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EA201591339A1 - Тиазолкарбоксамиды и пиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы - Google Patents

Тиазолкарбоксамиды и пиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы

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Publication number
EA201591339A1
EA201591339A1 EA201591339A EA201591339A EA201591339A1 EA 201591339 A1 EA201591339 A1 EA 201591339A1 EA 201591339 A EA201591339 A EA 201591339A EA 201591339 A EA201591339 A EA 201591339A EA 201591339 A1 EA201591339 A1 EA 201591339A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bond
tiazolkarboksamida
pyridinkarboxamides
kinase inhibitors
pim
Prior art date
Application number
EA201591339A
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English (en)
Other versions
EA035929B1 (ru
Inventor
Чу-Бяо Сюэ
Юнь-Лун Ли
Хао Фэн
Цзюнь Пань
Аньлай Ван
Ке Чжан
Вэньцин Яо
Фэнлэй Чжан
Цзиньцун Чжо
Original Assignee
Инсайт Корпорейшн
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Publication date
Application filed by Инсайт Корпорейшн filed Critical Инсайт Корпорейшн
Publication of EA201591339A1 publication Critical patent/EA201591339A1/ru
Publication of EA035929B1 publication Critical patent/EA035929B1/ru

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Abstract

Изобретение описывает производные тиазолкарбоксамида и пиридинкарбоксамида формулы (I) или их фармацевтически приемлемые соли, где X представляет собой С или N; А, В и D представляют собой кольца; связьпредставляет собой нормализованную связь в ароматическом кольце, содержащем как N, так и X, которая формально представляет собой связь С=С, когда X представляет собой С, и одинарную связь, когда X представляет собой N; кольцо А имеет формулу (А-1) или (А-2), где Е1 и Е2 представляют собой кольца; их композиции и способы использования. Соединения ингибируют активность Pim-киназ и эффективны при лечении заболеваний, связанных с активностью Pim-киназ, в том числе, например, рака и других заболеваний.
EA201591339A 2013-01-15 2014-01-14 ТИАЗОЛКАРБОКСАМИДЫ И ПИРИДИНКАРБОКСАМИДЫ, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ Pim-КИНАЗЫ EA035929B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361752897P 2013-01-15 2013-01-15
US201361790952P 2013-03-15 2013-03-15
US201361859118P 2013-07-26 2013-07-26
PCT/US2014/011486 WO2014113388A1 (en) 2013-01-15 2014-01-14 Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201591339A1 true EA201591339A1 (ru) 2015-12-30
EA035929B1 EA035929B1 (ru) 2020-09-02

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EA201591339A EA035929B1 (ru) 2013-01-15 2014-01-14 ТИАЗОЛКАРБОКСАМИДЫ И ПИРИДИНКАРБОКСАМИДЫ, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ Pim-КИНАЗЫ

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US (7) US9200004B2 (ru)
EP (3) EP2945939B1 (ru)
JP (3) JP6554037B2 (ru)
KR (2) KR102403306B1 (ru)
CN (2) CN105051029B (ru)
AR (1) AR094664A1 (ru)
AU (3) AU2014207691B2 (ru)
BR (2) BR112015016793B1 (ru)
CA (1) CA2897333C (ru)
CL (1) CL2015001985A1 (ru)
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Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3812387A1 (en) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
US9278950B2 (en) 2013-01-14 2016-03-08 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
SI2945939T1 (sl) * 2013-01-15 2020-08-31 Incyte Holdings Corporation Spojine tiazolkarboksamidov in piridinkarboksamida uporabne kot zaviralci PIM kinaze
AU2014308703A1 (en) 2013-08-23 2016-03-24 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
PL3212629T3 (pl) * 2014-10-31 2019-05-31 Genoscience Pharma Sas Podstawione 2,4-diamino-chinoliny jako nowe środki przeciwnowotworowe
CN104876929B (zh) * 2015-05-15 2016-10-05 华南理工大学 一种1,2,3,4-四氢萘啶类化合物的合成方法及应用
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
EP3365340B1 (en) 2015-10-19 2022-08-10 Incyte Corporation Heterocyclic compounds as immunomodulators
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
SI3394033T1 (sl) 2015-12-22 2021-03-31 Incyte Corporation Heterociklične spojine kot imunomodulatorji
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
MA45116A (fr) 2016-05-26 2021-06-02 Incyte Corp Composés hétérocycliques comme immunomodulateurs
DK3472167T3 (da) 2016-06-20 2022-09-05 Incyte Corp Heterocykliske forbindelser som immunomodulatorer
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
CN106336371A (zh) * 2016-08-16 2017-01-18 成都百事兴科技实业有限公司 叔丁氧羰基‑l‑焦谷氨酸甲酯的合成方法
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3047980A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
MA47120A (fr) 2016-12-22 2021-04-28 Incyte Corp Dérivés pyridine utilisés en tant qu'immunomodulateurs
TWI808955B (zh) 2016-12-22 2023-07-21 美商英塞特公司 作為免疫調節劑之雜環化合物
WO2018177993A1 (de) 2017-03-31 2018-10-04 Bayer Cropscience Aktiengesellschaft Pyrazole zur bekämpfung von arthropoden
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
CR20240101A (es) 2018-03-08 2024-05-24 Incyte Corp COMPUESTOS DIÓLICOS DE AMINOPIRAZINA COMO INHIBIDORES DE PI3K-y (DIVISIONAL 2020-464)
FI3774791T3 (fi) 2018-03-30 2023-03-21 Incyte Corp Heterosyklisiä yhdisteitä immunomodulaattoreina
CA3095580A1 (en) 2018-04-13 2019-10-17 Sumitomo Dainippon Pharma Oncology, Inc. Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer
SMT202300127T1 (it) 2018-05-11 2023-05-12 Incyte Corp Derivati di tetraidro-imidazo[4,5-c]piridina come immunomodulatori di pd-l1
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
MA54157A (fr) * 2018-11-09 2021-09-15 Prelude Therapeutics Inc Dérivés de spiro-sulfonamide en tant qu'inhibiteurs de la protéine de la leucémie myéloïde -1 (mcl-1)
KR20210146290A (ko) 2019-02-12 2021-12-03 스미토모 다이니폰 파마 온콜로지, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제
WO2020221334A1 (en) * 2019-04-30 2020-11-05 City University Of Hong Kong Pim1 inhibitors for use in treatment of viral infection and pharmaceutical compositions thereof
JP2022540200A (ja) 2019-07-11 2022-09-14 エスケイプ・バイオ・インコーポレイテッド Ｌｒｒｋ２阻害剤としてのインダゾールおよびアザインダゾール
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
BR112022005826A2 (pt) 2019-09-30 2022-06-21 Incyte Corp Compostos de pirido[3,2-d]pirimidina como imunomoduladores
PE20230407A1 (es) 2019-11-11 2023-03-07 Incyte Corp Sales y formas cristalinas de un inhibidor de pd-1/pd-l1
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
AR124001A1 (es) 2020-11-06 2023-02-01 Incyte Corp Proceso para fabricar un inhibidor pd-1 / pd-l1 y sales y formas cristalinas del mismo
WO2023170024A1 (en) * 2022-03-11 2023-09-14 University Of Copenhagen Camk2 modulators and their use in medicine
WO2024097653A1 (en) 2022-10-31 2024-05-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
WO2025117722A1 (en) * 2023-11-27 2025-06-05 Rubedo Life Sciences, Inc. Carbon linked bcl inhibitors and senolytic compounds and uses thereof

Family Cites Families (194)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2225624T3 (es) 2000-06-28 2005-03-16 Smithkline Beecham Plc Procedimiento de molienda por via humeda.
AU2002246864A1 (en) 2000-12-27 2002-07-24 The Trustees Of Columbia University In The City Of New York Pim kinase-related methods
DE10123055A1 (de) 2001-05-11 2003-03-20 Gruenenthal Gmbh Screeningverfahren mit PIM1-Kinase oder PIM3-Kinase
DE10226702A1 (de) 2002-06-14 2004-09-09 Grünenthal GmbH Antisense Oligonukleotide gegen PIM1
AU2003272548A1 (en) 2002-09-16 2004-04-30 Plexxikon, Inc. Crystal structure of pim-1 kinase
WO2006078228A1 (en) 2002-09-16 2006-07-27 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
TW200413273A (en) * 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
CL2003002287A1 (es) 2002-11-25 2005-01-14 Wyeth Corp COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS
WO2004090106A2 (en) 2003-04-04 2004-10-21 Vertex Pharmaceuticals Incorporated Crystal structures of human pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
WO2005033310A1 (de) 2003-10-01 2005-04-14 Grünenthal GmbH Pim-1-spezifische dsrna-verbindungen
WO2006006569A1 (ja) 2004-07-12 2006-01-19 Nihon Nohyaku Co., Ltd. フェニルピリジン類又はその塩類、これらを有効成分とする除草剤及びその使用方法
EP1836169B9 (en) 2004-12-28 2012-07-04 Kinex Pharmaceuticals, LLC Compositions and methods of treating cell proliferation disorders
ES2371397T3 (es) 2005-06-22 2011-12-30 Plexxikon, Inc. Derivados de pirrolo[2,3-b]piridina como inhibidores de proteínas cinasas.
WO2007011760A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
US8053454B2 (en) 2005-10-06 2011-11-08 Exelixis, Inc. Pyridopyrimidinone inhibitors of PIM-1 and/or PIM-3
AR056206A1 (es) 2005-10-06 2007-09-26 Schering Corp Pirazolpirimidinas como inhibidores de protein quinasas
CA2626742A1 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
WO2007052843A1 (ja) 2005-11-04 2007-05-10 Takeda Pharmaceutical Company Limited 複素環アミド化合物およびその用途
WO2007084857A2 (en) 2006-01-13 2007-07-26 President And Fellows Of Harvard College Methods and compositions for treating cell proliferative disorders
US20090253156A1 (en) 2006-05-05 2009-10-08 Perkinelmer Las, Inc. Mass spectrometry methods for multiplexed quantification of protein kinases and phosphatases
JP5564251B2 (ja) 2006-06-29 2014-07-30 キネックス ファーマシューティカルズ， エルエルシー キナーゼカスケードを調節するためのビアリール組成物および方法
PT2041071E (pt) 2006-06-29 2014-09-23 Kinex Pharmaceuticals Llc Composições de biarilo e processos para a regulação de uma cascata de cinases
CA2660560A1 (en) 2006-08-16 2008-02-21 Boehringer Ingelheim International Gmbh Pyrazine compounds, their use and methods of preparation
WO2008045252A2 (en) 2006-10-04 2008-04-17 The Board Of Trustees Of The Leland Stanford Junior University Engineered integrin binding peptides
CN101568527A (zh) * 2006-10-31 2009-10-28 先灵公司 作为蛋白激酶抑制剂的2-氨基噻唑-4-羧酰胺
NZ576234A (en) 2006-11-06 2011-06-30 Supergen Inc Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008106692A1 (en) 2007-03-01 2008-09-04 Novartis Vaccines And Diagnostics, Inc. Pim kinase inhibitors and methods of their use
US20100144751A1 (en) 2007-03-28 2010-06-10 Array Biopharma Inc. IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
CN103214482B (zh) 2007-04-03 2016-06-29 阵列生物制药公司 作为受体酪氨酸激酶抑制剂的咪唑并[1,2-a]吡啶化合物
EP2074103A1 (en) 2007-04-25 2009-07-01 Exelixis, Inc. 6-phenylpyrimidinones as pim modulators
CN102317281A (zh) 2007-04-25 2012-01-11 埃克塞利希斯股份有限公司 作为酪蛋白激素ⅱ(ck2)调节剂的嘧啶酮
EP2178861B1 (en) 2007-07-19 2014-08-20 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
MX2010001340A (es) 2007-07-31 2010-06-02 Schering Corp Combianacion de agente antimitotico e inhibidor de aurora quinasa como tratamiento anticancerigeno.
US8853406B2 (en) 2007-08-06 2014-10-07 Janssen Pharmaceutica Nv Substituted phenylenediamines as inhibitors of the interaction between MDM2 and P53
CA2743756A1 (en) 2007-11-15 2009-05-22 Musc Foundation For Research Development Inhibitors of pim protein kinases, compositions, and methods for treating cancer
US8617534B2 (en) 2007-11-16 2013-12-31 San Diego State University (Sdsu) Foundation Compositions and method for manipulating PIM-1 activity in circulatory system cells
WO2009108912A1 (en) 2008-02-29 2009-09-03 Cylene Pharmaceuticals, Inc. Protein kinase modulators
AR070531A1 (es) * 2008-03-03 2010-04-14 Novartis Ag Inhibidores de cinasa pim y metodos para su uso
US8168794B2 (en) * 2008-03-03 2012-05-01 Novartis Ag Pim kinase inhibitors and methods of their use
MX2010012104A (es) 2008-05-12 2011-04-05 Amnestix Inc Compuestos para mejorar el aprendizaje y la memoria.
KR20110025996A (ko) 2008-06-30 2011-03-14 사일린 파마슈티칼스, 인크 옥신돌 화합물
TWI461423B (zh) 2008-07-02 2014-11-21 Astrazeneca Ab 用於治療Pim激酶相關病狀及疾病之噻唑啶二酮化合物
FR2933409B1 (fr) 2008-07-03 2010-08-27 Centre Nat Rech Scient NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物
WO2010022081A1 (en) 2008-08-19 2010-02-25 Array Biopharma Inc. Triazolopyridine compounds as pim kinase inhibitors
JP5412519B2 (ja) 2008-09-02 2014-02-12 ノバルティス アーゲー キナーゼ阻害剤としてのピコリンアミド誘導体
EA201100427A1 (ru) 2008-09-02 2011-10-31 Новартис Аг Гетероциклические ингибиторы киназы
EP2342190A1 (en) 2008-09-02 2011-07-13 Novartis AG Bicyclic kinase inhibitors
PT3372605T (pt) 2008-10-22 2021-12-09 Array Biopharma Inc Compostos de pirazolo[1,5-a]pirimidina substituídos como inibidores de quinase trk
GB0821307D0 (en) 2008-11-21 2008-12-31 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
TW201035100A (en) 2008-12-19 2010-10-01 Cephalon Inc Pyrrolotriazines as ALK and JAK2 inhibitors
JP5709276B2 (ja) 2009-04-20 2015-04-30 オースペックス ファーマシューティカルズ，エルエルシー ヤヌスキナーゼ３のピペリジンインヒビター
WO2010135401A2 (en) 2009-05-19 2010-11-25 San Diego State University Foundation Kinase-mediated cytoprotection and enhanced cellular engraftment and persistence
AU2010249493A1 (en) 2009-05-20 2011-12-08 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as kinase inhibitors
US20100298302A1 (en) 2009-05-20 2010-11-25 Fabrice Pierre Novel protein kinase modulators
JP5775070B2 (ja) 2009-05-22 2015-09-09 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体
WO2010148351A1 (en) 2009-06-18 2010-12-23 Cylene Pharmaceuticals, Inc. Rhodanines and related heterocycles as kinase inhibitors
BRPI1015135B1 (pt) 2009-06-29 2021-08-03 Incyte Holdings Corporation Pirimidinonas inibidoras de pi3k, composição compreendendo tais compostos, bem como usos dos mesmos
EP2470544A1 (en) 2009-08-26 2012-07-04 Cylene Pharmaceuticals, Inc. Condensed quinolines as protein kinase modulators
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
CN102625807B (zh) * 2009-09-08 2016-03-09 霍夫曼-拉罗奇有限公司 4-取代的吡啶-3-基-甲酰胺化合物和使用方法
US8435976B2 (en) 2009-09-08 2013-05-07 F. Hoffmann-La Roche 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
MX2012002994A (es) 2009-09-11 2012-07-17 Cylene Pharmaceuticals Inc Lactamas heterociclo-substituidas farmaceuticamente utiles.
CA2774148A1 (en) 2009-09-16 2011-03-24 Cylene Pharmaceuticals, Inc. Tricyclic compounds and pharmaceutical uses thereof
JP2013505252A (ja) 2009-09-16 2013-02-14 サイリーン ファーマシューティカルズ インコーポレーティッド 三環式タンパク質キナーゼ調節剤
NZ599040A (en) 2009-10-29 2014-11-28 Genosco 2,4-disubstituted pyrido[4,3-d]pyrimidin-5(6h)-one compounds for selective inhibitors of lrrk2 and syk kinases
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
CN102712601A (zh) 2009-11-12 2012-10-03 赛尔维他股份公司 化合物、其制备方法、药物组合物、化合物的用途、用于调节或调控丝氨酸/苏氨酸激酶的方法以及丝氨酸/苏氨酸激酶调节剂
CN102811619B (zh) 2009-11-13 2015-04-22 金纳斯克公司 激酶抑制剂
US8853235B2 (en) 2009-11-23 2014-10-07 Senhwa Biosciences, Inc. Polymorphs and salts of a kinase inhibitor
EP2509602B9 (en) 2009-12-04 2017-11-01 Senhwa Biosciences, Inc. Pyrazolopyrimidines and related heterocycles as ck2 inhibitors
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
WO2011075630A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors
WO2011075613A1 (en) 2009-12-18 2011-06-23 Sanofi Azaindole derivatives, their preparation and their therapeutic application
KR101858097B1 (ko) 2009-12-23 2018-05-15 자스코 파머수티컬스, 엘엘씨 아미노피리미딘 키나제 억제제
GB201002861D0 (en) 2010-02-19 2010-04-07 Cxr Biosciences Ltd Compositions
DK3050882T3 (en) 2010-03-10 2018-03-19 Incyte Holdings Corp PIPERIDIN-4-YL-AZETIDINE DERIVATIVES AS JAK1 INHIBITORS
PE20130405A1 (es) 2010-04-07 2013-04-10 Hoffmann La Roche Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
JP5816678B2 (ja) 2010-04-14 2015-11-18 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ＰＩ３Ｋδ阻害剤としての縮合誘導体
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
WO2012004217A1 (en) 2010-07-06 2012-01-12 Novartis Ag Cyclic ether compounds useful as kinase inhibitors
CN102985426B (zh) 2010-07-13 2015-10-07 弗·哈夫曼-拉罗切有限公司 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物
US8227773B2 (en) 2010-07-29 2012-07-24 Axcelis Technologies, Inc. Versatile beam glitch detection system
BR112013002112B1 (pt) 2010-07-29 2021-04-06 Rigel Pharmaceuticals, Inc. Composto, composição farmacêutica, e, uso de um composto, ou de um respectivo sal farmaceuticamente aceitável, ou de uma composição
EP2662078A1 (en) 2010-11-10 2013-11-13 National Jewish Health Methods to Treat Allergic Conditions
WO2012065297A1 (en) 2010-11-16 2012-05-24 Impact Therapeutics, Inc. 3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
MX2013006467A (es) 2010-12-09 2013-10-01 Amgen Inc Compuestos biciclicos como inhibidores pim.
US8541576B2 (en) 2010-12-17 2013-09-24 Nerviano Medical Sciences Srl Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
EP3660016A1 (en) 2010-12-20 2020-06-03 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
RU2591191C2 (ru) 2011-01-26 2016-07-10 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Трициклические пирроло производные, способ их получения и их применение в качестве ингибиторов киназы
US8916577B2 (en) 2011-01-26 2014-12-23 Nerviano Medical Sciences S.R.L. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
HUE027675T2 (en) 2011-02-25 2016-11-28 Array Biopharma Inc Triazolopyridine compounds as pim kinase inhibitors
EP2681197A1 (en) 2011-03-04 2014-01-08 Novartis AG Tetrasubstituted cyclohexyl compounds as kinase inhibitors
UY33930A (es) 2011-03-04 2012-10-31 Novartis Ag Inhibidores novedosos de quinasas
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
AU2012230890A1 (en) 2011-03-22 2013-09-26 Amgen Inc. Azole compounds as Pim inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
BR112013025792A2 (pt) 2011-04-05 2018-04-24 Pfizer Ltd Inibidores de quinase relacionada à pirrolo[2,3-d] pirimidina tropomisina
WO2012139930A1 (en) 2011-04-11 2012-10-18 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
EP2699569B1 (en) 2011-04-22 2017-08-30 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
GB201107176D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Pyrrolnitrin derivatives
GB201107197D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Compounds
CA2834166A1 (en) 2011-04-29 2012-11-01 Amgen Inc. Bicyclic pyridazine compounds as pim inhibitors
JP6121991B2 (ja) 2011-05-17 2017-04-26 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ Ｍｋｎｋ１キナーゼ阻害剤としてのアミノ置換イミダゾピリダジン
MX349366B (es) 2011-05-19 2017-07-26 Centro Nac De Investigaciones Oncologicas (Cnio) Compuestos novedosos.
EP2714048A4 (en) 2011-05-27 2014-11-05 Univ Temple SUBSTITUTED 2-BENZYLIDENE-2H-BENZO- [B -] [1,4-] THIAZIN-3- (4H-) ONE, DERIVATIVES THEREOF AND THERAPEUTIC APPLICATIONS THEREOF
JP6073868B2 (ja) 2011-06-01 2017-02-01 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換アミノイミダゾピリダジン
WO2012170827A2 (en) 2011-06-08 2012-12-13 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as ck2 inhibitors
EP2721028B1 (en) 2011-06-20 2015-11-04 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
CA2839958A1 (en) 2011-06-22 2012-12-27 Knut Eis Heterocyclyl aminoimidazopyridazines
EP3812387A1 (en) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
CN102924444B (zh) 2011-08-11 2015-07-08 上海吉铠医药科技有限公司 Pim激酶抑制剂及其制备方法与在制药中的应用
CA2838784A1 (en) 2011-08-12 2013-02-21 F. Hoffmann-La Roche Ag Pyrazolo[3,4-c]pyridine compounds and methods of use
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
JP5843524B2 (ja) 2011-09-02 2016-01-13 キヤノン株式会社 有機無機複合組成物、有機無機複合材料、光学素子および積層型回折光学素子
MX389479B (es) 2011-09-02 2025-03-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k)
UA117092C2 (uk) 2011-09-06 2018-06-25 Байєр Інтеллектуал Проперті Гмбх Амінозаміщені імідазопіридазини
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US9320737B2 (en) 2011-09-23 2016-04-26 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
AU2012314518B2 (en) 2011-09-27 2017-06-29 F. Hoffmann-La Roche Ag Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
US9145418B2 (en) 2011-10-07 2015-09-29 Nerviano Medical Sciences S.R.L. Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors
EP2788350B1 (en) 2011-10-07 2017-12-06 Nerviano Medical Sciences S.r.l. 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
EP2776432B1 (en) 2011-11-04 2017-03-29 Jasco Pharmaceuticals LLC Aminopyrimidine kinase inhibitors
US9394297B2 (en) 2012-02-28 2016-07-19 Amgen Inc. Amides as pim inhibitors
WO2013134079A1 (en) 2012-03-05 2013-09-12 Amgen Inc. Oxazolidinone compounds and derivatives thereof
EP2858993B1 (en) 2012-03-29 2018-01-10 Bayer Intellectual Property GmbH Amino-substituted imidazopyridazines
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
CA2869212A1 (en) 2012-04-04 2013-10-10 Bayer Pharma Aktiengesellschaft Amino-substituted imidazopyridazines
PT3632919T (pt) 2012-04-26 2023-01-06 Univ Montreal Composições farmacêuticas compreendendo derivados de imidazotiadiazol e imidazopirazina como inibidores de recetor 4 ativado por protéase (par4) para o tratamento da agregação plaquetária
KR20150013194A (ko) 2012-04-27 2015-02-04 노파르티스 아게 시클릭 브리지헤드 에테르 dgat1 억제제
KR102163377B1 (ko) 2012-05-09 2020-10-08 바이오젠 엠에이 인코포레이티드 핵 수송 조절인자 및 이의 용도
PE20210667A1 (es) 2012-05-15 2021-04-05 Novartis Ag Derivados de benzamida para la inhibicion de la actividad abl1, abl2 y bcr-abl1
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
AU2013264831B2 (en) 2012-05-21 2016-04-21 Novartis Ag Novel ring-substituted N-pyridinyl amides as kinase inhibitors
MD20140134A2 (ru) 2012-05-22 2015-04-30 Idenix Pharmaceuticals, Inc. Соединения D-аминокислот для лечения болезней печени
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
RU2665462C2 (ru) 2012-06-27 2018-08-30 Ф. Хоффманн-Ля Рош Аг Соединения 5-азаиндазола и способы их применения
TW201408652A (zh) 2012-07-11 2014-03-01 Hoffmann La Roche 作爲ＲＯＲｃ調節劑之芳基磺內醯胺衍生物
TW201414737A (zh) 2012-07-13 2014-04-16 必治妥美雅史谷比公司 作爲激酶抑制劑之咪唑并三□甲腈
WO2014022752A1 (en) 2012-08-03 2014-02-06 Amgen Inc. Macrocycles as pim inhibitors
WO2014033631A1 (en) 2012-08-31 2014-03-06 Novartis Ag N-(3-pyridyl) biarylamides as kinase inhibitors
WO2014033630A1 (en) 2012-08-31 2014-03-06 Novartis Ag Novel aminothiazole carboxamides as kinase inhibitors
CN103664878A (zh) 2012-09-12 2014-03-26 山东亨利医药科技有限责任公司 杂芳环及其衍生物类酪氨酸激酶抑制剂
HK1212684A1 (zh) 2012-09-14 2016-06-17 AbbVie Deutschland GmbH & Co. KG 三環喹啉和喹喔啉衍生物
UA119229C2 (uk) 2012-09-26 2019-05-27 Ф. Хоффманн-Ля Рош Аг Циклічні ефіри піразол-4-ілгетероциклілкарбоксамідних сполук та способи їх застосування
WO2014053568A1 (en) 2012-10-02 2014-04-10 Sanofi Indolyldihydroimidazopyrimidinone derivatives, preparation thereof and therapeutic use thereof
EP2909195B1 (en) 2012-10-16 2017-06-14 Janssen Sciences Ireland UC Rsv antiviral compounds
WO2014071031A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
EP2920176B1 (en) 2012-11-19 2017-09-13 Bayer Pharma Aktiengesellschaft Aminoimidazopyridazines as mknk1 kinase inhibitors
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
PT3486245T (pt) 2012-12-07 2021-07-30 Vertex Pharma 2-amino-n-(piperidin-1-il-piridin-3- il)pirazolo[1,5alfa]pirimidina-3-carboxamida como inibidor da quinase atr
DK2935302T3 (en) 2012-12-18 2018-08-13 Vertex Pharma MANNOS DERIVATIVES FOR TREATING BACTERIAL INFECTIONS
CA2895448A1 (en) 2012-12-19 2014-06-26 Novartis Ag Autotaxin inhibitors
US20150336960A1 (en) 2012-12-19 2015-11-26 Novartis Ag Aryl-substituted fused bicyclic pyridazine compounds
LT3608325T (lt) 2012-12-21 2022-09-12 Gilead Sciences, Inc. Policikliniai karbamoilpiridono junginiai ir jų farmacinis naudojimas
SMT201800669T1 (it) 2012-12-21 2019-01-11 Epizyme Inc Inibitori di prmt5 e loro usi
FR3000569B1 (fr) 2013-01-03 2015-02-13 Peugeot Citroen Automobiles Sa Dispositif d'eclairage a ecran a bord(s) lumineux
US9278950B2 (en) 2013-01-14 2016-03-08 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
SI2945939T1 (sl) 2013-01-15 2020-08-31 Incyte Holdings Corporation Spojine tiazolkarboksamidov in piridinkarboksamida uporabne kot zaviralci PIM kinaze
TWI736135B (zh) 2013-03-01 2021-08-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
PE20200298A1 (es) 2013-03-06 2020-02-06 Incyte Holdings Corp Procesos e intermedios para hacer un inhibidor de jak
JO3383B1 (ar) 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
US20160052926A1 (en) 2013-03-15 2016-02-25 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
DK2970236T3 (en) 2013-03-15 2017-10-16 Idorsia Pharmaceuticals Ltd Pyridin-4-yl derivatives
JO3279B1 (ar) 2013-03-15 2018-09-16 Respivert Ltd مشتقات 2-((4- امينو -3- (3- فلورو-5- هيدروكسي فينيل)-h1- بيرازولو [d-3,4] بيرمدين-1-يل )ميثيل )- 3- (2- تراي فلورو ميثيل ) بينزيل ) كوينازولين -4 (h3)- واحد واستخدامها كمثبطات فوسفواينوسيتايد 3- كاينيز
CA2904985C (en) 2013-03-15 2021-07-20 Japan Tobacco Inc. Pyrazole-amide compound and medicinal uses therefor
UY35421A (es) 2013-03-15 2014-10-31 Nihon Nohyaku Co Ltd Compuesto heterocíclico condensado o su sal, insecticida agrícola u hortícola que comprende el comp uesto y método de uso del insecticida
AP2015008718A0 (en) 2013-03-15 2015-09-30 Global Blood Therapeutics Inc Compounds and uses thereof for the modulation of hemoglobin
TWI689490B (zh) 2013-03-15 2020-04-01 英商邊緣生物科技有限公司 用於治療纖維化之經取代之芳族化合物及相關方法
RU2672584C2 (ru) 2013-03-15 2018-11-16 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи 4-амино-6-(гетероциклил)пиколинаты и 6-амино-2-(гетероциклил)пиримидин-4-карбоксилаты и их применение в качестве гербицидов
US20140275108A1 (en) 2013-03-15 2014-09-18 Galderma Research & Development Novel benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
US9308236B2 (en) 2013-03-15 2016-04-12 Bristol-Myers Squibb Company Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
AR095443A1 (es) 2013-03-15 2015-10-14 Fundación Centro Nac De Investig Oncológicas Carlos Iii Heterociclos condensados con acción sobre atr
BR112015022942B1 (pt) 2013-03-15 2022-02-22 Incyte Holdings Corporation Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos
KR101971385B1 (ko) 2013-03-15 2019-04-22 글로벌 블러드 테라퓨틱스, 인크. 헤모글로빈 조정을 위한 화합물 및 이의 용도
LT2970265T (lt) 2013-03-15 2018-09-25 Plexxikon Inc. Heterocikliniai junginiai ir jų panaudojimas
TWI742541B (zh) 2013-03-15 2021-10-11 英商邊緣生物科技有限公司 用於治療肺纖維化、肝纖維化、皮膚纖維化及心臟纖維化之經取代之芳族化合物
IL277554B2 (en) 2013-08-07 2024-03-01 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
AU2014308703A1 (en) 2013-08-23 2016-03-24 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as Pim kinase inhibitors
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
RS61058B1 (sr) 2014-04-08 2020-12-31 Incyte Corp Lečenje b-ćelijskih maligniteta sa kombinacijom inhibitora jak i pi3k
PE20170300A1 (es) 2014-04-30 2017-04-19 Incyte Corp Procesos para preparar un inhibidor de jak 1 y nuevas formas de este
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
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors

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