ATE482213T1 - Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine - Google Patents

Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine

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Publication number
ATE482213T1
ATE482213T1 AT05816516T AT05816516T ATE482213T1 AT E482213 T1 ATE482213 T1 AT E482213T1 AT 05816516 T AT05816516 T AT 05816516T AT 05816516 T AT05816516 T AT 05816516T AT E482213 T1 ATE482213 T1 AT E482213T1
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Austria
Prior art keywords
inhibitors
protein kinases
aüpyrimidines
compounds
compositions
Prior art date
Application number
AT05816516T
Other languages
English (en)
Inventor
Juan-Miguel Jimenez
Ronald Knegtel
Jean-Damien Charrier
Dean Stamos
Pan Li
Jon Come
Alex Aronov
Original Assignee
Vertex Pharma
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Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE482213T1 publication Critical patent/ATE482213T1/de

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
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    • A61P35/00Antineoplastic agents
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    • A61P37/08Antiallergic agents
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    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Child & Adolescent Psychology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
AT05816516T 2004-11-04 2005-11-04 Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine ATE482213T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62544604P 2004-11-04 2004-11-04
PCT/US2005/040344 WO2006052913A1 (en) 2004-11-04 2005-11-04 PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES

Publications (1)

Publication Number Publication Date
ATE482213T1 true ATE482213T1 (de) 2010-10-15

Family

ID=35809833

Family Applications (1)

Application Number Title Priority Date Filing Date
AT05816516T ATE482213T1 (de) 2004-11-04 2005-11-04 Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine

Country Status (20)

Country Link
US (1) US7528138B2 (de)
EP (1) EP1812440B1 (de)
JP (2) JP5030229B2 (de)
KR (1) KR20070090172A (de)
CN (1) CN101094853B (de)
AT (1) ATE482213T1 (de)
AU (1) AU2005304784B2 (de)
CA (1) CA2586375A1 (de)
DE (1) DE602005023763D1 (de)
DK (1) DK1812440T3 (de)
ES (1) ES2354824T3 (de)
IL (1) IL182893A0 (de)
MX (1) MX337817B (de)
NO (1) NO20072795L (de)
NZ (1) NZ555236A (de)
PT (1) PT1812440E (de)
RU (1) RU2417996C2 (de)
SI (1) SI1812440T1 (de)
WO (1) WO2006052913A1 (de)
ZA (1) ZA200704476B (de)

Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
EP1812440B1 (de) * 2004-11-04 2010-09-22 Vertex Pharmaceuticals, Inc. Als inhibitoren von proteinkinasen geeignete pyrazolo[1,5-a]pyrimidine
SI1853588T1 (sl) * 2005-02-16 2008-10-31 Astrazeneca Ab Kemične spojine
AU2006247833A1 (en) * 2005-05-12 2006-11-23 Merck & Co., Inc. Tyrosine kinase inhibitors
BRPI0610184A2 (pt) * 2005-05-16 2012-09-25 Astrazeneca Ab composto, sal farmaceuticamente aceitável de um composto, processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, métodos para a inibição da atividade de trk, para o tratamento ou profilaxia de cáncer e para a produção de um efeito anti-proliferativo em um animal de sanque quente, e, composição farmacêutica
WO2007046867A2 (en) * 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
NZ564065A (en) * 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
DK1945631T3 (da) * 2005-10-28 2012-10-22 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidinderivater til anvendelse som tyrosinkinaseinhibitorer til behandling af cancer
TWI630207B (zh) 2005-12-13 2018-07-21 英塞特控股公司 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶
GB0601638D0 (en) * 2006-01-27 2006-03-08 Merck Sharp & Dohme Therapeutic treatment
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
WO2008054827A2 (en) * 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
CN101778825A (zh) * 2007-03-22 2010-07-14 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的n-杂环类化合物
WO2008129255A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
UA99459C2 (en) * 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
US20100137398A1 (en) * 2007-05-04 2010-06-03 Novartis Ag Use of hdac inhibitors for the treatment of gastrointestinal cancers
EP3070090B1 (de) 2007-06-13 2018-12-12 Incyte Holdings Corporation Verwendung der salze des janus-kinasehemmers (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropannitril
US8729264B2 (en) 2007-09-28 2014-05-20 Kyowa Hakko Kirin Co., Ltd. Agent for prevention and/or treatment of skin diseases
ES2569528T3 (es) * 2007-11-16 2016-05-11 Incyte Holdings Corporation 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
CL2008003798A1 (es) * 2007-12-19 2009-10-09 Amgen Inc Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades.
CN101932583A (zh) 2007-12-19 2010-12-29 沃泰克斯药物股份有限公司 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类
JP5638961B2 (ja) * 2008-03-13 2014-12-10 ザ ジェネラル ホスピタル コーポレイション Bmpシグナル伝達経路のインヒビター
CN102119157A (zh) * 2008-06-11 2011-07-06 阿斯利康(瑞典)有限公司 用于治疗癌症和骨髓增生性疾病的三环2,4-二氨基-l,3,5-三嗪衍生物
EP2376492B1 (de) * 2008-09-19 2015-04-08 Nerviano Medical Sciences S.r.l. 3,4 dihydro-2h-pyrrolo[1,2-a]pyrazin-1-on derivate
DK2350075T3 (da) 2008-09-22 2014-05-26 Array Biopharma Inc Substituerede imidazo[1,2b]pyridazinforbindelser som trk-kinase-inhibitorer
JP2012504157A (ja) * 2008-09-30 2012-02-16 アストラゼネカ アクチボラグ 複素環式jakキナーゼ阻害剤
RU2539568C2 (ru) * 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
EP3643312A1 (de) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- oder heptannitril als jak-inhibitoren
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
CA2762479A1 (en) * 2009-05-28 2010-12-02 Vertex Pharmaceuticals Incorporated Inhibitors of c-met protein kinase
GEAP202213376A (en) 2009-06-17 2022-02-25 Vertex Pharmaceuticals Incorporated Us Inhibitors of influenza viruses replication
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
AR078012A1 (es) * 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
CA2771822C (en) 2009-09-04 2020-08-11 Daniel A. Erlanson Bruton's tyrosine kinase inhibitors
EP3050882B1 (de) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl-azetidin-derivate als jak1-inhibitoren
WO2011130515A1 (en) * 2010-04-14 2011-10-20 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production
ES2715611T3 (es) 2010-05-17 2019-06-05 Incozen Therapeutics Pvt Ltd Compuestos novedosos de 3H-imidazo[4,5-b]piridina-3,5-disustituida y 3H-[1,2,3]triazolo[4,5-b]piridina 3,5-disustituida como moduladores de proteína cinasas
RU2735545C2 (ru) 2010-05-20 2020-11-03 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
SI2575968T1 (sl) 2010-06-01 2016-06-30 Summit Therapeutics Plc Spojine za zdravljenje bolezni, ki je povezana s clostridium difficile
GB2480814A (en) * 2010-06-01 2011-12-07 Summit Corp Plc Compounds for the treatment of clostridium difficile-associated disease
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
CN103492381A (zh) * 2010-12-16 2014-01-01 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
LT2718270T (lt) * 2011-06-10 2022-08-10 Merck Patent Gmbh Pirimidino ir piridino junginių, turinčių btk inhibitorinį aktyvumą, kompozicijos ir gamybos būdai
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
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
US9096605B2 (en) * 2011-08-24 2015-08-04 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CN107082779A (zh) 2012-03-30 2017-08-22 理森制药股份公司 作为c‑met 蛋白激酶调节剂的新化合物
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
AR091273A1 (es) 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
ES2750640T3 (es) * 2012-08-16 2020-03-26 Scripps Research Inst Ligandos opioides kappa novedosos
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
WO2014081996A1 (en) * 2012-11-23 2014-05-30 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
WO2014089379A1 (en) 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
TW201501713A (zh) * 2013-03-01 2015-01-16 Kyowa Hakko Kirin Co Ltd 眼炎症性疾病之預防及/或治療劑
CN105189509B (zh) 2013-03-06 2017-12-19 因赛特公司 用于制备jak抑制剂的方法及中间体
US9682983B2 (en) 2013-03-14 2017-06-20 The Brigham And Women's Hospital, Inc. BMP inhibitors and methods of use thereof
EP2970289A1 (de) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Als atr-kinaseinhibitoren nützliche verbindungen
EP2970288A1 (de) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Als atr-kinaseinhibitoren nützliche verbindungen
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2014175370A1 (ja) * 2013-04-25 2014-10-30 塩野義製薬株式会社 ピロリジン誘導体およびそれらを含有する医薬組成物
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
HUE052178T2 (hu) 2013-11-13 2021-04-28 Vertex Pharma Eljárások influenzavírus-replikáció inhibitorainak elõállítására
WO2015073267A1 (en) * 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN104650092B (zh) * 2013-11-16 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
WO2015085132A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
PE20211782A1 (es) 2014-05-23 2021-09-08 Hoffmann La Roche Compuestos de 5-cloro-2-difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
HRP20200186T1 (hr) 2014-06-05 2020-05-29 Vertex Pharmaceuticals Inc. Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici
JP6936007B2 (ja) 2014-06-17 2021-09-15 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Chk1阻害剤とatr阻害剤との組み合わせを使用してがんを処置する方法
WO2016011019A1 (en) 2014-07-15 2016-01-21 The Brigham And Women's Hospital, Inc. Compositions and methods for inhibiting bmp
EP3218380B1 (de) 2014-11-16 2021-03-17 Array Biopharma, Inc. Herstellung einer kristallinen form von (s)-n-(5-((r)-2-(2,5-difluorphenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid-schwefelwasserstoff
JP6857617B2 (ja) 2015-05-13 2021-04-14 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated インフルエンザウイルスの複製の阻害剤
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
EP3355926B1 (de) 2015-09-30 2025-12-24 Vertex Pharmaceuticals Inc. Kombination von dna-schädigenden mitteln und atr-inhibitoren zur verwendung in einem verfahren zur behandlung von krebs
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
IL304018A (en) 2016-04-04 2023-08-01 Loxo Oncology Inc Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
ES2952056T3 (es) 2016-05-18 2023-10-26 Loxo Oncology Inc Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
RU2753905C2 (ru) 2016-07-18 2021-08-24 Юниверсити Хелс Нетуорк Твердые формы ингибитора ttk
JP7214632B2 (ja) 2016-07-21 2023-01-30 バイオジェン エムエー インク. ブルトン型チロシンキナーゼ阻害剤のコハク酸塩形態および組成物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CA3059232A1 (en) 2017-04-27 2018-11-01 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Novel alk2 inhibitors and methods for inhibiting bmp signaling
PL233595B1 (pl) * 2017-05-12 2019-11-29 Celon Pharma Spolka Akcyjna Pochodne pirazolo[1,5-a]pirymidyny jako inhibitory kinazy JAK
RU2769696C2 (ru) 2017-05-22 2022-04-05 Ф. Хоффманн-Ля Рош Аг Терапевтические соединения и композиции и способы их применения
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
JP7229257B2 (ja) * 2018-01-29 2023-02-28 メルク パテント ゲーエムベーハー Gcn2阻害剤およびその使用
KR20200115620A (ko) 2018-01-29 2020-10-07 메르크 파텐트 게엠베하 Gcn2 억제제 및 이의 용도
EP3746429B1 (de) 2018-01-30 2022-03-09 Incyte Corporation Verfahren zur herstellung von (1-(3-fluor-2-trifluormethyl)isonicotinyl)piperidin-4-on)
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
JP7504880B2 (ja) * 2018-10-26 2024-06-24 ケロス セラピューティクス インコーポレイテッド Alk2阻害剤の結晶形
KR20210116488A (ko) 2018-12-20 2021-09-27 인사이트 코포레이션 액티빈 수용체-유사 키나제-2의 억제제로서의 이미다조피리다진 및 이미다조피리딘 화합물
WO2021222875A1 (en) 2020-04-30 2021-11-04 Keros Therapeutics, Inc. Methods of using alk2 inhibitors
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022098812A1 (en) 2020-11-04 2022-05-12 Keros Therapeutics, Inc. Methods of treating iron overload
US20250042873A1 (en) * 2021-08-24 2025-02-06 The Johns Hopkins University Compositions and methods for treating proteotoxicity-associated diseases
CN116987083A (zh) * 2022-04-25 2023-11-03 杭州健崃生物科技有限公司 吡唑并[1,5-a]嘧啶衍生物及其制备方法和用途
KR102912267B1 (ko) 2023-04-20 2026-01-15 한국화학연구원 신규한 헤테로고리 화합물 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 포함하는 바이러스성 질환의 예방 또는 치료용 약학적 조성물

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU734009B2 (en) * 1997-05-30 2001-05-31 Merck & Co., Inc. Novel angiogenesis inhibitors
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
US6245759B1 (en) * 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0103926D0 (en) * 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
WO2004052315A2 (en) * 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1812440B1 (de) * 2004-11-04 2010-09-22 Vertex Pharmaceuticals, Inc. Als inhibitoren von proteinkinasen geeignete pyrazolo[1,5-a]pyrimidine

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