JP6625551B2 - Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体 - Google Patents

Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体 Download PDF

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JP6625551B2
JP6625551B2 JP2016558669A JP2016558669A JP6625551B2 JP 6625551 B2 JP6625551 B2 JP 6625551B2 JP 2016558669 A JP2016558669 A JP 2016558669A JP 2016558669 A JP2016558669 A JP 2016558669A JP 6625551 B2 JP6625551 B2 JP 6625551B2
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cancer
compound
formula
alkyl
compounds
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JP2017511311A (ja
JP2017511311A5 (enExample
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ウィム、フェレメレン
スティーブン、アナ、ホスティン
フィリップ、アルベール、セリーヌ、キュイケン
ラッセル、マーク、ジョーンズ
ディエゴ、フェルナンド、ドメニコ、ブロッジーニ
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Astex Therapeutics Ltd
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Astex Therapeutics Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016558669A 2014-03-26 2015-03-26 Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体 Active JP6625551B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161820.7 2014-03-26
EP14161820 2014-03-26
PCT/EP2015/056507 WO2015144803A1 (en) 2014-03-26 2015-03-26 Quinoxaline derivatives useful as fgfr kinase modulators

Publications (3)

Publication Number Publication Date
JP2017511311A JP2017511311A (ja) 2017-04-20
JP2017511311A5 JP2017511311A5 (enExample) 2018-05-10
JP6625551B2 true JP6625551B2 (ja) 2019-12-25

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JP2016558669A Active JP6625551B2 (ja) 2014-03-26 2015-03-26 Ｆｇｆｒキナーゼ調節剤として有用なキノキサリン誘導体

Country Status (38)

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US (2) US9902714B2 (enExample)
EP (1) EP3122742B1 (enExample)
JP (1) JP6625551B2 (enExample)
KR (1) KR102469506B1 (enExample)
CN (1) CN106459010B (enExample)
AP (1) AP2016009536A0 (enExample)
AR (1) AR099854A1 (enExample)
AU (1) AU2015238300C1 (enExample)
BR (1) BR112016022060B1 (enExample)
CA (1) CA2943683A1 (enExample)
CL (1) CL2016002382A1 (enExample)
CR (1) CR20160501A (enExample)
CY (1) CY1120969T1 (enExample)
DK (1) DK3122742T3 (enExample)
EA (1) EA032145B1 (enExample)
ES (1) ES2702450T3 (enExample)
HR (1) HRP20182073T1 (enExample)
HU (1) HUE041738T2 (enExample)
IL (1) IL247658B (enExample)
JO (1) JO3512B1 (enExample)
LT (1) LT3122742T (enExample)
MA (1) MA39783B1 (enExample)
MX (1) MX380829B (enExample)
MY (1) MY194074A (enExample)
NI (1) NI201600144A (enExample)
NZ (1) NZ724907A (enExample)
PH (1) PH12016501898B1 (enExample)
PL (1) PL3122742T3 (enExample)
PT (1) PT3122742T (enExample)
RS (1) RS58088B1 (enExample)
SG (1) SG11201607961QA (enExample)
SI (1) SI3122742T1 (enExample)
SM (1) SMT201800670T1 (enExample)
TR (1) TR201819138T4 (enExample)
TW (1) TWI686391B (enExample)
UA (1) UA117958C2 (enExample)
WO (1) WO2015144803A1 (enExample)
ZA (1) ZA201606942B (enExample)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
HRP20161774T1 (hr) 2012-06-13 2017-02-24 F. Hoffmann - La Roche Ag Novi diazaspirocikloalkan i azaspirocikloalkan
BR112015004111A2 (pt) 2012-09-25 2017-07-04 Hoffmann La Roche novos derivados bicíclicos
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
KR20160087900A (ko) 2013-11-26 2016-07-22 에프. 호프만-라 로슈 아게 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일
SI3102576T1 (sl) 2014-02-03 2019-08-30 Vitae Pharmaceuticals, Llc Inhibitorji dihidropirolopiridina ROR-gama
SI3122750T1 (sl) 2014-03-26 2019-12-31 F. Hoffmann-La Roche Ag Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA)
KR20160128428A (ko) 2014-03-26 2016-11-07 에프. 호프만-라 로슈 아게 오토탁신(atx) 및 리소포스파티드산(lpa) 생성 억제제로서의 축합형 [1,4]다이아제핀 화합물
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
HUE053654T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR- és CMET-inhibitorok kombinációi a rák kezelésére
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
JOP20200201A1 (ar) * 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
JP6886967B2 (ja) 2015-09-04 2021-06-16 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ フェノキシメチル誘導体
CA2996857C (en) 2015-09-23 2024-05-21 Janssen Pharmaceutica Nv Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer
EP3353164B1 (en) * 2015-09-23 2021-11-03 Janssen Pharmaceutica, N.V. Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
CN107635995B (zh) 2015-09-24 2022-08-19 豪夫迈·罗氏有限公司 作为atx抑制剂的二环化合物
JP6877413B2 (ja) 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 二重ａｔｘ／ｃａ阻害剤としての新規な二環式化合物
RU2018112230A (ru) 2015-09-24 2019-10-30 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов atx
WO2017087608A1 (en) 2015-11-20 2017-05-26 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
EP3596059B1 (en) 2017-03-16 2024-04-24 F. Hoffmann-La Roche AG Heterocyclic compounds useful as dual atx/ca inhibitors
KR20200053481A (ko) 2017-07-24 2020-05-18 비타이 파마슈티컬즈, 엘엘씨 RORγ의 억제제
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
JP2022515198A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド 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
CN113474337A (zh) * 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物
WO2020208592A1 (en) * 2019-04-12 2020-10-15 Dr. Reddy’S Laboratories Limited Process for preparation of erdafitinib, its purification and amorphous solid dispersion
CN117203202A (zh) * 2021-02-05 2023-12-08 黑钻治疗公司 喹喔啉衍生物及其用途
CA3207475A1 (en) * 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Quinoxaline derivatives and uses thereof

Family Cites Families (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2940972A (en) 1957-06-27 1960-06-14 Thomae Gmbh Dr K Tri-and tetra-substituted pteridine derivatives
GB1583753A (en) 1976-07-14 1981-02-04 Science Union & Cie Piperidine derivatives processes for their preparation and pharmaceutical compositions containing them
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
GB9125001D0 (en) 1991-11-25 1992-01-22 Ici Plc Heterocyclic compounds
TW219935B (enExample) 1991-12-25 1994-02-01 Mitsubishi Chemicals Co Ltd
EP0698015A1 (en) 1993-05-14 1996-02-28 Genentech, Inc. Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
CA2744096C (en) 1996-07-31 2013-07-30 Laboratory Corporation Of America Holdings Biomarkers and targets for diagnosis, prognosis and management of prostate disease
TW472045B (en) 1996-09-25 2002-01-11 Astra Ab Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation
AU747026B2 (en) 1997-05-28 2002-05-09 Aventis Pharmaceuticals Inc. Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
US6235740B1 (en) 1997-08-25 2001-05-22 Bristol-Myers Squibb Co. Imidazoquinoxaline protein tyrosine kinase inhibitors
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
WO2000042026A1 (en) 1999-01-15 2000-07-20 Novo Nordisk A/S Non-peptide glp-1 agonists
NZ514195A (en) 1999-03-17 2004-05-28 Astrazeneca Ab Amide derivatives
EA005287B1 (ru) 1999-09-15 2004-12-30 Уорнер-Ламберт Компани Птеридиноны в качестве ингибиторов киназ
DE10013318A1 (de) 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US20030114448A1 (en) 2001-05-31 2003-06-19 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
JP4286146B2 (ja) 2001-12-18 2009-06-24 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−５のヘテロアリール置換ピラゾール系調節剤
ES2333702T3 (es) 2001-12-24 2010-02-26 Astrazeneca Ab Derivados de quinazolina sustituidos que actuan como unhibidores de cinasas aurora.
JP2003213463A (ja) 2002-01-17 2003-07-30 Sumitomo Chem Co Ltd 金属腐食防止剤および洗浄液
AU2002249275A1 (en) 2002-03-08 2003-09-22 Warner-Lambert Company Llc Oxo azabicyclic compounds
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
US7265378B2 (en) 2002-07-10 2007-09-04 E. I. Du Pont De Nemours And Company Electronic devices made with electron transport and/or anti-quenching layers
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
CA2500727A1 (en) 2002-10-03 2004-04-15 Targegen, Inc. Vasculostatic agents and methods of use thereof
AR043059A1 (es) 2002-11-12 2005-07-13 Bayer Pharmaceuticals Corp Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
JP2006516561A (ja) 2003-01-17 2006-07-06 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー 細胞増殖の阻害剤としての２−アミノピリジン置換ヘテロ環類
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
EP1628666B1 (en) 2003-05-14 2015-09-23 NeuroGenetic Pharmaceuticals, Inc. Compouds and uses thereof in modulating amyloid beta
ES2316985T3 (es) 2003-05-23 2009-04-16 Aterna Zentaris Gmbh Nuevas piridopirazidinas y su uso como moduladores de quinasas.
DE10323345A1 (de) 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
WO2005007099A2 (en) 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
EP1646383A4 (en) 2003-07-21 2009-03-25 Bethesda Pharmaceuticals Inc DESIGN AND SYNTHESIS OF OPTIMIZED LIGANDS FOR PPAR
BRPI0413234A (pt) 2003-08-01 2006-10-03 Genelabs Tech Inc derivados de imidazola bicìclica contra flaviviridae
ES2293354T3 (es) 2003-10-17 2008-03-16 4 Aza Ip Nv Derivados de pteridina sustituidos por heterociclos y su uso en terapia.
WO2005047244A2 (en) 2003-11-07 2005-05-26 Chiron Corporation Inhibition of fgfr3 and treatment of multiple myeloma
EA009875B1 (ru) 2003-11-20 2008-04-28 Янссен Фармацевтика Н.В. 6-алкенил и 6-фенилалкил замещенные 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы
MXPA06005735A (es) 2003-11-24 2006-08-17 Hoffmann La Roche Pirazolil e imidazolil pirimidinas.
PL1706385T3 (pl) 2003-12-23 2011-03-31 Astex Therapeutics Ltd Pochodne pirazolu jako modulatory kinazy białkowej
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
EP1789399A1 (en) 2004-08-31 2007-05-30 AstraZeneca AB Quinazolinone derivatives and their use as b-raf inhibitors
CA2583192A1 (en) 2004-10-14 2006-04-20 F. Hoffmann-La Roche Ag 1,5-naphthyridine azolidinones having cdk1 antiproliferative activity
MX2007004480A (es) 2004-10-15 2007-05-08 Astrazeneca Ab Quinoxalinas como inhibidores b raf.
CN102861019B (zh) 2004-12-24 2016-05-25 诺华股份有限公司 治疗或预防神经性疼痛的药物
US8278290B2 (en) 2005-02-14 2012-10-02 Biononics Limited Tubulin polymerisation inhibitors
US9271963B2 (en) 2005-03-03 2016-03-01 Universitat Des Saarlandes Selective inhibitors of human corticosteroid synthases
AU2006247833A1 (en) 2005-05-12 2006-11-23 Merck & Co., Inc. Tyrosine kinase inhibitors
BRPI0611521A2 (pt) 2005-05-18 2010-09-14 Wyeth Corp inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
WO2007023186A1 (en) 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
CA2628039A1 (en) 2005-11-11 2007-05-18 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
PT1966214T (pt) 2005-12-21 2017-02-03 Janssen Pharmaceutica Nv Triazolpiridazinas como moduladores de tirosina quinase
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
ATE549338T1 (de) 2006-05-24 2012-03-15 Boehringer Ingelheim Int Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
WO2008003702A2 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Fused bicyclic compounds interacting with the histamine h4 receptor
JP2008127446A (ja) 2006-11-20 2008-06-05 Canon Inc １，５−ナフチリジン化合物及び有機発光素子
CN102123712B (zh) 2006-12-13 2014-03-19 默沙东公司 使用igf1r抑制剂治疗癌症的方法
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
AU2007336893A1 (en) 2006-12-22 2008-07-03 Novartis Ag Quinazolines for PDK1 inhibition
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
US7592342B2 (en) 2007-05-10 2009-09-22 Smithkline Beecham Corporation Quinoxaline derivatives as PI3 kinase inhibitors
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
WO2008150827A1 (en) 2007-05-29 2008-12-11 Smithkline Beecham Corporation Naphthyridine, derivatives as p13 kinase inhibitors
AR066879A1 (es) 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
KR20130008625A (ko) 2007-06-20 2013-01-22 미쓰비시 타나베 파마 코퍼레이션 신규한 말론산술폰아미드 유도체 및 그 의약 용도
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
JP2010532758A (ja) 2007-07-06 2010-10-14 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 組み合わせ抗癌療法
ES2424977T3 (es) 2007-08-08 2013-10-10 Glaxosmithkline Intellectual Property Development Limited Derivados de 2-[(2-{fenilamino}-1H-pirrolo[2,3-D]pirimidin-4-il)amino]benzamida como inhibidores de IGF-1R para el tratamiento del cáncer
WO2009021083A1 (en) 2007-08-09 2009-02-12 Smithkline Beecham Corporation Quinoxaline derivatives as pi3 kinase inhibitors
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
ES2569528T3 (es) 2007-11-16 2016-05-11 Incyte Holdings Corporation 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
US20110129456A1 (en) 2008-05-05 2011-06-02 Yaolin Wang Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
MY155535A (en) 2008-05-23 2015-10-30 Novartis Ag Derivatives of quinolines and quinoxalines as protien tyrosine kinase inhibitors
EP2356116A1 (en) 2008-11-20 2011-08-17 OSI Pharmaceuticals, Inc. Substituted pyrroloý2,3-b¨-pyridines and-pyrazines
US8716280B2 (en) 2009-01-21 2014-05-06 Basilea Pharmaceutica Ag Bicyclic antibiotics
WO2010088177A1 (en) 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
TR201910781T4 (tr) 2009-06-12 2019-08-21 Abivax Kanser tedavisi için yararlı bileşikler.
CN102656163B (zh) 2009-09-03 2016-01-13 拜奥埃内杰尼克斯公司 抑制pask的杂环化合物
CA2772790C (en) 2009-09-04 2017-06-27 Benjamin Bader Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
US9095596B2 (en) 2009-10-15 2015-08-04 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
US20110123545A1 (en) 2009-11-24 2011-05-26 Bristol-Myers Squibb Company Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases
EP2332939A1 (en) 2009-11-26 2011-06-15 Æterna Zentaris GmbH Novel Naphthyridine derivatives and the use thereof as kinase inhibitors
EP2560966B1 (en) 2010-03-30 2021-01-06 Verseon International Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
WO2011146591A1 (en) 2010-05-19 2011-11-24 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
CN103153062B (zh) 2010-05-24 2015-07-15 因特利凯有限责任公司 杂环化合物及其用途
GB201020179D0 (en) * 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
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
MX343706B (es) 2011-01-31 2016-11-18 Novartis Ag Derivados heterocíclicos novedosos.
US20140037642A1 (en) 2011-02-02 2014-02-06 Amgen Inc. Methods and compositions relating to inhibition of igf-1r
JP6130305B2 (ja) 2011-02-23 2017-05-17 インテリカイン， エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
US9896730B2 (en) 2011-04-25 2018-02-20 OSI Pharmaceuticals, LLC Use of EMT gene signatures in cancer drug discovery, diagnostics, and treatment
ES2648820T3 (es) 2011-05-10 2018-01-08 Gilead Sciences, Inc. Compuestos heterocíclicos condensados como moduladores de los canales de sodio
WO2013032951A1 (en) 2011-08-26 2013-03-07 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP3332785B1 (en) 2011-09-14 2020-05-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2757885B1 (en) 2011-09-21 2017-03-15 Neupharma, Inc. Certain chemical entites, compositions, and methods
CN104024257A (zh) 2011-10-04 2014-09-03 吉利德卡利斯托加有限责任公司 Pi3k的新的喹喔啉抑制剂
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
BR112014009890A2 (pt) 2011-10-28 2020-10-27 Novartis Ag derivados de purina e seu uso no tratamento de doença
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
US9481911B2 (en) 2012-03-08 2016-11-01 Astellas Pharma Inc. Methods for detecting FGFR3/TACC3 fusion genes
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
US10980804B2 (en) 2013-01-18 2021-04-20 Foundation Medicine, Inc. Methods of treating cholangiocarcinoma
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US10028956B2 (en) 2013-08-02 2018-07-24 Ignyta, Inc. Methods of treating various cancers using an AXL/cMET inhibitor in combination with other agents
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
HUE053654T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR- és CMET-inhibitorok kombinációi a rák kezelésére
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
MX2017010595A (es) 2015-02-19 2018-11-12 Bioclin Therapeutics Inc Métodos, composiciones, y equipos para tratamiento de cáncer.
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer

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