CN101228161B - 适用作蛋白激酶抑制剂的吡咯并吡啶类 - Google Patents

适用作蛋白激酶抑制剂的吡咯并吡啶类 Download PDF

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Publication number
CN101228161B
CN101228161B CN2006800263918A CN200680026391A CN101228161B CN 101228161 B CN101228161 B CN 101228161B CN 2006800263918 A CN2006800263918 A CN 2006800263918A CN 200680026391 A CN200680026391 A CN 200680026391A CN 101228161 B CN101228161 B CN 101228161B
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compound
disease
group
pyrrolo
pyridin
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Expired - Fee Related
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Chinese (zh)
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CN101228161A (zh
Inventor
M·W·里德博尔
M·W·万纳梅克
L·J·法默
王天生
A·C·皮尔斯
G·马蒂内兹-伯塔拉
R·S·贝希尔
G·W·比米斯
王健
F·G·萨里图罗
M·J·阿诺斯特
J·H·科姆
J·格林
M·斯特沃特
C·马赫夫卡
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • 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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    • 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
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CN2006800263918A 2005-05-20 2006-05-22 适用作蛋白激酶抑制剂的吡咯并吡啶类 Expired - Fee Related CN101228161B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US68355405P 2005-05-20 2005-05-20
US60/683,554 2005-05-20
PCT/US2006/019711 WO2006127587A1 (en) 2005-05-20 2006-05-22 Pyrrolopyridines useful as inhibitors of protein kinase

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Publication Number Publication Date
CN101228161A CN101228161A (zh) 2008-07-23
CN101228161B true CN101228161B (zh) 2012-10-10

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

Families Citing this family (174)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1696920E (pt) 2003-12-19 2015-01-14 Plexxikon Inc Compostos e métodos para o desenvolvimento de moduladores de ret
DE602005027825D1 (de) 2004-03-30 2011-06-16 Vertex Pharma Als inhibitoren von jak und anderen proteinkinasen geeignete azaindole
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
KR20080027775A (ko) 2005-05-17 2008-03-28 플렉시콘, 인코퍼레이티드 피롤(2,3-b)피리딘 유도체 단백질 키나제 억제제
US8921376B2 (en) * 2005-05-20 2014-12-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
PL1893612T3 (pl) 2005-06-22 2012-01-31 Plexxikon Inc Pochodne pirolo-[2,3-b]pirydyny jako inhibitory kinazy białkowej
US8163767B2 (en) 2005-07-14 2012-04-24 Astellas Pharma Inc. Heterocyclic Janus Kinase 3 inhibitors
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
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic 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
ATE525374T1 (de) * 2005-12-13 2011-10-15 Incyte Corp Heteroarylsubstituierte pyrroloä2,3-büpyridine und pyrroloä2,3-büpyrimidine als januskinaseinhibitoren
WO2007076423A2 (en) * 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
EP2537849A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of janus kinases
AU2007207055B2 (en) * 2006-01-18 2011-06-02 F. Hoffmann-La Roche Ag Thiazoles as 11 beta-HSD1 inhibitors
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
CA2648250A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
CA2651732C (en) * 2006-05-18 2014-10-14 Mannkind Corporation Intracellular kinase inhibitors
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ES2372955T3 (es) 2006-07-06 2012-01-30 Array Biopharma, Inc. Ciclopenta[d]pirimidinas como inhibidores de la proteína cinasa akt.
ATE493418T1 (de) 2006-07-06 2011-01-15 Array Biopharma Inc Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren
JP5231411B2 (ja) 2006-07-06 2013-07-10 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阻害剤としてのジヒドロチエノピリミジン
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
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
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
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
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
JP5492565B2 (ja) 2006-12-22 2014-05-14 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置換複素環
JP5287253B2 (ja) 2007-01-12 2013-09-11 アステラス製薬株式会社 縮合ピリジン化合物
JP5642973B2 (ja) 2007-03-22 2014-12-17 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 Jak阻害薬として有用なn−複素環式化合物
CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
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.
ES2467665T5 (es) 2007-06-13 2022-11-03 Incyte Holdings Corp Sales del inhibidor de cinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
NZ582692A (en) 2007-07-05 2012-05-25 Array Biopharma Inc Pyrimidyl cyclopentanes as akt protein kinase inhibitors
US8377937B2 (en) * 2007-07-05 2013-02-19 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 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
BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
EP2242755B1 (en) 2008-01-08 2012-09-12 Array Biopharma, Inc. Pyrrolopyridines as kinase inhibitors
WO2009089459A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
CA2711692A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
EP2242757B1 (en) * 2008-01-09 2012-08-01 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
SG191660A1 (en) 2008-03-11 2013-07-31 Incyte Corp Azetidine and cyclobutane derivatives as jak inhibitors
GB0804592D0 (en) * 2008-03-12 2008-04-16 Glaxo Group Ltd Novel compounds
AR071717A1 (es) 2008-05-13 2010-07-07 Array Biopharma Inc Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion 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
WO2010074776A2 (en) * 2008-06-16 2010-07-01 The University Of Tennessee Research Foundation Compounds for the treatment of cancer
US8822513B2 (en) 2010-03-01 2014-09-02 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
EA020548B1 (ru) 2008-12-19 2014-12-30 Бёрингер Ингельхайм Интернациональ Гмбх Циклические пиримидин-4-карбоксамиды в качестве антагонистов рецептора ccr2, предназначенные для лечения воспаления, астмы и хозл
MY160737A (en) 2009-04-03 2017-03-15 Hoffmann La Roche Propane-i-sulfonic acid {3- [5-(4-chloro-phenyl) -1h -pyrrolo [2, 3-b] pyridine-3-carbonyl] -2,4 difluoro-phenyl} - amide compositions and uses thereof
WO2010135650A1 (en) 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
JP6172939B2 (ja) * 2009-05-22 2017-08-02 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害薬としての3−[4−(7h−ピロロ[2,3−d]ピリミジン−4−イル)−1h−ピラゾール−1−イル]オクタン−またはヘプタン−ニトリル
SG10201405826RA (en) 2009-06-17 2014-12-30 Vertex Pharma Inhibitors of influenza viruses replication
CN102574857B (zh) 2009-07-08 2015-06-10 利奥制药有限公司 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
WO2011017142A1 (en) 2009-08-06 2011-02-10 Merck Patent Gmbh Novel bicyclic urea compounds
AU2010281503B2 (en) 2009-08-07 2016-01-28 Merck Patent Gmbh Novel azaheterocyclic compounds
ES2534326T3 (es) 2009-08-20 2015-04-21 Karus Therapeutics Limited Compuestos tricíclicos heterocíclicos como inhibidores de la fosfoinositida 3-cinasa
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
BR112012005382A2 (pt) 2009-09-10 2016-03-29 Hoffmann La Roche inibidores de jak
KR101805936B1 (ko) 2009-10-09 2017-12-07 인사이트 홀딩스 코포레이션 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
SG10201407129SA (en) 2009-11-06 2014-12-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
ME01908B (me) 2009-12-17 2014-12-20 Boehringer Ingelheim Int Novi antagonisti ccr2 receptora i njihova primjena
USRE49251E1 (en) 2010-01-04 2022-10-18 Mapi Pharma Ltd. Depot systems comprising glatiramer or pharmacologically acceptable salt thereof
BR112012020693B1 (pt) * 2010-02-18 2020-05-12 Incyte Holdings Corporation Derivados de ciclobutano e metilciclobutano como inibidores de janus quinase e composição que os compreende
WO2011109059A1 (en) 2010-03-01 2011-09-09 Gtx, Inc. Compounds for treatment of cancer
PE20130038A1 (es) 2010-03-10 2013-01-28 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de jak1
US8877745B2 (en) 2010-05-12 2014-11-04 Boehringer Ingelheim International Gmbh CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments
WO2011141477A1 (en) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
KR102303885B1 (ko) 2010-05-21 2021-09-24 인사이트 홀딩스 코포레이션 Jak 저해제에 대한 국소 제형
WO2011147772A1 (en) 2010-05-25 2011-12-01 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists
EP2576538B1 (en) 2010-06-01 2015-10-28 Boehringer Ingelheim International GmbH New CCR2 antagonists
EP2397482A1 (en) * 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
EA026201B1 (ru) * 2010-11-19 2017-03-31 Инсайт Холдингс Корпорейшн Циклобутилзамещенные производные пирролопиридина и пирролопиримидина как ингибиторы jak
WO2012068440A1 (en) 2010-11-19 2012-05-24 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
RU2013136906A (ru) * 2011-01-07 2015-02-20 Лео Фарма А/С Новые производные сульфамидпиперазина в качестве ингибиторов протеинтирозинкиназы и их фармацевтическое применение
CN103517710B (zh) 2011-02-07 2017-05-31 普莱希科公司 用于激酶调节的化合物
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
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
RS56759B2 (sr) 2011-04-01 2024-10-31 Genentech Inc Kombinacija akt inhibitor jedinjenja i abiraterona za upotrebu pri terapeutskim tretiranjima
CA2831932A1 (en) 2011-04-01 2012-10-04 Genentech, Inc. Combinations of akt and mek inhibitor compounds, and methods of use
CA2839767A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
CN106432311A (zh) 2011-07-05 2017-02-22 沃泰克斯药物股份有限公司 生产氮杂吲哚类的方法和中间体
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
HK1198579A1 (en) 2011-08-10 2015-04-30 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
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
AU2013239816B2 (en) 2012-03-29 2017-08-24 G1 Therapeutics, Inc. Lactam kinase inhibitors
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
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
CN104797573A (zh) 2012-11-07 2015-07-22 卡鲁斯治疗有限公司 新的组蛋白脱乙酰基酶抑制剂及其在治疗中的用途
RS62329B1 (sr) 2012-11-15 2021-10-29 Incyte Holdings Corp Dozni oblici ruksolitiniba sa produženim vremenom oslobađanja
FR3001219A1 (fr) * 2013-01-22 2014-07-25 Centre Nat Rech Scient Inhibiteurs de kinases
AU2014225889B2 (en) * 2013-03-06 2018-12-06 The Johns Hopkins University CaMKII inhibitors and uses thereof
TR201820520T4 (tr) 2013-03-06 2019-01-21 Incyte Holdings Corp Bir jak inhibitörü yapmaya yönelik prosesler ve ara ürünler.
RS59790B1 (sr) 2013-03-15 2020-02-28 G1 Therapeutics Inc Privremena zaštita normalnih ćelija tokom hemoterapije
HK1222766A1 (zh) 2013-03-15 2017-07-14 G1治疗公司 高效的抗赘生剂和抗增生剂
BR112015025250A2 (pt) * 2013-04-02 2017-07-18 Hoffmann La Roche inibidores de tirosina quinase de bruton
KR101790090B1 (ko) * 2013-05-02 2017-10-25 후지필름 가부시키가이샤 에칭 방법, 이에 이용하는 에칭액 및 에칭액의 키트, 및 반도체 기판 제품의 제조 방법
DK2994465T3 (en) 2013-05-10 2018-10-08 Karus Therapeutics Ltd HISTONDEACETYLASE INHIBITORS UNKNOWN
DK3030227T3 (da) 2013-08-07 2020-04-20 Incyte Corp Vedvarende frigivelses-doseringsformer for en jak1-inhibitor
PT3068776T (pt) 2013-11-13 2019-08-26 Vertex Pharma Inibidores da replicação de vírus da gripe
WO2015073481A1 (en) 2013-11-13 2015-05-21 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
SG11201605072VA (en) * 2014-02-04 2016-08-30 Taiho Pharmaceutical Co Ltd Azaindole derivative
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
EP2924026A1 (en) 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
US20150297606A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic Lactams for Use in the Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation
CA2948444C (en) * 2014-05-28 2022-07-26 Astrazeneca Ab Processes for the preparation of azd5363 and intermediate used therein
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
CN107108581B (zh) * 2014-08-21 2020-06-23 百时美施贵宝公司 作为强效rock抑制剂的回接苯甲酰胺衍生物
CN107074856A (zh) 2014-09-05 2017-08-18 阿略斯泰罗斯医疗公司 CaMKII抑制剂及其用途
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
WO2016040858A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419228D0 (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
EP3294735B8 (en) 2015-05-13 2022-01-05 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
AU2016287584B2 (en) 2015-07-02 2020-03-26 Centrexion Therapeutics Corporation (4-((3R,4R)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4yl)methanone citrate
GB201514758D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
GB201514751D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514754D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514760D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds and method of use
HK1250707B (zh) 2015-12-11 2020-07-03 四川科伦博泰生物医药股份有限公司 氮杂环丁烷衍生物、其制备方法及用途
CN106928252B (zh) * 2015-12-31 2019-09-27 成都先导药物开发股份有限公司 一种抑制rock的化合物及其制备方法与应用
JP6978098B2 (ja) * 2016-07-26 2021-12-08 スーヂョウ ロングバイオテック ファーマシューティカルズ カンパニー リミテッドSuzhou Longbiotech Pharmaceuticals Co., Ltd. 選択的jak阻害剤としての化合物、該化合物の塩類および治療への使用
US12097292B2 (en) 2016-08-28 2024-09-24 Mapi Pharma Ltd. Process for preparing microparticles containing glatiramer acetate
LT3506921T (lt) 2016-08-31 2023-08-10 Mapi Pharma Ltd Ilgesnio atpalaidavimo sistemos, kuriose yra glatiramero acetato
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
ES2930106T3 (es) * 2017-03-23 2022-12-05 Daegu Gyeongbuk Medical Innovation Found Compuesto derivado de pirrol-piridina, procedimiento para preparar el mismo y composición farmacéutica que contiene el mismo como ingrediente activo para la prevención o el tratamiento de enfermedades relacionadas con la proteína quinasa
AU2018242998B2 (en) 2017-03-26 2023-11-02 Mapi Pharma Ltd. Glatiramer depot systems for treating progressive forms of multiple sclerosis
CA3063616A1 (en) 2017-06-30 2019-12-06 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
JP7039802B2 (ja) * 2017-06-30 2022-03-23 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、rho-関連プロテインキナーゼ阻害剤を含む医薬組成物、当該医薬組成物の調製方法及び使用
CN110573501B (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
PT3672967T (pt) * 2017-08-23 2021-12-28 Sprint Bioscience Ab Compostos de azaindolilpiridona e diazaindolilpiridona
WO2019057103A1 (zh) * 2017-09-21 2019-03-28 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
CN119119039A (zh) 2017-11-03 2024-12-13 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
US10800775B2 (en) * 2017-11-03 2020-10-13 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
WO2019152374A1 (en) 2018-01-30 2019-08-08 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
US11485707B2 (en) 2018-03-23 2022-11-01 Fochon Pharmaceuticals, Ltd. Deuterated compounds as rock inhibitors
CA3095487A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
SG11202100525SA (en) 2018-08-10 2021-02-25 Aclaris Therapeutics Inc Pyrrolopyrimidine itk inhibitors
CA3113081A1 (en) 2018-10-16 2020-04-23 Dana-Farber Cancer Institute, Inc. Azaindole inhibitors of wild-type and mutant forms of lrrk2
CA3168211A1 (en) 2019-01-18 2020-07-23 Voronoi Co., Ltd. Pyrrolopyridine derivative and use thereof for preventing or treating protein kinase related disease
JP2022527972A (ja) 2019-04-02 2022-06-07 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 前悪性病変を有する患者において癌を予測及び予防する方法
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
WO2020223728A1 (en) * 2019-05-02 2020-11-05 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as jak inhibitors
US20220252599A1 (en) * 2019-07-12 2022-08-11 The Johns Hopkins University Compositions and methods for treating cerebral vasospasm
JP2022549506A (ja) 2019-09-27 2022-11-25 ディスク・メディシン・インコーポレイテッド 骨髄線維症および関連状態を処置するための方法
WO2021102258A1 (en) 2019-11-22 2021-05-27 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
EP4149548A4 (en) 2020-05-13 2024-05-08 Disc Medicine, Inc. ANTI-HEMOJUVELIN ANTIBODIES (HJV) FOR THE TREATMENT OF MYELOFIBROSIS
EP3915990A1 (en) * 2020-05-26 2021-12-01 Centre National de la Recherche Scientifique 4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridine-1-(2h)-carboxamide derivatives as limk and/or rock kinases inhibitors for use in the treatment of cancer
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
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
EP4471004A1 (en) 2022-01-28 2024-12-04 Nippon Soda Co., Ltd. Method for producing amide compound
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003000688A1 (en) * 2001-06-21 2003-01-03 Aventis Pharma Limited Azaindoles
WO2004099205A1 (en) * 2003-05-09 2004-11-18 Astrazeneca Ab Azaindole compounds as kinase inhibitors
WO2005013986A1 (en) * 2003-08-08 2005-02-17 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
CN101102773A (zh) * 2004-12-27 2008-01-09 爱尔康公司 治疗青光眼和其他rho激酶-介导疾病的氨基吡嗪类似物

Family Cites Families (52)

* 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
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
CN100379734C (zh) 1999-12-24 2008-04-09 阿文蒂斯药物有限公司 氮杂吲哚类化合物
WO2001081345A1 (en) * 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
EP1506962B1 (en) 2000-10-20 2008-07-02 Eisai R&D Management Co., Ltd. Nitrogen-containing aromatic heterocycles
GB0202679D0 (en) 2002-02-05 2002-03-20 Glaxo Group Ltd Novel compounds
WO2003091246A1 (en) * 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
WO2004039796A1 (de) 2002-10-28 2004-05-13 Bayer Healthcare Ag Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
GB0227240D0 (en) 2002-11-21 2002-12-31 Glaxo Group Ltd Compounds
DE60326646D1 (de) 2002-12-18 2009-04-23 Vertex Pharma Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen
CA2515132C (en) 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles useful as inhibitors of protein kinases
CN100482662C (zh) * 2003-02-14 2009-04-29 惠氏公司 作为5-羟基色胺-6配体的杂环基-3-磺酰基氮杂吲哚或-氮杂吲唑衍生物
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
FR2857661B1 (fr) * 2003-07-15 2006-09-22 Snc Eurokera Produit en vitroceramique avec joint(s) de soudure; fabrication
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
FR2861729B1 (fr) * 2003-10-31 2006-09-08 Fabre Pierre Dermo Cosmetique Monomere d'alkyl-rhamnose ou d'alkyl-fucose, medicament comprenant un monomere d'alkyl-sucre reducteur
FR2862363B1 (fr) * 2003-11-18 2007-01-26 Antonov Automotive Europ Dispositif de transmission a rapports multiples, notamment pour l'automobile
CN102786482A (zh) * 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂
PT1696920E (pt) 2003-12-19 2015-01-14 Plexxikon Inc Compostos e métodos para o desenvolvimento de moduladores de ret
FR2868273B1 (fr) * 2004-03-30 2006-07-07 Parfums Christian Dior Sa Presentoir d'articles tels que des produits cosmetiques
DE602005027825D1 (de) 2004-03-30 2011-06-16 Vertex Pharma Als inhibitoren von jak und anderen proteinkinasen geeignete azaindole
MXPA06011328A (es) 2004-04-02 2006-12-15 Vertex Pharma Azaindoles utiles como inhibidotes de roca y otras proteinas cinasas.
DE102004020570A1 (de) * 2004-04-27 2005-11-24 Bayer Healthcare Ag Substituierte Phenylaminopyrimidine
US7880000B2 (en) * 2004-05-07 2011-02-01 Amgen Inc. Protein kinase modulators and method of use
US20060122213A1 (en) 2004-06-30 2006-06-08 Francoise Pierard Azaindoles useful as inhibitors of protein kinases
WO2006017443A2 (en) 2004-08-02 2006-02-16 Osi Pharmaceuticals, Inc. Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds
CA2583428A1 (en) * 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
FR2874920B1 (fr) * 2004-09-09 2006-10-20 Sanofi Aventis Sa Derives de 3-spiro-indolin-2-one comme ligand des recepteurs de la vasopressine
DK1809622T3 (da) * 2004-09-22 2010-11-08 Janssen Pharmaceutica Nv Inhibitorer af interaktionen mellem MDM2 og P53
DE602005023333D1 (de) * 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
UY29177A1 (es) * 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) * 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
MX337817B (es) 2004-11-04 2011-11-04 Vertex Pharma Pirazolo [1,5-a] pirimidinas de utilidad como inhibidores de proteina quinasas.
US7511056B2 (en) * 2004-11-10 2009-03-31 Eli Lilly And Company TGF-β inhibitors
CN101098872B (zh) 2004-11-22 2012-09-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
GB0501999D0 (en) * 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
JP5227032B2 (ja) 2005-02-03 2013-07-03 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 プロテインキナーゼの阻害剤として有用なピロロピリミジン
US20080300267A1 (en) * 2005-05-16 2008-12-04 Barun Okram Compounds and Compositions as Protein Kinase Inhibitors
US8921376B2 (en) * 2005-05-20 2014-12-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
KR20080063809A (ko) 2005-09-30 2008-07-07 버텍스 파마슈티칼스 인코포레이티드 야누스 키나아제의 억제제로서 유용한 데아자퓨린
EP2537849A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of janus kinases
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
CA2648250A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
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
JP2009123635A (ja) * 2007-11-19 2009-06-04 Nissan Diesel Motor Co Ltd ハーネス組立体
SG10201405826RA (en) 2009-06-17 2014-12-30 Vertex Pharma Inhibitors of influenza viruses replication
CA2822062A1 (en) 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003000688A1 (en) * 2001-06-21 2003-01-03 Aventis Pharma Limited Azaindoles
WO2004099205A1 (en) * 2003-05-09 2004-11-18 Astrazeneca Ab Azaindole compounds as kinase inhibitors
WO2005013986A1 (en) * 2003-08-08 2005-02-17 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
CN101102773A (zh) * 2004-12-27 2008-01-09 爱尔康公司 治疗青光眼和其他rho激酶-介导疾病的氨基吡嗪类似物

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