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PE20040522A1 - Derivados de diarilurea dependientes de la cinasa de proteina - Google Patents

Derivados de diarilurea dependientes de la cinasa de proteina

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Publication number
PE20040522A1
PE20040522A1 PE2003000513A PE2003000513A PE20040522A1 PE 20040522 A1 PE20040522 A1 PE 20040522A1 PE 2003000513 A PE2003000513 A PE 2003000513A PE 2003000513 A PE2003000513 A PE 2003000513A PE 20040522 A1 PE20040522 A1 PE 20040522A1
Authority
PE
Peru
Prior art keywords
phenyl
protein kinase
dependent
pyridin
oxy
Prior art date
Application number
PE2003000513A
Other languages
English (en)
Inventor
Paul William Manley
Guido Bold
Eugen Boss
Andrea Vaupel
Vito Guagnano
Andreas Floersheimer
Pascal Furet
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0212413A external-priority patent/GB0212413D0/en
Priority claimed from GB0305684A external-priority patent/GB0305684D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20040522A1 publication Critical patent/PE20040522A1/es

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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DERIVADO DE DIARILUREA, DONDE G NO ESTA PRESENTE O ES ALQUILENO INFERIOR, CICLOALQUILENO C3-C5, ENTE OTROS; Z ES (A), (B); A ES CH, N O NàO; A' ES N O NàO CON LA CONDICION DE QUE NO MAS DE UNO DE A Y A' PUEDE SER Nà O; n ES 1 O 2; m ES 0, 1, O 2; p ES 0, 2 O 3; r ES DE 0 A 5; X ES N, NH, CH2, ENTRE OTROS; Y1 ES O, S, CH2; Y2 ES O, S, NH; R1, R2 Y R3 SON CADA UNO H, METILO, PROPILO, ENTRE OTROS; R4 ES METILO, METOXILO, p-HIDROXIFENILAMINO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS N-(4-PIRIDIN-4-IL-OXI-FENIL)-N'-(4-ETIL-FENIL)-UREA; N-(4-PIRIDIN-4-IL-OXI-FENIL)-N'-(3-TRIFLUOROMETIL-FENIL)-UREA; N-(4-PIRIDIN-4-IL-OXI-FENIL)-N'-(4-(2,2,2-TRIFLUOROETOXI)-3-TRIFLUOROMETILFENIL-FENIL)-UREA. SE REFIERE TAMBIEN A UNA PREPARACION FARMACEUTICA UTIL EN EL TRATAMIENTO DE ENFERMEDADES DEPENDIENTES DE LA CINASA DE PROTEINA
PE2003000513A 2002-05-29 2003-05-27 Derivados de diarilurea dependientes de la cinasa de proteina PE20040522A1 (es)

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Families Citing this family (279)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
ME00275B (me) 1999-01-13 2011-02-10 Bayer Corp ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE
HK1042251B (en) 1999-01-13 2012-07-20 Bayer Healthcare Llc 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
EP1478358B1 (en) 2002-02-11 2013-07-03 Bayer HealthCare LLC Sorafenib tosylate for the treatment of diseases characterized by abnormal angiogenesis
AU2003209119A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
WO2004014871A1 (en) * 2002-08-08 2004-02-19 Amgen Inc. Vanilloid receptor ligands and their use in treatments
JP4927533B2 (ja) * 2003-02-28 2012-05-09 ニッポネックス インコーポレイテッド 癌その他の疾患の治療に有用な置換ピリジン誘導体
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
PT1626714E (pt) 2003-05-20 2007-08-24 Bayer Pharmaceuticals Corp Diarilureias para doenças mediadas por pdgfr
DE602004010407T2 (de) 2003-07-23 2008-10-16 Bayer Pharmaceuticals Corp., West Haven Fluorsubstituierter omega-carboxyaryldiphenylharnstoff zur behandlung und prävention von krankheiten und leiden
DE10334663A1 (de) * 2003-07-30 2005-03-10 Merck Patent Gmbh Harnstoffderivate
PL1660057T3 (pl) 2003-08-27 2012-10-31 Ophthotech Corp Terapia łączona do leczenia zaburzeń związanych z neowaskularyzacją gałki ocznej
US20050165031A1 (en) 2003-11-13 2005-07-28 Ambit Biosciences Corporation Urea derivatives as ABL modulators
PE20051046A1 (es) * 2003-11-28 2006-01-11 Novartis Ag Derivados de diaril-urea en el tratamiento de enfermedades dependientes de la quinasa de proteina
EA011402B1 (ru) * 2004-01-23 2009-02-27 Эмджен Инк. Азотсодержащие гетероциклические производные и их фармацевтические применения
CA2554878A1 (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
NZ588139A (en) 2004-04-08 2012-02-24 Targegen Inc 7-Aryl-3-arylamino-benzo[1,2,4]triazine derivatives
AU2011253934C1 (en) * 2004-06-17 2013-08-22 Cytokinetics, Inc. Substituted urea derivatives for treating cardiac diseases
CN101035525A (zh) 2004-06-17 2007-09-12 赛特凯恩蒂克公司 用于治疗心脏疾病的经取代的脲衍生物
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
RU2007110731A (ru) 2004-09-23 2008-10-27 Редди Юс Терапевтикс Новые соединения пиримидина, способ их получения и содержащие их композиции
GB0421525D0 (en) 2004-09-28 2004-10-27 Novartis Ag Inhibitors of protein kineses
CA2581516C (en) 2004-10-12 2013-06-11 Astrazeneca Ab Quinazoline derivatives
WO2006040056A1 (en) * 2004-10-13 2006-04-20 Merck Patent Gmbh Heterocyclic substituted bisarylurea derivatives as kinase inhibitors
MX2007006204A (es) * 2004-11-24 2007-06-20 Novartis Ag Combinaciones que comprenden inhibidores de jak y cuando menos uno de entre inhibidores de bcr-abl, flt-3, fak o raf cinasa.
EP1836169B9 (en) 2004-12-28 2012-07-04 Kinex Pharmaceuticals, LLC Compositions and methods of treating cell proliferation disorders
US7968574B2 (en) 2004-12-28 2011-06-28 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
US7625931B2 (en) 2005-01-14 2009-12-01 Cgi Pharmaceuticals, Inc. Certain substituted diphenyl 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
PL1879573T3 (pl) 2005-05-10 2013-05-31 Incyte Holdings Corp Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania
MY146795A (en) 2005-06-09 2012-09-28 Novartis Ag Process for the synthesis of organic compounds
GT200600207A (es) * 2005-06-09 2007-01-15 Novartis Ag Proceso para la síntesis de compuestos orgánicos
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
RS52902B (sr) * 2005-08-24 2014-02-28 Eisai R & D Management Co. Ltd. Novi piridinski derivati i pirimidinski derivati (3)
GT200600411A (es) 2005-09-13 2007-05-21 Novartis Ag Combinaciones que comprenden un inhibidor del receptor del factor de crecimiento endotelial vascular
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
CN101340909B (zh) 2005-10-18 2012-01-11 詹森药业有限公司 抑制flt3激酶的方法
KR101467723B1 (ko) 2005-11-01 2014-12-03 탈자진 인코포레이티드 키나제의 비-아릴 메타-피리미딘 억제제
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
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
SI3184526T1 (sl) 2005-12-13 2019-03-29 Incyte Holdings Corporation Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze
WO2007068381A1 (en) * 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating inflammatory skin, eye and/or ear diseases
AR058347A1 (es) 2005-12-15 2008-01-30 Cytokinetics Inc Entidades quimias composiciones y metodos
MEP3808A (xx) 2005-12-21 2010-02-10 Novartis Ag Derivati pirimidinil aril uree kao fgf inhibitori
TW200804349A (en) * 2005-12-23 2008-01-16 Kalypsys Inc Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases
WO2007076474A1 (en) * 2005-12-23 2007-07-05 Kalypsys, Inc. Novel substituted pyridinyloxy and pyrimidinyloxy amides useful 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
JP2009532440A (ja) 2006-04-07 2009-09-10 ノバルティス アクチエンゲゼルシャフト a)ピリミジルアミノベンズアミド化合物、およびb)Thr315Ileキナーゼ阻害剤を含む、組合せ剤
CA2650057C (en) 2006-04-20 2014-07-29 Janssen Pharmaceutica N.V. Phenyl- or pyridinyl-amide as inhibitors of c-fms kinase
JP5089681B2 (ja) 2006-04-20 2012-12-05 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ c−fmsキナーゼの阻害剤としての複素環式化合物
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
EP2041071B1 (en) 2006-06-29 2014-06-18 Kinex Pharmaceuticals, LLC Biaryl compositions and methods for modulating a kinase cascade
KR101380444B1 (ko) * 2006-08-23 2014-04-01 에자이 알앤드디 매니지먼트 가부시키가이샤 페녹시피리딘 유도체의 염 또는 그 결정 및 이들의 제조 방법
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
BRPI0720741A2 (pt) * 2006-12-22 2014-01-28 Hoffmann La Roche Derivados de primidila como inibidores da proteína cinase.
EP2121692B1 (en) 2006-12-22 2013-04-10 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
PT2154967E (pt) 2007-04-16 2014-06-05 Hutchison Medipharma Entpr Ltd Derivados de pirimidina
KR20100016584A (ko) 2007-04-17 2010-02-12 노파르티스 아게 암 치료제로서의 나프탈렌 카르복실산 아미드의 에테르
CA2684666A1 (en) * 2007-04-20 2008-11-20 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
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.
WO2009009041A2 (en) * 2007-07-06 2009-01-15 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
US7982036B2 (en) * 2007-10-19 2011-07-19 Avila Therapeutics, Inc. 4,6-disubstitued pyrimidines useful as kinase inhibitors
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
US8309718B2 (en) 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
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
JPWO2009104520A1 (ja) * 2008-02-18 2011-06-23 エーザイ・アール・アンド・ディー・マネジメント株式会社 フェノキシピリジン誘導体の製造方法(2)
CN102026999B (zh) 2008-03-11 2014-03-05 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
US8871753B2 (en) 2008-04-24 2014-10-28 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
US20110160249A1 (en) 2008-05-23 2011-06-30 Schaab Kevin Murray 5-lipoxygenase-activating protein inhibitor
HRP20141094T1 (hr) 2008-07-08 2015-01-16 Incyte Corporation 1,2,5-oksadiazoli kao inhibitori indolamin 2,3-dioksigenaze
US8546431B2 (en) 2008-10-01 2013-10-01 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
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
US8765727B2 (en) 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
EP2400985A2 (en) 2009-02-25 2012-01-04 OSI Pharmaceuticals, LLC Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor
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
WO2010099363A1 (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
US8465912B2 (en) 2009-02-27 2013-06-18 OSI Pharmaceuticals, LLC 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
WO2010135650A1 (en) 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
WO2010135621A1 (en) 2009-05-22 2010-11-25 Incyte Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
KR20120016676A (ko) * 2009-06-09 2012-02-24 아브락시스 바이오사이언스, 엘엘씨 우레이도페닐치환 트리아진 유도체와 이들의 치료적 용도
PT2448938E (pt) 2009-06-29 2014-07-31 Incyte Corp Pirimidinonas como inibidoras de pi3k
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
US8729265B2 (en) 2009-08-14 2014-05-20 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
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MX2012004180A (es) 2009-10-09 2012-07-17 Incyte Corp Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-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
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp 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
ES2539170T3 (es) 2010-01-12 2015-06-26 Ab Science Inhibidores de quinasas de oxazol
AU2011209586B2 (en) * 2010-02-01 2016-01-21 Cancer Research Technology Limited 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro- 4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo [4,5-b]pyridin-7-yloxy)-phenyl] -urea and related compounds and their use in therapy
AU2011217961B2 (en) 2010-02-18 2016-05-05 Incyte Holdings Corporation Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors
CA2791680A1 (en) * 2010-03-01 2011-09-09 Myrexis, Inc. Compounds and therapeutic uses thereof
US8912184B1 (en) 2010-03-01 2014-12-16 Alzheimer's Institute Of America, Inc. Therapeutic and diagnostic methods
PE20130038A1 (es) 2010-03-10 2013-01-28 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de jak1
WO2011130342A1 (en) 2010-04-14 2011-10-20 Incyte Corporation FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS
EP2558085B1 (en) 2010-04-16 2017-08-30 Athenex, Inc. Compositions and methods for the prevention and treatment of cancer
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
RU2560683C2 (ru) 2010-06-25 2015-08-20 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство, задействующее соединения с ингибирующим эффектом к киназам в комбинации
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
BR112013012502A2 (pt) 2010-11-19 2019-03-06 Incyte Corporation pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン
CA2827673C (en) 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
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
WO2012149014A1 (en) 2011-04-25 2012-11-01 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
EP2721028B1 (en) 2011-06-20 2015-11-04 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
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
EP3196202B1 (en) 2011-09-02 2019-02-27 Incyte Holdings Corporation Heterocyclylamines as pi3k inhibitors
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
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
NZ702747A (en) 2012-06-13 2017-03-31 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
EP2882757B1 (en) 2012-08-07 2016-10-05 Janssen Pharmaceutica, N.V. Process for the preparation of heterocyclic ester derivatives
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
EP2890380A2 (en) * 2012-08-29 2015-07-08 Merck Patent GmbH Ddr2 inhibitors for the treatment of osteoarthritis
SI2890680T1 (en) 2012-08-30 2018-08-31 Athenex, Inc. Conventus Building N- (3-FLUOROBENZYL) -2- (5- (4-MORFOLINOPHENYL) PIRIDIN-2-IL) ACETAMIDE AS PROTEIN TIROZINE KINASE PROTECTORS
KR101738063B1 (ko) 2012-09-21 2017-05-19 아로그 파마슈티칼스, 인코퍼레이티드 구조적으로 활성인 인산화된 flt3 키나제의 억제 방법
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
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
WO2014071031A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
WO2014098176A1 (ja) 2012-12-21 2014-06-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
BR112015016282A2 (en) 2013-01-07 2017-07-11 Arog Pharmaceuticals, Inc. crenolanib for treatment of mutated flt3 proliferative disorders
TWI657090B (zh) 2013-03-01 2019-04-21 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
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
EP2981535B8 (en) 2013-04-02 2021-03-10 Oxular Acquisitions Limited Urea derivatives useful as kinase inhibitors
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
RU2658601C2 (ru) 2013-05-14 2018-06-21 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Биомаркер для прогнозирования и оценки чувствительности субъектов с раком эндометрия к соединениям ленватиниба
FI4275756T3 (fi) 2013-05-17 2025-10-20 Incyte Holdings Corp Bipyratsolin johdannaisia jak-estäjinä
LT3030227T (lt) 2013-08-07 2020-06-10 Incyte Corporation Prailginto atpalaidavimo jak1 inhibitoriaus dozavimo formos
US20150065447A1 (en) 2013-08-20 2015-03-05 Incyte Corporation Survival benefit in patients with solid tumors with elevated c-reactive protein levels
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
JP6514703B2 (ja) * 2013-12-20 2019-05-15 トピバート ファーマ リミテッド キナーゼインヒビターとして有用な尿素誘導体
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
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
WO2015157257A1 (en) 2014-04-08 2015-10-15 Incyte Corporation Treatment of b-cell malignancies by a combination jak and pi3k inhibitor
SG10201809518QA (en) 2014-04-30 2018-11-29 Incyte Corp 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
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
EP3174859B1 (en) 2014-07-31 2020-04-29 INSERM - Institut National de la Santé et de la Recherche Médicale Flt3 receptor antagonists
ES2926687T3 (es) 2014-08-28 2022-10-27 Eisai R&D Man Co Ltd Derivado de quinolina muy puro y método para su producción
MX389591B (es) 2014-08-29 2025-03-20 Tes Pharma S R L INHIBIDORES DE ACIDO A-AMINO-ß-CARBOXIMUCONICO SEMIALDEHIDO DESCARBOXILASA
SG11201701694QA (en) 2014-09-10 2017-04-27 Glaxosmithkline Ip Dev Ltd Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors
DK3191449T3 (da) 2014-09-10 2020-08-03 Glaxosmithkline Ip Dev Ltd Forbindelser som ret- (rearranged during transfection) hæmmere
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
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
RS65049B1 (sr) 2015-02-25 2024-02-29 Eisai R&D Man Co Ltd Metoda za suzbijanje gorčine derivata kinolina
PL3262046T3 (pl) 2015-02-27 2021-05-04 Incyte Corporation Sole inhibitora pi3k i sposoby ich wytwarzania
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
WO2016183062A1 (en) 2015-05-11 2016-11-17 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
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
CA2988707C (en) 2015-06-16 2023-10-10 Eisai R&D Management Co., Ltd. Combination of cbp/catenin inhibitor and immune checkpoint inhibitor for treating cancer
ES2887426T3 (es) 2015-08-20 2021-12-22 Eisai R&D Man Co Ltd Lenvatinib combinado con etopósido e ifosfamida para su uso en el tratamiento de un tumor
LT3371190T (lt) 2015-11-06 2022-08-10 Incyte Corporation Heterocikliniai junginiai, kaip pi3k-gama inhibitoriai
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 (en) 2016-06-08 2017-12-13 Universite De Montpellier Flt3 receptor inhibitor at low dosage for the treatment of neuropathic pain
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
SG11201903889TA (en) 2016-11-02 2019-05-30 Arog Pharmaceuticals Inc Crenolanib for treating flt3 mutated proliferative disorders associated mutations
JP6581320B2 (ja) 2017-02-08 2019-09-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
JP2020519665A (ja) 2017-05-17 2020-07-02 アンセルム(アンスティテュト ナショナル ド ラ サンテ エ ド ラ ルシェルシュ メディカル) オピオイドによる痛みの処置を改善する為のflt3阻害剤
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
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
JP7021356B2 (ja) * 2017-12-21 2022-02-16 ヘフェイ インスティテューツ オブ フィジカル サイエンス, チャイニーズ アカデミー オブ サイエンシーズ ピリミジン誘導体系キナーゼ阻害剤類
US11306079B2 (en) 2017-12-21 2022-04-19 Incyte Corporation 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors
MX2020007973A (es) 2018-01-30 2020-12-07 Incyte Corp Procesos para preparar (1-(3-fluoro-2-(trifluorometil)isonicotinil )piperidin-4-ona).
KR20240157777A (ko) 2018-02-16 2024-11-01 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
WO2019168847A1 (en) 2018-02-27 2019-09-06 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
CA3093445A1 (en) 2018-03-08 2019-11-28 Incyte Corporation Aminopyrazine diol compounds as pi3k-.gamma. inhibitors
SI3773593T1 (sl) 2018-03-30 2024-08-30 Incyte Corporation Zdravljenje hidradenitisa suppurative z zaviralci jak
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
CA3100731A1 (en) 2018-05-18 2019-11-21 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
US10947227B2 (en) 2018-05-25 2021-03-16 Incyte Corporation Tricyclic heterocyclic compounds as sting activators
KR102884803B1 (ko) 2018-06-01 2025-11-12 인사이트 코포레이션 Pi3k 관련 장애의 치료를 위한 투여 요법
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
SG11202013216RA (en) 2018-07-05 2021-01-28 Incyte Corp Fused pyrazine derivatives as a2a / a2b inhibitors
US10875872B2 (en) 2018-07-31 2020-12-29 Incyte Corporation Heteroaryl amide compounds as sting activators
US11008344B2 (en) 2018-07-31 2021-05-18 Incyte Corporation Tricyclic heteroaryl compounds as STING activators
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11396502B2 (en) 2018-11-13 2022-07-26 Incyte Corporation Substituted heterocyclic derivatives as PI3K inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 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
WO2020146237A1 (en) 2019-01-07 2020-07-16 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
US20200316064A1 (en) 2019-02-15 2020-10-08 Incyte Corporation Cyclin-dependent kinase 2 biomarkers and uses thereof
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
US11628162B2 (en) 2019-03-08 2023-04-18 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
MA56215A (fr) 2019-06-10 2022-04-20 Incyte Corp Traitement topique du vitiligo par un inhibiteur de jak
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
MX2022001133A (es) 2019-08-01 2022-04-25 Incyte Corp Regimen de dosificacion para un inhibidor de indolamina 2,3-dioxigenasa (ido).
AU2020328025A1 (en) 2019-08-14 2022-03-03 Incyte Corporation Imidazolyl pyrimidinylamine compounds as CDK2 inhibitors
JP7631317B2 (ja) 2019-08-26 2025-02-18 インサイト・コーポレイション A2a/a2b阻害剤としてのトリアゾロピリミジン
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN119930611A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
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)
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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)
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
AU2021230385A1 (en) 2020-03-06 2022-09-22 Incyte Corporation Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors
JP7753246B2 (ja) 2020-04-16 2025-10-14 インサイト・コーポレイション 融合三環式kras阻害剤
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
PT4157831T (pt) 2020-06-02 2024-12-20 Incyte Corp Processos de preparação de um inibidor de jak1
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11713310B2 (en) 2020-07-20 2023-08-01 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
JP2023542137A (ja) 2020-09-16 2023-10-05 インサイト・コーポレイション 白斑の局所処置
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
EP4259131A1 (en) 2020-12-08 2023-10-18 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
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
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
TW202308610A (zh) 2021-05-03 2023-03-01 美商英塞特公司 用於治療結節性癢疹之jak1途徑抑制劑
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
EP4367117A1 (en) 2021-07-07 2024-05-15 Incyte Corporation Tricyclic compounds as inhibitors of kras
CA3224841A1 (en) 2021-07-14 2023-01-19 Zhenwu Li Tricyclic compounds as inhibitors of kras
JP2024534187A (ja) 2021-08-31 2024-09-18 インサイト・コーポレイション Krasの阻害剤としてのナフチリジン化合物
US12030883B2 (en) 2021-09-21 2024-07-09 Incyte Corporation Hetero-tricyclic compounds as inhibitors of KRAS
US12030884B2 (en) 2021-10-01 2024-07-09 Incyte Corporation Pyrazoloquinoline KRAS inhibitors
AU2022367432A1 (en) 2021-10-14 2024-05-02 Incyte Corporation Quinoline compounds as inhibitors of kras
CA3239205A1 (en) 2021-11-22 2023-05-25 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
CA3244187A1 (en) 2021-12-22 2023-06-29 Incyte Corporation SALTS AND SOLID FORMS OF AN FGFR INHIBITOR AND THEIR METHODS OF PREPARATION
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
TW202341982A (zh) 2021-12-24 2023-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Cdk2抑制劑及其用途
KR20250004643A (ko) 2022-03-07 2025-01-08 인사이트 코포레이션 Cdk2 억제제의 고체 형태, 염 및 제조 방법
WO2023245053A1 (en) 2022-06-14 2023-12-21 Incyte Corporation Solid forms of a jak inhibitor and process of preparing the same
AR129675A1 (es) 2022-06-22 2024-09-18 Incyte Corp Inhibidores de cdk12 de aminas biciclicas
WO2024015731A1 (en) 2022-07-11 2024-01-18 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
JP2025527297A (ja) 2022-08-05 2025-08-20 インサイト・コーポレイション Jak阻害剤を使用した蕁麻疹の処置
US20240390340A1 (en) 2023-04-18 2024-11-28 Incyte Corporation Pyrrolidine kras inhibitors
US20240368156A1 (en) 2023-04-18 2024-11-07 Incyte Corporation 2-azabicyclo[2.2.1]heptane kras inhibitors
WO2024254245A1 (en) 2023-06-09 2024-12-12 Incyte Corporation Bicyclic amines as cdk2 inhibitors
WO2025096738A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Kras inhibitors
US20250195536A1 (en) 2023-12-13 2025-06-19 Incyte Corporation Bicyclooctane kras inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993015043A1 (fr) * 1992-01-24 1993-08-05 Yoshitomi Pharmaceutical Industries, Ltd. Compose arylalkananilide et utilisation pharmaceutique
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
KR100704977B1 (ko) * 1997-12-22 2007-04-09 바이엘 코포레이션 대칭성 및 비대칭성 치환디페닐우레아를 이용한 raf키나제의 저해
JP3887769B2 (ja) * 1997-12-22 2007-02-28 バイエル コーポレイション 対称および非対称ジフェニル尿素を用いるp38キナーゼの阻害
US6462036B1 (en) 1998-11-06 2002-10-08 Basf Aktiengesellschaft Tricyclic pyrazole derivatives
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
WO2000042012A1 (en) * 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS
HK1042251B (en) 1999-01-13 2012-07-20 Bayer Healthcare Llc Omega-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
DZ3004A1 (fr) * 1999-01-13 2004-03-27 Bayer Corp Omega-carboxyaryl diphényl urées substitués comme inhibiteurs de raf kinase.
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
EP1415987B1 (en) 2000-10-20 2007-02-28 Eisai R&D Management Co., Ltd. Nitrogenous aromatic ring compounds as anti cancer agents
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
AR041992A1 (es) 2002-11-06 2005-06-08 Smithkline Beecham Corp Compuesto de piridinil benzoheterociclico, composicion farmaceutica que lo comprende y su uso para prepararla

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WO2003099771A3 (en) 2004-04-01
IL164784A0 (en) 2005-12-18
AR037647A1 (es) 2004-12-01
KR101036394B1 (ko) 2011-05-23
AU2003242591A1 (en) 2003-12-12
EP1511730B8 (en) 2009-04-08
KR20050006281A (ko) 2005-01-15
JP4608312B2 (ja) 2011-01-12
US20060128734A1 (en) 2006-06-15
BR0311313A (pt) 2005-02-15
NZ536781A (en) 2007-12-21
MXPA04011789A (es) 2005-03-31
PL372426A1 (en) 2005-07-25
WO2003099771A2 (en) 2003-12-04
CA2484288A1 (en) 2003-12-04
TW200406374A (en) 2004-05-01
CN1656073A (zh) 2005-08-17
US7652022B2 (en) 2010-01-26
ATE417037T1 (de) 2008-12-15
PT1511730E (pt) 2009-02-18
NO20045521L (no) 2004-12-17
CN1656073B (zh) 2010-05-26
EP1511730A2 (en) 2005-03-09
AU2003242591B2 (en) 2007-07-26
DE60325209D1 (de) 2009-01-22
JP2005527622A (ja) 2005-09-15
ES2318158T3 (es) 2009-05-01

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