EA202192575A1 - Соединения dbait в сочетании с ингибиторами киназ для лечения рака - Google Patents

Соединения dbait в сочетании с ингибиторами киназ для лечения рака

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Publication number
EA202192575A1
EA202192575A1 EA202192575A EA202192575A EA202192575A1 EA 202192575 A1 EA202192575 A1 EA 202192575A1 EA 202192575 A EA202192575 A EA 202192575A EA 202192575 A EA202192575 A EA 202192575A EA 202192575 A1 EA202192575 A1 EA 202192575A1
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EA
Eurasian Patent Office
Prior art keywords
dbait
combination
compounds
kinase inhibitors
cancer treatment
Prior art date
Application number
EA202192575A
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English (en)
Inventor
Франсуаза Боно
Жиль Фавр
Оливье Кальвейрак
Original Assignee
Онксео
Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль)
Юниверсите Поль Сабатье Тулуз Iii
Энститю Клодиус Рего
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Application filed by Онксео, Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль), Юниверсите Поль Сабатье Тулуз Iii, Энститю Клодиус Рего filed Critical Онксео
Publication of EA202192575A1 publication Critical patent/EA202192575A1/ru

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    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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Abstract

Изобретение относится к комбинации соединения Dbait с ингибитором протеинкиназы для лечения рака.
EA202192575A 2019-03-21 2020-03-19 Соединения dbait в сочетании с ингибиторами киназ для лечения рака EA202192575A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19305349 2019-03-21
PCT/EP2020/057555 WO2020188015A1 (en) 2019-03-21 2020-03-19 A dbait molecule in combination with kinase inhibitor for the treatment of cancer

Publications (1)

Publication Number Publication Date
EA202192575A1 true EA202192575A1 (ru) 2022-01-14

Family

ID=66103004

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202192575A EA202192575A1 (ru) 2019-03-21 2020-03-19 Соединения dbait в сочетании с ингибиторами киназ для лечения рака

Country Status (12)

Country Link
US (1) US20220143049A1 (ru)
EP (1) EP3942045A1 (ru)
JP (1) JP2022526713A (ru)
KR (1) KR20210142154A (ru)
CN (1) CN114364798A (ru)
AU (1) AU2020242287A1 (ru)
BR (1) BR112021018168B1 (ru)
CA (1) CA3129665A1 (ru)
EA (1) EA202192575A1 (ru)
IL (1) IL284856A (ru)
MX (1) MX2021009863A (ru)
WO (1) WO2020188015A1 (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20200130856A (ko) * 2018-03-13 2020-11-20 옹쎄오 암 치료에서 획득한 내성에 대한 디베이트 분자
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR102657354B1 (ko) * 2021-06-08 2024-04-15 한국과학기술원 Syk 저해제를 포함하는 대장암 예방 또는 치료용 병용투여 조성물
TW202340177A (zh) 2021-12-30 2023-10-16 美商拜歐米富士恩股份有限公司 作為 flt3抑制劑之吡嗪化合物

Family Cites Families (637)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ501276A (en) 1997-07-01 2000-10-27 Warner Lambert Co 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors in treating proliferative disorders
US5932580A (en) 1997-12-01 1999-08-03 Yissum Research And Development Company Of The Hebrew University Of Jerusalem PDGF receptor kinase inhibitory compounds their preparation and compositions
EP1071658B1 (en) 1998-04-17 2004-06-16 Parker Hughes Institute Btk inhibitors and methods for their identification and use
JP2002514572A (ja) 1998-05-04 2002-05-21 ツェンタリス アクチエンゲゼルシャフト インドール誘導体および悪性疾患および病理的細胞増殖にもとづく他の疾患を治療するためのその使用
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
CA2355470C (en) 1999-01-13 2008-09-30 Warner-Lambert Company Benzoheterocycles and their use as mek inhibitors
CA2349832A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
EP1144372B1 (en) 1999-01-13 2005-11-30 Warner-Lambert Company Llc Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors
CA2362380A1 (en) 1999-03-19 2000-09-28 Bristol-Meyers Squibb Pharma Company Amino-thio-acrylonitriles as mek inhibitors
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
US8137695B2 (en) 2006-08-18 2012-03-20 Arrowhead Madison Inc. Polyconjugates for in vivo delivery of polynucleotides
AU5107900A (en) 1999-06-09 2000-12-28 Yamanouchi Pharmaceutical Co., Ltd. Novel heterocyclic carboxamide derivatives
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
EP1222187B1 (en) 1999-10-06 2004-09-22 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
UA74803C2 (ru) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стойкий полиморф гидрохлорида n-(3-этинилфенил)-6,7-бис(2-метоксиэтокси)-4-хиназолинамина, способ его получения (варианты) и фармацевтическое применение
OA12514A (en) 1999-12-24 2006-05-29 Aventis Pharma Ltd Azaindoles.
IL150763A0 (en) 2000-01-24 2003-02-12 Genzyme Corp Jak/stat inhibitors and pharmaceutical compositions containing the same
SI1255752T1 (sl) 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
US7087608B2 (en) 2000-03-03 2006-08-08 Robert Charles Atkins Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
BR0109188A (pt) 2000-03-15 2003-03-18 Warner Lambert Co Diarilaminas 5-amida substituìdas como inibidores de mex
AR035851A1 (es) 2000-03-28 2004-07-21 Wyeth Corp 3-cianoquinolinas, 3-ciano-1,6-naftiridinas y 3-ciano-1,7-naftiridinas como inhibidoras de proteina quinasas
AR028261A1 (es) 2000-03-28 2003-04-30 Wyeth Corp Inhibidores triciclicos de la proteina quinasa
DE10017480A1 (de) 2000-04-07 2001-10-11 Transmit Technologietransfer Verwendung von Substanzen, die als MEK Inhibitor wirken, zur Herstellung eines Arneimittels gegen DNA- und RNA-Viren
JP2001302667A (ja) 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
ATE345788T1 (de) 2001-03-06 2006-12-15 Dorian Bevec Verwendung von mek hemmern zur behandlung von virusvermitteltem hämorragischem schock oder fieber
EP1389209B1 (en) 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
JP2005503361A (ja) 2001-06-29 2005-02-03 アブ サイエンス 肥満細胞症治療のための強力で選択的かつ非毒性のc−kit阻害剤の使用
EP1401412A2 (en) 2001-06-29 2004-03-31 AB Science Use of potent, selective and non toxic c-kit inhibitors for treating tumor angiogenesis
JP2005500041A (ja) 2001-06-29 2005-01-06 アブ サイエンス 強力で選択的かつ非毒性のc−kit阻害剤
ATE388711T1 (de) 2001-09-20 2008-03-15 Ab Science C-kithemmer zur behandlung von bakteriellen infektionen
ATE343575T1 (de) 2001-09-27 2006-11-15 Smithkline Beecham Corp Azaoxoindol derivate als trk protein kinase hemmstoffe zur behandlung von krebs und chronischem schmerz
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
SG2013013339A (en) 2002-03-13 2014-12-30 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
EP1482944A4 (en) 2002-03-13 2006-04-19 Array Biopharma Inc NZ ALKYL BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
AU2003233946A1 (en) 2002-03-15 2003-09-29 Novartis Ag 4-(4-methylpiperazin-1-ylmethyl)-n-(4-methyl-3(4-pyridin-3-yl)pyrimidin-2-yl-amino)phenyl)-benzamide for treating ang ii-mediated diseases
EP1501829B1 (en) 2002-05-06 2010-11-24 Vertex Pharmaceuticals Incorporated Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase
JP2005528443A (ja) 2002-05-30 2005-09-22 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 Jakキナーゼおよびcdk2プロテインキナーゼのインヒビター
GB0215823D0 (en) 2002-07-09 2002-08-14 Astrazeneca Ab Quinazoline derivatives
EP1527071A1 (en) 2002-07-25 2005-05-04 Pfizer Products Inc. Isothiazole derivatives useful as anticancer agents
CA2494695C (en) 2002-08-02 2011-04-05 Ab Science 2-(3-aminoaryl)amino-4-aryl-thiazoles and their use as c-kit inhibitors
JP2006512314A (ja) 2002-11-01 2006-04-13 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 Jakインヒビターおよび他のプロテインキナーゼインヒビターとしての組成物の使用
EP1562938B1 (en) 2002-11-04 2007-08-29 Vertex Pharmaceuticals Incorporated Heteroaryl-pyrimidine derivatives as jak inhibitors
EP1560824A1 (en) 2002-11-05 2005-08-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
ATE508747T1 (de) 2003-03-10 2011-05-15 Eisai R&D Man Co Ltd C-kit kinase-hemmer
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
JP4836788B2 (ja) 2003-07-23 2011-12-14 エグゼリクシス, インコーポレイテッド 未分化リンパ腫キナーゼ変調因子及びその使用法
BRPI0413255A (pt) 2003-08-01 2006-10-03 Wyeth Corp uso de uma combinação de um inibidor de quinase do receptor do fator de crescimento epidérmico e agentes citotóxicos para tratamento e inibição do cáncer
NZ585188A (en) 2003-08-15 2011-09-30 Novartis Ag 2,4-Pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
EP1664032B1 (en) 2003-08-21 2008-11-05 OSI Pharmaceuticals, Inc. N-substituted pyrazolyl-amidyl-benzimidazolyl c-kit inhibitors
AU2004268949A1 (en) 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl C-kit inhibitors
DE602004020073D1 (de) 2003-08-21 2009-04-30 Osi Pharm Inc 3-substituierte imidazopyridinderivate als c-kit-inhibitoren
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
DE10342794A1 (de) 2003-09-16 2005-04-21 Basf Ag Sekretion von Proteinen aus Hefen
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
US8084645B2 (en) 2003-09-19 2011-12-27 Chugai Seiyaku Kabushiki Kaisha 4-phenylamino-benzaldoxime derivatives and uses thereof as mitogen-activated protein kinase kinase (MEK) inhibitors
BRPI0414698A (pt) 2003-09-23 2006-11-28 Novartis Ag combinação de um inibidor receptor de vegf com um agente quimioterapêutico
KR100872204B1 (ko) 2003-10-15 2008-12-09 오에스아이 파마슈티컬스, 인코포레이티드 이미다조피라진 티로신 키나제 억제제
EP1526177A1 (en) 2003-10-24 2005-04-27 Institut Curie Nucleic acids useful for triggering tumor cell lethality
US7476729B2 (en) * 2003-10-24 2009-01-13 Institut Curie Dbait and uses thereof
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
CA2546353A1 (en) 2003-11-19 2005-06-09 Array Biopharma Inc. Bicyclic inhibitors of mek and methods of use thereof
DE102004001607A1 (de) 2004-01-09 2005-08-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittelkombinationen auf der Basis von Scopin- oder Tropensäureestern mit EGFR-Kinase-Hemmern
CA2554925A1 (en) 2004-01-30 2005-08-11 Ab Science 2-(3-substituted-aryl)amino-4-aryl-thiazoles as tyrosine kinase inhibitors
EP1719762B1 (en) 2004-02-27 2012-06-27 Eisai R&D Management Co., Ltd. Novel pyridine derivative and pyrimidine derivative (1)
TWI372624B (en) 2004-03-30 2012-09-21 Vertex Pharma Azaindoles useful as inhibitors of jak and other protein kinases
FR2868422B1 (fr) 2004-03-31 2006-07-14 Aventis Pharma Sa Nouveaux derives pyrrolo(2,3-b) pyridine, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
TWI378934B (en) 2004-04-02 2012-12-11 Osi Pharm Inc 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
CA2568756A1 (en) 2004-06-15 2005-12-29 Astrazeneca Ab Substituted quinazolones as anti-cancer agents
TW200616974A (en) 2004-07-01 2006-06-01 Astrazeneca Ab Chemical compounds
CN103251953A (zh) 2004-07-19 2013-08-21 约翰·霍普金斯大学 供免疫抑制的flt3抑制剂
MY144232A (en) 2004-07-26 2011-08-15 Chugai Pharmaceutical Co Ltd 5-substituted-2-phenylamino benzamides as mek inhibitors
WO2007040469A2 (en) 2005-09-15 2007-04-12 Kosak Ken M Chloroquine coupled compositions and methods for their synthesis
BRPI0514691A (pt) 2004-08-31 2008-06-17 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, composição farmacêutica, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo
EP1789400A1 (en) 2004-09-01 2007-05-30 AstraZeneca AB Quinazolinone derivatives and their use as b-raf inhibitors
KR20070057955A (ko) 2004-09-17 2007-06-07 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 디아미노트리아졸 화합물
WO2006040568A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
WO2006056427A1 (en) 2004-11-24 2006-06-01 Laboratoires Serono S.A. Novel 4-arylamino pyridone derivatives as mek inhibitors for the treatment of hyperproliferative disorders
EP1831206B1 (en) 2004-12-01 2011-08-24 OSI Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library
JP2008521858A (ja) 2004-12-01 2008-06-26 ラボラトワール セローノ ソシエテ アノニム 過増殖性疾患を処置するための[1,2,4]トリアゾロ[4,3−a]ピリジン誘導体
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.
UY29300A1 (es) 2004-12-22 2006-07-31 Astrazeneca Ab Compuestos quimicos
AU2006208834A1 (en) 2005-01-25 2006-08-03 Astrazeneca Ab Chemical compounds
WO2006080450A1 (ja) 2005-01-27 2006-08-03 Kyowa Hakko Kogyo Co., Ltd. Igf-1r阻害剤
DK1846394T3 (da) 2005-02-04 2012-01-16 Astrazeneca Ab Pyrazolylaminopyridinderivater, der er egnede som kinaseinhibitorer
PT1853588E (pt) 2005-02-16 2008-08-25 Astrazeneca Ab Compostos químicos
CA2598076A1 (en) 2005-02-16 2006-08-24 Astrazeneca Ab Chemical compounds
WO2006093247A1 (ja) 2005-02-28 2006-09-08 Japan Tobacco Inc. Syk阻害活性を有する新規なアミノピリジン化合物
AU2006229343A1 (en) 2005-03-28 2006-10-05 Kirin Pharma Kabushiki Kaisha Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency
AU2006231929B2 (en) 2005-04-04 2012-09-06 Ab Science Substituted oxazole derivatives and their use as tyrosine kinase inhibitors
WO2006112479A1 (ja) 2005-04-19 2006-10-26 Kyowa Hakko Kogyo Co., Ltd. 含窒素複素環化合物
EP1899323A2 (en) 2005-05-16 2008-03-19 AstraZeneca AB Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
SG177981A1 (en) 2005-05-18 2012-02-28 Array Biopharma Inc 4-(phenylamino)-6-oxo-1, 6-dihydropyridazine-3-carboxamide derivatives as mek inhibitors for the treatment of hyperproliferative diseases
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
WO2006133417A1 (en) 2005-06-07 2006-12-14 Valeant Pharmaceuticals International Phenylamino isothiazole carboxamidines as mek inhibitors
US20070021435A1 (en) 2005-06-10 2007-01-25 Gaul Michael D Aminopyrimidines as kinase modulators
RU2408584C2 (ru) 2005-06-23 2011-01-10 Мерк Шарп Энд Домэ Корп. Ингибиторы тирозинкиназы
TW200738638A (en) 2005-06-23 2007-10-16 Merck & Co Inc Tyrosine kinase inhibitors
TW200740820A (en) 2005-07-05 2007-11-01 Takeda Pharmaceuticals Co Fused heterocyclic derivatives and use thereof
WO2007007919A2 (en) 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
EP1904065A2 (en) 2005-07-14 2008-04-02 AB Science Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma
AR054834A1 (es) 2005-07-15 2007-07-18 Glaxo Group Ltd Derivados de 1,1-dioxido-2,3-dihidro-1,2-benzoisotiazol-6-il-1h-indazol-4-il-2,4 pirimidina diamina
WO2007028445A1 (en) 2005-07-15 2007-03-15 Glaxo Group Limited 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives
WO2009018233A1 (en) 2007-07-30 2009-02-05 Ardea Biosciences, Inc. Derivatives of n-(arylamino) sulfonamides including polymorphs as inhibitors of mek as well as compositions, methods of use and methods for preparing the same
MX2008002114A (es) 2005-07-21 2008-04-17 Ardea Biosciences Inc Inhibidores de n-(arilamino)-sulfonamida de mek.
HRP20130719T1 (en) 2005-08-24 2013-09-30 Eisai R&D Management Co., Ltd. Novel pyridine derivative and pyrimidine derivative (3)
WO2007030680A2 (en) 2005-09-07 2007-03-15 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as axl inhibitors
FR2891273B1 (fr) 2005-09-27 2007-11-23 Aventis Pharma Sa NOUVEAUX DERIVES BENZIMIDAZOLES ET BENZOTHIAZOLES, LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE NOTAMMENT COMME INHIBITEURS DE CMet
EP1928236B1 (en) 2005-09-27 2011-11-23 Irm Llc Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors
HRP20110498T1 (hr) 2005-10-07 2011-08-31 Exelixis Azetidini kao inhibitori mek za liječenje proliferativnih bolesti
WO2007042298A1 (en) 2005-10-13 2007-04-19 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
KR101146852B1 (ko) 2005-12-05 2012-05-16 화이자 프로덕츠 인크. C?met/hgfr 억제제의 다형체
EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
JP2009520028A (ja) 2005-12-19 2009-05-21 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド Igfr抑制剤および抗癌剤の併用
EP1966155A1 (en) 2005-12-21 2008-09-10 AstraZeneca AB Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer
JP2009520784A (ja) 2005-12-22 2009-05-28 アストラゼネカ アクチボラグ キナゾリン誘導体、その製造方法および抗癌剤としてのその使用
CN102532133A (zh) 2006-01-17 2012-07-04 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的吖吲哚类
FR2896503B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives soufres d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
FR2896504B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
TW200740776A (en) 2006-02-06 2007-11-01 Osi Pharm Inc N-phenylbenzotriazolyl c-kit inhibitors
ES2336625T3 (es) 2006-03-22 2010-04-14 Vertex Pharmaceuticals Incorporated Inhibidores de la proteina quinasa c-met para el tratamiento de trastornos proliferativos.
CN101415688A (zh) 2006-04-05 2009-04-22 阿斯利康(瑞典)有限公司 具有b-raf抑制活性的喹唑啉酮衍生物
WO2007113557A1 (en) 2006-04-05 2007-10-11 Astrazeneca Ab Substituted quinazolines with anti-cancer activity
JP2009532475A (ja) 2006-04-05 2009-09-10 バーテックス ファーマシューティカルズ インコーポレイテッド ヤヌスキナーゼの阻害剤として有用なデアザプリン
US20090203718A1 (en) 2006-04-13 2009-08-13 Smithkline Beecham (Cork) Ltd. Cancer treatment method
MX2008013097A (es) 2006-04-18 2008-10-27 Ardea Biosciences Inc Piridona sulfonamidas y piridona sulfamidas como inhibidores de metiletilcetona.
CN101421253A (zh) 2006-04-18 2009-04-29 阿斯利康(瑞典)有限公司 喹唑啉-4-酮衍生物、其制备方法及含有它们的药用组合物
ZA200807263B (en) 2006-04-19 2009-11-25 Serono Lab Novel heteroaryl-substituted arylaminopyrldine derivatives as MEK inhibitors
JP5182088B2 (ja) 2006-04-19 2013-04-10 アステラス製薬株式会社 アゾールカルボキサミド誘導体
EA016611B1 (ru) 2006-04-20 2012-06-29 Янссен Фармацевтика Н.В. Способ лечения мастоцитоза
EP2026775B1 (en) 2006-05-09 2015-04-29 Novaremed Ltd. Use of syk tyrosine kinase inhibitors for the treatment of cell proliferative disorders
RU2448708C3 (ru) 2006-05-18 2017-09-28 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство против рака щитовидной железы
WO2008005877A2 (en) 2006-06-30 2008-01-10 Board Of Regents, The University Of Texas System Inhibitors of c-kit and uses thereof
TW200813021A (en) 2006-07-10 2008-03-16 Merck & Co Inc Tyrosine kinase inhibitors
DE602007004638D1 (de) 2006-07-20 2010-03-18 Amgen Inc Benzoädüisoxazol-derivate als c-kit-tyrosinkinase-hemmer zur behandlung von erkrankungen im zusammenhang mit der überproduktion von histamin
PE20080538A1 (es) 2006-08-04 2008-06-18 Takeda Pharmaceutical Derivado heterociclico fusionado y su uso
US20100216791A1 (en) 2006-08-17 2010-08-26 Astrazeneca Pyridinylquinazolinamine derivatives and their use as b-raf inhibitors
CA2661333C (en) 2006-08-23 2014-08-05 Eisai R&D Management Co., Ltd. Salt of phenoxypyridine derivative or crystal thereof and process for producing the same
CL2007002617A1 (es) 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
BRPI0622054B8 (pt) 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
CA2666116A1 (en) 2006-10-16 2008-04-24 Novartis Ag Phenylacetamides useful as protein kinase inhibitors
JPWO2008047831A1 (ja) 2006-10-17 2010-02-25 協和発酵キリン株式会社 Jak阻害剤
TW200829566A (en) 2006-12-08 2008-07-16 Astrazeneca Ab Chemical compounds
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
WO2008076143A1 (en) 2006-12-18 2008-06-26 Osi Pharmaceuticals, Inc. Combination of igfr inhibitor and anti-cancer agent
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
WO2008080134A2 (en) 2006-12-22 2008-07-03 Rigel Pharmaceuticals, Inc. 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
ES2672172T3 (es) 2006-12-29 2018-06-12 Rigel Pharmaceuticals, Inc. Triazoles N3-heteroarilsustituidos y triazoles N5-heteroarilsustituidos útiles como inhibidores de Axl
EP2079736B1 (en) 2006-12-29 2017-10-18 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
WO2008083353A1 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2078010B1 (en) 2006-12-29 2014-01-29 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2114955B1 (en) 2006-12-29 2013-02-13 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP1944369A1 (en) * 2007-01-12 2008-07-16 The Centre National de la Recherche Scientifique Dbait and its standalone uses thereof
MX2009007661A (es) 2007-01-19 2009-12-14 Ardea Biosciences Inc Inhibidores de mek.
WO2008098139A2 (en) 2007-02-07 2008-08-14 The Regents Of The University Of Colorado Axl tyrosine kinase inhibitors and methods of making and using the same
EP2119706A4 (en) 2007-02-23 2011-04-27 Eisai R&D Man Co Ltd PYRIDINE OR PYRIMIDINE DERIVATIVITY WITH EXCELLENT CELL GROWTH-INHIBITORY EFFECT AND EXCELLENT ANTITUMOR EFFECT ON A CELL STRAIN WITH AN AMPLIFIED HGFR GENE
KR20090115866A (ko) 2007-03-05 2009-11-09 교와 핫꼬 기린 가부시키가이샤 의약 조성물
HRP20151386T1 (hr) 2007-03-12 2016-02-26 Ym Biosciences Australia Pty Ltd Fenil aminopirimidinski spojevi i njihova primjena
CN101778825A (zh) 2007-03-22 2010-07-14 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的n-杂环类化合物
IL295053A (en) 2007-03-28 2022-09-01 Pharmacyclics Llc Broton tyrosine kinase inhibitors
EP2139869A2 (en) 2007-04-13 2010-01-06 SuperGen, Inc. Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders
UA99459C2 (en) 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
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.
GB0714384D0 (en) 2007-07-23 2007-09-05 Ucb Pharma Sa theraputic agents
UA99731C2 (ru) 2007-07-30 2012-09-25 Ардеа Биосайенсис, Инк Кристаллические полиморфные формы n-(ариламино)сульфонамидов как ингибиторы мэк, композиция (варианты) и применение
PA8792501A1 (es) 2007-08-09 2009-04-23 Sanofi Aventis Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met.
WO2009031011A2 (en) 2007-09-05 2009-03-12 Pfizer Limited Xinafoate salt of n4-(2, 2-difluoro-4h-benz0 [1,4] 0xazin-3-one) -6-yl] -5-fluoro-n2- [3- (methylaminocar bonylmethyleneoxy) phenyl] 2, 4-pyrimidinediamine
WO2009053269A1 (en) 2007-10-23 2009-04-30 F. Hoffmann-La Roche Ag Novel kinase inhibitors
RU2461551C2 (ru) 2007-10-24 2012-09-20 Астеллас Фарма Инк. Азолкарбоксамидное соединение или его фармацевтически приемлемая соль
WO2009054864A1 (en) 2007-10-26 2009-04-30 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
EP3109249A1 (en) 2007-11-15 2016-12-28 YM BioSciences Australia Pty Ltd N-containing heterocyclic compounds
US20110039856A1 (en) 2007-11-29 2011-02-17 Pfizer Inc. Polymorphs of a c-met/hgfr inhibitor
WO2009093008A1 (en) 2008-01-21 2009-07-30 Ucb Pharma S.A. Thieno-pyridine derivatives as mek inhibitors
GB0801416D0 (en) 2008-01-25 2008-03-05 Piramed Ltd Pharmaceutical compounds
KR101599082B1 (ko) 2008-02-01 2016-03-02 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
CA2710462C (en) 2008-02-05 2015-11-24 F. Hoffmann-La Roche Ag Pyridinones and pyridazinones
CA2714700C (en) 2008-02-22 2013-07-30 Irm Llc Heterocyclic compounds and compositions as c-kit and pdgfr kinase inhibitors
JP2011513331A (ja) 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド ピラゾール[3,4−b]ピリジンRAF阻害剤
PE20091561A1 (es) 2008-02-29 2009-10-30 Array Biopharma Inc Compuestos inhibidores de raf y metodos para su uso
ES2392482T3 (es) 2008-02-29 2012-12-11 Array Biopharma, Inc. Derivados de imidazo[4,5-b] piridina usados como inhibidores de RAF
JP2011513332A (ja) 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド 癌の治療のためのraf阻害剤としてのn−(6−アミノピリジン−3−イル)−3−(スルホンアミド)ベンズアミド誘導体
US8158616B2 (en) 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
JP5628145B2 (ja) 2008-03-19 2014-11-19 ケムブリッジ・コーポレーション 新規チロシンキナーゼ阻害剤
WO2009126933A2 (en) 2008-04-11 2009-10-15 Alnylam Pharmaceuticals, Inc. Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
US8808742B2 (en) 2008-04-14 2014-08-19 Ardea Biosciences, Inc. Compositions and methods for preparing and using same
EP2262772B8 (en) 2008-04-16 2013-03-13 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinoline derivatives as axl kinase inhibitors
SG2014015085A (en) 2008-04-16 2014-06-27 Portola Pharm Inc 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors
EA024109B1 (ru) 2008-04-16 2016-08-31 Портола Фармасьютиклз, Инк. Ингибиторы протеинкиназ
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
WO2009132202A2 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
WO2009143211A2 (en) 2008-05-21 2009-11-26 Incyte Corporation Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same
GB0811304D0 (en) 2008-06-19 2008-07-30 Ucb Pharma Sa Therapeutic agents
MX2010014234A (es) 2008-06-19 2011-03-25 Astrazeneca Ab Compuestos pirazol 436.
EP2288260A4 (en) 2008-06-20 2013-10-23 Genentech Inc TRIAZOLOPYRIDINE-JAK HEMMER COMPOUNDS AND METHOD
BRPI0909945A2 (pt) 2008-06-20 2015-07-28 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
ES2552320T3 (es) 2008-06-24 2015-11-27 F. Hoffmann-La Roche Ag Nuevas piridín-2-onas y piridazín-3-onas sustituidas
US8431594B2 (en) 2008-07-09 2013-04-30 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors
CA2730231C (en) 2008-07-09 2016-10-18 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
ES2660418T3 (es) 2008-07-16 2018-03-22 Pharmacyclics Llc Inhibidores de la tirosina quinasa de Bruton para el tratamiento de tumores sólidos
PE20110560A1 (es) 2008-07-18 2011-08-29 Sanofi Aventis NUEVOS DERIVADOS DE TRIAZOLO[4,3-a]PIRIDINA, SU PROCEDIMIENTO DE PREPARACION, SU APLICACION COMO MEDICAMENTOS, COMPOSICIONES FARMACEUTICAS Y NUEVA UTILIZACION PARTICULARMENTE COMO INHIBIDORES DE MET
KR20110039559A (ko) 2008-07-18 2011-04-19 사노피-아벤티스 신규 이미다조[1,2-a]피리딘 유도체, 그의 제조 방법, 의약으로서의 그의 용도, 제약 조성물, 및 특히 met 억제제로서의 신규 용도
FR2933982A1 (fr) 2008-07-18 2010-01-22 Sanofi Aventis Nouveaux derives imidazo°1,2-a!pyrimidine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met
UA107183C2 (uk) 2008-08-04 2014-12-10 Феніламіно-ізонікотинамідні сполуки, їх застосування, фармацевтична композиція, що їх містить, та спосіб лікування гіперпроліферативних захворювань
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
PT2350075E (pt) 2008-09-22 2014-06-09 Array Biopharma Inc Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase
AR074052A1 (es) 2008-10-22 2010-12-22 Array Biopharma Inc Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa
CN102271515B (zh) 2008-10-31 2014-07-02 健泰科生物技术公司 吡唑并嘧啶jak抑制剂化合物和方法
WO2010056875A1 (en) 2008-11-12 2010-05-20 Cgi Pharmaceuticals, Inc. Pyridazinones and their use as btk inhibitors
NZ592825A (en) 2008-11-19 2013-01-25 Vertex Pharma A triazolothiadiazole inhibitor of c-met protein kinase
EA021293B1 (ru) 2008-12-08 2015-05-29 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
CN102307474B (zh) 2008-12-08 2015-04-01 吉利德康涅狄格股份有限公司 咪唑并吡嗪syk抑制剂
ITMI20082336A1 (it) 2008-12-29 2010-06-30 Univ Parma Composti inibitori irreversibili di egfr con attivita' antiproliferativa
AU2010219097A1 (en) 2009-01-13 2011-08-04 Glaxo Group Limited Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase
CA3121743A1 (en) 2009-01-15 2010-07-22 Incyte Holdings Corporation Processes for preparing jak inhibitors and related intermediate compounds
SG172997A1 (en) 2009-01-16 2011-08-29 Rigel Pharmaceuticals Inc Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer
US8765727B2 (en) 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
FR2941952B1 (fr) 2009-02-06 2011-04-01 Sanofi Aventis Derives de 6-(6-substitue-triazolopyridazine-sulfanyl) 5-fluoro-benzothiazoles et 5-fluoro-benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met.
FR2941951B1 (fr) 2009-02-06 2011-04-01 Sanofi Aventis Derives de 6-(6-nh-substitue-triazolopyridazine-sulfanyl) benzothiazoles et benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met.
US20100204221A1 (en) 2009-02-09 2010-08-12 Hariprasad Vankayalapati Pyrrolopyrimidinyl axl kinase inhibitors
CN106478496A (zh) 2009-03-27 2017-03-08 阿迪生物科学公司 作为mek抑制剂的二氢吡啶磺酰胺和二氢吡啶硫酰胺
BRPI0925050A2 (pt) 2009-04-21 2015-08-04 Novartis Ag Compostos heterocíclicos como inibidores de mek
EP2424368B1 (en) 2009-04-29 2014-12-31 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
EP3613729A1 (en) 2009-06-10 2020-02-26 Chugai Seiyaku Kabushiki Kaisha Tetracyclic compounds
AR077033A1 (es) 2009-06-11 2011-07-27 Hoffmann La Roche Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas
WO2010147898A2 (en) 2009-06-15 2010-12-23 Rigel Pharmaceuticals, Inc. Small molecule inhibitors of spleen tyrosine kinase (syk)
CN102134218A (zh) 2009-06-15 2011-07-27 凯美隆(北京)药业技术有限公司 6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂
TWI462920B (zh) 2009-06-26 2014-12-01 葛萊伯格有限公司 用於治療退化性及發炎疾病之新穎化合物
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
TW201105669A (en) 2009-07-30 2011-02-16 Irm Llc Compounds and compositions as Syk kinase inhibitors
JP2013501002A (ja) 2009-07-30 2013-01-10 アイアールエム・リミテッド・ライアビリティ・カンパニー Sykキナーゼ阻害剤としての化合物および組成物
US20130018033A1 (en) 2009-08-28 2013-01-17 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
WO2011025951A1 (en) 2009-08-28 2011-03-03 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
CN102666498A (zh) 2009-08-28 2012-09-12 健泰科生物技术公司 Raf抑制剂化合物及其使用方法
EP2470532A1 (en) 2009-08-28 2012-07-04 Array Biopharma, Inc. 1h-pyrazolo [ 3, 4-b]pyridine compounds for inhibiting raf kinase
PT2473049T (pt) 2009-09-04 2019-03-04 Sunesis Pharmaceuticals Inc Inibidores de tirosina quinase de bruton
US9029359B2 (en) 2009-09-04 2015-05-12 Biogen Idec Ma, Inc. Heteroaryl Btk inhibitors
CA2772127A1 (en) 2009-09-30 2011-04-07 Merck Sharp & Dohme Ltd Formulations for c-met kinase inhibitors
CN102666512B (zh) 2009-10-13 2014-11-26 奥斯特姆医疗公司 对疾病治疗有用的mek抑制剂
US8703781B2 (en) 2009-10-16 2014-04-22 Glaxosmithkline Llc Pharmaceutical combination of MEK inhibitor and B-RAF inhibitors
JP5466767B2 (ja) 2009-11-04 2014-04-09 ノバルティス アーゲー Mek阻害剤として有用なヘテロ環式スルホンアミド誘導体
WO2011075517A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US8735417B2 (en) 2009-12-17 2014-05-27 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
PH12012501293A1 (en) 2009-12-23 2013-01-07 Arqule Inc Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same
SG181857A1 (en) 2009-12-23 2012-07-30 Takeda Pharmaceutical Fused heteroaromatic pyrrolidinones as syk inhibitors
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
MX2012008083A (es) 2010-01-12 2012-08-15 Ab Science Inhibidores de triazol y oxazol quinaza.
NZ600857A (en) 2010-01-29 2014-06-27 Boehringer Ingelheim Int Substituted naphthyridines and their use as syk kinase inhibitors
CN103168039B (zh) 2010-03-11 2016-08-03 吉利德康涅狄格公司 咪唑并吡啶类syk抑制剂
US8481541B2 (en) 2010-03-22 2013-07-09 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
ES2677356T3 (es) 2010-03-24 2018-08-01 Amitech Therapeutics Solutions, Inc. Compuestos heterocíclicos útiles para la inhibición de quinasas
WO2011121223A1 (fr) 2010-03-30 2011-10-06 Sanofi-Aventis Derives de 6-(alkyl- ou cycloalkyl-triazolopyridazine-sulfanyl) benzothiazoles: preparation, application comme medicaments et utilisation comme inhibiteurs de met
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
EP2566858A2 (en) 2010-05-04 2013-03-13 Pfizer Inc. Heterocyclic derivatives as alk inhibitors
WO2011143646A1 (en) 2010-05-14 2011-11-17 OSI Pharmaceuticals, LLC Fused bicyclic kinase inhibitors
CA2799904A1 (en) 2010-05-20 2011-11-24 F. Hoffmann-La Roche Ag Pyrrolo [2, 3 - b] pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
CN102906095A (zh) 2010-05-20 2013-01-30 弗·哈夫曼-拉罗切有限公司 作为syk和jak抑制剂的吡咯并吡嗪衍生物
JP2013527195A (ja) 2010-05-27 2013-06-27 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 c−Metプロテインキナーゼのアミノピラゾールトリアゾロチアジアゾールインヒビター
WO2011147764A1 (en) 2010-05-28 2011-12-01 N.V. Organon Thieno (2, 3b) pyrazine compounds as b - raf inhibitors
BR112012030711B1 (pt) 2010-05-31 2020-10-13 Ono Pharmaceutical Co. Ltd derivado de purinona
CN107898791A (zh) 2010-06-03 2018-04-13 药品循环有限责任公司 布鲁顿酪氨酸激酶(btk)抑制剂的应用
US9205099B2 (en) 2010-06-22 2015-12-08 Dna Therapeutics Optimized in vivo delivery system with endosomolytic agents for nucleic acid conjugates
WO2012002577A1 (ja) 2010-06-30 2012-01-05 富士フイルム株式会社 新規なニコチンアミド誘導体またはその塩
WO2012005299A1 (ja) 2010-07-07 2012-01-12 日本新薬株式会社 Rosチロシンキナーゼ阻害剤
WO2012006960A1 (en) 2010-07-14 2012-01-19 Zhejiang Beta Pharma Inc. NOVEL FUSED HETEROCYCLIC DERIVATIVES USEFUL AS c-MET TYROSINE KINASE INHIBITORS
KR20130091331A (ko) 2010-07-16 2013-08-16 교와 핫꼬 기린 가부시키가이샤 함질소 방향족 복소환 유도체
WO2012008564A1 (ja) 2010-07-16 2012-01-19 協和発酵キリン株式会社 含窒素芳香族複素環誘導体
AR085183A1 (es) 2010-07-30 2013-09-18 Lilly Co Eli Compuesto 6-(1-metil-1h-pirazol-4-il)-3-(2-metil-2h-indazol-5-iltio)-[1,2,4]triazol[4,3-b]piridazina, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para tratar cancer
UY33539A (es) 2010-08-02 2012-02-29 Astrazeneca Ab Compuestos químicos alk
CN105566229A (zh) 2010-08-10 2016-05-11 西建阿维拉米斯研究公司 Btk抑制剂的苯磺酸盐及其用途和制备方法
CA2808210C (en) 2010-08-20 2019-10-01 Chugai Seiyaku Kabushiki Kaisha Tetracyclic compounds having alk inhibitory activity and compositions thereof
WO2012025186A1 (en) 2010-08-27 2012-03-01 Merck Patent Gmbh Triazolopyrazine derivatives
AU2011295441B2 (en) 2010-08-27 2015-04-09 Merck Patent Gmbh Furopyridine derivatives
EP2423208A1 (en) 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmaceutically active compounds as Axl inhibitors
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
US8664244B2 (en) 2010-09-12 2014-03-04 Advenchen Pharmaceuticals, LLC Compounds as c-Met kinase inhibitors
WO2012037155A2 (en) 2010-09-13 2012-03-22 Gtx, Inc. Tyrosine kinase inhibitors
JO3062B1 (ar) 2010-10-05 2017-03-15 Lilly Co Eli R)-(e)-2-(4-(2-(5-(1-(3، 5-داي كلورو بيريدين-4-يل)إيثوكسي)-1h-إندازول-3-يل)?ينيل)-1h-بيرازول-1-يل)إيثانول بلوري
WO2012048258A2 (en) 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds as kinase inhibitor compounds
EP2635556B1 (en) 2010-11-01 2017-06-21 Portola Pharmaceuticals, Inc. Benzamides and nicotinamides as syk modulators
CN102020651B (zh) 2010-11-02 2012-07-18 北京赛林泰医药技术有限公司 6-芳基氨基吡啶酮甲酰胺mek抑制剂
CN102532141A (zh) 2010-12-08 2012-07-04 中国科学院上海药物研究所 [1,2,4]三唑并[4,3-b][1,2,4]三嗪类化合物、其制备方法和用途
US20130004481A1 (en) 2011-01-12 2013-01-03 Boehringer Ingelheim International Gmbh Anticancer therapy
WO2012116217A1 (en) 2011-02-25 2012-08-30 Irm Llc Compounds and compositions as trk inhibitors
US20140005188A1 (en) 2011-03-11 2014-01-02 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
EP2691399B1 (en) 2011-03-28 2016-07-13 F.Hoffmann-La Roche Ag Thiazolopyrimidine compounds
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
BR112013025387B1 (pt) 2011-04-01 2021-07-27 University Of Utah Research Foundation Compostos análogos substituídos da n-fenilpirimidin-2-amina como inibidores da quinase axl, uso dos ditos compostos para o tratamento de um distúrbio de proliferação celular descontrolada, bem como kit compreendendo ditos compostos
ES2581848T3 (es) 2011-04-05 2016-09-07 Pfizer Limited Derivados de pirrolo[2,3-d]pirimidina como inhibidores de quinasas relacionadas con tropomiosina
BR112013028430A2 (pt) 2011-05-04 2017-08-01 Merck Sharp & Dohme composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto
EP2707357B1 (en) 2011-05-10 2017-01-18 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
MX2013013090A (es) 2011-05-10 2013-12-16 Merck Sharp & Dohme Aminopirimidinas como inhibidores de tirosina cinaza del bazo.
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
AU2012256237B2 (en) 2011-05-13 2017-01-05 Array Biopharma Inc. Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as TrkA kinase inhibitors
EP2527440A1 (en) * 2011-05-27 2012-11-28 Institut Curie Cancer treatment by combining DNA molecules mimicking double strand breaks with hyperthermia
WO2012167423A1 (en) 2011-06-08 2012-12-13 Hutchison Medipharma Limited Substituted pyridopyrazines as novel syk inhibitors
KR20180084153A (ko) 2011-06-10 2018-07-24 메르크 파텐트 게엠베하 Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물의 조성물 및 제조방법
CN102816162B (zh) 2011-06-10 2016-04-27 中国科学院广州生物医药与健康研究院 嘧啶并嘧啶酮类化合物及其药用组合物和应用
CN102393896B (zh) 2011-07-11 2014-08-27 成都西谷曙光数字技术有限公司 一种简单精确的射频定位系统和方法
EP2731439A4 (en) 2011-07-12 2014-12-03 Merck Sharp & Dohme TRKA KINASE INHIBITORS, COMPOSITIONS AND METHOD THEREFOR
JP2014522860A (ja) 2011-07-19 2014-09-08 メルク・シャープ・アンド・ドーム・ベー・フェー Btk阻害剤としての4−イミダゾピリダジン−1−イル−ベンズアミドおよび4−イミダゾトリアジン−1−イル−ベンズアミド
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
BR112014001255B1 (pt) 2011-07-19 2019-07-02 Merck Sharp & Dohme B.V. Composto, uso de um composto, combinação, composição farmacêutica, e, sal farmaceuticamente aceitável de um composto
EP2739617A4 (en) 2011-07-27 2015-01-28 Nanjing Allgen Pharma Co Ltd SPIROCYCLIC MOLECULES AS PROTEIN KINASE INHIBITORS
EP2736904B1 (en) 2011-07-27 2016-03-16 AB Science Oxazole and thiazole derivatives as selective protein kinase inhibitors (c-kit)
EA201490537A1 (ru) 2011-09-01 2014-07-30 АйАрЭм ЭлЭлСи СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ C-Kit
US20150051206A1 (en) 2011-09-01 2015-02-19 Irm Llc Compounds and compositions as c-kit kinase inhibitors
CN103797011B (zh) 2011-09-01 2016-03-30 诺华股份有限公司 作为c-Kit激酶抑制剂的化合物和组合物
US9199981B2 (en) 2011-09-01 2015-12-01 Novartis Ag Compounds and compositions as C-kit kinase inhibitors
CN108794411B (zh) 2011-09-14 2022-06-07 润新生物公司 某些化学实体、组合物及方法
WO2013047813A1 (ja) 2011-09-30 2013-04-04 大鵬薬品工業株式会社 1,2,4-トリアジン-6-カルボキサミド誘導体
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
UA111382C2 (uk) 2011-10-10 2016-04-25 Оріон Корпорейшн Інгібітори протеїнкінази
WO2013059738A2 (en) 2011-10-19 2013-04-25 Pharmacyclics, Inc. Use of inhibitors of bruton's tyrosine kinase (btk)
RU2662443C2 (ru) 2011-11-01 2018-07-26 Ф. Хоффманн-Ля Рош Аг Имидазопиридазины
MX2014005289A (es) 2011-11-03 2014-05-30 Hoffmann La Roche Compuestos de piperazina alquilados.
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
WO2013067264A1 (en) 2011-11-03 2013-05-10 Genentech, Inc. 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity
EP2780338B1 (en) 2011-11-14 2016-11-09 Ignyta, Inc. Uracil derivatives as axl and c-met kinase inhibitors
DK2786996T3 (en) 2011-11-29 2016-12-19 Ono Pharmaceutical Co Hydrochloride PURINONDERIVAT
KR20140105508A (ko) 2011-12-12 2014-09-01 닥터 레디스 레보러터리즈 리미티드 트로포미오신 수용체 키나제(Trk) 억제제인 치환된 피라졸로[1,5-a]피리딘
KR102032934B1 (ko) 2011-12-21 2019-10-16 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피롤 6원 헤테로아릴 고리 유도체, 그의 제조 방법, 및 그의 의약 용도
DK2799431T3 (en) 2011-12-28 2018-03-26 Fujifilm Corp Hitherto unknown nicotinamide derivatives or salts thereof
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
WO2013104573A1 (en) 2012-01-10 2013-07-18 F. Hoffmann-La Roche Ag Pyridazine amide compounds and their use as syk inhibitors
RU2637925C2 (ru) 2012-01-10 2017-12-08 Ф. Хоффманн-Ля Рош Аг Соединения тиенопиримидина
CN103204827B (zh) 2012-01-17 2014-12-03 上海科州药物研发有限公司 作为蛋白激酶抑制剂的苯并噻二唑化合物及其制备方法和用途
CN103204844A (zh) 2012-01-17 2013-07-17 上海艾力斯医药科技有限公司 氨基杂芳基化合物及其制备方法与应用
DK2657233T3 (da) 2012-01-19 2014-09-22 Taiho Pharmaceutical Co Ltd 3,5-disubstitueret alkynylbenzenforbindelse og salt deraf
US8871778B2 (en) 2012-01-20 2014-10-28 Genosco Substituted pyrimidine compounds and their use as SYK inhibitors
US8501724B1 (en) 2012-01-31 2013-08-06 Pharmacyclics, Inc. Purinone compounds as kinase inhibitors
RS55728B1 (sr) 2012-01-31 2017-07-31 Daiichi Sankyo Co Ltd Derivat piridona
WO2013124869A2 (en) 2012-02-21 2013-08-29 Amrita Vishwa Vidyapeetham University The art, method,manner process and system of fibrous bio-degradable polymeric wafers for the local delivery of therapeutic agents in combinations
CA2863723C (en) 2012-02-21 2020-09-22 Carl Deutsch 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors
ES2552518T3 (es) 2012-02-21 2015-11-30 Merck Patent Gmbh Derivados cíclicos de diaminopiridina como inhibidores de Syk
AU2013224420B2 (en) 2012-02-21 2016-12-15 Merck Patent Gmbh Furopyridine derivatives
EA026953B1 (ru) 2012-02-28 2017-06-30 Астеллас Фарма Инк. Азотсодержащее ароматическое гетероциклическое соединение
KR20140138910A (ko) 2012-03-14 2014-12-04 루핀 리미티드 헤테로사이클릴 화합물
KR102081042B1 (ko) 2012-03-15 2020-02-26 셀젠 카르 엘엘씨 상피 성장 인자 수용체 키나제 억제제의 고체 형태
EP2828259B1 (en) 2012-03-22 2018-08-08 Oscotec, Inc. Substituted pyridopyrimidine compounds and their use as flt3 inhibitors
US9365566B2 (en) 2012-03-27 2016-06-14 Takeda Pharmaceutical Company Limited Cinnoline derivatives
US20150072019A1 (en) 2012-03-30 2015-03-12 Novartis Ag Fgfr inhibitor for use in the treatment of hypophosphatemic disorders
JP2015512425A (ja) 2012-04-03 2015-04-27 ノバルティス アーゲー チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用
EP2833886B1 (en) 2012-04-04 2020-08-12 HangzhouDeRenYuCheng Biotechnology Ltd. Substituted quinolines as bruton's tyrosine kinase inhibitors
PT2840080T (pt) 2012-04-17 2018-02-06 Fujifilm Corp Composto heterocíclico que contém azoto ou sal do mesmo
DK2838998T3 (en) 2012-04-18 2018-01-15 Cell Signaling Technology Inc EGFR AND ROS1 IN CANCER
TW201350479A (zh) 2012-04-26 2013-12-16 Ono Pharmaceutical Co Trk阻害化合物
JP6114820B2 (ja) 2012-05-14 2017-04-12 イースト チャイナ ユニバーシティ オブ サイエンス アンド テクノロジー プテリジノン誘導体およびegfr、blk、flt3の阻害剤としての応用
EP2858501A4 (en) 2012-05-22 2015-12-09 Merck Sharp & Dohme TRKA KINASE INHIBITORS, COMPOSITIONS AND METHOD THEREFOR
AU2013268400B2 (en) 2012-05-30 2017-07-13 Nippon Shinyaku Co., Ltd. Aromatic heterocyclic derivative and pharmaceutical
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物
AR091273A1 (es) 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
CA2871659C (en) 2012-06-14 2017-04-04 Eli Lilly And Company Inhibitor of jak1 and jak2
US9487504B2 (en) 2012-06-20 2016-11-08 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2863914B1 (en) 2012-06-20 2018-10-03 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
EP2863916B1 (en) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
EP2863915B1 (en) 2012-06-22 2017-12-06 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
TWI520962B (zh) 2012-06-29 2016-02-11 As the c-Met tyrosine kinase inhibitors novel fused pyridine derivatives
CA2782774A1 (en) 2012-07-06 2014-01-06 Pharmascience Inc. Protein kinase inhibitors
WO2014009319A1 (en) 2012-07-11 2014-01-16 Boehringer Ingelheim International Gmbh Indolinone derivatives anticancer compounds
ES2618004T3 (es) 2012-08-07 2017-06-20 Merck Patent Gmbh Derivados de piridopirimidina como inhibidores de proteínas quinasas
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
SG11201500499TA (en) 2012-08-10 2015-03-30 Boehringer Ingelheim Int Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors
KR20150042256A (ko) 2012-08-13 2015-04-20 노파르티스 아게 비장 티로신 키나제 (syk)의 억제제로서의 비시클릭 헤테로아릴 시클로알킬디아민 유도체
EP2884982B1 (en) 2012-08-20 2017-09-20 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CN104507945B (zh) 2012-08-21 2018-03-23 霍夫曼-拉罗奇有限公司 作为syk抑制剂的吡咯并[2,3‑b]吡嗪
CN103122000B (zh) 2012-09-03 2013-12-25 中美冠科生物技术(太仓)有限公司 用作抗肿瘤药物的高选择性的c-Met激酶抑制剂
ME03455B (me) 2012-09-10 2020-01-20 Principia Biopharma Inc Jedinjenja pirazolopirimidina kao inhibitori kinaze
EP2897950A1 (en) 2012-09-18 2015-07-29 Ziarco Pharma Ltd 2-(2-aminocyclohexyl)amino-pyrimidine-5-carboxamides as spleen tyrosine kinasei(syk) inhibitors
SI2902029T1 (sl) 2012-09-25 2018-11-30 Chugai Seiyaku Kabushiki Kaisha Inhibitor ret
HK1213181A1 (zh) 2012-09-27 2016-06-30 Portola Pharmaceuticals, Inc. 雙環氧雜內酰胺激酶抑制劑
EP2900665B1 (en) 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
WO2014055928A2 (en) 2012-10-04 2014-04-10 University Of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
US9296703B2 (en) 2012-10-04 2016-03-29 University Of Utah Research Foundation Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
HK1211024A1 (en) 2012-10-19 2016-05-13 霍夫曼-拉罗奇有限公司 Inhibitors of syk
RU2015117950A (ru) 2012-10-26 2016-12-20 Ф. Хоффманн-Ля Рош Аг 3,4-дизамещенный 1н-пиразол и 4,5-дизамещенный тиазол в качестве ингибиторов тирозинкиназы syk
JP6178861B2 (ja) 2012-11-02 2017-08-09 ファイザー・インク ブルトン型チロシンキナーゼ阻害剤
CN102977014B (zh) 2012-11-05 2015-01-07 沈阳药科大学 新的喹啉类化合物及其用途
WO2014074422A1 (en) 2012-11-07 2014-05-15 Merck Sharp & Dohme Corp. Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
MY178262A (en) 2012-11-13 2020-10-07 Array Biopharma Inc Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9790210B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
EA201590855A1 (ru) 2012-11-15 2015-11-30 Фармасайкликс, Инк. Соединения пирролопиримидина как ингибиторы киназ
CN103848810A (zh) 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
US20150307491A1 (en) 2012-12-07 2015-10-29 Hutchison Medipharma Limited Substituted pyridopyrazines as syk inhibitors
WO2014093191A1 (en) 2012-12-12 2014-06-19 Merck Sharp & Dohme Corp. AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2934525B1 (en) 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
US9422267B2 (en) 2012-12-26 2016-08-23 Medivation Technologies, Inc. Fused pyrimidine compounds and use thereof
BR112015015477B1 (pt) 2012-12-28 2022-07-12 Crystalgenomics, Inc Derivados de 2,3-di-hidro-isoindol-1-ona e métodos de uso dos mesmos como inibidores de btk
US9745320B2 (en) 2013-01-18 2017-08-29 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Five-and-six-membered heterocyclic compound, and preparation method, pharmaceutical composition and use thereof
WO2014113942A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014113932A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014114185A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
JP6248948B2 (ja) 2013-02-08 2017-12-20 日産化学工業株式会社 3環性ピロロピリジン化合物及びjak阻害剤
MX362181B (es) 2013-02-19 2019-01-08 Ono Pharmaceutical Co Compuesto inhibidor de cinasa del receptor de tropomiosina (trk).
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
WO2014130693A1 (en) 2013-02-25 2014-08-28 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
HK1217193A1 (zh) 2013-03-11 2016-12-30 伊尼塔公司 喹唑啉衍生物的固态形式及其作为braf抑制剂的用途
JO3377B1 (ar) 2013-03-11 2019-03-13 Takeda Pharmaceuticals Co مشتقات بيريدينيل وبيريدينيل مندمج
US9963452B2 (en) 2013-03-14 2018-05-08 Augusta Pharmaceuticals Inc. Methods, compounds, and compositions for inhibition of ROS
JP6403751B2 (ja) 2013-03-14 2018-10-10 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 5−チアゾールカルボキサミン誘導体及びbtk阻害剤としてのその使用
WO2014152114A1 (en) 2013-03-15 2014-09-25 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
KR20150130311A (ko) 2013-03-19 2015-11-23 머크 샤프 앤드 돔 코포레이션 야누스 키나제 억제제로서의 n-(2-시아노 헤테로시클릴)피라졸로 피리돈
EP2981264B1 (en) 2013-04-02 2018-04-25 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
TWI628176B (zh) 2013-04-04 2018-07-01 奧利安公司 蛋白質激酶抑制劑
US10072298B2 (en) * 2013-04-17 2018-09-11 Life Technologies Corporation Gene fusions and gene variants associated with cancer
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
EP2988744A4 (en) 2013-04-26 2016-11-02 Merck Sharp & Dohme THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR
EP2988749B1 (en) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
AU2014262326B2 (en) 2013-05-10 2018-03-22 Jiangsu Hansoh Pharmaceutical Co., Ltd. [1,2,4] triazol [4,3-a] pyridine derivate, preparation method therefor or medical application thereof
SMT201900223T1 (it) 2013-05-17 2019-07-11 Incyte Corp Sale di bipirazolo come inibitore di jak
WO2014187319A1 (en) 2013-05-21 2014-11-27 Jiangsu Medolution Ltd Substituted pyrazolopyrimidines as kinases inhibitors
HK1222848A1 (zh) 2013-05-29 2017-07-14 Cephalon, Inc. 用作alk抑制剂的吡咯并三嗪
TW201534597A (zh) 2013-06-20 2015-09-16 Ab Science 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物
WO2014204263A1 (en) 2013-06-20 2014-12-24 The Asan Foundation Substituted pyridinone compounds as mek inhibitors
JP6509838B2 (ja) 2013-06-26 2019-05-08 アッヴィ・インコーポレイテッド Btk阻害薬としての一級カルボキサミド類
US9670203B2 (en) 2013-06-28 2017-06-06 Beigene, Ltd. Fused tricyclic urea compounds as Raf kinase and/or Raf kinase dimer inhibitors
JP6458018B2 (ja) 2013-07-02 2019-01-23 ファーマサイクリックス エルエルシー キナーゼ阻害剤としてのプリノン化合物
TWI649308B (zh) 2013-07-24 2019-02-01 小野藥品工業股份有限公司 喹啉衍生物
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
NZ715747A (en) 2013-07-31 2017-03-31 Gilead Sciences Inc Syk inhibitors
CA2918242C (en) 2013-07-31 2022-06-21 Merck Patent Gmbh Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof
HK1226058A1 (zh) 2013-08-02 2017-09-22 亚尼塔公司 单独地或与其它试剂联合地使用axl/cmet抑制剂治疗多种癌症的方法
KR101828187B1 (ko) 2013-08-12 2018-02-09 다이호야쿠힌고교 가부시키가이샤 신규 축합 피리미딘 화합물 또는 그 염
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
JP6479812B2 (ja) 2013-08-28 2019-03-06 ノバルティス アーゲー 細胞増殖性疾患を治療するためのalk阻害剤とcdk阻害剤との組合せ
KR101879422B1 (ko) 2013-09-18 2018-07-17 베이징 한미 파마슈티컬 컴퍼니 리미티드 Btk 및/또는 jak3 키나제의 활성을 억제하는 화합물
WO2015039334A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2015039333A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CA2925124A1 (en) 2013-09-30 2015-04-02 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
JP6615752B2 (ja) 2013-09-30 2019-12-04 グアンジョウ・イノケア・ファーマ・テク・カンパニー・リミテッド Btkの置換ニコチンイミド阻害剤およびそれらの調製、ならびにがん、炎症および自己免疫疾患の治療における使用
CN105683167B (zh) 2013-10-16 2018-10-23 富士胶片株式会社 含氮杂环化合物的盐或其结晶、药品组合物及flt3抑制剂
BR112016008632A8 (pt) 2013-10-21 2020-03-17 Merck Patent Gmbh compostos de heteroarila como inibidores de btk, seus usos, e composição farmacêutica
MY184561A (en) 2013-10-21 2021-04-03 Genosco Substituted pyrimidine compounds and their use as syk inhibitors
CN105683188B (zh) 2013-10-25 2018-02-09 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
BR112016007396B1 (pt) 2013-10-25 2021-01-19 Shanghai Hengrui Pharmaceutical Co., Ltd. Composto de fórmula (ii), seu processo de preparação e seu uso, composto de fórmula(iia) e composição farmacêutica
WO2015068767A1 (ja) 2013-11-08 2015-05-14 小野薬品工業株式会社 ピロロピリミジン誘導体
EP3078659B1 (en) 2013-12-02 2017-11-15 Jenkem Technology Co., Ltd. (Beijing) 3-furyl-2-cyano-2-acrylamide derivative, preparation method therefor, pharmaceutical composition and use thereof
AU2014360446A1 (en) 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
US9067914B1 (en) 2013-12-10 2015-06-30 Genzyme Corporation Tropomyosin-related kinase (TRK) inhibitors
US9637486B2 (en) 2013-12-20 2017-05-02 Merck Sharp & Dohme Corp. Btk inhibitors
WO2015095102A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
EP3083560B1 (en) 2013-12-20 2021-10-27 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
TWI662037B (zh) 2013-12-23 2019-06-11 美商基利科學股份有限公司 脾酪胺酸激酶抑制劑
KR20160110390A (ko) 2013-12-26 2016-09-21 이그니타, 인코포레이티드 피라졸로[1,5-a]피리딘 유도체 및 그의 용도
WO2015116485A1 (en) 2014-01-29 2015-08-06 Boehringer Ingelheim International Gmbh Pyrazole compounds as btk inhibitors
MX2016009403A (es) 2014-02-03 2016-09-16 Cadila Healthcare Ltd Compuestos heterociclicos.
CA2938818C (en) 2014-02-04 2023-03-07 Astellas Pharma Inc. Pharmaceutical composition comprising diamino heterocyclic carboxamide compound as active ingredient
AU2014384476B2 (en) 2014-02-27 2017-12-21 Ascentage Pharma (Suzhou) Co., Ltd. Indoloquinolone compounds as anaplastic lymphoma kinase (ALK) inhibitors
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
CN106255689B (zh) 2014-03-19 2019-09-17 勃林格殷格翰国际有限公司 杂芳基syk抑制剂
CN106414433A (zh) 2014-03-24 2017-02-15 Ab科学有限公司 作为脾酪氨酸激酶抑制剂的二氮杂螺烷酮取代的噁唑衍生物
WO2015143654A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143652A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143653A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
CN106132967B (zh) 2014-03-27 2019-05-28 詹森药业有限公司 作为ros1抑制剂的化合物
EP3129376B1 (en) 2014-03-27 2018-12-26 Janssen Pharmaceutica NV Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo[1,5-a][1,4]diazepine derivatives as ros1 inhibitors
CN106458914B (zh) 2014-03-28 2020-01-14 常州捷凯医药科技有限公司 作为axl抑制剂的杂环化合物
CN105017256A (zh) 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
CN105085474B (zh) 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2015174376A1 (ja) 2014-05-14 2015-11-19 日産化学工業株式会社 3環性化合物及びjak阻害剤
CA2949160C (en) 2014-05-15 2023-03-21 Array Biopharma Inc. 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor
AU2015266453C1 (en) 2014-05-30 2018-09-13 Shanghai Emerald Wellcares Pharmaceutical Co., Ltd Alk kinase inhibitor, and preparation method and use thereof
CA2952787A1 (en) 2014-06-17 2015-12-23 Korea Research Institute Of Chemical Technology Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
EP3157921A1 (en) 2014-06-23 2017-04-26 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
TWI690525B (zh) 2014-07-07 2020-04-11 日商第一三共股份有限公司 具有四氫吡喃基甲基之吡啶酮衍生物及其用途
TW201617074A (zh) 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
AU2015296215A1 (en) 2014-08-01 2017-03-23 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
WO2016021629A1 (ja) 2014-08-06 2016-02-11 塩野義製薬株式会社 TrkA阻害活性を有する複素環および炭素環誘導体
NO2721710T3 (ru) 2014-08-21 2018-03-31
KR101710127B1 (ko) 2014-08-29 2017-02-27 한화제약주식회사 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민
US20170281641A1 (en) 2014-09-03 2017-10-05 Genzyme Corporation CYCLIC UREA COMPOUNDS AS TROPOMYOSIN-RELATED KINASE (TRK) iNHIBITORS
CN105524068B (zh) 2014-09-30 2017-11-24 上海海雁医药科技有限公司 氮杂双环衍生物、其制法与医药上的用途
JP6585167B2 (ja) 2014-10-03 2019-10-02 ノバルティス アーゲー Fgfr4阻害剤としての縮環二環式ピリジル誘導体の使用
ES2907622T3 (es) 2014-10-06 2022-04-25 Merck Patent Gmbh Compuestos de heteroarilo como inhibidores de BTK y usos de estos
CN117069700B (zh) 2014-10-11 2026-01-30 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
JP6592512B2 (ja) 2014-10-24 2019-10-16 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 三環式アトロプ異性体の化合物
EP3212653A2 (en) 2014-10-30 2017-09-06 Sandoz AG Active acrylamides
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
EP3221309B1 (en) 2014-11-20 2019-11-13 Council of Scientific and Industrial Research Novel benzimidazole based egfr inhibitors
CN105601573B (zh) 2014-11-24 2021-07-02 中国科学院上海药物研究所 2-氨基嘧啶类化合物及其药物组合物和应用
EP3229800A2 (en) 2014-12-11 2017-10-18 Bayer Pharma Aktiengesellschaft Use of pan fgfr inhibitors and method of identifying patients with cancer eligible for treatment with a pan fgfr inhibitor
ES2746839T3 (es) 2014-12-18 2020-03-09 Pfizer Derivados de pirimidina y triazina y su uso como inhibidores de AXL
WO2016104617A1 (ja) 2014-12-25 2016-06-30 小野薬品工業株式会社 キノリン誘導体
WO2016106624A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Tertiary alcohol imidazopyrazine btk inhibitors
WO2016106623A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Benzamide imidazopyrazine btk inhibitors
WO2016106627A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016106629A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016106626A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors
WO2016106652A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors
WO2016106628A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
CN104530063B (zh) 2015-01-13 2017-01-18 北京赛特明强医药科技有限公司 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用
CN105837576B (zh) 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
EP3248980B1 (en) 2015-01-20 2023-09-06 Wuxi Fortune Pharmaceutical Co., Ltd Jak inhibitor
CA2974784A1 (en) 2015-01-23 2016-07-28 Gvk Biosciences Private Limited Inhibitors of trka kinase
CA2974442A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Novel fluorinated derivatives as egfr inhibitors useful for treating cancers
US10221165B2 (en) 2015-02-03 2019-03-05 Council Of Scientific And Industrial Research Flavone based EGFR inhibitors and process for preparation thereof
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
WO2016161570A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Azacarbazole btk inhibitors
WO2016161571A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Indazole and azaindazole btk inhibitors
WO2016161572A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
PH12017501822B1 (en) 2015-04-14 2022-05-04 Lead Discovery Center Gmbh Quinoline derivatives as tam rtk inhibitors
ES2734048T3 (es) 2015-04-29 2019-12-04 Wuxi Fortune Pharmaceutical Co Ltd Inhibidores de Janus cinasas (JAK)
JP6692836B2 (ja) 2015-05-28 2020-05-13 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー Jakキナーゼ阻害剤としてのナフチリジン化合物
ES2822748T3 (es) 2015-05-29 2021-05-04 Wuxi Fortune Pharmaceutical Co Ltd Inhibidor de cinasa Janus
BR112017025986A2 (pt) 2015-06-02 2018-08-14 Pharmacyclics Llc inibidores de tirosina quinase de bruton.
UA124090C2 (uk) 2015-06-03 2021-07-21 Прінсіпіа Байофарма Інк. Інгібітори тирозинкінази
WO2016192074A1 (en) 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. Btk inhibitors
TW201718572A (zh) 2015-06-24 2017-06-01 普林斯匹亞生物製藥公司 酪胺酸激酶抑制劑
JP6812059B2 (ja) 2015-07-07 2021-01-13 塩野義製薬株式会社 TrkA阻害活性を有する複素環誘導体
HK1251223A1 (en) 2015-07-07 2019-01-25 Japan Tobacco, Inc. Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof
CN108137559B (zh) 2015-07-09 2021-11-02 默克专利有限公司 用作btk抑制剂的嘧啶衍生物及其用途
BR112018000808A2 (pt) 2015-07-16 2018-09-04 Array Biopharma Inc compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase
JP6970081B2 (ja) 2015-07-16 2021-11-24 正大天晴▲藥▼▲業▼集▲団▼股▲フン▼有限公司 アニリンピリミジン誘導体及びその使用
US10550112B2 (en) 2015-07-20 2020-02-04 Dana-Farber Cancer Institute, Inc. Pyrimidines as EGFR inhibitors and methods of treating disorders
JP6457696B2 (ja) * 2015-07-23 2019-01-23 アンスティテュ・キュリInstitut Curie 癌を処置するためのDbait分子とPARPインヒビターとの組合せの使用
WO2017016463A1 (zh) 2015-07-24 2017-02-02 上海海雁医药科技有限公司 Egfr抑制剂及其药学上可接受的盐和多晶型物及其应用
KR101766194B1 (ko) 2015-08-07 2017-08-10 한국과학기술연구원 RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물
CN106467541B (zh) 2015-08-18 2019-04-05 暨南大学 取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用
EP3339305B1 (en) 2015-08-20 2022-05-04 Zhejiang Hisun Pharmaceutical Co., Ltd Indole derivative, preparation method thereof, and use thereof in pharmaceutical drug
MA41559A (fr) 2015-09-08 2017-12-26 Taiho Pharmaceutical Co Ltd Composé de pyrimidine condensé ou un sel de celui-ci
EA201890730A1 (ru) 2015-09-16 2018-10-31 Локсо Онколоджи, Инк. Производные пиразолопиримидина в качестве ингибиторов btk для лечения злокачественного новообразования
EP3144307A1 (en) 2015-09-18 2017-03-22 AB Science Novel oxazole derivatives that inhibit syk
CN106554347B (zh) 2015-09-25 2020-10-30 浙江博生医药有限公司 Egfr激酶抑制剂及其制备方法和应用
WO2017059280A1 (en) 2015-10-02 2017-04-06 The University Of North Carolina At Chapel Hill Novel pan-tam inhibitors and mer/axl dual inhibitors
EP3414234B1 (en) 2015-10-14 2022-06-29 Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. Bruton's tyrosine kinase inhibitors
AU2016341445B2 (en) 2015-10-23 2020-08-27 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
HK1252685A1 (zh) 2015-11-03 2019-05-31 Theravance Biopharma R&D Ip, Llc 用於治疗呼吸疾病的jak激酶抑制剂化合物
CN106699743B (zh) 2015-11-05 2020-06-12 湖北生物医药产业技术研究院有限公司 嘧啶类衍生物及其用途
CN108602827B (zh) 2015-11-06 2021-08-20 安塞塔制药公司 Bruton酪氨酸激酶的咪唑并吡嗪抑制剂
MX2018006195A (es) 2015-11-19 2018-09-05 Blueprint Medicines Corp Compuestos y composiciones utiles para el tratamiento de trastornos relacionados con ntrk.
ES2784523T3 (es) 2015-11-24 2020-09-28 Theravance Biopharma R&D Ip Llc Profármacos de un compuesto inhibidor de JAK para el tratamiento de enfermedades inflamatorias gastrointestinales
WO2017097224A1 (zh) 2015-12-11 2017-06-15 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
US9975882B2 (en) 2015-12-16 2018-05-22 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as BTK inhibitors
CN106928231B (zh) 2015-12-31 2021-06-01 合肥中科普瑞昇生物医药科技有限公司 一类新型的egfr野生型和突变型的激酶抑制剂
CA3008312A1 (en) 2016-01-06 2017-07-13 Trillium Therapeutics Inc. Novel fluorinated quinazoline derivatives as egfr inhibitors
SG11201805869XA (en) 2016-01-11 2018-08-30 Merck Patent Gmbh Quinolin-2-one derivatives
US10570118B2 (en) 2016-01-13 2020-02-25 Boehringer Ingelheim International Gmbh Isoquinolones as BTK inhibitors
US10662187B2 (en) 2016-01-21 2020-05-26 Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. Bruton's tyrosine kinase inhibitors
JP6770580B2 (ja) 2016-01-26 2020-10-14 杭州華東医薬集団生物医薬有限公司Hangzhou Huadong Medicine Group Biopharmaceutical Co., Ltd. ピロロピリミジン5員環アザ環状誘導体およびその利用
CN107021963A (zh) 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
EP3412663B1 (en) 2016-02-04 2022-09-07 Shionogi & Co., Ltd. Nitrogen-containing heterocycle and carbocycle derivatives having trka inhibitory activity
BR112018015369A2 (pt) 2016-02-19 2018-12-18 Jiangsu Hengrui Medicine Co., Ltd. composição farmacêutica contendo inibidor de jak cinase ou sal farmaceuticamente aceitável do mesmo
ES2775751T3 (es) 2016-02-23 2020-07-28 Taiho Pharmaceutical Co Ltd Nuevo compuesto de pirimidina condensada o sal del mismo
US10821128B2 (en) * 2016-03-01 2020-11-03 Onxeo Treatment of cancer by systemic administration of Dbait molecules
CN107151249B (zh) 2016-03-04 2020-08-14 华东理工大学 作为flt3抑制剂的蝶啶酮衍生物及应用
TW201738228A (zh) 2016-03-17 2017-11-01 藍圖醫藥公司 Ret之抑制劑
CN107286077B (zh) 2016-04-01 2021-04-02 合肥中科普瑞昇生物医药科技有限公司 一种选择性的c-kit激酶抑制剂
MA44789A (fr) 2016-04-29 2019-03-06 X Chem Inc Inhibiteurs covalents de btk et leurs utilisations
AU2017269335B2 (en) 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
CN107759600A (zh) 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
EP3476848A4 (en) 2016-06-27 2020-01-15 Hangzhou Rex Pharmaceutical Co., Ltd BENZOFURANE-PYRAZOLE-AMINE PROTEIN KINASE INHIBITOR
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
JP6715357B2 (ja) 2016-06-30 2020-07-01 杭州三因泰医薬科技有限公司Hangzhou Sanyintai Pharmaceutical Technology Co., Ltd. イミダゾピリジンアミンフェニル誘導体およびその使用
CN109153680B (zh) 2016-07-07 2021-04-23 株式会社大熊制药 4-氨基吡唑并[3,4-d]嘧啶基氮杂双环衍生物及含其的药物组合物
CN107619388A (zh) 2016-07-13 2018-01-23 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
US10227329B2 (en) 2016-07-22 2019-03-12 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
WO2018022761A1 (en) 2016-07-27 2018-02-01 Blueprint Medicines Corporation Substituted cyclopentane-amides for treating disorders related to ret
CN107698593A (zh) 2016-08-09 2018-02-16 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
AU2017312970B2 (en) 2016-08-16 2021-08-12 Merck Patent Gmbh 2-oxo-imidazopyridines as reversible BTK inhibitors and uses thereof
EP3504203B1 (en) 2016-08-29 2022-09-28 The Regents of The University of Michigan Aminopyrimidines as alk inhibitors
US10111882B2 (en) 2016-09-14 2018-10-30 Gilead Sciences, Inc. SYK inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
CN107840842A (zh) 2016-09-19 2018-03-27 北京天诚医药科技有限公司 炔代杂环化合物、其制备方法及其在医药学上的应用
CN107840846B (zh) 2016-09-19 2020-11-24 郑州泰基鸿诺医药股份有限公司 一种含嘧啶环的化合物、egfr抑制剂及其应用
JP2018052878A (ja) 2016-09-29 2018-04-05 第一三共株式会社 ピリジン化合物
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
WO2018079759A1 (ja) 2016-10-31 2018-05-03 塩野義製薬株式会社 TrkA阻害活性を有する縮合複素環および縮合炭素環誘導体
KR102686957B1 (ko) 2016-11-08 2024-07-22 주식회사 대웅제약 신규한 피롤로피리미딘 유도체 및 이를 포함하는 약학적 조성물
JP6782855B2 (ja) 2016-11-15 2020-11-11 杭州和正医薬有限公司 選択性ブルトン型チロシンキナーゼ阻害剤及びその使用
EP3541816A1 (en) 2016-11-18 2019-09-25 The Regents of The University of Michigan 5,6-dihydro-11h-indolo[2,3-b]quinolin-11-ones as alk inhibitors
CN108101905A (zh) 2016-11-24 2018-06-01 中国科学院上海药物研究所 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途
US11142535B2 (en) 2016-12-12 2021-10-12 Hangzhou Innogate Pharma Co., Ltd. Heterocyclic compound as Syk inhibitor and/or Syk-HDAC dual inhibitor
WO2018108064A1 (zh) 2016-12-13 2018-06-21 南京明德新药研发股份有限公司 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物
EA201991197A1 (ru) 2016-12-15 2020-01-13 Ариад Фармасьютикалз, Инк. БЕНЗИМИДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ c-Kit
IL312378A (en) 2016-12-15 2024-06-01 Ariad Pharma Inc Aminothiazole compounds as C-KIT inhibitors
CN108250200A (zh) 2016-12-28 2018-07-06 中国科学院上海药物研究所 一种具有Axl抑制活性的化合物及其制备和应用
CN110139865B (zh) 2016-12-29 2022-02-18 石药集团中奇制药技术(石家庄)有限公司 Fgfr抑制剂
EP3567030B1 (en) 2016-12-30 2022-02-09 Medshine Discovery Inc. Quinazoline compound for egfr inhibition
CN108276410B (zh) 2017-01-06 2021-12-10 首药控股(北京)股份有限公司 一种间变性淋巴瘤激酶抑制剂及其制备方法和用途
WO2018129645A1 (en) 2017-01-10 2018-07-19 Wang, Wei Lasofoxifene modulation of membrane-initiated estrogen signals and methods for tumor treatment
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN106831787B (zh) 2017-01-20 2018-10-23 成都倍特药业有限公司 用作布鲁顿酪氨酸激酶抑制剂的化合物及其制备方法和应用
CN110072865B (zh) 2017-02-08 2022-02-11 中国医药研究开发中心有限公司 吡咯并芳杂环类化合物及其制备方法和医药用途
US10464923B2 (en) 2017-02-27 2019-11-05 Merck Patent Gmbh Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone
JP6876833B2 (ja) 2017-02-27 2021-05-26 ▲貝▼▲達▼▲薬▼▲業▼股▲フン▼有限公司Betta Pharmaceuticals Co., Ltd. Fgfr阻害剤およびその使用
WO2018153293A1 (zh) 2017-02-27 2018-08-30 北京赛特明强医药科技有限公司 二噁烷并喹唑啉与二噁烷并喹啉类化合物及其制备方法与应用
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
KR102627756B1 (ko) 2017-03-22 2024-01-23 쑤저우 바이지부공 파마수티컬 테크널러지 컴퍼니 리미티드 브루톤 타이로신 키나제 억제제
WO2018187355A1 (en) 2017-04-03 2018-10-11 Health Research Inc. Met kinase inhibitors and uses therefor
CN108727382B (zh) 2017-04-19 2022-07-19 华东理工大学 作为btk抑制剂的杂环化合物及其应用
CN108721298A (zh) 2017-04-19 2018-11-02 华东理工大学 作为布鲁顿酪氨酸激酶抑制剂的嘧啶并杂环化合物及其应用
CN107043366B (zh) 2017-04-25 2020-05-26 中国药科大学 4-氨基嘧啶类化合物、其制备方法及医药用途
ES2992887T3 (en) 2017-04-27 2024-12-19 Mochida Pharm Co Ltd Novel tetrahydronaphthyl urea derivatives as inhibitors of tropomyosin receptor kinase a for the treatment of pain
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
WO2018208132A1 (en) 2017-05-12 2018-11-15 Korea Research Institute Of Chemical Technology Pyrazolopyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer, autoimmune disease and brain disease containing the same as an active ingredient
WO2018215389A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
CN110678467B (zh) 2017-05-22 2023-06-13 豪夫迈·罗氏有限公司 治疗化合物和组合物及其使用方法
CN107176954B (zh) 2017-06-02 2019-01-11 无锡双良生物科技有限公司 一种egfr抑制剂的药用盐及其晶型、制备方法和应用
ES2906205T3 (es) 2017-06-14 2022-04-13 Chia Tai Tianqing Pharmaceutical Group Co Ltd Inhibidor de Syk y método de uso para el mismo
CN109111446B (zh) 2017-06-22 2021-11-30 上海度德医药科技有限公司 一种具有药物活性的杂芳基化合物
EP3645526B1 (en) 2017-06-27 2024-09-04 Janssen Pharmaceutica NV New quinolinone compounds
CN111093645A (zh) 2017-07-05 2020-05-01 Cs制药技术有限公司 Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
WO2019034075A1 (zh) 2017-08-15 2019-02-21 南京明德新药研发股份有限公司 Fgfr和egfr抑制剂
WO2019034076A1 (zh) 2017-08-15 2019-02-21 南京明德新药研发股份有限公司 Fgfr抑制剂及其医药用途
EP3668867B1 (en) 2017-08-18 2023-10-04 Universität Regensburg Synthesis, pharmacology and use of new and selective fms-like tyrosine kinase 3 (flt3) flt3 inhibitors
CN109400610A (zh) 2017-08-18 2019-03-01 浙江海正药业股份有限公司 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途
WO2019034153A1 (zh) 2017-08-18 2019-02-21 北京韩美药品有限公司 一种化合物,其药物组合物及其用途及应用

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