JP2022515198A5 - - Google Patents

Info

Publication number
JP2022515198A5
JP2022515198A5 JP2021536038A JP2021536038A JP2022515198A5 JP 2022515198 A5 JP2022515198 A5 JP 2022515198A5 JP 2021536038 A JP2021536038 A JP 2021536038A JP 2021536038 A JP2021536038 A JP 2021536038A JP 2022515198 A5 JP2022515198 A5 JP 2022515198A5
Authority
JP
Japan
Prior art keywords
cancer
fgfr
ring
alkyl
fused
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
JP2021536038A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022515198A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2019/066278 external-priority patent/WO2020131627A1/en
Publication of JP2022515198A publication Critical patent/JP2022515198A/ja
Publication of JP2022515198A5 publication Critical patent/JP2022515198A5/ja
Ceased legal-status Critical Current

Links

JP2021536038A 2018-12-19 2019-12-13 FGFRチロシンキナーゼの阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物 Ceased JP2022515198A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862781990P 2018-12-19 2018-12-19
US62/781,990 2018-12-19
PCT/US2019/066278 WO2020131627A1 (en) 2018-12-19 2019-12-13 Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases

Publications (2)

Publication Number Publication Date
JP2022515198A JP2022515198A (ja) 2022-02-17
JP2022515198A5 true JP2022515198A5 (https=) 2022-12-20

Family

ID=69160414

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021536038A Ceased JP2022515198A (ja) 2018-12-19 2019-12-13 FGFRチロシンキナーゼの阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物

Country Status (5)

Country Link
US (1) US12180207B2 (https=)
EP (1) EP3898626A1 (https=)
JP (1) JP2022515198A (https=)
CN (1) CN113490666A (https=)
WO (1) WO2020131627A1 (https=)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12441707B2 (en) 2019-12-30 2025-10-14 Tyra Biosciences, Inc. Indazole compounds
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN115605477B (zh) * 2020-04-22 2024-07-05 深圳众格生物科技有限公司 一种吡唑并[1,5-a]吡啶类衍生物及其制备方法,组合物以及用途
EP4210702A1 (en) * 2020-09-14 2023-07-19 JANSSEN Pharmaceutica NV Fgfr inhibitor combination therapies
EP4244223A1 (en) * 2020-11-13 2023-09-20 Biogen MA Inc. Pyrazolo[1,5-a]pyrazine derivatives as btk inhibitors
BR112023015210A2 (pt) 2021-01-29 2023-11-07 Cedilla Therapeutics Inc Inibidores de cdk2 e métodos de uso dos mesmos
TWI820622B (zh) * 2021-03-04 2023-11-01 美商美國禮來大藥廠 Fgfr3抑制劑化合物
WO2022206939A1 (zh) * 2021-04-03 2022-10-06 海南耀臻生物医药科技有限公司 作为fgfr抑制剂的杂环化合物及其应用
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
US20240287081A1 (en) * 2021-06-09 2024-08-29 Icahn School Of Medicine At Mount Sinai Perfluoroalkane substituted pyrazolo[3,4-d]pyrimidin and pyrrolo[2,3-d]pyrimidin compounds and uses thereof
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3225439A1 (en) 2021-06-26 2022-12-29 Cedilla Therapeutics, Inc. Cdk2 inhibitors and methods of using the same
CN115772170B (zh) * 2021-12-03 2025-05-16 徐诺药业(南京)有限公司 一种吡唑并[1,5-a]吡啶衍生物及其制备方法和应用
JP2025515466A (ja) * 2022-04-25 2025-05-15 イーライ リリー アンド カンパニー Fgfr2阻害剤化合物
AU2023338193A1 (en) * 2022-09-07 2025-03-20 Eli Lilly And Company Pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine derivatives as fgfr3 inhibitors for the treatment of cancer
EP4584270A1 (en) * 2022-09-07 2025-07-16 Eli Lilly And Company Co-crystals of 4-[4-[3-chloro-4-[1-(2-pyridyl)-2-hydroxy-ethoxy]pyrazolo[1,5-a]pyridin-6-yl]-5-methyl- triazol-1-yl]piperidine-1 -carbonitrile derivatives with gallic acid and nicotine amide
WO2024083111A1 (zh) * 2022-10-18 2024-04-25 首药控股(北京)股份有限公司 一种新型杂环化合物
CN120344533A (zh) * 2022-11-22 2025-07-18 海思科医药集团股份有限公司 一种嘧啶衍生物及其在医药上的应用
WO2024137587A1 (en) * 2022-12-19 2024-06-27 Tyra Biosciences, Inc. Fgfr3 inhibitor compounds
KR20250141720A (ko) * 2023-01-10 2025-09-29 코젠트 바이오사이언시스, 인크. Fgfrs 억제제용 화합물
WO2024182447A1 (en) * 2023-02-28 2024-09-06 Vividion Therapeutics, Inc. Compounds and methods for modulating ras-pi3k
CN120712269A (zh) * 2023-03-20 2025-09-26 英矽智能科技知识产权有限公司 Fgfr2和fgfr3的抑制剂及其用途
JP2025004966A (ja) * 2023-06-27 2025-01-16 東京応化工業株式会社 レジスト組成物、レジストパターン形成方法、化合物及び高分子化合物
AU2024319770A1 (en) * 2023-08-07 2026-02-19 Cogent Biosciences, Inc. Compounds for fgfr inhibition
WO2025102600A1 (zh) * 2023-11-16 2025-05-22 首药控股(北京)股份有限公司 一种新型杂环化合物
CN119258066B (zh) * 2024-10-14 2025-07-04 暨南大学附属第一医院(广州华侨医院) Alw-ii-41-27在治疗眼科疾病中的新应用

Family Cites Families (213)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU22545A1 (es) 1994-11-18 1999-03-31 Centro Inmunologia Molecular Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico
US4304777A (en) 1979-08-30 1981-12-08 Sterling Drug Inc. 6-(Pyridinyl)-3(2H)-pyridazinones and their use as cardiotonics
US4305943A (en) 1980-04-28 1981-12-15 Sterling Drug Inc. 4-Amino-6-(pyridinyl)-3(2H)-pyridazinones and their use as cardiotonics
US4943533A (en) 1984-03-01 1990-07-24 The Regents Of The University Of California Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor
US4826835A (en) 1985-10-23 1989-05-02 Rorer Pharmaceutical Corporation Pyridyl-pyridazinone and pyridyl-pyrazolinone compounds and their use in the treatment of congestive heart failure
WO1989008108A1 (en) 1988-02-23 1989-09-08 Rorer International (Overseas) Inc. Pyridyl-pyridazinone and pyridyl-pyrazolinone compounds and their use in the treatment of congestive heart failure
EP0491007B1 (en) 1989-09-08 1996-03-13 The Johns Hopkins University Structural alterations of the egf receptor gene in human gliomas
DE4127404A1 (de) 1991-08-19 1993-02-25 Thomae Gmbh Dr K Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
DE69523857T2 (de) 1994-09-16 2002-06-13 Merck Patent Gmbh Immunokonjugate
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
EA001595B1 (ru) 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
EA003786B1 (ru) 1998-11-19 2003-10-30 Варнер Ламберт Компани N-[4-(3-хлор-4-фторфениламино)-7-(3-морфолин-4-илпропокси)хиназолин-6-ил]акриламид - необратимый ингибитор тирозинкиназ
CA2412494C (en) 2000-06-22 2012-10-23 Genentech, Inc. Agonist anti-trk-c monoclonal antibodies
WO2004022540A2 (en) 2002-09-06 2004-03-18 Fujisawa Pharmaceutical Co., Ltd. Pyridazinone and pyridone derivatives as adenosine antagonists
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005099363A2 (en) 2004-03-26 2005-10-27 Whitehead Institute For Biomedical Research Methods of diagnosing, preventing and treating cancer metastasis
WO2005095384A1 (en) 2004-04-01 2005-10-13 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
US20080090827A1 (en) 2004-11-30 2008-04-17 Artesian Therapeutics, Inc. Compounds With Mixed Pde-Inhibitory and Beta-Adrenergic Antagonist or Partial Agonist Activity For Treatment of Heart Failure
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
US20080287437A1 (en) 2005-05-16 2008-11-20 Astrazeneca Ab Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
ITRM20050290A1 (it) 2005-06-07 2006-12-08 Lay Line Genomics Spa Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato.
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
WO2007022999A1 (en) 2005-08-25 2007-03-01 Creabilis Therapeutics S.P.A. Polymer conjugates of k-252a and derivatives thereof
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
EP1966141A1 (en) 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
HRP20170103T1 (hr) 2005-12-21 2017-03-24 Janssen Pharmaceutica N.V. Triazolopiridazini kao modulatori tirozin kinaze
BRPI0709680B8 (pt) 2006-03-27 2021-05-25 Nerviano Medical Sciences Srl derivados de pirrol, tiofeno e furano substituídos por piridil e piridimil como inibidores de quinase
SG177225A1 (en) 2006-12-01 2012-01-30 Agency Science Tech & Res Cancer-related protein kinases
JP2010514695A (ja) 2006-12-21 2010-05-06 プレキシコン,インコーポレーテッド キナーゼ調節のための化合物および方法およびそのための適応症
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
US20130012485A1 (en) 2006-12-22 2013-01-10 Baeschlin Daniel Kaspar Organic compounds
EA019524B1 (ru) 2007-05-04 2014-04-30 Айрм Ллк СОЕДИНЕНИЯ И КОМПОЗИЦИИ КАК ИНГИБИТОРЫ КИНАЗЫ с-kit И PDGFR
DE102007025717A1 (de) 2007-06-01 2008-12-11 Merck Patent Gmbh Arylether-pyridazinonderivate
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염
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.
EP2170894A1 (en) 2007-06-21 2010-04-07 Janssen Pharmaceutica N.V. Polymorphic and hydrate forms, salts and process for preparing 6-{difluoro[6-(1-methyl-1h-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline
AU2008273889B2 (en) 2007-07-09 2012-03-08 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
MY150032A (en) 2007-07-19 2013-11-29 Merck Sharp & Dohme Heterocyclic amide compounds as protein kinase inhibitors
PT2176231T (pt) 2007-07-20 2016-12-09 Nerviano Medical Sciences Srl Derivados de indazol substituídos activos como inibidores de quinases
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
EP2214706A1 (en) 2007-10-23 2010-08-11 Novartis AG Use of trkb antibodies for the treatment of respiratory disorders
WO2009071480A2 (en) 2007-12-04 2009-06-11 Nerviano Medical Sciences S.R.L. Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
PE20091326A1 (es) 2008-01-17 2009-09-18 Irm Llc Anticuerpos anti-trkb mejorados
EP2254886B1 (en) 2008-03-28 2016-05-25 Nerviano Medical Sciences S.r.l. 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
CA2723237A1 (en) 2008-05-06 2009-11-12 Peter A. Blomgren Substituted amides, method of making, and use as btk inhibitors
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009142732A2 (en) 2008-05-20 2009-11-26 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
ES2554513T3 (es) 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
JP5767965B2 (ja) 2008-06-10 2015-08-26 プレキシコン インコーポレーテッドPlexxikon Inc. キナーゼを調節する5h−ピロロ[2,3−b]ピラジン誘導体、およびその適応症
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
JP2010013369A (ja) 2008-07-01 2010-01-21 Astellas Pharma Inc ピラジン誘導体の製造法
EP2323664B1 (en) 2008-07-29 2015-01-07 Nerviano Medical Sciences S.r.l. Use of a cdk inhibitor for the treatment of glioma
JP2011530511A (ja) * 2008-08-05 2011-12-22 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
JP5746032B2 (ja) 2008-09-19 2015-07-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 3,4−ジヒドロ−2H−ピロロ[1,2−a]ピラジン−1−オン誘導体
WO2010033941A1 (en) 2008-09-22 2010-03-25 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
MY169791A (en) 2008-10-22 2019-05-15 Array Biopharma Inc Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors
US8598174B2 (en) 2008-11-12 2013-12-03 Genetech, Inc. Pyridazinones, method of making, and method of use thereof
WO2010058006A1 (en) 2008-11-24 2010-05-27 Nerviano Medical Sciences S.R.L. Cdk inhibitor for the treatment of mesothelioma
ES2548882T3 (es) 2008-12-08 2015-10-21 Arena Pharmaceuticals, Inc. Moduladores del receptor de prostaciclina (PGl2) útiles para el tratamiento de trastornos relacionados con los mismos
JO3265B1 (ar) 2008-12-09 2018-09-16 Novartis Ag مثبطات بيريديلوكسى اندولات vegf-r2 واستخدامها لعلاج المرض
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
TWI720517B (zh) 2009-01-15 2021-03-01 美商英塞特公司 製造jak抑制劑之方法及相關中間化合物
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
US8546413B2 (en) 2009-06-15 2013-10-01 Nerviano Medical Sciences S.R.L. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EA201200260A1 (ru) 2009-08-12 2012-09-28 Новартис Аг Гетероциклические гидразоны и их применение для лечения рака и воспаления
JP2013504325A (ja) 2009-09-09 2013-02-07 アビラ セラピューティクス, インコーポレイテッド Pi3キナーゼインヒビターおよびその使用
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
WO2011092120A1 (en) 2010-01-29 2011-08-04 Nerviano Medical Sciences S.R.L. 6,7- dihydroimidazo [1,5-a] pyrazin-8 (5h) - one derivatives as protein kinase modulators
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
ES2594927T3 (es) 2010-02-18 2016-12-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Métodos para prevenir las metástasis cancerosas
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
ME03376B (me) 2010-05-20 2020-01-20 Array Biopharma Inc Makrociklička jedinjenja kао inhibiтori trk kinaze
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
EP2668190B1 (en) 2011-01-26 2016-08-17 Nerviano Medical Sciences S.r.l. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
WO2012101029A1 (en) 2011-01-26 2012-08-02 Nerviano Medical Sciences S.R.L. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
JP5620417B2 (ja) * 2011-02-07 2014-11-05 中外製薬株式会社 アミノピラゾール誘導体を含む医薬
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN103403002B (zh) 2011-02-24 2016-06-22 内尔维阿诺医学科学有限公司 作为激酶抑制剂的噻唑基苯基-苯磺酰氨基衍生物
MA34969B1 (fr) 2011-02-25 2014-03-01 Irm Llc Composes et compositions en tant qu inibiteurs de trk
EP2702055A1 (en) 2011-04-11 2014-03-05 Nerviano Medical Sciences S.r.l. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
JP5970537B2 (ja) 2011-04-19 2016-08-17 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害薬として活性な置換ピリミジニル−ピロール
PT2707359T (pt) 2011-05-12 2017-01-09 Nerviano Medical Sciences Srl Derivados de indazol substituídos ativos como inibidores de quinase
CA2835835C (en) 2011-05-13 2019-04-02 Array Biopharma Inc. Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors
JP6016915B2 (ja) 2011-07-28 2016-10-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール
US9267176B2 (en) 2011-08-05 2016-02-23 Astellas Pharma Inc. Method for detecting novel FGFR4 mutant
CA2841801A1 (en) 2011-08-17 2013-02-21 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
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
JP6063945B2 (ja) 2011-10-07 2017-01-18 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としての4−アルキル置換3,4−ジヒドロピロロ[1,2−a]ピラジン−1(2H)−オン誘導体
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
MX2014005282A (es) 2011-11-03 2014-05-30 Hoffmann La Roche Compuestos de 8-fluoroftalazin-1 (2h) -ona.
EP2779833A4 (en) 2011-11-14 2015-03-18 Tesaro Inc MODULATION OF SPECIFIC TYROSINE KINASES
US9133328B2 (en) 2011-12-12 2015-09-15 Sa Des Eaux Minerales D'evian Saeme Plastic compositions and containers made 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
DK2820009T3 (en) 2012-03-01 2018-04-16 Array Biopharma Inc Serine / threonine kinase inhibitors
TW201350479A (zh) 2012-04-26 2013-12-16 Ono Pharmaceutical Co Trk阻害化合物
US9254288B2 (en) 2012-05-07 2016-02-09 The Translational Genomics Research Institute Susceptibility of tumors to tyrosine kinase inhibitors and treatment thereof
ES2751944T3 (es) 2012-05-23 2020-04-02 Nerviano Medical Sciences Srl Proceso para la preparación de N-[5-(3,5-difluoro-bencil)-1H-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida
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
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
SG11201500125QA (en) * 2012-07-11 2015-02-27 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
US20140030259A1 (en) 2012-07-27 2014-01-30 Genentech, Inc. Methods of treating fgfr3 related conditions
BR112015002152B1 (pt) 2012-08-02 2021-04-27 Nerviano Medical Sciences S.R.L. Compostos de pirróis substituídos ativos como inibidores de quinases, processo para a preparação de tais compostos, composição farmacêutica, método in vitro para a inibição da atividade de proteínas quinases da família jak e produto compreendendo os referidos compostos
US11230589B2 (en) 2012-11-05 2022-01-25 Foundation Medicine, Inc. Fusion molecules and uses thereof
ES2755772T3 (es) 2012-11-07 2020-04-23 Nerviano Medical Sciences Srl Pirimidinil y piridinilpirrolopiridinonas sustituidas, proceso para su preparación y su uso como inhibidores de cinasas
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
RS55593B1 (sr) 2012-11-13 2017-06-30 Array Biopharma Inc Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-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
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
MX374242B (es) 2012-11-13 2025-03-05 Array Biopharma Inc Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa.
CA2877847A1 (en) 2012-11-29 2014-06-05 Yeda Research And Development Co. Ltd. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors
CA3150658A1 (en) 2013-01-18 2014-07-24 Foundation Medicine, Inc. Methods of treating cholangiocarcinoma
HUE032863T2 (en) 2013-02-07 2017-11-28 Merck Patent Gmbh Piridazinonamid derivatives
AU2014219855B2 (en) 2013-02-19 2017-09-28 Ono Pharmaceutical Co., Ltd. Trk-inhibiting compound
MX2015011428A (es) 2013-03-06 2016-02-03 Genentech Inc Metodos para tratar y prevenir la resistencia a los farmacos para el cancer.
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
US9850038B2 (en) 2013-03-15 2017-12-26 Reynolds Presto Products Inc. Child resistant zipper closure for recloseable pouch with double slider and methods
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
EP2997030B1 (en) 2013-05-14 2017-08-09 Nerviano Medical Sciences S.R.L. Pyrrolo[2,3-d]pyrimidine derivatives, process for their preparation and their use as kinase inhibitors
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
WO2015000949A1 (en) 2013-07-03 2015-01-08 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone amide compounds
US10124003B2 (en) 2013-07-18 2018-11-13 Taiho Pharmaceutical Co., Ltd. Therapeutic agent for FGFR inhibitor-resistant cancer
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
EP3027654B1 (en) 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
BR112016005199B1 (pt) * 2013-08-23 2022-02-22 Neupharma, Inc Certos compostos químicos, composições, e métodos
WO2015035415A1 (en) 2013-09-09 2015-03-12 Nantomics, Llc Method of detecting suceptibility to breast cancer through mutations in the fgfr3 and tp53 genes
KR101879422B1 (ko) 2013-09-18 2018-07-17 베이징 한미 파마슈티컬 컴퍼니 리미티드 Btk 및/또는 jak3 키나제의 활성을 억제하는 화합물
TWI664977B (zh) 2013-10-08 2019-07-11 第一三共股份有限公司 抗fgfr2抗體及其與其他藥劑之組合
WO2015058129A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
SI3057969T1 (sl) 2013-10-17 2018-10-30 Blueprint Medicines Corporation Sestavki, uporabni za zdravljenje motenj, povezanih s KIT
RS63405B1 (sr) 2013-10-25 2022-08-31 Blueprint Medicines Corp Inhibitori receptora faktora rasta fibroblasta
WO2015082583A1 (en) 2013-12-05 2015-06-11 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality
EP3089970B1 (en) 2013-12-09 2018-10-17 AbbVie Inc. Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors
US10767222B2 (en) 2013-12-11 2020-09-08 Accuragen Holdings Limited Compositions and methods for detecting rare sequence variants
JP6514645B2 (ja) 2013-12-27 2019-05-15 中外製薬株式会社 Fgfrゲートキーパー変異遺伝子およびそれを標的とする医薬
US9695165B2 (en) * 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
CN103772352B (zh) 2014-01-16 2017-01-18 四川百利药业有限责任公司 哒嗪酮类衍生物及其制备方法和用途
ES2933350T3 (es) 2014-01-24 2023-02-06 Turning Point Therapeutics Inc Macrociclos de diarilo como moduladores de proteína quinasas
US20160340742A1 (en) 2014-02-04 2016-11-24 Mayo Foundation For Medical Education And Research Method of Identifying Tyrosine Kinase Receptor Rearrangements in Patients
PT3102577T (pt) 2014-02-07 2018-10-23 Principia Biopharma Inc Derivados de quinolona como inibidores do recetor do fator de crescimento de fibroblastos
TWI672141B (zh) 2014-02-20 2019-09-21 美商醫科泰生技 投予ros1突變癌細胞之分子
US11037129B1 (en) 2014-02-24 2021-06-15 Groupon, Inc. Consumer device presence-based transaction session
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
CN106459993A (zh) 2014-03-31 2017-02-22 德彪药业国际股份公司 Fgfr融合体
WO2015160636A1 (en) 2014-04-16 2015-10-22 Merck Sharp & Dohme Corp. Factor ixa inhibitors
US9808445B2 (en) 2014-04-16 2017-11-07 Merck Sharp & Dohme Corp. Factor IXa inhibitors
US20170044621A1 (en) 2014-04-18 2017-02-16 Blueprint Medicines Corporation Met fusions
WO2015161274A1 (en) 2014-04-18 2015-10-22 Blueprint Medicines Corporation Pik3ca fusions
MA40434B1 (fr) 2014-05-15 2019-09-30 Array Biopharma Inc 1-((3s,4r)-4-(3-fluorophényl)-1-(2-méthoxyéthyl)pyrrolidin-3-yl)-3-(4-méthyl-3-(2-méthylpyrimidin-5-yl)-1-phényl-1h-pyrazol-5-yl)urée comme inhibiteur de la kinase trka
EA028614B1 (ru) 2014-05-22 2017-12-29 Общество С Ограниченной Ответственностью "Русские Фармацевтические Технологии" Селективные ингибиторы, нарушающие взаимодействие рецептора фактора роста фибробластов и frs2, для профилактики и лечения рака
EP3155118A1 (en) 2014-06-10 2017-04-19 Blueprint Medicines Corporation Pkn1 fusions
WO2015191666A2 (en) 2014-06-10 2015-12-17 Blueprint Medicines Corporation Raf1 fusions
US9949971B2 (en) 2014-06-17 2018-04-24 Acerta Pharma B.V. Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor and/or a JAK-2 inhibitor
US10370724B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation PRKC fusions
US10370725B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation FGR fusions
WO2016011144A1 (en) 2014-07-17 2016-01-21 Blueprint Medicines Corporation Tert fusions
US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
US10399959B2 (en) 2014-08-18 2019-09-03 Ono Pharmaceutical Co., Ltd. Acid-addition salt of Trk-inhibiting compound
US20170281642A1 (en) 2014-08-28 2017-10-05 Oncoethix Gmbh Methods of treating acute myeloid leukemia or acute lymphoid leukemia using pharmaceutical compositions containing thienotriazolodiazepine compounds
CN107074828B (zh) 2014-09-12 2020-05-19 诺华股份有限公司 用作raf激酶抑制剂的化合物和组合物
KR102562866B1 (ko) 2014-11-14 2023-08-04 네르비아노 메디칼 사이언시스 에스.알.엘. 단백질 키나아제 억제제로서의 6-아미노-7-바이사이클로-7-데아자-퓨린 유도체
CN113354649B (zh) 2014-11-16 2024-12-10 阵列生物制药公司 一种新的晶型
EP3221700B1 (en) 2014-11-18 2022-06-22 Blueprint Medicines Corporation Prkacb fusions
JP2018027019A (ja) 2014-11-26 2018-02-22 国立研究開発法人国立がん研究センター 胆道がんにおける新規治療標的融合遺伝子
WO2016105503A1 (en) 2014-12-24 2016-06-30 Genentech, Inc. Therapeutic, diagnostic and prognostic methods for cancer of the bladder
US9909016B2 (en) 2015-02-28 2018-03-06 Matthew Fontaine Elastomeric coating composition
EP3265462A1 (en) 2015-03-03 2018-01-10 INSERM - Institut National de la Santé et de la Recherche Médicale Fgfr3 antagonists
EP3298011B1 (en) 2015-05-22 2021-11-17 Principia Biopharma Inc. Quinolone derivatives as fibroblast growth factor receptor inhibitors
JP6887997B2 (ja) 2015-10-02 2021-06-16 フレックスデックス, インク.Flexdex, Inc. 無制限ロールを付与するハンドル機構
US10208024B2 (en) 2015-10-23 2019-02-19 Array Biopharma Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
US9640210B1 (en) 2015-11-13 2017-05-02 Kabushiki Kaisha Toshiba Virtual window mode for guide spiral servo demodulation
CN107793395B (zh) * 2016-09-01 2021-01-05 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂及其用途
CN108082275B (zh) 2016-11-23 2021-08-24 操纵技术Ip控股公司 电动转向系统
AU2017378943B2 (en) * 2016-12-19 2020-06-18 Abbisko Therapeutics Co., Ltd. FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof
TWI798199B (zh) 2017-02-06 2023-04-11 比利時商健生藥品公司 癌症治療

Similar Documents

Publication Publication Date Title
JP2022515198A5 (https=)
JP2022515197A5 (https=)
JP2024522766A5 (https=)
JP2014513704A5 (https=)
JP2020531447A5 (https=)
MX2025000642A (es) Compuestos macrociclicos para el tratamiento de cancer
JP2023515235A5 (https=)
ES2862314T3 (es) Compuestos de imidazo[1,2-a]piridina, composiciones que los comprenden, métodos para el tratamiento de enfermedades que los utilizan y métodos para prepararlos
ES2822654T3 (es) Benzimidazol-2-aminas como inhibidores de mIDH1
JP2014503574A5 (https=)
RU2010116274A (ru) Аналоги азацитидина и их применение
RU2012120288A (ru) Новые производные нафтиридина и их применение в качестве ингибиторов киназы
JP2005505618A5 (https=)
JP2022500383A5 (https=)
JPWO2021060453A5 (https=)
JP2004517843A5 (https=)
JP2008526999A5 (https=)
JP2021514395A5 (https=)
CN107949557A (zh) 作为mIDH1抑制剂的2‑芳基‑和2‑芳烷基‑苯并咪唑类
WO2014180182A1 (zh) [1,2,4]三唑并[4,3-a]吡啶类衍生物,其制备方法或其在医药上的应用
CN111511745A (zh) 吡唑并[1,5-a][1,3,5]三嗪-2-胺类衍生物、其制备方法及其在医药上的应用
JP2019519512A5 (https=)
JP2013511526A5 (https=)
JP2023548190A5 (https=)
JP2023509944A5 (https=)