DK2776435T3 - ANTICANCER PYRIDOPYRAZINES BY INHIBITION OF FGFR KINASES - Google Patents

ANTICANCER PYRIDOPYRAZINES BY INHIBITION OF FGFR KINASES Download PDF

Info

Publication number
DK2776435T3
DK2776435T3 DK12794745.5T DK12794745T DK2776435T3 DK 2776435 T3 DK2776435 T3 DK 2776435T3 DK 12794745 T DK12794745 T DK 12794745T DK 2776435 T3 DK2776435 T3 DK 2776435T3
Authority
DK
Denmark
Prior art keywords
alkyl
substituted
galkyl
cancer
formula
Prior art date
Application number
DK12794745.5T
Other languages
Danish (da)
English (en)
Inventor
Valerio Berdini
Patrick René Angibaud
Olivier Alexis Georges Querolle
Virginie Sophie Poncelet
Bruno Roux
Lieven Meerpoel
Gordon Saxty
Original Assignee
Astex Therapeutics Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Application granted granted Critical
Publication of DK2776435T3 publication Critical patent/DK2776435T3/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
DK12794745.5T 2011-10-28 2012-10-26 ANTICANCER PYRIDOPYRAZINES BY INHIBITION OF FGFR KINASES DK2776435T3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161552888P 2011-10-28 2011-10-28
GBGB1118656.6A GB201118656D0 (en) 2011-10-28 2011-10-28 New compounds
PCT/GB2012/052672 WO2013061080A1 (en) 2011-10-28 2012-10-26 Anticancer pyridopyrazines via the inhibition of fgfr kinases

Publications (1)

Publication Number Publication Date
DK2776435T3 true DK2776435T3 (en) 2018-10-15

Family

ID=45373584

Family Applications (1)

Application Number Title Priority Date Filing Date
DK12794745.5T DK2776435T3 (en) 2011-10-28 2012-10-26 ANTICANCER PYRIDOPYRAZINES BY INHIBITION OF FGFR KINASES

Country Status (33)

Country Link
US (2) US9309242B2 (OSRAM)
EP (1) EP2776435B1 (OSRAM)
JP (1) JP6169583B2 (OSRAM)
KR (1) KR102066496B1 (OSRAM)
CN (1) CN104011051B (OSRAM)
AP (1) AP4060A (OSRAM)
AR (1) AR088567A1 (OSRAM)
AU (1) AU2012328170B2 (OSRAM)
BR (1) BR112014010206B8 (OSRAM)
CA (1) CA2853390C (OSRAM)
CL (1) CL2014001065A1 (OSRAM)
CO (1) CO6940422A2 (OSRAM)
CR (1) CR20140190A (OSRAM)
DK (1) DK2776435T3 (OSRAM)
EA (1) EA027563B1 (OSRAM)
EC (1) ECSP14013325A (OSRAM)
ES (1) ES2688868T3 (OSRAM)
GB (1) GB201118656D0 (OSRAM)
HR (1) HRP20181533T1 (OSRAM)
IL (1) IL232083B (OSRAM)
IN (1) IN2014MN00948A (OSRAM)
JO (1) JO3419B1 (OSRAM)
LT (1) LT2776435T (OSRAM)
MX (1) MX353654B (OSRAM)
MY (1) MY185666A (OSRAM)
NI (1) NI201400032A (OSRAM)
PH (1) PH12014500867A1 (OSRAM)
SG (1) SG11201401055XA (OSRAM)
SI (1) SI2776435T1 (OSRAM)
TW (1) TWI602814B (OSRAM)
UA (1) UA111386C2 (OSRAM)
UY (1) UY34418A (OSRAM)
WO (1) WO2013061080A1 (OSRAM)

Families Citing this family (43)

* 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
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118656D0 (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
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
AU2014338549B2 (en) 2013-10-25 2017-05-25 Novartis Ag Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
AR098145A1 (es) * 2013-10-25 2016-05-04 Novartis Ag Compuestos derivados de piridilo bicíclicos fusionados como inhibidores de fgfr4
MA55696A (fr) 2014-03-26 2022-02-23 Astex Therapeutics Ltd Combinaisons
JP6980385B2 (ja) * 2014-03-26 2021-12-15 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited Fgfr阻害剤とigf1r阻害剤の組合せ
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JP5925978B1 (ja) 2014-08-18 2016-05-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 単環ピリジン誘導体の塩およびその結晶
ES2756748T3 (es) 2014-10-03 2020-04-27 Novartis Ag Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4
TWI695837B (zh) 2014-12-04 2020-06-11 比利時商健生藥品公司 作為激酶調節劑之三唑並嗒
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
CA2974937C (en) 2015-03-25 2023-09-05 National Cancer Center Therapeutic agent for bile duct cancer
US9802917B2 (en) * 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
HRP20220012T1 (hr) 2015-09-23 2022-04-01 Janssen Pharmaceutica Nv Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka
BR112018005637B1 (pt) 2015-09-23 2023-11-28 Janssen Pharmaceutica Nv Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos
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
KR102486722B1 (ko) 2015-12-17 2023-01-11 에자이 알앤드디 매니지먼트 가부시키가이샤 유방암 치료제
KR20170114254A (ko) * 2016-03-24 2017-10-13 재단법인 대구경북첨단의료산업진흥재단 신규한 피리딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 fgfr 관련 질환의 예방 또는 치료용 약학적 조성물
JP7088906B2 (ja) 2016-08-12 2022-06-21 江▲蘇▼豪森▲薬▼▲業▼集▲団▼有限公司 Fgfr4阻害剤並びにその製造方法及び使用
CN108101857B (zh) * 2016-11-24 2021-09-03 韶远科技(上海)有限公司 制取2-氨基-3-溴-6-氯吡嗪的可放大工艺
CN108264510A (zh) * 2017-01-02 2018-07-10 上海喆邺生物科技有限公司 一种选择性抑制激酶化合物及其用途
US11219619B2 (en) 2018-03-28 2022-01-11 Eisai R&D Management Co., Ltd. Therapeutic agent for hepatocellular carcinoma
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
JP2022515197A (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 がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体
WO2021138392A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Aminopyrimidine compounds
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
JP2023512482A (ja) * 2020-01-17 2023-03-27 ベータ・ファーマ・インコーポレイテッド Fgfrキナーゼ阻害剤としてのピリダジンおよび1,2,4-トリアジン誘導体
CA3205986A1 (en) 2020-12-30 2022-07-07 Tyra Biosciences, Inc. Indazole compounds as kinase inhibitors
EP4297873A1 (en) 2021-02-26 2024-01-03 Tyra Biosciences, Inc. Aminopyrimidine compounds and methods of their use
TW202416961A (zh) 2022-06-29 2024-05-01 美商泰拉生物科學公司 吲唑化合物
EP4547670A1 (en) 2022-06-29 2025-05-07 Tyra Biosciences, Inc. Polymorphic compounds and uses thereof
WO2024138112A1 (en) 2022-12-22 2024-06-27 Tyra Biosciences, Inc. Indazole compounds
TW202535368A (zh) 2023-12-15 2025-09-16 美商泰拉生物科學公司 吲唑化合物
WO2025222097A1 (en) 2024-04-19 2025-10-23 Tyra Biosciences, Inc. Indazole-based protac degraders and their anticancer activity

Family Cites Families (117)

* 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
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
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
WO1998004689A1 (en) 1995-07-31 1998-02-05 Urocor, Inc. 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
JP2002500675A (ja) 1997-05-28 2002-01-08 アヴェンティス ファーマシューティカルズ プロダクツ インコーポレイテッド 血小板由来成長因子及び/又はp56▲上lck▼チロシンキナーゼを阻害するキノリン及びキノキサリン化合物
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
NZ516872A (en) 1999-09-15 2003-10-31 Warner Lambert Co Pteridinones as kinase inhibitors
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
DE60223720T2 (de) 2001-12-18 2008-10-30 Merck & Co., Inc. Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5
UA82058C2 (uk) 2001-12-24 2008-03-11 Астразенека Аб Заміщені похідні хіназоліну як інгібітори ауроракінази, спосіб їх одержання, фармацевтична композиція на їх основі
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
AU2003223467B2 (en) 2002-04-08 2007-10-04 Merck Sharp & Dohme Corp. 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
MXPA05012281A (es) 2003-05-14 2006-05-19 Torreypines Therapeutics Inc Compuestos y uso de los mismos en la modulacion beta amiloide.
WO2004104003A1 (de) * 2003-05-23 2004-12-02 Zentaris Gmbh Neue pyridopyrazine und deren verwendung als modulatoren von kinasen
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
CA2533417A1 (en) 2003-07-21 2005-02-03 Mitchell A. Avery Design and synthesis of optimized ligands for ppar
ZA200600424B (en) 2003-08-01 2007-05-30 Genelabs Tech Inc Bicyclic imidazol derivatives against flaviviridae
WO2005039587A1 (en) 2003-10-17 2005-05-06 4 Aza Bioscience Nv Heterocycle-substituted pteridine derivatives and their use in therapy
KR101224410B1 (ko) 2003-11-07 2013-01-23 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 퀴놀리논 화합물을 합성하는 방법
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.
HRP20100675T1 (hr) 2003-12-23 2011-01-31 Astex Therapeutics Limited Derivati pirazola kao modulatori protein kinaze
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
AU2005278959A1 (en) 2004-08-31 2006-03-09 Astrazeneca Ab Quinazolinone derivatives and their use as B-Raf inhibitors
WO2006040052A1 (en) 2004-10-14 2006-04-20 F. Hoffmann-La Roche Ag 1,5-naphthyridine azolidinones having cdk1 antiproliferative activity
EP2650011A1 (en) 2004-12-24 2013-10-16 Spinifex Pharmaceuticals Pty Ltd Method of treatment or prophylaxis
EP1848704A4 (en) 2005-02-14 2011-05-11 Bionomics Ltd Novel tubulin polymerisation inhibitors
EP1853261B1 (de) 2005-03-03 2017-01-11 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
JP2008540535A (ja) 2005-05-12 2008-11-20 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害剤
AU2006247315A1 (en) 2005-05-18 2006-11-23 Wyeth 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of Tpl2 kinase and methods of making and using the same
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
UA100358C2 (xx) 2005-08-26 2012-12-25 Мерк Сероно Са Похідні піразину та їх застосування
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
KR101400905B1 (ko) 2005-11-11 2014-05-29 아에테르나 젠타리스 게엠베하 신규한 피리도피라진 및 키나제의 조절제로서의 이의 용도
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
ME02736B (me) 2005-12-21 2017-10-20 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
JP2009535393A (ja) 2006-05-01 2009-10-01 ファイザー・プロダクツ・インク 置換2−アミノ縮合複素環式化合物
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
WO2007135027A1 (de) 2006-05-24 2007-11-29 Boehringer Ingelheim International Gmbh Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
CA2657702A1 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs Wetenschappelijk Onderzoek E N Patieentenzorg Quinazolines and related heterocyclic comp0unds, and their therapeutic use
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
JP2010513278A (ja) 2006-12-13 2010-04-30 シェーリング コーポレイション Igf1rインヒビターを用いた癌の処置方法
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
KR20090092287A (ko) 2006-12-22 2009-08-31 노파르티스 아게 Pdk1 억제를 위한 퀴나졸린
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
EP2150255A4 (en) 2007-05-10 2011-10-05 Glaxosmithkline Llc CHINOXALINE DERIVATIVES AS P13 KINASE INHIBITORS
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
KR101251933B1 (ko) 2007-06-20 2013-04-09 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
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
WO2009021083A1 (en) 2007-08-09 2009-02-12 Smithkline Beecham Corporation Quinoxaline derivatives as pi3 kinase inhibitors
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
JP5480813B2 (ja) 2007-11-16 2014-04-23 インサイト・コーポレイション Janusキナーゼ阻害剤としての置換複素環
US20110129456A1 (en) 2008-05-05 2011-06-02 Yaolin Wang Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
KR101257158B1 (ko) 2008-05-23 2013-04-23 노파르티스 아게 단백질 티로신 키나제 억제제로서의 퀴놀린 및 퀴녹살린의 유도체
US8592448B2 (en) 2008-11-20 2013-11-26 OSI Pharmaceuticals, LLC Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
CN102361863B (zh) 2009-01-21 2014-12-03 巴斯利尔药物股份公司 新的二环抗生素
EP2391623A4 (en) 2009-02-02 2012-09-05 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
KR20120051643A (ko) 2009-06-12 2012-05-22 쏘시에떼 스플리코 조기 노화, 구체적으로 조로증을 치료하는데 유용한 화합물
MX2012002274A (es) 2009-09-03 2012-09-07 Bioenergenix Compuestos heterociclicos para la inhibicion de pask.
US9340528B2 (en) 2009-09-04 2016-05-17 Bayer Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
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
RU2639876C2 (ru) 2010-03-30 2017-12-25 Версеон Корпорейшн Мультизамещенные ароматические соединения в качестве ингибиторов тромбина
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
US8513421B2 (en) 2010-05-19 2013-08-20 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
JP5894980B2 (ja) 2010-05-24 2016-03-30 インテリカイン, エルエルシー 複素環式化合物およびその使用
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
US8987257B2 (en) 2011-01-31 2015-03-24 Novartis Ag Heterocyclic derivatives
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
JP6002223B2 (ja) 2011-08-26 2016-10-05 ニューファーマ, インコーポレイテッド 特定の化学的実体、組成物、および方法
US9518029B2 (en) 2011-09-14 2016-12-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2757885B1 (en) 2011-09-21 2017-03-15 Neupharma, Inc. Certain chemical entites, compositions, and methods
JP2014528451A (ja) 2011-10-04 2014-10-27 ギリアード カリストガ エルエルシー Pi3kの新規キノキサリン阻害剤
GB201118656D0 (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
KR20140090218A (ko) 2011-10-28 2014-07-16 노파르티스 아게 신규 퓨린 유도체 및 질환의 치료에서의 그의 용도
GB201118654D0 (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
CN104379740B (zh) 2012-03-08 2019-05-14 安斯泰来制药株式会社 新型fgfr3融合体
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (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
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
JP6980385B2 (ja) 2014-03-26 2021-12-15 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited Fgfr阻害剤とigf1r阻害剤の組合せ
MA55696A (fr) 2014-03-26 2022-02-23 Astex Therapeutics Ltd Combinaisons
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
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

Also Published As

Publication number Publication date
CN104011051B (zh) 2017-05-10
NZ622702A (en) 2016-08-26
UY34418A (es) 2013-05-31
CL2014001065A1 (es) 2014-07-25
HRP20181533T1 (hr) 2018-11-16
BR112014010206B8 (pt) 2021-08-03
US20160235744A1 (en) 2016-08-18
CA2853390A1 (en) 2013-05-02
SI2776435T1 (sl) 2018-11-30
KR102066496B1 (ko) 2020-01-15
UA111386C2 (uk) 2016-04-25
SG11201401055XA (en) 2014-09-26
US9309242B2 (en) 2016-04-12
JP2014534211A (ja) 2014-12-18
JO3419B1 (ar) 2019-10-20
BR112014010206B1 (pt) 2020-12-08
CO6940422A2 (es) 2014-05-09
AP4060A (en) 2017-03-08
CR20140190A (es) 2014-05-26
MX2014004855A (es) 2014-08-21
LT2776435T (lt) 2018-10-10
MY185666A (en) 2021-05-28
GB201118656D0 (en) 2011-12-07
IL232083A0 (en) 2014-05-28
JP6169583B2 (ja) 2017-07-26
US20140288053A1 (en) 2014-09-25
KR20140096034A (ko) 2014-08-04
AP2014007540A0 (en) 2014-03-31
CA2853390C (en) 2020-12-15
ES2688868T3 (es) 2018-11-07
IL232083B (en) 2018-06-28
US10045982B2 (en) 2018-08-14
EA027563B1 (ru) 2017-08-31
CN104011051A (zh) 2014-08-27
AR088567A1 (es) 2014-06-18
EP2776435B1 (en) 2018-06-27
NI201400032A (es) 2015-11-24
ECSP14013325A (es) 2015-04-30
IN2014MN00948A (OSRAM) 2015-04-24
MX353654B (es) 2018-01-22
AU2012328170A1 (en) 2014-05-22
PH12014500867A1 (en) 2014-06-30
WO2013061080A1 (en) 2013-05-02
TW201333004A (zh) 2013-08-16
TWI602814B (zh) 2017-10-21
EA201490891A1 (ru) 2014-09-30
AU2012328170B2 (en) 2017-08-24
BR112014010206A2 (pt) 2017-05-16
EP2776435A1 (en) 2014-09-17

Similar Documents

Publication Publication Date Title
DK2776435T3 (en) ANTICANCER PYRIDOPYRAZINES BY INHIBITION OF FGFR KINASES
EP2855480B1 (en) Pteridines as fgfr inhibitors
AU2012328167B9 (en) New compounds
AU2012328171B2 (en) Anticancer benzopyrazines via the inhibition of FGFR kinases
US9737544B2 (en) Compounds
DK2776397T3 (en) QUINOLINES AS FGFR CHINA MODULATORS
EP2646432A1 (en) Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases
HK1197411B (en) Anticancer pyridopyrazines via the inhibition of fgfr kinases
HK1197411A (en) Anticancer pyridopyrazines via the inhibition of fgfr kinases