DE60325209D1 - Diarylharnstoffderivate, die sich zur behandlung von proteinkinaseabhängigen krankheiten eignen - Google Patents

Diarylharnstoffderivate, die sich zur behandlung von proteinkinaseabhängigen krankheiten eignen

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Publication number
DE60325209D1
DE60325209D1 DE60325209T DE60325209T DE60325209D1 DE 60325209 D1 DE60325209 D1 DE 60325209D1 DE 60325209 T DE60325209 T DE 60325209T DE 60325209 T DE60325209 T DE 60325209T DE 60325209 D1 DE60325209 D1 DE 60325209D1
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Germany
Prior art keywords
diarylute
treatment
protein kinase
dependent diseases
derivatives suitable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
DE60325209T
Other languages
English (en)
Inventor
Andreas Floersheimer
Pascal Furet
Paul William Manley
Guido Bold
Eugen Boss
Vito Guagnano
Andrea Vaupel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis Pharma GmbH
Novartis AG
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Filing date
Publication date
Priority claimed from GB0212413A external-priority patent/GB0212413D0/en
Priority claimed from GB0305684A external-priority patent/GB0305684D0/en
Application filed by Novartis Pharma GmbH, Novartis AG filed Critical Novartis Pharma GmbH
Application granted granted Critical
Publication of DE60325209D1 publication Critical patent/DE60325209D1/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Families Citing this family (261)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2725000A (en) 1999-01-13 2000-08-01 Bayer Corporation Omega-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
MXPA04007832A (es) 2002-02-11 2005-09-08 Bayer Pharmaceuticals Corp Aril-ureas con actividad inhibitoria de angiogenesis.
AU2003209119A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
NZ537952A (en) * 2002-08-08 2008-04-30 Amgen Inc Vanilloid receptor ligands and their use in treatments
MXPA05009102A (es) * 2003-02-28 2006-05-31 Bayer Pharmaceuticals Corp Derivados de piridina sustituida utiles en el tratamiento del cancer y otros trastornos.
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
WO2004113274A2 (en) 2003-05-20 2004-12-29 Bayer Pharmaceuticals Corporation Diaryl ureas with kinase inhibiting activity
PL1663978T3 (pl) 2003-07-23 2008-04-30 Bayer Healthcare Llc Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów
DE10334663A1 (de) * 2003-07-30 2005-03-10 Merck Patent Gmbh Harnstoffderivate
ES2388138T3 (es) 2003-08-27 2012-10-09 Ophthotech Corporation Terapia de combinación para tratamiento de trastornos neovasculares oculares
US7767670B2 (en) 2003-11-13 2010-08-03 Ambit Biosciences Corporation Substituted 3-carboxamido isoxazoles as kinase modulators
JP2007515400A (ja) * 2003-11-28 2007-06-14 ノバルティス アクチエンゲゼルシャフト タンパク質キナーゼ依存性疾患の処置におけるジアリール尿素誘導体
AU2005206571B8 (en) * 2004-01-23 2010-09-02 Amgen Inc. Compounds and methods of use
AU2005211448A1 (en) * 2004-01-30 2005-08-18 Merck Patent Gmbh Bisarylurea derivatives
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
PL1765327T3 (pl) 2004-06-17 2015-01-30 Cytokinetics Inc Związki, kompozycje i sposoby
AU2011253934C1 (en) * 2004-06-17 2013-08-22 Cytokinetics, Inc. Substituted urea derivatives for treating cardiac diseases
GB0512324D0 (en) * 2005-06-16 2005-07-27 Novartis Ag Organic compounds
PE20060664A1 (es) * 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
GB0421525D0 (en) * 2004-09-28 2004-10-27 Novartis Ag Inhibitors of protein kineses
ATE540935T1 (de) 2004-10-12 2012-01-15 Astrazeneca Ab Chinazolinderivate
KR20070062998A (ko) * 2004-10-13 2007-06-18 메르크 파텐트 게엠베하 키나제 억제제로서의 복소환 치환된 비스아릴우레아 유도체
CA2586605A1 (en) * 2004-11-24 2006-06-01 Novartis Ag Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
US7968574B2 (en) 2004-12-28 2011-06-28 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
DK1836169T5 (da) 2004-12-28 2023-10-09 Atnx Spv Llc Sammensætninger og fremgangsmåder til behandling af celleproliferationslidelser
WO2006076592A1 (en) 2005-01-14 2006-07-20 Cgi Pharmaceuticals, Inc. 1,3 substituted diaryl ureas as modulators of kinase activity
US7777040B2 (en) 2005-05-03 2010-08-17 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
BRPI0608604B8 (pt) 2005-05-10 2021-05-25 Incyte Corp moduladores de 2,3-dioxigenase de indolamina e composição farmacêutica
GT200600207A (es) * 2005-06-09 2007-01-15 Novartis Ag Proceso para la síntesis de compuestos orgánicos
MY146795A (en) * 2005-06-09 2012-09-28 Novartis Ag Process for the synthesis of organic compounds
US8071768B2 (en) 2005-06-10 2011-12-06 Janssen Pharmaceutica, N.V. Alkylquinoline and alkylquinazoline kinase modulators
US7825244B2 (en) 2005-06-10 2010-11-02 Janssen Pharmaceutica Nv Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
US20060281788A1 (en) 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
EP1889836B1 (de) * 2005-08-24 2013-06-12 Eisai R&D Management Co., Ltd. Neues pyridinderivat und pyrimidinderivat (3)
GT200600411A (es) 2005-09-13 2007-05-21 Novartis Ag Combinaciones que comprenden un inhibidor del receptor del factor de crecimiento endotelial vascular
EP2270014A1 (de) 2005-09-22 2011-01-05 Incyte Corporation Azepinhemmer von Janus-Kinasen
CA2626623C (en) 2005-10-18 2016-08-30 Janssen Pharmaceutica N.V. Method of inhibiting flt3 kinase
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
GB2431927B (en) 2005-11-04 2010-03-17 Amira Pharmaceuticals Inc 5-Lipoxygenase-activating protein (FLAP) inhibitors
US8399666B2 (en) 2005-11-04 2013-03-19 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
BRPI0619817B8 (pt) 2005-12-13 2021-05-25 Incyte Corp composto 3-ciclopentil-3-[4-(7h-pirrol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]propanonitrila e sua composição
CA2633411A1 (en) * 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating inflammatory skin, eye and/or ear diseases
TW200808321A (en) 2005-12-15 2008-02-16 Cytokinetics Inc Certain chemical entities, compositions and methods
CN101336237B (zh) 2005-12-21 2015-09-30 诺华股份有限公司 作为fgf抑制剂的嘧啶基芳基脲衍生物
US20070155746A1 (en) * 2005-12-23 2007-07-05 Kalypsys, Inc. Novel substituted pyridinyloxy and pyrimidinyloxy amides useful as inhibitors of protein kinases
TW200804349A (en) * 2005-12-23 2008-01-16 Kalypsys Inc Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases
UY30183A1 (es) 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
GB0605120D0 (en) 2006-03-14 2006-04-26 Novartis Ag Organic Compounds
AU2007235900A1 (en) 2006-04-07 2007-10-18 Novartis Ag Combination comprising a) a pyrimidylaminobenzamide compound, and b) a Thr315lle kinase inhibitor
ATE510832T1 (de) 2006-04-20 2011-06-15 Janssen Pharmaceutica Nv Heterocyclische verbindungen als c-fms- kinasehemmer
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
UA93085C2 (en) 2006-04-20 2011-01-10 Янссен Фармацевтика Н.В. Inhibitors of c-fms kinase
JP5564251B2 (ja) * 2006-06-29 2014-07-30 キネックス ファーマシューティカルズ， エルエルシー キナーゼカスケードを調節するためのビアリール組成物および方法
EP2062886B1 (de) 2006-08-23 2011-11-30 Eisai R&D Management Co., Ltd. Salz eines phenoxypyridinderivats oder kristall davon und verfahren zu dessen herstellung
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
US8080552B2 (en) * 2006-12-22 2011-12-20 Hoffmann-La Roche Inc. Pyrimidyl derivatives as protein kinase inhibitors
US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
US7935697B2 (en) 2006-12-28 2011-05-03 Kinex Pharmaceuticals, Llc Compositions for modulating a kinase cascade and methods of use thereof
DK2154967T5 (en) 2007-04-16 2014-11-17 Hutchison Medipharma Entpr Ltd Pyriminderivater
KR20100016584A (ko) 2007-04-17 2010-02-12 노파르티스 아게 암 치료제로서의 나프탈렌 카르복실산 아미드의 에테르
CN101878031A (zh) * 2007-04-20 2010-11-03 迪赛孚尔制药有限公司 用于治疗骨髓增生性疾病和其他增生性疾病的激酶抑制剂
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
MX2009013402A (es) 2007-06-13 2010-02-24 Incyte Corp Sales de inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3-d]piri midin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
US8124605B2 (en) 2007-07-06 2012-02-28 Kinex Pharmaceuticals, Llc Compositions and methods for modulating a kinase cascade
JO3240B1 (ar) 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
TWI552752B (zh) * 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
EP2220068B1 (de) 2007-11-16 2016-01-27 Incyte Holdings Corporation 4-pyrazolyl-n-arylpyrimidin-2-amine und 4-pyrazolyl-n-heteroarylpyrimidin-2-amine als janus-kinase-inhibitoren
JP2009132660A (ja) * 2007-11-30 2009-06-18 Eisai R & D Management Co Ltd 食道癌治療用組成物
US20090227556A1 (en) * 2008-01-31 2009-09-10 Eisai R&D Management Co., Ltd. Receptor tyrosine kinase inhibitors comprising pyridine and pyrimidine derivatives
EP2248810A4 (de) * 2008-02-18 2011-05-25 Eisai R&D Man Co Ltd Verfahren zur herstellung eines phenoxypyridin-derivats
NZ587928A (en) 2008-03-11 2012-08-31 Incyte Corp Azetidine and cyclobutane derivatives as jak inhibitors
JP2011518836A (ja) 2008-04-24 2011-06-30 インサイト・コーポレイション 大環状化合物およびそれらのキナーゼ阻害剤としての使用
EP2285803A4 (de) 2008-05-23 2011-10-05 Amira Pharmaceuticals Inc Hemmer des 5-lipoxygenase aktivierenden proteins
PT2824100T (pt) 2008-07-08 2018-05-10 Incyte Holdings Corp 1,2,5-oxadiazoles como inibidores da indoleamina 2,3-dioxigenase
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JO3265B1 (ar) 2008-12-09 2018-09-16 Novartis Ag مثبطات بيريديلوكسى اندولات vegf-r2 واستخدامها لعلاج المرض
WO2010085597A1 (en) 2009-01-23 2010-07-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
US20120189641A1 (en) 2009-02-25 2012-07-26 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US8642834B2 (en) 2009-02-27 2014-02-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
JP2012519282A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
CN101671301B (zh) * 2009-05-05 2014-02-26 江苏省药物研究所有限公司 杂环取代的二苯脲类衍生物及其用途
EP2432472B1 (de) 2009-05-22 2019-10-02 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- oder heptannitril als jak-inhibitoren
BRPI1012159B1 (pt) 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
EP2440056A4 (de) * 2009-06-09 2012-12-05 California Capital Equity Llc Ureidophenylsubstituierte triazinderivate und deren therapeutische anwendungen
ME01838B (me) 2009-06-29 2014-12-20 Lncyte Holdings Corp Pirimidinoni kao inhibitori pi3k
US8933227B2 (en) * 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
WO2011018517A1 (en) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
WO2011025798A1 (en) * 2009-08-28 2011-03-03 Glaxosmithkline Llc Compounds and methods
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
ES2435491T3 (es) 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
CN101717373B (zh) * 2009-11-09 2012-06-20 东南大学 二芳基脲类衍生物及其用途
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
WO2011075630A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors
HUE045270T2 (hu) 2010-01-05 2019-12-30 Inst Nat Sante Rech Med FLT3 receptor anatgonisták fájdalom rendellenességek kezelésére
NZ601143A (en) 2010-01-12 2014-10-31 Ab Science Thiazole and oxazole kinase inhibitors
PL2531502T3 (pl) * 2010-02-01 2014-08-29 Cancer Research Tech Ltd 1-(5-tert-Butylo-2-fenylo-2H-pirazol-3-ilo)-3-[2-fluoro-4-(1-metylo-2-okso-2,3-dihydro-1H-imidazo[4,5-b]pirydyn-7-yloksy)-fenylo]-mocznik i związki pokrewne oraz ich zastosowanie w terapii
JP5858434B2 (ja) 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
MX2012010011A (es) * 2010-03-01 2012-10-05 Myrexis Inc Compuestos y usos terapeuticos de los mismos.
US8912184B1 (en) 2010-03-01 2014-12-16 Alzheimer's Institute Of America, Inc. Therapeutic and diagnostic methods
EP4036088B1 (de) 2010-03-10 2024-04-03 Incyte Holdings Corporation Piperidin-4-yl-azetidin-derivate als jak1-inhibitoren
AR081823A1 (es) 2010-04-14 2012-10-24 Incyte Corp DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd
EP2558085B1 (de) 2010-04-16 2017-08-30 Athenex, Inc. Zusammensetzungen und verfahren zur prävention und behandlung von krebs
EP3087972A1 (de) 2010-05-21 2016-11-02 Incyte Holdings Corporation Topische formulierung für einen jak-hemmer
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
WO2011162343A1 (ja) 2010-06-25 2011-12-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 キナーゼ阻害作用を有する化合物の併用による抗腫瘍剤
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
JP5917545B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としてのシクロブチル置換ピロロピリジンおよびピロロピリミジン誘導体
AR084366A1 (es) 2010-12-20 2013-05-08 Incyte Corp N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
EP2702173A1 (de) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Verwendung von emt-gensignaturen bei der entdeckung von krebswirkstoffen, -diagnostika und -behandlungen
AU2012273164B2 (en) 2011-06-20 2015-05-28 Incyte Holdings Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
EP2741747A1 (de) 2011-08-10 2014-06-18 Novartis Pharma AG Jak-/p13k-mtor-kombinationstherapie
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
EA033646B1 (ru) 2011-09-02 2019-11-13 Incyte Holdings Corp Гетероциклиламины как ингибиторы pi3k
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US8841301B2 (en) 2011-09-26 2014-09-23 Bristol-Myers Squibb Company Selective NR2B antagonists
US8722670B2 (en) 2011-09-30 2014-05-13 Bristol-Myers Squibb Company Selective NR2B antagonists
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP3822273B1 (de) 2012-06-13 2024-04-10 Incyte Holdings Corporation Substituierte tricyclische verbindungen als fgfr-inhibitoren
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
JP6359537B2 (ja) 2012-08-07 2018-07-18 ヤンセン ファーマシューティカ エヌ．ベー． 複素環エステル誘導体の調製プロセス
US20150225369A1 (en) * 2012-08-29 2015-08-13 Merck Patent Gmbh Ddr2 inhibitors for the treatment of osteoarthritis
WO2014036426A1 (en) 2012-08-30 2014-03-06 Kinex Pharmaceuticals, Llc N-(3-fluorobenzyl)-2-(5-(4-morpholinophenyl)pyridin-2-yl) acetamide as protein|tyrosine kinase modulators
JP6407504B2 (ja) 2012-09-21 2018-10-17 アログ・ファーマシューティカルズ・インコーポレイテッドＡｒｏｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 恒常的に活性であるリン酸化型ｆｌｔ３キナーゼの阻害方法
CN103664797A (zh) * 2012-09-25 2014-03-26 杨子娇 一类治疗房角狭窄的化合物及其用途
KR20150074193A (ko) 2012-11-01 2015-07-01 인사이트 코포레이션 Jak 억제제로서 트리사이클릭 융합된 티오펜 유도체
CN103804349A (zh) * 2012-11-01 2014-05-21 杨子娇 一类治疗青光眼的化合物及其用途
IL291391B (en) 2012-11-15 2022-11-01 Incyte Holdings Corp Sustained release dosage forms of roxolitinib
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
BR112015016282A2 (pt) 2013-01-07 2017-07-11 Arog Pharmaceuticals Inc crenolanibe para tratamento de distúrbios proliferativos de flt3 mutado
TWI736135B (zh) 2013-03-01 2021-08-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
PT2964650T (pt) 2013-03-06 2019-02-26 Incyte Holdings Corp Processos e intermediários para a preparação de um inibidor de jak
EP2981526B1 (de) 2013-04-02 2021-11-03 Oxular Acquisitions Limited Zwischenprodukte zur synthese von naphthyl-harnstoffderivate zur verwendung als kinasehemmer
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
JP6411379B2 (ja) 2013-05-14 2018-10-24 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する子宮内膜がん対象の応答性を予測及び評価するためのバイオマーカー
SI3527263T1 (sl) 2013-05-17 2021-05-31 Incyte Corporation Derivati bipirazola kot zaviralci JAK
MX2016001639A (es) 2013-08-07 2016-10-07 Incyte Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
AR097388A1 (es) 2013-08-20 2016-03-09 Incyte Corp Beneficio de supervivencia en pacientes con tumores sólidos con niveles elevados de proteína c reactiva
WO2015051149A1 (en) * 2013-10-04 2015-04-09 The Trustees Of Columbia University In The City Of New York Sorafenib analogs and uses thereof
US10463658B2 (en) 2013-10-25 2019-11-05 Videra Pharmaceuticals, Llc Method of inhibiting FLT3 kinase
CN106029651A (zh) * 2013-12-20 2016-10-12 瑞斯比维特有限公司 用作激酶抑制剂的脲衍生物
KR20160136323A (ko) 2014-02-28 2016-11-29 인사이트 코포레이션 골수형성이상증후군 치료용 jak1 억제제
LT3129021T (lt) 2014-04-08 2020-12-10 Incyte Corporation B ląstelių piktybiškumo gydymas jak ir pi3k inhibitorių deriniu
CN104974132B (zh) 2014-04-08 2017-05-17 北大方正集团有限公司 多取代的吡啶化合物、制备方法、用途及药物组合物
AU2015253192B2 (en) 2014-04-30 2019-05-16 Incyte Holdings Corporation Processes of preparing a JAK1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
CN107001283B (zh) 2014-07-31 2021-05-25 国家健康与医学研究院 Flt3受体拮抗剂
EP3825305A1 (de) 2014-08-28 2021-05-26 Eisai R&D Management Co., Ltd. Verfahren zur herstellung von lenvatinib
MX2017002610A (es) 2014-08-29 2017-10-11 Tes Pharma S R L INHIBIDORES DE ACIDO A-AMINO-ß-CARBOXIMUCONICO SEMIALDEHIDO DESCARBOXILASA.
CR20170094A (es) * 2014-09-10 2017-05-08 Glaxosmithkline Ip Dev Ltd Nuevos compuestos como inhibidores de reorganizado durante la transfección (ret)
CR20170093A (es) 2014-09-10 2017-07-17 Glaxosmithkline Ip Dev Ltd Nuevos compuestos como inhibidores de ret (reorganizado durante la transfección)
MA40774A (fr) * 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
PT3263106T (pt) 2015-02-25 2024-01-12 Eisai R&D Man Co Ltd Método para suprimir o amargor do derivado de quinolina
WO2016138363A1 (en) 2015-02-27 2016-09-01 Incyte Corporation Salts of pi3k inhibitor and processes for their preparation
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
US20160362424A1 (en) 2015-05-11 2016-12-15 Incyte Corporation Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
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
KR20180018695A (ko) 2015-06-16 2018-02-21 가부시키가이샤 프리즘 파마 항암제
HRP20220599T1 (hr) 2015-11-06 2022-06-24 Incyte Corporation Heterociklički spojevi kao inhibitori pi3k-gama
AR107293A1 (es) 2016-01-05 2018-04-18 Incyte Corp COMPUESTOS DE PIRIDINA Y PIRIDIMINA COMO INHIBIDORES DE PI3K-g
US20190060286A1 (en) 2016-02-29 2019-02-28 University Of Florida Research Foundation, Incorpo Chemotherapeutic Methods
EP3254698A1 (de) 2016-06-08 2017-12-13 Universite De Montpellier Flt3-rezeptor-inhibitoren bei niedriger dosierung zur behandlung von neuropathischem schmerz
TW201803871A (zh) 2016-06-24 2018-02-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
SG11201903889TA (en) 2016-11-02 2019-05-30 Arog Pharmaceuticals Inc Crenolanib for treating flt3 mutated proliferative disorders associated mutations
CN111093640A (zh) 2017-05-17 2020-05-01 国家健康与医学研究院 用于改善阿片类药物疼痛治疗的flt3抑制剂
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019057649A1 (en) 2017-09-19 2019-03-28 INSERM (Institut National de la Santé et de la Recherche Médicale) METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
HUE056615T2 (hu) 2017-10-18 2022-02-28 Incyte Corp Tercier hidroxicsoportokkal szubsztituált kondenzált imidazol-származékok mint PI3K-gamma inhibitorok
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
WO2019126505A1 (en) 2017-12-21 2019-06-27 Incyte Corporation 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as pi3k-gamma kinase inhibitors for treating e.g. cancer
EP3730483B1 (de) * 2017-12-21 2023-08-30 Hefei Institutes of Physical Science, Chinese Academy of Sciences Klasse von pyrimidinderivaten als kinaseinhibitoren
RS63312B1 (sr) 2018-01-30 2022-07-29 Incyte Corp Procesi za pripremu (1-(3-fluoro-2-(trifluorometil)izonikotinil)piperidin-4-on)
CN111936135A (zh) 2018-02-16 2020-11-13 因赛特公司 用于治疗细胞因子相关的病症的jak1通路抑制剂
CN117903140A (zh) 2018-02-27 2024-04-19 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
JP7268049B2 (ja) 2018-03-08 2023-05-02 インサイト・コーポレイション ＰＩ３Ｋ－γ阻害剤としてのアミノピラジンジオール化合物
JP2021519772A (ja) 2018-03-30 2021-08-12 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ 炎症性皮膚疾患のバイオマーカー
MX2020010322A (es) 2018-03-30 2022-11-30 Incyte Corp Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak).
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
CR20200591A (es) 2018-05-04 2021-03-31 Incyte Corp Sales de un inhibidor de fgfr
AU2019262195A1 (en) 2018-05-04 2020-12-24 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
ES2929415T3 (es) 2018-05-25 2022-11-29 Incyte Corp Compuestos heterocíclicos tricíclicos como activadores de STING
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
JP7490631B2 (ja) 2018-07-05 2024-05-27 インサイト・コーポレイション Ａ２ａ／ａ２ｂ阻害剤としての縮合ピラジン誘導体
WO2020028566A1 (en) 2018-07-31 2020-02-06 Incyte Corporation Heteroaryl amide compounds as sting activators
US11008344B2 (en) 2018-07-31 2021-05-18 Incyte Corporation Tricyclic heteroaryl compounds as STING activators
HRP20240252T1 (hr) 2018-09-05 2024-05-24 Incyte Corporation Kristalni oblici inhibitora fosfoinozitid 3 kinaze (pi3k)
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
US20220056049A1 (en) 2019-01-07 2022-02-24 Incyte Corporation Heteroaryl amide compounds as sting activators
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
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
EP3923949A1 (de) 2019-02-15 2021-12-22 Incyte Corporation Cyclinabhängige kinase-2-biomarker und deren verwendungen
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
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
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11602536B2 (en) 2019-06-10 2023-03-14 Incyte Corporation Topical treatment of vitiligo by a JAK inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN114502196A (zh) 2019-08-01 2022-05-13 因赛特公司 Ido抑制剂的给药方案
JP2023509260A (ja) 2019-08-14 2023-03-08 インサイト・コーポレイション Ｃｄｋ２阻害剤としてのイミダゾリルピリミジニルアミン化合物
WO2021041360A1 (en) 2019-08-26 2021-03-04 Incyte Corporation Triazolopyrimidines as a2a / a2b inhibitors
KR20220099970A (ko) 2019-10-11 2022-07-14 인사이트 코포레이션 Cdk2 억제제로서의 이환식 아민
MX2022004513A (es) 2019-10-14 2022-07-19 Incyte Corp Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr).
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021076124A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp)
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
EP4069696A1 (de) 2019-12-04 2022-10-12 Incyte Corporation Tricyclische heterocyclen als fgfr-inhibitoren
KR20230017165A (ko) 2020-03-06 2023-02-03 인사이트 코포레이션 Axl/mer 및 pd-1/pd-l1 억제제를 포함하는 병행 요법
CA3179692A1 (en) 2020-04-16 2021-10-21 Incyte Corporation Fused tricyclic kras inhibitors
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
PE20231102A1 (es) 2020-06-02 2023-07-19 Incyte Corp Procesos para preparar un inhibidor de jak1
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022019998A1 (en) 2020-07-20 2022-01-27 Arog Pharmaceuticals, Inc. Crystal forms of crenolanib and methods of use thereof
US11999752B2 (en) 2020-08-28 2024-06-04 Incyte Corporation Vinyl imidazole compounds as inhibitors of KRAS
CA3195357A1 (en) 2020-09-16 2022-03-24 Incyte Corporation Topical treatment of vitiligo
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
TW202237089A (zh) 2020-12-08 2022-10-01 美商英塞特公司 用於治療白斑病之ｊａｋ１途徑抑制劑
WO2022155941A1 (en) 2021-01-25 2022-07-28 Qilu Regor Therapeutics Inc. Cdk2 inhibitors
WO2022206888A1 (en) 2021-03-31 2022-10-06 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
CR20240059A (es) 2021-07-07 2024-03-21 Incyte Corp Compuestos tricíclicos como inhibidores de kras.
US20230114765A1 (en) 2021-07-14 2023-04-13 Incyte Corporation Tricyclic compounds as inhibitors of kras
US20230174555A1 (en) 2021-08-31 2023-06-08 Incyte Corporation Naphthyridine compounds as inhibitors of kras
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
CA3234375A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
IL312114A (en) 2021-10-14 2024-06-01 Incyte Corp Quinoline compounds as Kras inhibitors
US20230226040A1 (en) 2021-11-22 2023-07-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a kras inhibitor
WO2023102184A1 (en) 2021-12-03 2023-06-08 Incyte Corporation Bicyclic amine compounds as cdk12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
US20230192722A1 (en) 2021-12-22 2023-06-22 Incyte Corporation Salts and solid forms of an fgfr inhibitor and processes of preparing thereof
WO2023116884A1 (en) 2021-12-24 2023-06-29 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
WO2023172921A1 (en) 2022-03-07 2023-09-14 Incyte Corporation Solid forms, salts, and processes of preparation of a cdk2 inhibitor
US20230399331A1 (en) 2022-06-14 2023-12-14 Incyte Corporation Solid forms of jak inhibitor and process of preparing the same
WO2023250430A1 (en) 2022-06-22 2023-12-28 Incyte Corporation Bicyclic amine cdk12 inhibitors
US20240101557A1 (en) 2022-07-11 2024-03-28 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
CN115108998B (zh) * 2022-07-19 2023-06-30 重庆医科大学 用于抗乙型肝炎病毒的化合物及其应用
US20240058343A1 (en) 2022-08-05 2024-02-22 Incyte Corporation Treatment of urticaria using jak inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993015043A1 (en) * 1992-01-24 1993-08-05 Yoshitomi Pharmaceutical Industries, Ltd. Arylalkananilide compound and pharmaceutical use thereof
WO1998050346A2 (en) 1997-04-18 1998-11-12 Smithkline Beecham Plc Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders
US6093742A (en) * 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
PT1042305E (pt) * 1997-12-22 2005-10-31 Bayer Pharmaceuticals Corp Inibicao de quinase p38 utilizando difenilureias simetricas e assimetricas
NZ505843A (en) 1997-12-22 2003-06-30 Bayer Ag Diphenyl ureas compounds for treating cancer and raf kinase related diseases
US6462036B1 (en) 1998-11-06 2002-10-08 Basf Aktiengesellschaft Tricyclic pyrazole derivatives
AU2725000A (en) 1999-01-13 2000-08-01 Bayer Corporation Omega-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
EP1140840B1 (de) * 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituierte diphenyl harnstoffe als raf kinase inhibitoren
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
MEP36908A (en) * 1999-01-13 2011-02-10 Bayer Corp omega-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS
HN2001000008A (es) * 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
ATE399766T1 (de) 2000-10-20 2008-07-15 Eisai R&D Man Co Ltd Stickstoff enthaltende aromatische heterozyklen
US6706751B2 (en) 2000-12-21 2004-03-16 Hoffman-La Roche Inc. Dihydroindole and tetrahydroquinoline derivatives
CN1705645A (zh) 2002-10-24 2005-12-07 默克专利有限公司 作为raf－激酶抑制剂的亚甲基脲衍生物
TW200418466A (en) 2002-11-06 2004-10-01 Smithkline Beecham Corp Chemical compounds

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