JP2013508332A5 - - Google Patents

Download PDF

Info

Publication number
JP2013508332A5
JP2013508332A5 JP2012534661A JP2012534661A JP2013508332A5 JP 2013508332 A5 JP2013508332 A5 JP 2013508332A5 JP 2012534661 A JP2012534661 A JP 2012534661A JP 2012534661 A JP2012534661 A JP 2012534661A JP 2013508332 A5 JP2013508332 A5 JP 2013508332A5
Authority
JP
Japan
Prior art keywords
pyrazolo
methyl
pyrazol
pyrimidin
amine
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.)
Granted
Application number
JP2012534661A
Other languages
English (en)
Japanese (ja)
Other versions
JP5744887B2 (ja
JP2013508332A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/EP2010/065700 external-priority patent/WO2011048082A1/en
Publication of JP2013508332A publication Critical patent/JP2013508332A/ja
Publication of JP2013508332A5 publication Critical patent/JP2013508332A5/ja
Application granted granted Critical
Publication of JP5744887B2 publication Critical patent/JP5744887B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2012534661A 2009-10-20 2010-10-19 Jak阻害剤としてのヘテロシクリルピラゾロピリミジン類似体 Expired - Fee Related JP5744887B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09173535 2009-10-20
EP09173535.7 2009-10-20
US37535810P 2010-08-20 2010-08-20
US61/375,358 2010-08-20
PCT/EP2010/065700 WO2011048082A1 (en) 2009-10-20 2010-10-19 Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors

Publications (3)

Publication Number Publication Date
JP2013508332A JP2013508332A (ja) 2013-03-07
JP2013508332A5 true JP2013508332A5 (enExample) 2013-12-05
JP5744887B2 JP5744887B2 (ja) 2015-07-08

Family

ID=41531257

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012534661A Expired - Fee Related JP5744887B2 (ja) 2009-10-20 2010-10-19 Jak阻害剤としてのヘテロシクリルピラゾロピリミジン類似体

Country Status (15)

Country Link
US (1) US9242987B2 (enExample)
EP (1) EP2491039A1 (enExample)
JP (1) JP5744887B2 (enExample)
KR (1) KR20120102601A (enExample)
CN (1) CN102666545B (enExample)
AR (1) AR078675A1 (enExample)
AU (1) AU2010309882B2 (enExample)
BR (1) BR112012009327A2 (enExample)
CA (1) CA2775009A1 (enExample)
EA (1) EA022120B1 (enExample)
IL (1) IL218751A0 (enExample)
MX (1) MX2012004020A (enExample)
NZ (1) NZ598907A (enExample)
TW (1) TW201125867A (enExample)
WO (1) WO2011048082A1 (enExample)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
RU2539568C2 (ru) 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP3050882B1 (en) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
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
JP2013534233A (ja) * 2010-08-20 2013-09-02 セルゾーム リミティッド 選択的jak阻害剤としてのヘテロシクリルピラゾロピリミジン類似体
RU2013114352A (ru) 2010-09-15 2014-10-20 Ф. Хоффманн-Ля Рош Аг Азабензотиазолы, композиции и способы применения
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
CA2817785A1 (en) * 2010-11-19 2012-05-24 Toby Blench Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012125629A1 (en) 2011-03-14 2012-09-20 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
WO2012143320A1 (en) 2011-04-18 2012-10-26 Cellzome Limited (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
CN103781780B (zh) * 2011-07-28 2015-11-25 赛尔佐姆有限公司 作为jak抑制剂的杂环基嘧啶类似物
WO2013017480A1 (en) 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
WO2013017479A1 (en) 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Pi3k 억제제로서 헤테로시클릴아민
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2760863A1 (en) 2011-09-20 2014-08-06 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors
US20150005281A1 (en) 2011-12-23 2015-01-01 Cellzome Limited Pyrimidine-2,4-diamine derivatives as kinase inhibitors
CN103193600B (zh) * 2012-01-07 2016-04-06 浙江九洲药物科技有限公司 卡巴拉汀中间体的制备方法
CA2862694C (en) * 2012-01-28 2020-07-28 Merck Patent Gmbh Triazolo[4,5-d]pyrimidine derivatives
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
JP6197031B2 (ja) 2012-05-24 2017-09-13 セルゾーム リミティッド Tyk2阻害剤としてのヘテロシクリルピリミジン類似体
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
MA38287B1 (fr) 2013-01-23 2018-08-31 Astrazeneca Ab Nouveaux dérivés aminopyrazine pour le traitement ou la prévention du cancer
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
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
WO2015038417A1 (en) * 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
CN105636445B (zh) 2013-10-17 2018-12-07 美国陶氏益农公司 制备杀虫化合物的方法
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
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
JP6499282B2 (ja) 2014-09-26 2019-04-10 ギリアード サイエンシーズ, インコーポレイテッド Tank結合キナーゼ阻害剤化合物として有用なアミノトリアジン誘導体
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
AU2016251253B2 (en) * 2015-04-24 2020-07-09 Guangzhou Maxinovel Pharmaceuticals Co., Ltd Condensed-ring pyrimidylamino derivative, preparation method therefor, and intermediate, pharmaceutical composition and applications thereof
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
CU20180059A7 (es) 2015-12-17 2018-10-04 Gilead Sciences Inc Compuestos inhibidores de la quinasa de unión a tank
ES2925564T3 (es) * 2016-07-29 2022-10-18 Rapt Therapeutics Inc Derivados de azetidina tal como moduladores de receptores de quimiocinas y usos de los mismos
CN110139853B (zh) 2016-12-29 2023-06-16 美国陶氏益农公司 用于制备杀有害生物化合物的方法
CN110325036B (zh) * 2016-12-29 2021-10-26 美国陶氏益农公司 用于制备杀虫化合物的方法
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
AU2018381574B2 (en) 2017-12-05 2022-09-15 Oscotec Inc. Pyrrolo(pyrazolo)pyrimidine derivative as LRRK2 inhibitor
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
EP3746429B1 (en) 2018-01-30 2022-03-09 Incyte Corporation Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
CN111683528B (zh) 2018-02-28 2022-12-13 巴斯夫欧洲公司 吡唑炔丙基醚作为硝化抑制剂的用途
AU2019226359B2 (en) 2018-02-28 2023-08-17 Basf Se Use of N-functionalized alkoxy pyrazole compounds as nitrification inhibitors
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案
CN110885331B (zh) * 2018-09-11 2021-07-09 中国药科大学 一种6-氨基-1H-吡唑并[3,4-d]嘧啶类JAK激酶抑制剂的制备与应用
SG11202103011YA (en) 2018-10-11 2021-04-29 Basf As Aromatic compounds and pharmaceutical uses thereof
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
KR102916168B1 (ko) 2019-05-08 2026-01-21 비말란 바이오사이언스즈, 인크. Jak 억제제
TWI899080B (zh) * 2019-05-27 2025-10-01 大陸商迪哲(江蘇)醫藥股份有限公司 Dna依賴性蛋白激酶抑制劑
WO2021026465A1 (en) * 2019-08-08 2021-02-11 Vimalan Biosciences, Inc. Jak inhibitors
US20230065636A1 (en) * 2020-01-15 2023-03-02 KSQ Therapeutics, Inc. Compositions of substituted pyrazolopyrimidines and uses thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
KR20230098186A (ko) * 2020-10-30 2023-07-03 케이에스큐 세러퓨틱스 인코포레이티드 치환된 피라졸로피리미딘의 고체 상태 형태 및 이의 용도
EP4341248A1 (en) 2021-05-21 2024-03-27 Basf Se Use of an n-functionalized alkoxy pyrazole compound as nitrification inhibitor
WO2024238570A1 (en) * 2023-05-15 2024-11-21 Aleksia Therapeutics, Inc. Cdk2 inhibitor pyrazolopyrimidine compounds

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998035985A1 (en) 1997-02-12 1998-08-20 The Regents Of The University Of Michigan Protein markers for lung cancer and use thereof
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
DK1553097T3 (da) 1999-02-10 2010-12-13 Astrazeneca Ab Quinazolinderivat som angiogeneseinhibitor og mellemprodukter dertil
PL203782B1 (pl) 1999-11-05 2009-11-30 Astrazeneca Ab Pochodne chinazoliny,sposoby ich wytwarzania,ich kompozycje farmaceutyczne oraz ich zastosowania
PT1382339E (pt) 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
DE122008000002I1 (de) 2000-02-15 2008-04-17 Sugen Inc Pyrrol substituierte indolin-2-on protein kinase inhibitoren
CN1918158B (zh) * 2004-02-14 2011-03-02 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
ES2411975T3 (es) * 2005-01-14 2013-07-09 Janssen Pharmaceutica Nv Pirimidinas heterocíclicas anilladas de 5 miembros como inhibidores de cinasas
AU2006259153B2 (en) 2005-06-14 2012-04-12 Cellzome Gmbh Process for the identification of novel enzyme interacting compounds
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
ES2318616T3 (es) 2006-06-01 2009-05-01 Cellzome Ag Metodos para la identificacion de moleculas que interactuan con zap-70 y para la purificacion de zap-70.
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
CA2669686A1 (en) 2006-11-16 2008-05-22 Pharmacopeia, Llc 7-substituted purine derivatives for immunosuppression
WO2008094575A2 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. 1-h-pyrazolo(3,4b)pyrimidine derivatives and their use as modulators of mitotic kinases
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
EP2178563A2 (en) 2007-07-06 2010-04-28 OSI Pharmaceuticals, Inc. Combination anti-cancer therapy comprising an inhibitor of both mtorc1 and mtorc2
CN101981036B (zh) * 2008-02-06 2013-09-04 诺瓦提斯公司 吡咯并[2,3-d]嘧啶及其作为酪氨酸激酶抑制剂的用途
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.
EP2419423A1 (en) 2009-04-14 2012-02-22 Cellzome Limited Fluoro substituted pyrimidine compounds as jak3 inhibitors
US8637529B2 (en) * 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds

Similar Documents

Publication Publication Date Title
JP2013508332A5 (enExample)
RU2014152257A (ru) Гетероциклильные пиримидиновые аналоги в качестве ингибиторов tyk2
JP2013534233A5 (enExample)
JP2020505454A5 (enExample)
RU2013155456A (ru) Соединения пирролидинилмочевины и пирролидинилтиомочевины как ингибиторы киназы trka
RU2424242C2 (ru) Азолопиримидины в качестве ингибиторов активности каннабиноидного рецептора 1
JP2019535664A5 (enExample)
JP2010510319A5 (enExample)
JP2017530999A5 (enExample)
HRP20231730T1 (hr) Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primjene
RU2004106783A (ru) Производные 4-амино-6-фенилпирроло[2, 3] пиримидина
JP2018044008A5 (enExample)
JP2013523884A5 (enExample)
RU2012111701A (ru) Фенилпири(ми)динилазолы
RU2015112580A (ru) Ингибиторные соединения
RU2012104493A (ru) Замещенные соединения пиразоло [1,5-a] пиримидина как ингибиторы киназы trk
JP2015529192A5 (enExample)
JP2008519790A5 (enExample)
JP2002527436A5 (enExample)
JP2015516392A5 (enExample)
RU2017116598A (ru) Соединения и композиции для модуляции киназной активности мутантов egfr
JP2000159672A (ja) 硝酸誘発耐性の処置剤
JP2014531449A5 (enExample)
JP2019504821A5 (enExample)
RU2009125897A (ru) Ингибиторы фосфоинозитид-3-киназы и способы их применения