JP2007531760A5 - - Google Patents

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Publication number
JP2007531760A5
JP2007531760A5 JP2007506535A JP2007506535A JP2007531760A5 JP 2007531760 A5 JP2007531760 A5 JP 2007531760A5 JP 2007506535 A JP2007506535 A JP 2007506535A JP 2007506535 A JP2007506535 A JP 2007506535A JP 2007531760 A5 JP2007531760 A5 JP 2007531760A5
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heteroatoms
optionally substituted
compound
independently
nitrogen
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JP2007506535A
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English (en)
Japanese (ja)
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JP4937112B2 (ja
JP2007531760A (ja
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Priority claimed from PCT/US2005/010846 external-priority patent/WO2005095400A1/en
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Publication of JP2007531760A5 publication Critical patent/JP2007531760A5/ja
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Publication of JP4937112B2 publication Critical patent/JP4937112B2/ja
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JP2007506535A 2004-03-30 2005-03-30 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール Expired - Fee Related JP4937112B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US55750304P 2004-03-30 2004-03-30
US60/557,503 2004-03-30
US62559904P 2004-11-05 2004-11-05
US60/625,599 2004-11-05
PCT/US2005/010846 WO2005095400A1 (en) 2004-03-30 2005-03-30 Azaindoles useful as inhibitors of jak and other protein kinases

Related Child Applications (2)

Application Number Title Priority Date Filing Date
JP2008060340A Division JP5042888B2 (ja) 2004-03-30 2008-03-10 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2011264040A Division JP5566992B2 (ja) 2004-03-30 2011-12-01 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール

Publications (3)

Publication Number Publication Date
JP2007531760A JP2007531760A (ja) 2007-11-08
JP2007531760A5 true JP2007531760A5 (enExample) 2012-01-26
JP4937112B2 JP4937112B2 (ja) 2012-05-23

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ID=34971569

Family Applications (5)

Application Number Title Priority Date Filing Date
JP2007506535A Expired - Fee Related JP4937112B2 (ja) 2004-03-30 2005-03-30 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2008060340A Expired - Fee Related JP5042888B2 (ja) 2004-03-30 2008-03-10 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2011264040A Expired - Fee Related JP5566992B2 (ja) 2004-03-30 2011-12-01 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2013183669A Withdrawn JP2013249315A (ja) 2004-03-30 2013-09-05 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2015051664A Withdrawn JP2015113347A (ja) 2004-03-30 2015-03-16 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール

Family Applications After (4)

Application Number Title Priority Date Filing Date
JP2008060340A Expired - Fee Related JP5042888B2 (ja) 2004-03-30 2008-03-10 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2011264040A Expired - Fee Related JP5566992B2 (ja) 2004-03-30 2011-12-01 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2013183669A Withdrawn JP2013249315A (ja) 2004-03-30 2013-09-05 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール
JP2015051664A Withdrawn JP2015113347A (ja) 2004-03-30 2015-03-16 Jakおよび他のプロテインキナーゼの阻害剤として有用なアザインドール

Country Status (26)

Country Link
US (6) US7507826B2 (enExample)
EP (4) EP1730146B1 (enExample)
JP (5) JP4937112B2 (enExample)
KR (3) KR101216372B1 (enExample)
CN (3) CN103554104A (enExample)
AR (2) AR048454A1 (enExample)
AT (1) ATE508129T1 (enExample)
AU (3) AU2005228904C1 (enExample)
BR (1) BRPI0509369B1 (enExample)
CA (1) CA2560454C (enExample)
CY (2) CY1111716T1 (enExample)
DE (1) DE602005027825D1 (enExample)
DK (2) DK1730146T3 (enExample)
ES (2) ES2398712T3 (enExample)
HR (1) HRP20110566T8 (enExample)
IL (2) IL177807A (enExample)
MX (1) MXPA06011327A (enExample)
NO (2) NO340403B1 (enExample)
NZ (2) NZ549880A (enExample)
PL (2) PL2332940T3 (enExample)
PT (2) PT1730146E (enExample)
RS (1) RS51830B (enExample)
RU (2) RU2403252C2 (enExample)
SI (1) SI1730146T1 (enExample)
TW (3) TWI471133B (enExample)
WO (1) WO2005095400A1 (enExample)

Families Citing this family (179)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
CA2560454C (en) * 2004-03-30 2013-05-21 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
EP1778687A2 (en) 2004-07-27 2007-05-02 SGX Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
WO2006015123A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
HN2005000795A (es) * 2004-10-15 2010-08-19 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
WO2006050076A1 (en) * 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
EP1828180A4 (en) * 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
AU2005316599A1 (en) * 2004-12-14 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrimidine inhibitors of ERK protein kinase and uses therof
WO2006087530A1 (en) 2005-02-16 2006-08-24 Astrazeneca Ab Chemical compounds
US20060183758A1 (en) * 2005-02-17 2006-08-17 Cb Research And Development, Inc. Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans
BRPI0610828A2 (pt) * 2005-05-16 2010-07-27 Irm Llc compostos e composições como inibidores de proteìna quinase
MX2007014377A (es) 2005-05-17 2008-02-06 Plexxikon Inc Inhibidores de proteina cinasa de derivados de pirrol (2,3-b) piridina.
ES2380795T3 (es) 2005-05-20 2012-05-18 Vertex Pharmaceuticals, Inc. Pirrolopiridinas útiles como inhibidores de proteínas quinasas
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP2388259A1 (en) 2005-10-28 2011-11-23 AstraZeneca AB 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
DK3184526T3 (en) 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
KR20080083680A (ko) * 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
EP2537849A3 (en) * 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of janus kinases
EP1979353A2 (en) * 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
DE102006012617A1 (de) * 2006-03-20 2007-09-27 Merck Patent Gmbh 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
RU2008143361A (ru) * 2006-04-05 2010-05-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Деазапурины в качестве ингибиторов янус-киназ
WO2007136790A2 (en) * 2006-05-18 2007-11-29 Mannkind Corporation Intracellular kinase inhibitors
BRPI0719883A2 (pt) 2006-10-09 2015-05-05 Takeda Pharmaceutical Inibidores de quinase
EP2079696A2 (en) * 2006-10-09 2009-07-22 Takeda San Diego, Inc. Kinase inhibitors
CN101573335A (zh) * 2006-10-09 2009-11-04 武田药品工业株式会社 激酶抑制剂
CA2668159A1 (en) * 2006-11-01 2008-07-03 Vertex Pharmaceuticals Incorporated Tricyclic heteroaryl compounds useful as inhibitors of janus kinase
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
NZ577798A (en) * 2006-12-21 2012-04-27 Vertex Pharma 5-cyano-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
AU2008228768A1 (en) * 2007-03-22 2008-09-25 Vertex Pharmaceuticals Incorporated N-heterocyclic compounds useful as inhibitors of Janus Kinases
EP2078020A4 (en) 2007-04-10 2011-10-19 Sgx Pharmaceuticals Inc HETEROCYCLIC MODULATORS WITH FUSED CYCLES FOR KINASES
CN101678014B (zh) * 2007-05-21 2012-12-12 Sgx药品公司 杂环激酶调节剂
EP2740731B1 (en) 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
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.
DE102007028515A1 (de) * 2007-06-21 2008-12-24 Merck Patent Gmbh 6-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
EP2170830B1 (en) 2007-07-17 2014-10-15 Plexxikon, Inc. 2-FLUORO-BENZENESULFONAMIDE COMPOUNDS AS Raf KINASE MODULATORS
WO2009054941A1 (en) 2007-10-25 2009-04-30 Merck & Co., Inc. Therapeutic compounds
GB2455176A (en) * 2007-11-01 2009-06-03 Acucela Inc Amine derivatives useful for treating ophthalmic diseases and disorders
KR20100108390A (ko) * 2007-12-19 2010-10-06 버텍스 파마슈티칼스 인코포레이티드 JAK2 억제제로서 유용한 피라졸로[1,5-a]피리미딘
WO2009145814A2 (en) * 2008-03-10 2009-12-03 Vertex Pharmaceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
ES2602577T3 (es) 2008-03-11 2017-02-21 Incyte Holdings Corporation Derivados de azetidina y ciclobutano como inhibidores de JAK
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
DE102008031517A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
JP2011529062A (ja) * 2008-07-23 2011-12-01 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 ピラゾロピリジンキナーゼ阻害剤
BRPI0916295A2 (pt) * 2008-07-23 2019-09-24 Vertex Pharma inibidores de pirazolopiridina tricíclica cinase
NZ590887A (en) * 2008-08-04 2012-09-28 Chdi Foundation Inc Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
MX2011002825A (es) * 2008-09-18 2011-04-05 Astellas Pharma Inc Compuestos heterociclicos de carboxamida.
DE102008052943A1 (de) * 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
US8877772B2 (en) * 2008-11-25 2014-11-04 University Of Rochester Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors
AR074870A1 (es) * 2008-12-24 2011-02-16 Palau Pharma Sa Derivados de pirazolo (1,5-a ) piridina
KR20170058465A (ko) 2009-04-03 2017-05-26 에프. 호프만-라 로슈 아게 프로판-1-술폰산 {3-[5-(4-클로로-페닐)-1H-피롤로[2,3-b]피리딘-3-카르보닐]-2,4-디플루오로-페닐}-아미드 조성물 및 그의 용도
TW201040162A (en) 2009-05-06 2010-11-16 Portola Pharm Inc Inhibitors of JAK
ES2487542T3 (es) 2009-05-22 2014-08-21 Incyte Corporation 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 cinasas Janus
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
CN102458402B (zh) 2009-06-12 2013-10-02 百时美施贵宝公司 用作激酶调节剂的烟酰胺化合物
AU2016204286B2 (en) * 2009-06-17 2018-02-01 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
GEP20207129B (en) * 2009-06-17 2020-07-10 Vertex Pharma Inhibitors of influenza viruses replication
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
MX2012000711A (es) * 2009-07-15 2012-03-16 Abbott Lab Inhibidores de pirrolopirazina de cinasas.
WO2011008915A1 (en) * 2009-07-15 2011-01-20 Abbott Laboratories Pyrrolopyridine inhibitors of kinases
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CA2777114C (en) 2009-10-09 2018-10-23 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
AU2010315126B2 (en) 2009-11-06 2015-06-25 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2011060216A1 (en) 2009-11-12 2011-05-19 Concert Pharmaceuticals Inc. Substituted azaindoles
DE102009060174A1 (de) * 2009-12-23 2011-06-30 Merck Patent GmbH, 64293 Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
MX2012008644A (es) * 2010-01-27 2012-11-23 Vertex Pharma Inhibidores de cinasa de pirazolopiridinas.
EP2582702A1 (en) 2010-01-27 2013-04-24 Vertex Pharmaceuticals Incorporated Pyrazolopyrimidine kinase inhibitors
MX2012008642A (es) * 2010-01-27 2012-11-23 Vertex Pharma Inhibidores de cinasas de pirazolopiridinas.
CN102869663A (zh) 2010-01-27 2013-01-09 沃泰克斯药物股份有限公司 吡唑并吡嗪激酶抑制剂
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011109932A1 (en) * 2010-03-09 2011-09-15 F.Hoffmann-La Roche Ag Novel process for the manufacture of 5-halogenated-7-azaindoles
SMT201800137T1 (it) 2010-03-10 2018-07-17 Incyte Holdings Corp Derivati di piperidin-4-il azetidina come inibitori di jak1
PH12012502296B1 (en) 2010-05-21 2017-10-06 Incyte Holdings Corp Topical formulation for a jak inhibitor
US8779150B2 (en) 2010-07-21 2014-07-15 Hoffmann-La Roche Inc. Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
CA2822059A1 (en) * 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
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
WO2012083122A1 (en) 2010-12-16 2012-06-21 Vertex Pharmaceutical Incorporated Inhibitors of influenza viruses replication
DE102011009961A1 (de) 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
WO2012109075A1 (en) 2011-02-07 2012-08-16 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP2487159A1 (en) * 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
EP2688890B1 (en) 2011-03-22 2017-08-30 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
EP2729465A2 (en) * 2011-07-05 2014-05-14 Vertex Pharmaceuticals Incorporated Processes and intermediates for producing azaindoles
UA118010C2 (uk) * 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
JP2014521725A (ja) 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト JAKPI3K/mTOR併用療法
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
EA027451B1 (ru) 2011-08-30 2017-07-31 Схди Фаундейшн, Инк. Ингибиторы кинуренин-3-монооксигеназы, фармацевтические композиции и их применение
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AU2012336019A1 (en) 2011-11-07 2014-05-29 Vertex Pharmaceuticals Incorporated Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor
DE102011119127A1 (de) * 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
JP6039683B2 (ja) 2011-11-23 2016-12-07 ポートラ ファーマシューティカルズ, インコーポレイテッド ピラジンキナーゼ阻害剤
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2013184985A1 (en) 2012-06-08 2013-12-12 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
WO2014074471A1 (en) 2012-11-06 2014-05-15 Vertex Pharmaceuticals Incorporated Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor
PE20151157A1 (es) 2012-11-15 2015-08-19 Incyte Corp Formas de dosificacion de ruxolitinib de liberacion sostenida
KR20220143164A (ko) 2012-11-21 2022-10-24 피티씨 테라퓨틱스, 인크. 치환된 리버스 피리미딘 bmi-1 저해제
WO2014085795A1 (en) 2012-11-30 2014-06-05 University Of Rochester Mixed lineage kinase inhibitors for hiv/aids therapies
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
FR2999575A1 (fr) * 2012-12-18 2014-06-20 Centre Nat Rech Scient 3,5-diaryl-azaindoles comme inhibiteurs de la proteine dyrk1a pour le traitement des deficiences cognitives liees au syndrome de down et a la maladie d'alzheimer
WO2014110259A1 (en) 2013-01-09 2014-07-17 Vertex Pharmaceuticals Incorporated Solid forms of a jak inhibitor
FR3001219A1 (fr) * 2013-01-22 2014-07-25 Centre Nat Rech Scient Inhibiteurs de kinases
LT3489239T (lt) 2013-03-06 2022-03-10 Incyte Holdings Corporation Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai
JP6118453B2 (ja) * 2013-04-02 2017-04-19 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ブルトンチロシンキナーゼの阻害剤
US9206188B2 (en) * 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
WO2014201332A1 (en) 2013-06-14 2014-12-18 Vertex Pharmaceuticals Incorporated Pharmaceutical combinations useful for treating rheumatoid arthritis
ES2772131T3 (es) * 2013-08-07 2020-07-07 Pharmathen Sa Un nuevo proceso para la preparación de Febuxostat
UA120499C2 (uk) 2013-08-07 2019-12-26 Інсайт Корпорейшн Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1
RU2016110094A (ru) 2013-08-22 2017-09-27 Вертекс Фармасьютикалз Инкорпорейтед Изотопно-обогащенные азаиндолы
MX370588B (es) 2013-08-30 2019-12-16 Ptc Therapeutics Inc Inhibidores de la bmi-1 de pirimidina sustituida.
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
EP3421468B1 (en) 2013-11-13 2020-11-04 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
HRP20191525T1 (hr) 2013-11-13 2019-11-29 Vertex Pharma Inhibitori replikacije virusa influence
WO2015076800A1 (en) 2013-11-21 2015-05-28 Ptc Therapeutics, Inc. Substituted pyridine and pyrazine bmi-1 inhibitors
KR101662597B1 (ko) * 2014-04-02 2016-10-05 한국과학기술원 아자인돌 유도체 화합물, 이를 포함하는 c-KIT 저해제 조성물 및 c-KIT와 관련된 질환의 치료용 약학 조성물
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
CN114588157A (zh) 2014-07-17 2022-06-07 Chdi基金会股份有限公司 用于治疗hiv相关病症的方法和组合物
JP6577570B2 (ja) 2014-08-08 2019-09-18 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー インフルエンザウイルス感染に使用するためのインドール類
MA40772A (fr) 2014-10-02 2017-08-08 Vertex Pharma Variants du virus de la grippe a
MA40773A (fr) 2014-10-02 2017-08-08 Vertex Pharma Variants du virus influenza a
US10336748B2 (en) 2015-01-30 2019-07-02 Pfizer Inc. Methyoxy-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof
WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
JP6704416B2 (ja) 2015-05-13 2020-06-03 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を調製する方法
KR20250035597A (ko) * 2015-09-25 2025-03-12 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 Jak를 억제하기 위한 화합물 및 방법
RU2765154C2 (ru) * 2015-11-04 2022-01-26 Мерк Патент Гмбх Способы лечения злокачественной опухоли с использованием соединений пиримидина и пиридина с btk ингибирующей активностью
HRP20231547T1 (hr) 2015-11-17 2024-03-15 Merck Patent Gmbh Postupci liječenja multiple skleroze primjenom spojeva pirimidina i piridina s aktivnošću inhibicije btk
EP3362451B1 (en) 2015-12-09 2023-04-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
WO2017198122A1 (zh) * 2016-05-19 2017-11-23 四川大学 抗流感小分子化合物及其制备方法和用途
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
EP4183786A1 (en) * 2016-12-23 2023-05-24 Felicitex Therapeutics, Inc. Derivatives of quinolines as inhibitors of dyrk1a and/or dyrk1b kinases
JPWO2018159805A1 (ja) 2017-03-03 2020-01-09 国立大学法人京都大学 膵前駆細胞の製造方法
TWI778052B (zh) 2017-04-24 2022-09-21 美商共結晶製藥公司 流感病毒複製之抑制劑
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
IL276302B2 (en) 2018-01-30 2023-11-01 Incyte Corp Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one)
AR117398A1 (es) * 2018-03-12 2021-08-04 Abbvie Inc Inhibidores de la señalización mediada por tirosina cinasa 2
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
EP3829719B1 (en) 2018-07-27 2025-04-02 Cocrystal Pharma, Inc. Pyrrolo[2,3-b]pyridin derivatives as inhibitors of influenza virus replication
CN109232562A (zh) * 2018-10-24 2019-01-18 康化(上海)新药研发有限公司 一种7-氮杂吲哚-5-氯-6-羧酸的合成方法
EP3887355A1 (en) 2018-11-26 2021-10-06 Cocrystal Pharma, Inc. Inhibitors of influenza virus replication
US11174263B2 (en) 2018-12-31 2021-11-16 Biomea Fusion, Inc. Inhibitors of menin-MLL interaction
AU2019417833B2 (en) 2018-12-31 2024-11-07 Biomea Fusion, Inc. Irreversible inhibitors of menin-MLL interaction
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US20230151034A1 (en) 2020-03-17 2023-05-18 Cocrystal Pharma, Inc. Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CA3201540A1 (en) * 2020-12-24 2022-06-30 Xiaohui Gu Aromatic heterocyclic compound, pharmaceutical composition and use thereof
EP4340833B1 (fr) * 2021-05-21 2025-09-03 Centre National de la Recherche Scientifique (CNRS) Nouveaux derives azaindole en tant qu'agents antiviraux
CA3228627A1 (en) 2021-08-11 2023-02-16 Thomas Butler Covalent inhibitors of menin-mll interaction for diabetes mellitus
EP4387972A1 (en) 2021-08-20 2024-06-26 Biomea Fusion, Inc. Crystalline form of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(r)-[(1-oxo -2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide, an irreversible menin-mll inhibitor for the treatment of cancer
IL312157A (en) 2021-10-12 2024-06-01 Biosplice Therapeutics Inc History of pyrrolo[1,2-F][4,2,1]triazines as DYRK1A inhibitors
US20230192686A1 (en) * 2021-10-12 2023-06-22 Biosplice Therapeutics, Inc. 1h-pyrrolo[2,3-b]pyridines and preparation and uses thereof
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation
WO2024155710A1 (en) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6- yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2-pyridinecarboxamide as a covalent inhibitor of menin-mll interaction
US20250326772A1 (en) * 2024-04-19 2025-10-23 Kyorin Pharmaceutical Co., Ltd. Mrgprx2 antagonists, pharmaceutical composition including mrgprx2 antagonist, and method of treating mrgprx2-mediated disease or disorder

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT85662B (pt) 1986-09-10 1990-06-29 Sandoz Sa Processo para a preparacao de derivados de aza-indol e de indolizina e de composicoes farmaceuticas que os contem
FR2687402B1 (fr) 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
US6075037A (en) 1994-06-09 2000-06-13 Smithkline Beecham Corporation Endothelin receptor antagonists
GB9721437D0 (en) * 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
US6180096B1 (en) * 1998-03-26 2001-01-30 Schering Corporation Formulations for protection of peg-interferon alpha conjugates
AU2494300A (en) 1999-01-07 2000-07-24 American Home Products Corporation 3,4-dihydro-2h-benzo(1,4)oxazine derivatives
US6265403B1 (en) * 1999-01-20 2001-07-24 Merck & Co., Inc. Angiogenesis inhibitors
EP1196167B1 (en) 1999-07-02 2006-04-19 Stuart A. Lipton Use of p38 MAPK inhibitors in the treatment of ophthalmic conditions
CA2396693A1 (en) * 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
WO2001060816A1 (en) * 2000-02-17 2001-08-23 Amgen Inc. Kinase inhibitors
US7041277B2 (en) 2000-03-10 2006-05-09 Cadbury Adams Usa Llc Chewing gum and confectionery compositions with encapsulated stain removing agent compositions, and methods of making and using the same
CN1642973A (zh) * 2000-09-06 2005-07-20 奥索-麦克尼尔药品公司 治疗变态反应的方法
DK1355904T3 (da) 2000-12-22 2007-10-15 Wyeth Corp Heterocyclindazol- og -azaindazolforbindelser som 5-hydroxytryptamin-6-ligander
JP4343534B2 (ja) 2001-03-02 2009-10-14 ゲーペーツェー バイオテック アクチェンゲゼルシャフト 3ハイブリッド・アッセイ・システム
WO2002072587A1 (en) 2001-03-14 2002-09-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]quinoline
WO2002085896A1 (en) 2001-04-24 2002-10-31 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-benzodioxan
US6656950B2 (en) 2001-04-25 2003-12-02 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine
EP1381614B1 (en) 2001-04-26 2006-08-02 Wyeth ANTIDEPRESSANT AZAHETEROCYCLYLMETHYL DERIVATIVES OF 2,3-DIHYDRO-1,4-DIOXINO¬2,3-f|QUINOXALINE
CA2445543A1 (en) 2001-04-26 2002-11-07 Hong Gao Antidepressant azaheterocyclylmethyl derivatives of oxaheterocycle-fused-¬1,4|-benzodioxans
ES2247327T3 (es) 2001-04-26 2006-03-01 Wyeth Derivados azaheterociclimetilicos antidepresivos (isrs) de 7,8-dihidro-3h-6,9-dioxa-1,3-diazaciclopenta(a) naftaleno.
EP1392700B1 (en) 2001-04-30 2004-09-29 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-1,6,9-trioxa-3-aza-cyclopenta(a)naphthalene
AU2002309769B2 (en) 2001-05-17 2008-04-17 Wyeth Processes for the synthesis of derivatives of 2,3-dihydro-1,4-dioxino-[2,3-f] quinoline
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
US7429609B2 (en) * 2002-05-31 2008-09-30 Eisai R & D Management Co., Ltd. Pyrazole compound and medicinal composition containing the same
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
SE0202463D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
JP4787150B2 (ja) * 2003-03-06 2011-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 Jnk阻害剤
US7375228B2 (en) 2003-03-17 2008-05-20 Takeda San Diego, Inc. Histone deacetylase inhibitors
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
WO2004106298A1 (en) 2003-05-30 2004-12-09 Janssen Pharmaceutica N.V. Indole derivatives with an improved antipsychotic activity
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
GB0405055D0 (en) 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
CA2560454C (en) * 2004-03-30 2013-05-21 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
EP1756108A2 (en) * 2004-04-02 2007-02-28 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
ITMI20040874A1 (it) 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
US20060058339A1 (en) 2004-06-17 2006-03-16 Ibrahim Prabha N Compounds modulating c-kit activity and uses therefor
US20050288290A1 (en) * 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
WO2006015123A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
BRPI0610828A2 (pt) 2005-05-16 2010-07-27 Irm Llc compostos e composições como inibidores de proteìna quinase
ES2380795T3 (es) 2005-05-20 2012-05-18 Vertex Pharmaceuticals, Inc. Pirrolopiridinas útiles como inhibidores de proteínas quinasas
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
ES2401192T3 (es) * 2005-09-30 2013-04-17 Vertex Pharmceuticals Incorporated Deazapurinas útiles como inhibidores de janus cinasas
EP2537849A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of janus kinases
RU2008143361A (ru) 2006-04-05 2010-05-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Деазапурины в качестве ингибиторов янус-киназ
EP2729465A2 (en) * 2011-07-05 2014-05-14 Vertex Pharmaceuticals Incorporated Processes and intermediates for producing azaindoles

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