21 Astrazeneca Ab Derives de 4-anilinoquinazoline
US6734303B2 (en) 2001-05-18 2004-05-11 Pfizer Inc. Process for the production of quinazolines
DE10125432A1 (de) * 2001-05-25 2002-11-28 Bayer Ag Substituierte Benzoylketone
WO2003000188A2 (fr) 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Nouvelles quinazolines et leur utilisation
CA2454538A1 (fr) * 2001-06-22 2003-01-03 Kirin Beer Kabushiki Kaisha Derives de la quinoleine et de la quinozoline pouvant inhiber l'auto- phosphorylation des recepteurs du facteur de croissance des hepatocytes, et composition pharmaceutique ainsi constituee
KR100397792B1 (ko) 2001-06-28 2003-09-13 한국과학기술연구원 4-(페닐아미노)-[1,4]디옥사노[2,3-ｇ]퀴나졸린 유도체 및그의 제조방법
GB0118752D0 (en) 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
US7229774B2 (en) 2001-08-02 2007-06-12 Regents Of The University Of Michigan Expression profile of prostate cancer
US20030066060A1 (en) 2001-09-28 2003-04-03 Ford Richard L. Cross profile guided optimization of program execution
WO2003033472A1 (fr) * 2001-10-17 2003-04-24 Kirin Beer Kabushiki Kaisha Derives de quinoline ou de quinazoline inhibant l'autophosphorylation de recepteurs du facteur de croissance des fibroblastes
US7169788B2 (en) 2001-10-30 2007-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0126433D0 (en) 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
GB0128108D0 (en) 2001-11-23 2002-01-16 Astrazeneca Ab Therapeutic use
IL161921A0 (en) 2001-11-27 2005-11-20 Wyeth Corp 3-Cyanoquinolines as inhibitors of egf-r and her2 kinases
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
WO2003047584A1 (fr) 2001-12-05 2003-06-12 Astrazeneca Ab Derives de la quinoline
WO2003048159A1 (fr) 2001-12-05 2003-06-12 Astrazeneca Ab Derives de la quinoleine
IL161908A0 (en) 2001-12-12 2005-11-20 Pfizer Prod Inc Quinazoline derivatives for the treatment of abnormal cell growth
AP2004003059A0 (en) 2001-12-12 2004-06-30 Pfizer Prod Inc Salt forms of E-2-methoxy-N-(3-(4-(3-methyl-pyridin-3-yloxyl)-phenylamino)-quinazolin-6-yl)-allyl)-acetamide, its preparation and its use against cancer
WO2003055866A1 (fr) 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation Composes derives de quinazoline et de quinoline servant d'inhibiteurs de prolylpeptidase, d'inducteurs d'apoptose et d'agents therapeutiques anticancereux
TW200301123A (en) 2001-12-21 2003-07-01 Astrazeneca Uk Ltd New use
KR101029281B1 (ko) 2001-12-24 2011-04-18 아스트라제네카 아베 오로라 키나제의 억제제로서 치환된 퀴나졸린 유도체
US7312212B2 (en) 2002-01-29 2007-12-25 Glaxo Group Limited Aminopiperidine derivatives
WO2003064431A2 (fr) 2002-01-29 2003-08-07 Glaxo Group Limited Composes aminopiperidine, leur procede de preparation et compositions pharmaceutiques les contenant
CN1625555A (zh) 2002-02-01 2005-06-08 阿斯特拉曾尼卡有限公司 喹唑啉化合物
DE10204462A1 (de) 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
WO2003074497A1 (fr) * 2002-03-01 2003-09-12 Pintex Pharmaceutical, Inc. Composes de modulation de pin1 et methodes d'utilisation associees
DE10217689A1 (de) 2002-04-19 2003-11-13 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
US7598258B2 (en) * 2002-05-01 2009-10-06 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor
ES2400339T3 (es) 2002-07-15 2013-04-09 Symphony Evolution, Inc. Compuestos, composiciones farmacéuticas de los mismos y su uso en el tratamiento del cáncer
CN1688549A (zh) * 2002-08-23 2005-10-26 麒麟麦酒株式会社 具有TGFβ抑制活性的化合物和含所述化合物的药用组合物
GB0219746D0 (en) 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
JP3763414B2 (ja) 2002-10-21 2006-04-05 麒麟麦酒株式会社 Ｎ−｛２−クロロ−４−［（６，７−ジメトキシ−４−キノリル）オキシ］フェニル｝−ｎ’−（５−メチル−３−イソキサゾリル）ウレアの塩の結晶形
EP1566379A4 (fr) * 2002-10-29 2005-11-09 Kirin Brewery DERIVES DE QUINOLINE ET DE QUINAZOLINE INHIBANT L'AUTOPHOSPHORYLATION DE Flt3 ET COMPOSITIONS MEDICALES LES CONTENANT
US7462623B2 (en) 2002-11-04 2008-12-09 Astrazeneca Ab Quinazoline derivatives as Src tyrosine kinase inhibitors
WO2004055003A1 (fr) 2002-12-13 2004-07-01 Neurogen Corporation Analogues de quinazolin-4-ylamine 2-substituee comme modulateurs des recepteurs de la capsicine
EP1575592A1 (fr) 2002-12-18 2005-09-21 Pfizer Products Inc. Dérivés de 4-anilino quinazoline permettant de traiter une croissance cellulaire anormale
AU2003299943A1 (en) 2002-12-23 2004-07-22 Ariad Pharmaceuticals, Inc. Heterocycles and uses thereof
WO2004060373A1 (fr) * 2002-12-27 2004-07-22 Santen Pharmaceutical Co., Ltd. Agent therapeutique pour la degenerescence maculaire humide liee a l'age
US8176532B1 (en) * 2003-03-17 2012-05-08 Sprint Communications Company L.P. Secure access point for scada devices
KR100559180B1 (ko) * 2003-05-20 2006-03-14 김민서 조건부 거래에 따른 전자결제 방법 및 전자결제 서버
WO2005003140A1 (fr) 2003-07-02 2005-01-13 Pharmacia & Upjohn Company Llc 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxamides utilises comme agents antiviraux
US20070213374A1 (en) 2003-07-07 2007-09-13 Merck Patent Gmbh Malonamide Derivatives
CA2744997A1 (fr) * 2003-09-26 2005-04-07 Exelixis, Inc. Modulateurs de c-met et procede d'utilisation
CA2553433A1 (fr) 2004-01-23 2005-08-11 Amgen Inc. Composes de quinoleine, de quinazoline, de pyridine et de pyrimidine et utilisations connexes pour traiter l'inflammation, l'angiogenese et le cancer
US20050288290A1 (en) * 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
WO2006014325A2 (fr) * 2004-07-02 2006-02-09 Exelixis, Inc. Modulateurs de c-met et leur methode d'utilisation
JP2008537748A (ja) * 2005-04-06 2008-09-25 エクセリクシス、インコーポレイテッド ｃ−Ｍｅｔモジュレーター及び使用方法
US7594258B2 (en) * 2005-06-27 2009-09-22 Yahoo! Inc. Access control systems and methods using visibility tokens with automatic propagation
US20080004273A1 (en) * 2006-05-30 2008-01-03 Stephane Raeppel Inhibitors of protein tyrosine kinase activity
US20110229469A1 (en) 2008-10-01 2011-09-22 Ludwig Institute For Cancer Research Methods for the treatment of cancer
EP2367795A1 (fr) 2008-12-04 2011-09-28 Exelixis, Inc. Procédés de préparation de dérivés de quinoléine
EA038195B1 (ru) 2009-01-16 2021-07-22 Экселиксис, Инк. Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее применение для лечения рака почек и печени
EP2454238A1 (fr) 2009-07-17 2012-05-23 Exelixis, Inc. Formes cristallines du n [3 fluoro-4-({méthyloxy)-7-[(3-morpholin-4-yl- propyl)oxy]quinoléin-4-yl}oxy)phényl]-n'-(4-fluorophényl)cyclopropane- 1,1-dicarboxamide
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
EP2475390A4 (fr) 2009-09-09 2014-01-01 Quintiles Transnat Corp Méthodes et compositions pour le traitement de maladies ou troubles à médiation par le récepteur tyrosine kinase
JP5461213B2 (ja) 2010-01-29 2014-04-02 三洋電機株式会社 空気調和装置の室外ユニット
US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer

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