CR20150412A - Compuestos de tiazolcarboxamidas y piridinacarboxamida útiles como inhibidores de quinasa pim - Google Patents

Compuestos de tiazolcarboxamidas y piridinacarboxamida útiles como inhibidores de quinasa pim

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Publication number
CR20150412A
CR20150412A CR20150412A CR20150412A CR20150412A CR 20150412 A CR20150412 A CR 20150412A CR 20150412 A CR20150412 A CR 20150412A CR 20150412 A CR20150412 A CR 20150412A CR 20150412 A CR20150412 A CR 20150412A
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CR
Costa Rica
Prior art keywords
thyzolcarboxamides
pyridinacarboxamide
quinasa
pim
inhibitors
Prior art date
Application number
CR20150412A
Other languages
English (en)
Inventor
Chu-Biao Xue
Yun-Long Li
Hao Feng
Jun Pan
Anlai Wang
Ke Zhang
Wenqing Yao
Fenglei Zhang
Jincong Zhuo
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of CR20150412A publication Critical patent/CR20150412A/es

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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Abstract

Se describen derivados de carboxamida de tiazol y piridina de la fórmula (I), o su sal farmacéuticamente aceptable, en donde: X es C o N; A, B y D son anillos; se representa un enlace normalizado en donde el anillo aromático que contiene ambos, un N y X, que están representados formalmente por un enlace C=C cuando X es C y un enlace simple cuando X es N; el anillo A es de la fórmula (A-1) o (A-2): donde E1 y E2 son anillos; sus composiciones y métodos de uso.
CR20150412A 2013-01-15 2015-08-12 Compuestos de tiazolcarboxamidas y piridinacarboxamida útiles como inhibidores de quinasa pim CR20150412A (es)

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

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CR20150412A true CR20150412A (es) 2015-10-27

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Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2734205B1 (en) 2011-07-21 2018-03-21 Tolero Pharmaceuticals, 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
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
ME03780B (me) * 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
TW201605866A (zh) 2013-08-23 2016-02-16 英塞特公司 可用作pim激酶抑制劑之呋喃并-及噻吩并-吡啶甲醯胺化合物
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
CR20170177A (es) * 2014-10-31 2017-09-19 Genoscience Pharma Diamino-quinoleína 2,4 sustituida como nuevos agentes anticancerígenos
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
ES2928164T3 (es) 2015-10-19 2022-11-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
MD3377488T2 (ro) 2015-11-19 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
MY199705A (en) 2015-12-22 2023-11-20 Incyte Corp Heterocyclic compounds as immunomodulators
WO2017192961A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
KR102685249B1 (ko) 2016-06-20 2024-07-17 인사이트 코포레이션 면역조절제로서의 복소환식 화합물
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
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3558973B1 (en) 2016-12-22 2021-09-15 Incyte Corporation Pyridine derivatives as immunomodulators
CA3047991A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
WO2018119224A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
PE20191532A1 (es) 2016-12-22 2019-10-23 Incyte Corp Compuestos heterociclicos como inmunomoduladores
WO2018177993A1 (de) 2017-03-31 2018-10-04 Bayer Cropscience Aktiengesellschaft Pyrazole zur bekämpfung von arthropoden
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
MD3762368T2 (ro) 2018-03-08 2022-07-31 Incyte Corp Compuși diol aminopirazină ca inhibitori ai PI3K-Y
RS64055B1 (sr) 2018-03-30 2023-04-28 Incyte Corp Heterociklična jedinjenja kao imunomodulatori
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
MD3790877T2 (ro) 2018-05-11 2023-08-31 Incyte Corp Derivați de tetrahidro-imidazo[4,5-c]piridină în calitate de imunomodulatori PD-L1
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
US11130769B2 (en) * 2018-11-09 2021-09-28 Prelude Therapeutics, Incorporated Spiro-sulfonamide derivatives as inhibitors of myeloid cell leukemia-1 (MCL-1) protein
AU2020221247B2 (en) 2019-02-12 2024-12-12 Sumitomo Pharma America, Inc. Formulations comprising heterocyclic protein kinase inhibitors
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
CN114450274A (zh) 2019-07-11 2022-05-06 伊斯凯普生物公司 作为lrrk2抑制剂的吲唑及氮杂吲唑
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Pd-1/pd-l1阻害剤の塩
AR120109A1 (es) 2019-09-30 2022-02-02 Incyte Corp Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores
PE20230407A1 (es) 2019-11-11 2023-03-07 Incyte Corp Sales y formas cristalinas de un inhibidor de pd-1/pd-l1
WO2022099075A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Crystalline form of a pd-1/pd-l1 inhibitor
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
TW202233616A (zh) 2020-11-06 2022-09-01 美商英塞特公司 用於製備pd-1/pd-l1抑制劑以及其鹽及結晶形式之方法
WO2023170024A1 (en) * 2022-03-11 2023-09-14 University Of Copenhagen Camk2 modulators and their use in medicine
JP2026509318A (ja) 2022-10-31 2026-03-18 スミトモ・ファーマ・アメリカ・インコーポレイテッド 骨髄増殖性新生物を治療するためのpim1阻害剤
TW202542143A (zh) * 2023-11-27 2025-11-01 美商魯貝多生命科學公司 碳連結bcl抑制劑及抗衰老化合物及其用途

Family Cites Families (193)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
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
WO2006078228A1 (en) 2002-09-16 2006-07-27 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
CA2503905A1 (en) 2002-09-16 2004-03-25 Plexxikon, Inc. Crystal structure of pim-1 kinase
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
WO2005028624A2 (en) 2003-09-15 2005-03-31 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
BRPI0519424B8 (pt) 2004-12-28 2021-05-25 Athenex Inc compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
WO2007011760A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
CA2624882C (en) 2005-10-06 2014-05-20 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
US8053454B2 (en) 2005-10-06 2011-11-08 Exelixis, Inc. Pyridopyrimidinone inhibitors of PIM-1 and/or PIM-3
WO2007048064A2 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Amino-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
CN101595084B (zh) 2006-06-29 2013-01-02 金克斯医药品有限公司 用于调整激酶级联的二芳基组合物和方法
ES2500165T3 (es) 2006-06-29 2014-09-30 Kinex Pharmaceuticals, Llc Composiciones de biarilo y métodos para modular una cascada de quinasas
JP5252404B2 (ja) 2006-08-16 2013-07-31 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 ピラジン化合物、その使用及び調製方法
WO2008045252A2 (en) 2006-10-04 2008-04-17 The Board Of Trustees Of The Leland Stanford Junior University Engineered integrin binding peptides
AR063531A1 (es) * 2006-10-31 2009-01-28 Schering Corp Derivados de anilinopiperazina y composicion farmaceutica
MY146474A (en) 2006-11-06 2012-08-15 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
ES2431163T3 (es) 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
CN101679422A (zh) 2007-03-28 2010-03-24 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
NZ580327A (en) 2007-04-03 2012-02-24 Array Biopharma Inc IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
MX2009011578A (es) 2007-04-25 2009-11-11 Exelixis Inc 6-fenilpirimidinonas como moduladores de pim.
WO2008143759A1 (en) 2007-04-25 2008-11-27 Exelixis, Inc. Pyrimidinones as casein kinase ii (ck2) modulators
WO2009014637A2 (en) * 2007-07-19 2009-01-29 Schering Corporation Heterocyclic amide compounds as protein kinase inhibitors
RU2010106878A (ru) 2007-07-31 2011-09-10 Шеринг Корпорейшн (US) Комбинация антимитотического агента и ингибитора аврора киназы как средство для лечения рака
ES2534899T3 (es) 2007-08-06 2015-04-30 Janssen Pharmaceutica, N.V. Fenilendiaminas sustituidas como inhibidores de la interacción entre MDM2 y p53
WO2009064486A2 (en) 2007-11-15 2009-05-22 Musc Foundation For Research Development Inhibitors of pim protein kinases, compositions, and methods for treating cancer
EP2209889B1 (en) 2007-11-16 2016-07-20 San Diego State University Research Foundation Compositions for manipulating pim-1 activity in cardiac cells
CN102036561A (zh) 2008-02-29 2011-04-27 赛林药物股份有限公司 蛋白激酶调节剂
UY31679A1 (es) * 2008-03-03 2009-09-30 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
CN102088853A (zh) 2008-05-12 2011-06-08 安内斯蒂克斯公司 改善学习和记忆的化合物
WO2010002933A1 (en) 2008-06-30 2010-01-07 Cylene Pharmaceuticals, Inc. Oxindole compounds
UY31952A (es) 2008-07-02 2010-01-29 Astrazeneca Ab 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim
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
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
JP5564045B2 (ja) 2008-09-02 2014-07-30 ノバルティス アーゲー 二環式キナーゼ阻害剤
WO2010026124A1 (en) 2008-09-02 2010-03-11 Novartis Ag Picolinamide derivatives as kinase inhibitors
WO2010026122A1 (en) 2008-09-02 2010-03-11 Novartis Ag Heterocyclic pim-kinase inhibitors
HRP20140309T1 (hr) 2008-10-22 2014-05-09 Array Biopharma, Inc. SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIMIDINA KAO INHIBITORI TRK KINAZE
GB0821307D0 (en) 2008-11-21 2008-12-31 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
EP2376491B1 (en) 2008-12-19 2015-03-04 Cephalon, Inc. Pyrrolotriazines as alk and jak2 inhibitors
EP3026052A1 (en) 2009-04-20 2016-06-01 Auspex Pharmaceuticals, Inc. Preparation of deuterated piperidine inhibitors of janus kinase 3
WO2010135401A2 (en) 2009-05-19 2010-11-25 San Diego State University Foundation Kinase-mediated cytoprotection and enhanced cellular engraftment and persistence
WO2010135571A1 (en) 2009-05-20 2010-11-25 Cylene Pharmaceuticals, Inc. Novel protein kinase modulators
AU2010249493A1 (en) 2009-05-20 2011-12-08 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as kinase inhibitors
MY156727A (en) 2009-05-22 2016-03-15 Incyte Corp 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
US20100331315A1 (en) 2009-06-18 2010-12-30 Mustapha Haddach Rhodanines and related heterocycles as kinase inhibitors
EP2845856A1 (en) 2009-06-29 2015-03-11 Incyte Corporation Pyrimidinones as PI3K inhibitors
MX2012002426A (es) 2009-08-26 2012-06-27 Cylene Pharmaceuticals Inc Quinolinas condensadas como moduladores de proteina 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
ES2557316T3 (es) 2009-09-08 2016-01-25 F. Hoffmann-La Roche Ag Compuestos de piridín-3-il-carboxamida 4-sustituidos y métodos de utilización
KR20120104521A (ko) 2009-09-11 2012-09-21 사일린 파마슈티칼스, 인크 약제학적으로 유용한 헤테로사이클-치환된 락탐
SG179163A1 (en) 2009-09-16 2012-05-30 Cylene Pharmaceuticals Inc Novel tricyclic protein kinase modulators
BR112012005957A2 (pt) 2009-09-16 2019-09-24 Cylene Pharmaceuticals Inc compostos tricíclicos e usos farmacêuticos dos mesmos
MX2012004846A (es) 2009-10-29 2012-10-05 Genosco Inhibidores de cinasa.
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
EP2499117B1 (en) 2009-11-12 2015-10-21 Selvita S.A. A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
US8629132B2 (en) 2009-11-13 2014-01-14 Genosco Kinase inhibitors
WO2011063398A1 (en) 2009-11-23 2011-05-26 Cylene Pharamaceuticals, Inc. Polymorphs and salts of a kinase inhibitor
RU2607453C2 (ru) 2009-12-04 2017-01-10 Сенхва Байосайенсиз, Инк. Пиразолопиримидины и родственные гетероциклы как ск2 ингибиторы
WO2011075613A1 (en) 2009-12-18 2011-06-23 Sanofi Azaindole derivatives, their preparation and their therapeutic application
WO2011075630A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
BR112012015248B1 (pt) 2009-12-23 2022-01-04 Jasco Pharmaceuticals, LLC Composto
GB201002861D0 (en) 2010-02-19 2010-04-07 Cxr Biosciences Ltd Compositions
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EA201290957A1 (ru) 2010-04-07 2013-04-30 Ф.Хоффманн-Ля Рош Аг Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их применения
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
JP2013530199A (ja) 2010-07-06 2013-07-25 ノバルティス アーゲー キナーゼ阻害剤として有用な環状エーテル化合物
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
KR101764952B1 (ko) 2010-07-29 2017-08-03 리겔 파마슈티칼스, 인크. Ampk-활성화 헤테로시클릭 화합물 및 그의 사용 방법
US8227773B2 (en) 2010-07-29 2012-07-24 Axcelis Technologies, Inc. Versatile beam glitch detection system
US8802099B2 (en) 2010-11-10 2014-08-12 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
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US9090593B2 (en) 2010-12-09 2015-07-28 Amgen Inc. Bicyclic compounds as Pim inhibitors
BR112013008527A2 (pt) 2010-12-17 2016-07-12 Nerviano Medical Sciences Srl derivados de pirazolo-quinazolina substituídos como inibidores de cinase
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
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
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
UA111075C2 (uk) 2011-02-25 2016-03-25 Еррей Біофарма Інк. Триазолопіридинові сполуки як інгібітори кінази рім
UY33930A (es) * 2011-03-04 2012-10-31 Novartis Ag Inhibidores novedosos de quinasas
JP2014506915A (ja) 2011-03-04 2014-03-20 ノバルティス アーゲー キナーゼ阻害剤としての四置換シクロヘキシル化合物
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
CA2830780A1 (en) 2011-03-22 2012-09-27 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
CN103534257A (zh) 2011-04-05 2014-01-22 辉瑞有限公司 作为原肌球蛋白相关激酶抑制剂的吡咯并[2,3-d]嘧啶衍生物
WO2012139930A1 (en) 2011-04-11 2012-10-18 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
WO2012145617A2 (en) 2011-04-22 2012-10-26 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
GB201107197D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Compounds
GB201107176D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Pyrrolnitrin derivatives
US9187486B2 (en) 2011-04-29 2015-11-17 Amgen Inc. Bicyclic pyridazine compounds as Pim inhibitors
WO2012156367A1 (en) 2011-05-17 2012-11-22 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines as mknk1 kinase inhibitors
JP5997763B2 (ja) 2011-05-19 2016-09-28 フンダシオン セントロ ナシオナル デ インベスティガシオネス オンコロヒカス カルロス ザ サードFundacion Centro Nacional de Investigaciones Oncologicas Carlos III タンパク質キナーゼ阻害剤としての大環状化合物
AU2012262489A1 (en) 2011-05-27 2013-04-04 Icahn School Of Medicine At Mount Sinai Substituted 2-benzylidene-2H-benzo[b][1,4]thiazin-3(4H)-ones, derivatives thereof, and therapeutic uses thereof
CN103717604B (zh) 2011-06-01 2016-06-01 拜耳知识产权有限责任公司 取代的氨基咪唑并哒嗪
WO2012170827A2 (en) 2011-06-08 2012-12-13 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as ck2 inhibitors
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
HK1197063A1 (en) 2011-06-22 2015-01-02 拜耳知识产权有限责任公司 Heterocyclyl aminoimidazopyridazines
EP2734205B1 (en) 2011-07-21 2018-03-21 Tolero Pharmaceuticals, 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
KR20140071361A (ko) 2011-08-12 2014-06-11 에프. 호프만-라 로슈 아게 피라졸로[3,4-c]피리딘 화합물 및 사용 방법
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
UA121539C2 (uk) 2011-09-02 2020-06-25 Інсайт Холдинґс Корпорейшн Гетероцикліламіни як інгібітори рі3к
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
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
CN103814029B (zh) 2011-09-23 2016-10-12 拜耳知识产权有限责任公司 取代的咪唑并哒嗪
CA2845191A1 (en) 2011-09-27 2013-04-04 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
US9181258B2 (en) 2011-10-07 2015-11-10 Nerviano Medical Sciences S.R.L. Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase 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
US9340549B2 (en) 2012-03-05 2016-05-17 Amgen Inc. Oxazolidinone compounds and derivatives thereof
ES2663609T3 (es) 2012-03-29 2018-04-16 Bayer Intellectual Property Gmbh Imidazopiridazinas amino-sustituidas
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US9409889B2 (en) 2012-04-04 2016-08-09 Bayer Pharma Aktiengesellschaft Amino-substituted imidazopyridazines
SMT201700457T1 (it) 2012-04-26 2017-11-15 Bristol Myers Squibb Co DERlVATI IMIDAZOTIADIAZOLICI E IMIDAZOPIRAZINICI COME INIBITORI DEL RECETTORE ATTIVATO DA PROTEASI 4 (PAR4) PER IL TRATTAMENTO DELL'AGGREGAZIONE PIASTRINICA
MA37439B1 (fr) 2012-04-27 2017-02-28 Novartis Ag Inhibiteurs de dgat1 à ponts éthers cycliques pour le traitement de troubles medies par l'acyle coa-diacylglycerol transferase 1 (dgat1).
IN2014DN09434A (es) 2012-05-09 2015-07-17 Karyopharm Therapeutics Inc
PT2861579T (pt) 2012-05-15 2018-04-27 Novartis Ag Derivados de benzamida para inibir a atividade de abl1, abl2 e bcr-abl
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
PE20150194A1 (es) 2012-05-21 2015-02-08 Novartis Ag Novedosas n-piridinil amidas ciclicas sustituidas como inhibidores de quinasa
AP3913A (en) 2012-05-22 2016-11-26 Idenix Pharamaceuticals Inc D-amino acid compounds for liver disease
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
CA2871388A1 (en) 2012-06-27 2014-01-03 F. Hoffmann-La Roche Ag 5-azaindazole compounds and methods of use
AR092348A1 (es) 2012-07-11 2015-04-15 Hoffmann La Roche DERIVADOS DE ARIL-SULTAMO COMO MODULADORES DE RORc
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
KR20150056608A (ko) 2012-09-14 2015-05-26 아비에 도이치란트 게엠베하 운트 콤파니 카게 트리사이클릭 퀴놀린 및 퀴녹살린 유도체
WO2014048939A1 (en) 2012-09-26 2014-04-03 F. Hoffmann-La Roche Ag Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
WO2014053568A1 (en) 2012-10-02 2014-04-10 Sanofi Indolyldihydroimidazopyrimidinone derivatives, preparation thereof and therapeutic use thereof
NZ705759A (en) 2012-10-16 2019-01-25 Janssen Sciences Ireland Uc Rsv antiviral compounds
JP6359546B2 (ja) 2012-11-01 2018-07-18 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阻害薬としての三環式縮合チオフェン誘導体
HK1208025A1 (en) 2012-11-19 2016-02-19 拜耳医药股份公司 Aminoimidazopyridazines
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
DK2935302T3 (en) 2012-12-18 2018-08-13 Vertex Pharma MANNOS DERIVATIVES FOR TREATING BACTERIAL INFECTIONS
US20150336960A1 (en) 2012-12-19 2015-11-26 Novartis Ag Aryl-substituted fused bicyclic pyridazine compounds
EP2935249B1 (en) 2012-12-19 2018-12-12 Novartis AG Autotaxin inhibitors
US8993555B2 (en) 2012-12-21 2015-03-31 Epizyme, Inc. PRMT5 inhibitors and uses thereof
CA2893843C (en) 2012-12-21 2018-09-04 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
FR3000569B1 (fr) 2013-01-03 2015-02-13 Peugeot Citroen Automobiles Sa Dispositif d'eclairage a ecran a bord(s) lumineux
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
ME03780B (me) 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
TWI841376B (zh) 2013-03-01 2024-05-01 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
MX384910B (es) 2013-03-06 2025-03-14 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
WO2014151008A1 (en) 2013-03-15 2014-09-25 Dow Agrosciences Llc 4-amino-6-(heterocyclic)picolinates and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their use as herbicides
US9227985B2 (en) 2013-03-15 2016-01-05 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
AU2014237330A1 (en) 2013-03-15 2015-09-17 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
TWI689489B (zh) 2013-03-15 2020-04-01 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
HRP20181392T1 (hr) 2013-03-15 2018-10-19 Plexxikon Inc. Heterociklični spojevi i njihova uporaba
BR112015021982B1 (pt) 2013-03-15 2022-12-13 Global Blood Therapeutics, Inc Compostos e seus usos para a modulação de hemoglobina
AR095443A1 (es) 2013-03-15 2015-10-14 Fundación Centro Nac De Investig Oncológicas Carlos Iii Heterociclos condensados con acción sobre atr
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
JP6208603B2 (ja) 2013-03-15 2017-10-04 日本たばこ産業株式会社 ピラゾール−アミド化合物およびその医薬用途
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
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
CN105189487B (zh) 2013-03-15 2017-12-26 爱杜西亚药品有限公司 吡啶‑4‑基衍生物
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
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
US20160052926A1 (en) 2013-03-15 2016-02-25 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
SG11201600815WA (en) 2013-08-07 2016-03-30 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
TW201605866A (zh) 2013-08-23 2016-02-16 英塞特公司 可用作pim激酶抑制劑之呋喃并-及噻吩并-吡啶甲醯胺化合物
SG10201807952PA (en) 2014-02-28 2018-10-30 Incyte Corp Jak1 inhibitors for the treatment of myelodysplastic syndromes
CN106413716B (zh) 2014-04-08 2020-03-27 因赛特公司 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤
BR112016025427A2 (pt) 2014-04-30 2017-08-15 Incyte Corp processos de preparação de um inibidor de jak1 e formas do mesmo
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
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K 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
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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