JP2008545660A - プロテインキナーゼ阻害剤として有用なピロロピリジン化合物 - Google Patents

プロテインキナーゼ阻害剤として有用なピロロピリジン化合物 Download PDF

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JP2008545660A
JP2008545660A JP2008512591A JP2008512591A JP2008545660A JP 2008545660 A JP2008545660 A JP 2008545660A JP 2008512591 A JP2008512591 A JP 2008512591A JP 2008512591 A JP2008512591 A JP 2008512591A JP 2008545660 A JP2008545660 A JP 2008545660A
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compound
hydrogen
group
compound according
membered
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JP2008545660A5 (https=
Inventor
マーク ダブリュー. レデボーア,
マリオン ダブリュー. ワナメーカー,
ルーク ジェイ. ファーマー,
ティエンシェン ワン,
アルバート シー. ピアース,
ガブリエル マルティネス−ボテラ,
ランディー エス. ベシール,
ガイ ダブリュー. ビーミス,
チアン ワン,
フランセスコ ジー. サリトゥロ,
マイケル ジェイ. アーノスト,
ジョン エイチ. カム,
ジェレミー グリーン,
ミシェル スチュワート,
クレイグ マーヘフカ,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of JP2008545660A publication Critical patent/JP2008545660A/ja
Publication of JP2008545660A5 publication Critical patent/JP2008545660A5/ja
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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JP2008512591A 2005-05-20 2006-05-22 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物 Pending JP2008545660A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68355405P 2005-05-20 2005-05-20
PCT/US2006/019711 WO2006127587A1 (en) 2005-05-20 2006-05-22 Pyrrolopyridines useful as inhibitors of protein kinase

Related Child Applications (2)

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JP2009123635A Division JP2009179644A (ja) 2005-05-20 2009-05-21 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
JP2013196681A Division JP2013253114A (ja) 2005-05-20 2013-09-24 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物

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JP2008545660A true JP2008545660A (ja) 2008-12-18
JP2008545660A5 JP2008545660A5 (https=) 2009-07-30

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JP2008512591A Pending JP2008545660A (ja) 2005-05-20 2006-05-22 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
JP2009123635A Pending JP2009179644A (ja) 2005-05-20 2009-05-21 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
JP2013196681A Pending JP2013253114A (ja) 2005-05-20 2013-09-24 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物

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JP2009123635A Pending JP2009179644A (ja) 2005-05-20 2009-05-21 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
JP2013196681A Pending JP2013253114A (ja) 2005-05-20 2013-09-24 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物

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US (1) US8921376B2 (https=)
EP (3) EP2354140A1 (https=)
JP (3) JP2008545660A (https=)
KR (1) KR20080016659A (https=)
CN (1) CN101228161B (https=)
AT (1) ATE540948T1 (https=)
AU (1) AU2006251623A1 (https=)
CA (1) CA2609126A1 (https=)
ES (1) ES2380795T3 (https=)
IL (1) IL187438A0 (https=)
MX (1) MX2007014619A (https=)
NO (1) NO20076502L (https=)
NZ (1) NZ564065A (https=)
RU (2) RU2435769C2 (https=)
WO (1) WO2006127587A1 (https=)
ZA (1) ZA200710379B (https=)

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009519340A (ja) * 2005-12-13 2009-05-14 インサイト・コーポレイション JANUSキナーゼ阻害剤としてのヘテロアリール置換ピロロ[2,3−b]ピリジンおよびピロロ[2,3−b]ピリミジン
WO2011013785A1 (ja) * 2009-07-31 2011-02-03 日本たばこ産業株式会社 含窒素スピロ環化合物及びその医薬用途
JP2013501713A (ja) * 2009-08-07 2013-01-17 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規なアザ複素環化合物
JP2013522214A (ja) * 2010-03-10 2013-06-13 インサイト・コーポレイション Jak1阻害剤としてのピペリジン−4−イルアゼチジン誘導体
JP2013253114A (ja) * 2005-05-20 2013-12-19 Vertex Pharmaceuticals Inc プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
JP2014500260A (ja) * 2010-11-19 2014-01-09 インサイト・コーポレイション Jak阻害剤としてのシクロブチル置換ピロロピリジンおよびピロロピリミジン誘導体
WO2015119126A1 (ja) * 2014-02-04 2015-08-13 大鵬薬品工業株式会社 アザインドール誘導体
JP2016512198A (ja) * 2013-03-06 2016-04-25 アロステロス セラピューティクス, インコーポレイテッド CaMKII阻害剤及びその使用
JP2017506656A (ja) * 2014-03-28 2017-03-09 ノバルティス ティーアゲズントハイト アーゲー 新規化合物
US9611269B2 (en) 2011-06-20 2017-04-04 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
US9623029B2 (en) 2009-05-22 2017-04-18 Incyte Holdings Corporation 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors
US9714233B2 (en) 2013-03-06 2017-07-25 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US9718834B2 (en) 2011-09-07 2017-08-01 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US10561616B2 (en) 2013-08-07 2020-02-18 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
KR20200043412A (ko) * 2017-08-23 2020-04-27 스프린트 바이오사이언스 아베 아자인돌릴피리돈 및 디아자인돌릴피리돈 화합물
US10758543B2 (en) 2010-05-21 2020-09-01 Incyte Corporation Topical formulation for a JAK inhibitor
US10759792B2 (en) 2014-09-05 2020-09-01 The Johns Hopkins University CaMKII inhibitors and uses thereof
US10899736B2 (en) 2018-01-30 2021-01-26 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US11213528B2 (en) 2007-06-13 2022-01-04 Incyte Holdings Corporation Salts of the janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
JP2022504988A (ja) * 2018-10-16 2022-01-13 ダナ-ファーバー キャンサー インスティテュート,インコーポレイテッド Lrrk2の野生型および変異型のアザインドール阻害剤
US11304949B2 (en) 2018-03-30 2022-04-19 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
US11337927B2 (en) 2012-11-15 2022-05-24 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
JP2022531088A (ja) * 2019-05-02 2022-07-06 アクラリス セラピューティクス,インコーポレイテッド Jak阻害剤としての置換ピロロピリジン
JP2023527055A (ja) * 2020-05-26 2023-06-26 サントル ナショナル ドゥ ラ ルシェルシュ シアンティフィック がんの治療に使用するためのlimk及び/又はrockキナーゼ阻害剤としての4-(7h-ピロロ[2,3-d]ピリミジン-4-イル)-3,6-ジヒドロピリジン-1-(2h)-カルボキサミド誘導体
WO2023145372A1 (ja) * 2022-01-28 2023-08-03 日本曹達株式会社 アミド化合物の製造方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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* Cited by examiner, † Cited by third party
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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
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
US7846941B2 (en) 2005-05-17 2010-12-07 Plexxikon, Inc. Compounds modulating c-kit and c-fms activity and uses therefor
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
WO2007007919A2 (en) * 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
AU2015201850B2 (en) * 2005-12-13 2017-03-02 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
AU2012201894A1 (en) * 2005-12-13 2012-04-19 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
WO2007076423A2 (en) * 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
BRPI0710479A2 (pt) 2006-01-18 2012-08-14 Hoffmann La Roche composto, processo para sua preparaÇço, composiÇço farmacÊutica, uso de um composto e mÉtodo de tratamento de doenÇa ou desosrdem metabàlica.
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
SG170828A1 (en) * 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
WO2007136790A2 (en) * 2006-05-18 2007-11-29 Mannkind Corporation Intracellular kinase inhibitors
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
ATE523499T1 (de) * 2006-07-06 2011-09-15 Array Biopharma Inc Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer
US8063050B2 (en) * 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CA2656566C (en) 2006-07-06 2014-06-17 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
US8148361B2 (en) * 2006-11-10 2012-04-03 Bristol-Myers Squibb Company Kinase inhibitors
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US8071779B2 (en) 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
JP2010514695A (ja) 2006-12-21 2010-05-06 プレキシコン,インコーポレーテッド キナーゼ調節のための化合物および方法およびそのための適応症
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
CN101678022A (zh) 2006-12-21 2010-03-24 弗特克斯药品有限公司 可用作蛋白激酶抑制剂的5-氰基-4-(吡咯并[2,3b]吡啶-3-基)嘧啶衍生物
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
AR064879A1 (es) 2007-01-12 2009-04-29 Astellas Pharma Inc Compuesto de piridina condensado
MX2009010127A (es) * 2007-03-22 2009-11-05 Vertex Pharma Compuestos utiles como inhibidores de janus cinasas.
JP5603770B2 (ja) 2007-05-31 2014-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2受容体拮抗薬およびその使用
GB0710528D0 (en) * 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
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.
CN101918373B (zh) * 2007-07-05 2013-06-05 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2009006567A2 (en) 2007-07-05 2009-01-08 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CA2711614A1 (en) 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors
ES2422733T3 (es) * 2008-01-09 2013-09-13 Array Biopharma Inc Pirimidilciclopentanos hidroxilados como inhibidores de proteínas cinasas AKT
EP2240455B1 (en) * 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
CA2711741A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
GB0801416D0 (en) * 2008-01-25 2008-03-05 Piramed Ltd Pharmaceutical compounds
JP2011513483A (ja) * 2008-03-10 2011-04-28 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 タンパク質キナーゼの阻害剤として有用なピリミジンおよびピリジン
HUE029767T2 (en) 2008-03-11 2017-04-28 Incyte Holdings Corp JAK inhibitor azetidine and cyclobutane derivatives
GB0804592D0 (en) * 2008-03-12 2008-04-16 Glaxo Group Ltd Novel compounds
CL2009001152A1 (es) 2008-05-13 2009-10-16 Array Biopharma Inc Compuestos derivados de n-(4-(cicloalquilo nitrogenado-1-il)-1h-pirrolo[2,3-b]piridin-3-il)amida, inhibidores de cinasa; proceso de preparacion; composicion farmaceutica; y su uso para el tratamiento de una enfermedad proliferativa.
US8822513B2 (en) 2010-03-01 2014-09-02 Gtx, Inc. Compounds for treatment of cancer
MX2010014066A (es) 2008-06-16 2011-06-01 Univ Tennessee Res Foundation Compuestos para el tratamiento del cancer.
US9447049B2 (en) 2010-03-01 2016-09-20 University Of Tennessee Research Foundation Compounds for treatment of cancer
US9029408B2 (en) 2008-06-16 2015-05-12 Gtx, Inc. Compounds for treatment of cancer
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.
DE102008052943A1 (de) 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
CN102256963B (zh) 2008-12-19 2014-06-11 贝林格尔.英格海姆国际有限公司 作为ccr2受体拮抗剂用于治疗炎症、哮喘和copd的环状嘧啶-4-甲酰胺
MY172424A (en) 2009-04-03 2019-11-25 Hoffmann La Roche Propane- i-sulfonic acid {3- (4-chloro-phenyl)-1h-pyrrolo [2, 3-b] pyridine-3-carconyl] -2, 4-difluoro-phenyl} -amide compositions and uses thereof
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
LT3141252T (lt) 2009-06-17 2018-11-12 Vertex Pharmaceuticals Inc. Gripo virusų replikacijos inhibitoriai
WO2011003418A1 (en) 2009-07-08 2011-01-13 Leo Pharma A/S Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
CN102573994B (zh) * 2009-08-06 2015-06-24 默克专利有限公司 双环脲化合物
MX2012002059A (es) 2009-08-20 2012-04-19 Karus Therapeutics Ltd Compestos heterociclicos triciclicos como inhibidores de fosfoionositida 3-quinasa.
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
JP5658756B2 (ja) 2009-09-10 2015-01-28 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Jakの阻害剤
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
CN106220623A (zh) 2009-11-06 2016-12-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
ES2674275T3 (es) 2009-12-17 2018-06-28 Centrexion Therapeutics Corporation Antagonistas del receptor CCR2 y usos de los mismos
USRE49251E1 (en) 2010-01-04 2022-10-18 Mapi Pharma Ltd. Depot systems comprising glatiramer or pharmacologically acceptable salt thereof
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Janusキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
JP5879273B2 (ja) 2010-03-01 2016-03-08 ジーティーエックス・インコーポレイテッド 癌を処置するための化合物
WO2011141474A1 (en) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh Novel ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
JP5646736B2 (ja) 2010-05-12 2014-12-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ccr2受容体アンタゴニスト、これらの製造方法、及び薬物としてのこれらの使用
WO2011144501A1 (en) 2010-05-17 2011-11-24 Boehringer Ingelheim International Gmbh Ccr2 antagonists and uses thereof
WO2011147772A1 (en) 2010-05-25 2011-12-01 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists
US8962656B2 (en) 2010-06-01 2015-02-24 Boehringer Ingelheim International Gmbh CCR2 antagonists
EP2397482A1 (en) * 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
RU2013132681A (ru) 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
US9233964B2 (en) 2011-01-07 2016-01-12 Leo Pharma A/S Sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use therof
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
AR085279A1 (es) 2011-02-21 2013-09-18 Plexxikon Inc Formas solidas de {3-[5-(4-cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico
WO2012135781A1 (en) 2011-04-01 2012-10-04 Genentech, Inc. Combinations of akt inhibitor compounds and chemotherapeutic agents, and methods of use
RU2013148817A (ru) 2011-04-01 2015-05-10 Дженентек, Инк. Комбинации соединений-ингибиторов акт и мек и способы их применения
NZ714502A (en) 2011-07-05 2017-04-28 Vertex Pharma Processes and intermediates for producing azaindoles
EP2731941B1 (en) 2011-07-15 2019-05-08 Boehringer Ingelheim International GmbH Novel and selective ccr2 antagonists
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
EP2741747A1 (en) 2011-08-10 2014-06-18 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
GB201204125D0 (en) * 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
CA2868966C (en) 2012-03-29 2021-01-26 Francis Xavier Tavares Lactam kinase inhibitors
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
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
IN2015DN03235A (https=) 2012-11-07 2015-10-02 Karus Therapeutics Ltd
FR3001219A1 (fr) * 2013-01-22 2014-07-25 Centre Nat Rech Scient Inhibiteurs de kinases
CA2906157C (en) 2013-03-15 2022-05-17 G1 Therapeutics, Inc. Highly active anti-neoplastic and anti-proliferative agents
ME03557B (me) 2013-03-15 2020-07-20 G1 Therapeutics Inc Privremena zaštiтa normalnih ćelija током hemoterapije
RU2634723C2 (ru) * 2013-04-02 2017-11-03 Ф. Хоффманн-Ля Рош Аг Ингибиторы тирозинкиназы брутона
WO2014178426A1 (ja) * 2013-05-02 2014-11-06 富士フイルム株式会社 エッチング方法、これに用いるエッチング液およびエッチング液のキット、ならびに半導体基板製品の製造方法
PT2994465T (pt) 2013-05-10 2018-10-25 Karus Therapeutics Ltd Novos inibidores de histona desacetilase
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
JP6618901B2 (ja) 2013-11-13 2019-12-11 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
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
WO2015161288A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic lactams for use as anti-neoplastic and anti-proliferative agents
MX2016015613A (es) * 2014-05-28 2017-04-13 Astrazeneca Ab Procesos para la preparacion de azd5363 e intermedios novedosos utilizados en el mismo.
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
JP6633618B2 (ja) * 2014-08-21 2020-01-22 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 強力なrock阻害剤としてのタイドバックのベンズアミド誘導体
EP3191098A4 (en) 2014-09-12 2018-04-25 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
CN105837572B (zh) * 2015-02-02 2019-04-19 四川大学 N-取代苯基酰胺衍生物及其制备方法和用途
EP3294717B1 (en) 2015-05-13 2020-07-29 Vertex Pharmaceuticals Inc. Methods of preparing inhibitors of influenza viruses replication
EP3294735B8 (en) 2015-05-13 2022-01-05 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
PT3317270T (pt) 2015-07-02 2020-08-24 Centrexion Therapeutics Corp (4-((3r,4r)-3-metoxitetrahidro-pirano-4-ilamino)piperidina-1-il)(5-metil-6-(((2r,6s)-6-(p-tolil)tetrahidro-2h-pirano-2-il)metilamino)pirimidina-4-il)citrato de metanona
GB201514758D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
GB201514760D0 (en) * 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds and method of use
GB201514754D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514751D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
ES2830446T3 (es) 2015-12-11 2021-06-03 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Derivado de azetidina, método de preparación del mismo y uso del mismo
WO2017114275A1 (zh) * 2015-12-31 2017-07-06 成都先导药物开发有限公司 一种抑制rock的化合物及其制备方法与应用
KR102598246B1 (ko) 2016-07-26 2023-11-02 톈진 롱보진 파마시우티컬 씨오., 엘티디. Jak 저해제로서 헤테로사이클릭 화합물, 및 이의 염 및 치료학적 용도
US12097292B2 (en) 2016-08-28 2024-09-24 Mapi Pharma Ltd. Process for preparing microparticles containing glatiramer acetate
CN109982712A (zh) 2016-08-31 2019-07-05 Mapi医药公司 包含醋酸格拉替雷的储库系统
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
CN110662745B (zh) * 2017-03-23 2021-08-03 大邱庆北尖端医疗产业振兴财团 吡咯并吡啶衍生物、其制备方法、和用于预防或治疗蛋白激酶相关疾病的药物组合物
CN110382052A (zh) 2017-03-26 2019-10-25 Mapi医药公司 用于治疗进展型形式的多发性硬化症的格拉替雷储库系统
JP7311228B2 (ja) 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Rho-関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
CN110582491B (zh) 2017-06-30 2023-09-29 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
KR102563325B1 (ko) 2017-06-30 2023-08-03 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Rho-관련 단백질 키나아제 억제제, Rho-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
CN109535164B (zh) * 2017-09-21 2022-01-18 上海华汇拓医药科技有限公司 Jak激酶抑制剂及其制备方法和在医药领域的应用
KR102821964B1 (ko) 2017-11-03 2025-06-19 어클라리스 쎄라퓨틱스, 인코포레이티드 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법
WO2019090143A1 (en) * 2017-11-03 2019-05-09 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrimidine-5-carboxylate analogs and methods of making the same
US11485707B2 (en) 2018-03-23 2022-11-01 Fochon Pharmaceuticals, Ltd. Deuterated compounds as rock inhibitors
CN119080779A (zh) 2018-08-10 2024-12-06 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
EP3915985A4 (en) 2019-01-18 2022-09-28 Voronoi Co., Ltd. PYRROLOPYRIDE DERIVATIVE AND USE THEREOF FOR THE PREVENTION AND TREATMENT OF PROTEIN KINASE RELATED DISEASES
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
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
CN118619944A (zh) 2019-06-06 2024-09-10 北京泰德制药股份有限公司 作为atr激酶抑制剂的2,4,6-三取代的嘧啶化合物
GB201909468D0 (en) 2019-07-01 2019-08-14 Karus Therapeutics Ltd Compounds for treating cancer
CA3143636A1 (en) * 2019-07-12 2021-01-21 Michael Lim Compositions and methods for treating cerebral vasospasm
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
JP7717065B2 (ja) 2019-11-22 2025-08-01 インサイト コーポレーション Alk2阻害剤及びjak2阻害剤を含む併用療法
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
KR20220081631A (ko) 2020-12-09 2022-06-16 보로노이 주식회사 염증성 질환의 예방 및/또는 치료를 위한 피롤로-피리딘 유도체 화합물의 신규 용도
CN113402523B (zh) * 2021-07-13 2022-07-12 西安交通大学 一种靶向肥大细胞MrgX2小分子荧光探针及制备方法和应用
CN113735859A (zh) * 2021-08-12 2021-12-03 安徽医科大学 一种激酶抑制剂
CN117050075A (zh) * 2022-05-05 2023-11-14 中国药科大学 一类联芳环类bet抑制剂及合成方法与用途
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation
WO2026055338A1 (en) * 2024-09-06 2026-03-12 Genentech, Inc. Tmem175 modulators

Citations (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001081345A1 (en) * 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
JP2003503481A (ja) * 1999-07-02 2003-01-28 アゴウロン・ファーマスーティカルス・インコーポレーテッド インダゾール及びプロテインキナーゼ阻害のためのその使用
WO2003091246A1 (en) * 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
JP2004501152A (ja) * 2000-06-19 2004-01-15 フアルマシア・イタリア・エツセ・ピー・アー アザインドール誘導体、その調製のためのプロセス、および抗腫瘍剤としてのその使用
WO2004046124A1 (en) * 2002-11-21 2004-06-03 Glaxo Group Limited Benzoxazinone derivatives, preparation thereof and uses in the treatment of cns and other disorders
WO2004074286A1 (en) * 2003-02-14 2004-09-02 Wyeth Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
WO2004085425A1 (en) * 2003-03-21 2004-10-07 Amgen Inc Fused azoles such as 2,5-disubstituted benzimidazoles, benzoxazoles and benzothiazoles as kinase inhibitors
WO2004099205A1 (en) * 2003-05-09 2004-11-18 Astrazeneca Ab Azaindole compounds as kinase inhibitors
JP2004534826A (ja) * 2001-06-21 2004-11-18 アベンティス・フアーマ・リミテッド アザインドール
WO2005013986A1 (en) * 2003-08-08 2005-02-17 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
WO2005051304A2 (en) * 2003-11-21 2005-06-09 Array Biopharma Inc. Akt protein kinase inhibitors
WO2005062795A2 (en) * 2003-12-19 2005-07-14 Plexxikon, Inc. Compounds and methods for development of ret modulators
WO2005108397A1 (de) * 2004-04-27 2005-11-17 Bayer Healthcare Ag Substituierte phenylaminopyrimidine
WO2005113494A2 (en) * 2004-05-07 2005-12-01 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
WO2006026754A2 (en) * 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
WO2006044687A2 (en) * 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
WO2006046023A1 (en) * 2004-10-25 2006-05-04 Astex Therapeutics Limited Ortho- condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors
WO2006046024A1 (en) * 2004-10-25 2006-05-04 Astex Therapeutics Limited Ortho- condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors
WO2006052568A2 (en) * 2004-11-10 2006-05-18 Eli Lilly And Company Tgf-beta inhibitors
WO2006069080A2 (en) * 2004-12-22 2006-06-29 Incyte Corporation Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2m3-b]pyrimidin-4-yl-amines as janus kinase inhibitors
WO2006071548A2 (en) * 2004-12-27 2006-07-06 Alcon, Inc. Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases
WO2006124863A2 (en) * 2005-05-16 2006-11-23 Irm Llc Pyrrolopyridine derivatives as protein kinase inhibitors
WO2006131835A2 (en) * 2005-02-01 2006-12-14 Sentinel Oncology Limited Heterocyclic triazines as hypoxic selective protein kinase inhibitors
JP2007509913A (ja) * 2003-10-31 2007-04-19 ピエール、ファブレ、デルモ‐コスメティーク 炎症性疾患の処置のための還元アルキル−糖モノマー含有医薬
JP2007511723A (ja) * 2003-11-18 2007-05-10 アントーノフ オートモーティブ テクノロジーズ ベスローテン フェンノートシャップ 特に自動車のための多変速伝達装置
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
JP2007530399A (ja) * 2003-07-15 2007-11-01 ユーロケラ 溶融接合部を備えたガラスセラミック物品およびその製造方法
JP2007536949A (ja) * 2004-03-30 2007-12-20 パルフューン クリスチァン ディオール 化粧品などの品物用の陳列台
JP2008512430A (ja) * 2004-09-09 2008-04-24 サノフイ−アベンテイス バソプレッシン受容体リガンドとしての3−スピロインドリン−2−オン誘導体
JP2009123635A (ja) * 2007-11-19 2009-06-04 Nissan Diesel Motor Co Ltd ハーネス組立体
JP2009179644A (ja) * 2005-05-20 2009-08-13 Vertex Pharmaceut Inc プロテインキナーゼ阻害剤として有用なピロロピリジン化合物

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
WO2001047922A2 (en) 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
AU9598601A (en) 2000-10-20 2002-04-29 Eisai Co Ltd Nitrogenous aromatic ring compounds
GB0202679D0 (en) 2002-02-05 2002-03-20 Glaxo Group Ltd Novel compounds
ES2273047T3 (es) 2002-10-28 2007-05-01 Bayer Healthcare Ag Fenilaminopirimidinas sustituidas con heteroariloxi como inhibidores de rho-cinasa.
DE60326646D1 (de) 2002-12-18 2009-04-23 Vertex Pharma Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen
JP2006518381A (ja) 2003-02-07 2006-08-10 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 プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
AR049333A1 (es) 2004-04-02 2006-07-19 Vertex Pharma Azaindoles inhibidores de proteinquinasas rock y otras proteinas quinasas. composiciones farmaceuticas.
US20060122213A1 (en) 2004-06-30 2006-06-08 Francoise Pierard Azaindoles useful as inhibitors of protein kinases
JP2008508358A (ja) 2004-08-02 2008-03-21 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド アリール−アミノ置換ピロロピリミジンマルチキナーゼ阻害化合物
ATE474833T1 (de) 2004-09-22 2010-08-15 Janssen Pharmaceutica Nv Inhibitoren der wechselwirkung zwischen mdm2 und p53
PT1812440E (pt) 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases
WO2006058120A1 (en) 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
KR20070104641A (ko) 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
ZA200802685B (en) 2005-09-30 2009-10-28 Vertex Pharma Deazapurines useful as inhibitors of janus kinases
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
SG170828A1 (en) 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
CN101678022A (zh) 2006-12-21 2010-03-24 弗特克斯药品有限公司 可用作蛋白激酶抑制剂的5-氰基-4-(吡咯并[2,3b]吡啶-3-基)嘧啶衍生物
LT3141252T (lt) 2009-06-17 2018-11-12 Vertex Pharmaceuticals Inc. Gripo virusų replikacijos inhibitoriai
CN103562205A (zh) 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу

Patent Citations (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003503481A (ja) * 1999-07-02 2003-01-28 アゴウロン・ファーマスーティカルス・インコーポレーテッド インダゾール及びプロテインキナーゼ阻害のためのその使用
WO2001081345A1 (en) * 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
JP2004501152A (ja) * 2000-06-19 2004-01-15 フアルマシア・イタリア・エツセ・ピー・アー アザインドール誘導体、その調製のためのプロセス、および抗腫瘍剤としてのその使用
JP2004534826A (ja) * 2001-06-21 2004-11-18 アベンティス・フアーマ・リミテッド アザインドール
WO2003091246A1 (en) * 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
WO2004046124A1 (en) * 2002-11-21 2004-06-03 Glaxo Group Limited Benzoxazinone derivatives, preparation thereof and uses in the treatment of cns and other disorders
WO2004074286A1 (en) * 2003-02-14 2004-09-02 Wyeth Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
WO2004085425A1 (en) * 2003-03-21 2004-10-07 Amgen Inc Fused azoles such as 2,5-disubstituted benzimidazoles, benzoxazoles and benzothiazoles as kinase inhibitors
WO2004099205A1 (en) * 2003-05-09 2004-11-18 Astrazeneca Ab Azaindole compounds as kinase inhibitors
JP2007530399A (ja) * 2003-07-15 2007-11-01 ユーロケラ 溶融接合部を備えたガラスセラミック物品およびその製造方法
WO2005013986A1 (en) * 2003-08-08 2005-02-17 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
JP2007509913A (ja) * 2003-10-31 2007-04-19 ピエール、ファブレ、デルモ‐コスメティーク 炎症性疾患の処置のための還元アルキル−糖モノマー含有医薬
JP2007511723A (ja) * 2003-11-18 2007-05-10 アントーノフ オートモーティブ テクノロジーズ ベスローテン フェンノートシャップ 特に自動車のための多変速伝達装置
WO2005051304A2 (en) * 2003-11-21 2005-06-09 Array Biopharma Inc. Akt protein kinase inhibitors
JP2007512364A (ja) * 2003-11-21 2007-05-17 アレイ バイオファーマ、インコーポレイテッド Aktプロテインキナーゼインヒビター
WO2005062795A2 (en) * 2003-12-19 2005-07-14 Plexxikon, Inc. Compounds and methods for development of ret modulators
JP2007521334A (ja) * 2003-12-19 2007-08-02 プレキシコン,インコーポレーテッド Ret調節剤の開発のための化合物および方法
JP2007536949A (ja) * 2004-03-30 2007-12-20 パルフューン クリスチァン ディオール 化粧品などの品物用の陳列台
WO2005108397A1 (de) * 2004-04-27 2005-11-17 Bayer Healthcare Ag Substituierte phenylaminopyrimidine
JP2007534710A (ja) * 2004-04-27 2007-11-29 バイエル・ヘルスケア・アクチェンゲゼルシャフト 置換フェニルアミノピリミジン化合物
JP2007536280A (ja) * 2004-05-07 2007-12-13 アムジエン・インコーポレーテツド タンパク質キナーゼ調節剤および使用方法
WO2005113494A2 (en) * 2004-05-07 2005-12-01 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
JP2008512380A (ja) * 2004-09-03 2008-04-24 プレキシコン,インコーポレーテッド Pde4b阻害剤
WO2006026754A2 (en) * 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
JP2008512430A (ja) * 2004-09-09 2008-04-24 サノフイ−アベンテイス バソプレッシン受容体リガンドとしての3−スピロインドリン−2−オン誘導体
JP2008516973A (ja) * 2004-10-15 2008-05-22 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
WO2006044687A2 (en) * 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
WO2006046023A1 (en) * 2004-10-25 2006-05-04 Astex Therapeutics Limited Ortho- condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors
JP2008517983A (ja) * 2004-10-25 2008-05-29 アステックス、セラピューティックス、リミテッド プロテインキナーゼ阻害剤としてのオルト縮合ピリジンおよびピリミジン誘導体(例えば、プリン類)
JP2008517984A (ja) * 2004-10-25 2008-05-29 アステックス、セラピューティックス、リミテッド プロテインキナーゼ阻害剤としてのオルト縮合ピリジンおよびピリミジン誘導体(例えばプリン類)
WO2006046024A1 (en) * 2004-10-25 2006-05-04 Astex Therapeutics Limited Ortho- condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors
WO2006052568A2 (en) * 2004-11-10 2006-05-18 Eli Lilly And Company Tgf-beta inhibitors
WO2006069080A2 (en) * 2004-12-22 2006-06-29 Incyte Corporation Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2m3-b]pyrimidin-4-yl-amines as janus kinase inhibitors
JP2008525463A (ja) * 2004-12-22 2008-07-17 インサイト・コーポレイション JANUSキナーゼ阻害剤としてのピロロ[2,3−b]ピリジン−4−イル−アミンおよびピロロ[2,3−b]ピリミジン−4−イル−アミン
WO2006071548A2 (en) * 2004-12-27 2006-07-06 Alcon, Inc. Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases
JP2008525453A (ja) * 2004-12-27 2008-07-17 アルコン,インコーポレイティド 緑内障と、rhoキナーゼを媒介とした他の疾患および症状を治療するためのアミノピラジン・アナログ
WO2006131835A2 (en) * 2005-02-01 2006-12-14 Sentinel Oncology Limited Heterocyclic triazines as hypoxic selective protein kinase inhibitors
JP2008528679A (ja) * 2005-02-01 2008-07-31 センティネル、オンコロジー、リミテッド 低酸素選択的タンパク質キナーゼ阻害剤としての複素環トリアジン
WO2006124863A2 (en) * 2005-05-16 2006-11-23 Irm Llc Pyrrolopyridine derivatives as protein kinase inhibitors
JP2008540664A (ja) * 2005-05-16 2008-11-20 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としてのピロロピリジン誘導体
JP2009179644A (ja) * 2005-05-20 2009-08-13 Vertex Pharmaceut Inc プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
JP2009523812A (ja) * 2006-01-19 2009-06-25 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド 融合へテロ二環式キナーゼ阻害剤
JP2009123635A (ja) * 2007-11-19 2009-06-04 Nissan Diesel Motor Co Ltd ハーネス組立体

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
THUTEWOHL,MICHAEL, SYNTHESIS, vol. N4, JPN5008006241, 2006, pages 629 - 632, ISSN: 0002109456 *

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JP2013253114A (ja) * 2005-05-20 2013-12-19 Vertex Pharmaceuticals Inc プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
JP2015193641A (ja) * 2005-12-13 2015-11-05 インサイト・コーポレイションIncyte Corpor JANUSキナーゼ阻害剤としてのヘテロアリール置換ピロロ[2,3−b]ピリジンおよびピロロ[2,3−b]ピリミジン
US10398699B2 (en) 2005-12-13 2019-09-03 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US11331320B2 (en) 2005-12-13 2022-05-17 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US9662335B2 (en) 2005-12-13 2017-05-30 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-B] pyridines and pyrrolo[2,3-B] pyrimidines as janus kinase inhibitors
US10639310B2 (en) 2005-12-13 2020-05-05 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
JP2014051531A (ja) * 2005-12-13 2014-03-20 Incyte Corp JANUSキナーゼ阻害剤としてのヘテロアリール置換ピロロ[2,3−b]ピリジンおよびピロロ[2,3−b]ピリミジン
US9814722B2 (en) 2005-12-13 2017-11-14 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-B] pyridines and pyrrolo[2,3-B] pyrimidines as janus kinase inhibitors
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US9974790B2 (en) 2005-12-13 2018-05-22 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-B] pyridines and pyrrolo[2,3-B] pyrimidines as janus kinase inhibitors
US11744832B2 (en) 2005-12-13 2023-09-05 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US11213528B2 (en) 2007-06-13 2022-01-04 Incyte Holdings Corporation Salts of the janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
US9623029B2 (en) 2009-05-22 2017-04-18 Incyte Holdings Corporation 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors
JP2016029104A (ja) * 2009-07-31 2016-03-03 日本たばこ産業株式会社 含窒素スピロ環化合物及びその医薬用途
RU2630694C2 (ru) * 2009-07-31 2017-09-12 Джапан Тобакко Инк. Азотсодержащее спироциклическое соединение и его применение в медицине
WO2011013785A1 (ja) * 2009-07-31 2011-02-03 日本たばこ産業株式会社 含窒素スピロ環化合物及びその医薬用途
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US9718834B2 (en) 2011-09-07 2017-08-01 Incyte Corporation Processes and intermediates for making a JAK inhibitor
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US11337927B2 (en) 2012-11-15 2022-05-24 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
US11896717B2 (en) 2012-11-15 2024-02-13 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
US11576865B2 (en) 2012-11-15 2023-02-14 Incyte Corporation Sustained-release dosage forms of ruxolitinib
JP2016512198A (ja) * 2013-03-06 2016-04-25 アロステロス セラピューティクス, インコーポレイテッド CaMKII阻害剤及びその使用
US9714233B2 (en) 2013-03-06 2017-07-25 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US12151026B2 (en) 2013-08-07 2024-11-26 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
US10561616B2 (en) 2013-08-07 2020-02-18 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
US11045421B2 (en) 2013-08-07 2021-06-29 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
WO2015119126A1 (ja) * 2014-02-04 2015-08-13 大鵬薬品工業株式会社 アザインドール誘導体
JP5938533B2 (ja) * 2014-02-04 2016-06-22 大鵬薬品工業株式会社 アザインドール誘導体
US9676773B2 (en) 2014-02-04 2017-06-13 Taiho Pharmaceutical Co., Ltd. Azaindole derivative
US9782392B2 (en) 2014-02-04 2017-10-10 Taiho Pharmaceutical Co., Ltd. Azaindole derivative
JP2017506656A (ja) * 2014-03-28 2017-03-09 ノバルティス ティーアゲズントハイト アーゲー 新規化合物
US10759792B2 (en) 2014-09-05 2020-09-01 The Johns Hopkins University CaMKII inhibitors and uses thereof
US11325908B2 (en) 2014-09-05 2022-05-10 The Johns Hopkins University CaMKII inhibitors and uses thereof
JP2020531487A (ja) * 2017-08-23 2020-11-05 スプリント バイオサイエンス アクティエボラーグ アザインドリルピリドンおよびジアザインドリルピリドン化合物
KR20200043412A (ko) * 2017-08-23 2020-04-27 스프린트 바이오사이언스 아베 아자인돌릴피리돈 및 디아자인돌릴피리돈 화합물
JP7199738B2 (ja) 2017-08-23 2023-01-06 スプリント バイオサイエンス アクティエボラーグ アザインドリルピリドンおよびジアザインドリルピリドン化合物
KR102731945B1 (ko) 2017-08-23 2024-11-18 스프린트 바이오사이언스 아베 아자인돌릴피리돈 및 디아자인돌릴피리돈 화합물
JP2023021277A (ja) * 2017-08-23 2023-02-10 スプリント バイオサイエンス アクティエボラーグ アザインドリルピリドンおよびジアザインドリルピリドン化合物
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
US11278541B2 (en) 2017-12-08 2022-03-22 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
US10899736B2 (en) 2018-01-30 2021-01-26 Incyte Corporation Processes and intermediates for making a JAK inhibitor
US11304949B2 (en) 2018-03-30 2022-04-19 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
US12280054B2 (en) 2018-03-30 2025-04-22 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
US12275731B2 (en) 2018-10-16 2025-04-15 Dana-Farber Cancer Institute, Inc. Azaindole inhibitors of wild-type and mutant forms of LRRK2
JP7503054B2 (ja) 2018-10-16 2024-06-19 ダナ-ファーバー キャンサー インスティテュート,インコーポレイテッド Lrrk2の野生型および変異型のアザインドール阻害剤
JP2022504988A (ja) * 2018-10-16 2022-01-13 ダナ-ファーバー キャンサー インスティテュート,インコーポレイテッド Lrrk2の野生型および変異型のアザインドール阻害剤
JP2022531088A (ja) * 2019-05-02 2022-07-06 アクラリス セラピューティクス,インコーポレイテッド Jak阻害剤としての置換ピロロピリジン
JP2023527055A (ja) * 2020-05-26 2023-06-26 サントル ナショナル ドゥ ラ ルシェルシュ シアンティフィック がんの治療に使用するためのlimk及び/又はrockキナーゼ阻害剤としての4-(7h-ピロロ[2,3-d]ピリミジン-4-イル)-3,6-ジヒドロピリジン-1-(2h)-カルボキサミド誘導体
JP7719803B2 (ja) 2020-05-26 2025-08-06 サントル ナショナル ドゥ ラ ルシェルシュ シアンティフィック がんの治療に使用するためのlimk及び/又はrockキナーゼ阻害剤としての4-(7h-ピロロ[2,3-d]ピリミジン-4-イル)-3,6-ジヒドロピリジン-1-(2h)-カルボキサミド誘導体
US12440495B2 (en) 2020-06-03 2025-10-14 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2023145372A1 (ja) * 2022-01-28 2023-08-03 日本曹達株式会社 アミド化合物の製造方法

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