MY185666A - Anticancer pyridopyrazines via the inhibition of fgfr kinases - Google Patents

Anticancer pyridopyrazines via the inhibition of fgfr kinases

Info

Publication number
MY185666A
MY185666A MYPI2014001207A MYPI2014001207A MY185666A MY 185666 A MY185666 A MY 185666A MY PI2014001207 A MYPI2014001207 A MY PI2014001207A MY PI2014001207 A MYPI2014001207 A MY PI2014001207A MY 185666 A MY185666 A MY 185666A
Authority
MY
Malaysia
Prior art keywords
pyridopyrazines
anticancer
inhibition
fgfr kinases
compounds
Prior art date
Application number
MYPI2014001207A
Other languages
English (en)
Inventor
Gordon Saxty
Valerio Berdini
Patrick Rene Angibaud
Olivier Alexis Georges Querolle
Virginie Sophie Poncelet
Bruno Roux
Lieven Meerpoel
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
Publication of MY185666A publication Critical patent/MY185666A/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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
MYPI2014001207A 2011-10-28 2012-10-26 Anticancer pyridopyrazines via the inhibition of fgfr kinases MY185666A (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
MY185666A true MY185666A (en) 2021-05-28

Family

ID=45373584

Family Applications (1)

Application Number Title Priority Date Filing Date
MYPI2014001207A MY185666A (en) 2011-10-28 2012-10-26 Anticancer pyridopyrazines via the inhibition of fgfr kinases

Country Status (33)

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

Families Citing this family (41)

* 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
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
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
AR098145A1 (es) * 2013-10-25 2016-05-04 Novartis Ag Compuestos derivados de piridilo bicíclicos fusionados como inhibidores de fgfr4
PL3060563T3 (pl) * 2013-10-25 2018-10-31 Novartis Ag Pierścienio-skondensowane bicykliczne pochodne pirydylowe jako inhibitory fgfr4
DK3122359T3 (da) 2014-03-26 2021-03-08 Astex Therapeutics Ltd Kombinationer af en fgfr-inhibitor og en igf1r-hæmmer
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
KR102479693B1 (ko) * 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 조합물
WO2016027781A1 (ja) 2014-08-18 2016-02-25 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
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
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
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
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
CN108026095B (zh) 2015-09-23 2021-07-27 詹森药业有限公司 新化合物
HUE057090T2 (hu) 2015-09-23 2022-04-28 Janssen Pharmaceutica Nv BI-heteroaril-szubsztituált 1,4-benzodiazepinek és alkalmazásuk rák kezelésében
EP3365335B1 (en) 2015-10-23 2024-02-14 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
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
WO2019189241A1 (ja) 2018-03-28 2019-10-03 エーザイ・アール・アンド・ディー・マネジメント株式会社 肝細胞癌治療剤
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
US20230115528A1 (en) 2019-12-30 2023-04-13 Tyra Biosciences, Inc. Indazole compounds
EP4085055A1 (en) 2019-12-30 2022-11-09 Tyra Biosciences, Inc. Aminopyrimidine compounds
WO2021146163A1 (en) * 2020-01-17 2021-07-22 Beta Pharma, Inc. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors
MX2023007793A (es) 2020-12-30 2023-09-22 Tyra Biosciences Inc Compuestos de indazol como inhibidores de cinasas.
IL305178A (en) 2021-02-26 2023-10-01 Tyra Biosciences Inc Aminopyrimidine compounds and methods of using them
JP2025525433A (ja) 2022-06-29 2025-08-05 タイラ・バイオサイエンシーズ・インコーポレイテッド インダゾール化合物
WO2024006883A1 (en) 2022-06-29 2024-01-04 Tyra Biosciences, Inc. Polymorphic compounds and uses thereof
WO2024138112A1 (en) 2022-12-22 2024-06-27 Tyra Biosciences, Inc. Indazole compounds
WO2025129014A1 (en) 2023-12-15 2025-06-19 Tyra Biosciences, Inc. Indazole compounds for the treatment of cancer

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
CA2160786A1 (en) 1993-05-14 1994-11-24 James C. Marsters, Jr. Ras farnesyl transferase inhibitors
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
WO1998054156A1 (en) 1997-05-28 1998-12-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR P56lck TYROSINE KINASES
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
IL148614A0 (en) 1999-09-15 2002-09-12 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
US7402585B2 (en) 2001-12-24 2008-07-22 Astrazeneca Ab Substituted quinazoline derivatives as inhibitors of aurora kinases
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
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
WO2004030635A2 (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
DE602004021558D1 (de) 2003-01-17 2009-07-30 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
EP1620413A2 (en) 2003-04-30 2006-02-01 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.
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
CA2533417A1 (en) 2003-07-21 2005-02-03 Mitchell A. Avery Design and synthesis of optimized ligands for ppar
JP2007501189A (ja) 2003-08-01 2007-01-25 ジェネラブス テクノロジーズ,インコーポレイテッド フラビウイルス科に対する二環式イミダゾール誘導体
EP1673092B1 (en) 2003-10-17 2007-08-15 4 Aza Ip Nv Heterocycle-substituted pteridine derivatives and their use in therapy
KR20060111520A (ko) 2003-11-07 2006-10-27 카이론 코포레이션 Fgfr3의 억제 및 다발성 골수종의 치료
KR101118582B1 (ko) 2003-11-20 2012-02-27 얀센 파마슈티카 엔.브이. 폴리(adp-리보스)폴리머라제 저해제로서의 6-알케닐 및6-페닐알킬 치환된 2-퀴놀리논 및 2-퀴녹살리논
CA2545992A1 (en) 2003-11-24 2005-06-16 F. Hoffmann-La Roche Ag Pyrazolyl and imidazolyl pyrimidines
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
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
US20090118261A1 (en) 2004-08-31 2009-05-07 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
HRP20130738T1 (hr) 2004-12-24 2013-10-25 Spinifex Pharmaceuticals Pty Ltd Postupak lijeäśenja ili profilakse
AU2006212726C1 (en) 2005-02-14 2013-05-16 Bionomics Limited Novel tubulin polymerisation inhibitors
EP1853261B1 (de) 2005-03-03 2017-01-11 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
EP1881986A2 (en) 2005-05-12 2008-01-30 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
UA100358C2 (xx) 2005-08-26 2012-12-25 Мерк Сероно Са Похідні піразину та їх застосування
JP5527972B2 (ja) 2005-11-11 2014-06-25 エテルナ ツェンタリス ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規のピリドピラジン及び前記ピリドピラジンをキナーゼのモジュレーターとして用いる使用
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
CN101374843B (zh) 2005-12-21 2012-09-05 詹森药业有限公司 作为酪氨酸激酶调节剂的三唑并哒嗪
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
US20100234347A1 (en) 2006-05-24 2010-09-16 Boehringer Ingelheim Internationl Gmbh Substituted Pteridines substituted with a Four-Membered Heterocycle
JP2009541460A (ja) 2006-07-03 2009-11-26 ベレナギング ヴォー クリスタラク ホガー オンダーヴェイル ヴェーテンザパーリク オンダージーク エン パシェンテンゾーク ヒスタミンh4受容体と相互作用する縮合二環式化合物
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
EP2104501B1 (en) 2006-12-13 2014-03-12 Merck Sharp & Dohme Corp. Methods of cancer treatment with igf1r inhibitors
WO2008080015A2 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
US20100216767A1 (en) 2006-12-22 2010-08-26 Mina Aikawa Quinazolines for pdk1 inhibition
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
WO2008141065A1 (en) 2007-05-10 2008-11-20 Smithkline Beecham Corporation Quinoxaline 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
ES2442003T3 (es) 2007-06-20 2014-02-07 Mitsubishi Tanabe Pharma Corporation Nuevo derivado de sulfonamida de ácido malónico y uso farmacéutico del mismo
WO2008155378A1 (en) 2007-06-21 2008-12-24 Janssen Pharmaceutica Nv 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
EP2173354A4 (en) 2007-08-09 2011-10-05 Glaxosmithkline Llc CHINOXALIN 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
KR101580482B1 (ko) 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 4-피라졸릴-n-아릴피리미딘-2-아민 및 4-피라졸릴-n-헤테로아릴피리미딘-2-아민
WO2009137378A2 (en) 2008-05-05 2009-11-12 Schering Corporation 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
US8592448B2 (en) 2008-11-20 2013-11-26 OSI Pharmaceuticals, LLC Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
EP2389376A1 (en) 2009-01-21 2011-11-30 Basilea Pharmaceutica AG Novel bicyclic antibiotics
AU2010208480A1 (en) 2009-02-02 2011-07-28 Msd K.K. Inhibitors of Akt activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
EP2440547B1 (en) 2009-06-12 2022-11-30 Abivax New chemical molecules that inhibit the splicing mechanism for the treatment of diseases resulting from splicing defects
JP5696856B2 (ja) 2009-09-03 2015-04-08 バイオエナジェニックス Paskの阻害用複素環式化合物
CA2772790C (en) 2009-09-04 2017-06-27 Benjamin Bader 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
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp 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
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
UY33883A (es) 2011-01-31 2012-08-31 Novartis Ag Novedosos derivados heterocíclicos
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
EP2747767B8 (en) 2011-08-26 2019-07-17 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2755657B1 (en) 2011-09-14 2017-11-29 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2013043935A1 (en) 2011-09-21 2013-03-28 Neupharma, Inc. Certain chemical entites, compositions, and methods
CA2850763A1 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
ES2587533T3 (es) 2011-10-28 2016-10-25 Novartis Ag Derivados de purina y su uso en el tratamiento de enfermedades
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
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
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
MX365214B (es) 2012-03-08 2019-05-27 Astellas Pharma Inc Nuevo producto de fusion de fgfr3.
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
KR102479693B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 조합물
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
DK3122359T3 (da) 2014-03-26 2021-03-08 Astex Therapeutics Ltd Kombinationer af en fgfr-inhibitor og en igf1r-hæmmer
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
US10045982B2 (en) 2018-08-14
AP2014007540A0 (en) 2014-03-31
IN2014MN00948A (instruction) 2015-04-24
CO6940422A2 (es) 2014-05-09
US20160235744A1 (en) 2016-08-18
UY34418A (es) 2013-05-31
JO3419B1 (ar) 2019-10-20
HRP20181533T1 (hr) 2018-11-16
IL232083B (en) 2018-06-28
AU2012328170B2 (en) 2017-08-24
BR112014010206A2 (pt) 2017-05-16
BR112014010206B8 (pt) 2021-08-03
EA201490891A1 (ru) 2014-09-30
CN104011051B (zh) 2017-05-10
AR088567A1 (es) 2014-06-18
MX2014004855A (es) 2014-08-21
EP2776435B1 (en) 2018-06-27
CN104011051A (zh) 2014-08-27
AU2012328170A1 (en) 2014-05-22
TWI602814B (zh) 2017-10-21
NZ622702A (en) 2016-08-26
KR20140096034A (ko) 2014-08-04
CA2853390A1 (en) 2013-05-02
CL2014001065A1 (es) 2014-07-25
ECSP14013325A (es) 2015-04-30
TW201333004A (zh) 2013-08-16
CR20140190A (es) 2014-05-26
BR112014010206B1 (pt) 2020-12-08
PH12014500867A1 (en) 2014-06-30
US20140288053A1 (en) 2014-09-25
IL232083A0 (en) 2014-05-28
LT2776435T (lt) 2018-10-10
EP2776435A1 (en) 2014-09-17
ES2688868T3 (es) 2018-11-07
NI201400032A (es) 2015-11-24
MX353654B (es) 2018-01-22
KR102066496B1 (ko) 2020-01-15
CA2853390C (en) 2020-12-15
JP2014534211A (ja) 2014-12-18
AP4060A (en) 2017-03-08
EA027563B1 (ru) 2017-08-31
GB201118656D0 (en) 2011-12-07
WO2013061080A1 (en) 2013-05-02
UA111386C2 (uk) 2016-04-25
US9309242B2 (en) 2016-04-12
SI2776435T1 (sl) 2018-11-30
DK2776435T3 (en) 2018-10-15
JP6169583B2 (ja) 2017-07-26
SG11201401055XA (en) 2014-09-26

Similar Documents

Publication Publication Date Title
PH12014500867A1 (en) Anticancer pyridopyrazines via the inhibition of fgfr kinases
MX2014004861A (es) Benzopirazinas anticancerigenas via la inhibicion de cinasas del receptor del factor de crecimiento de fibroblasto (fgfr).
MX349004B (es) Nuevos compuestos.
MX366899B (es) Nuevos compuestos.
MX359418B (es) Pteridinas como inhibidores del receptor del factor de crecimiento de fribroblasto (fgfr).
MX365702B (es) Inhibidores de pirazolil quinoxalina cinasa.
IN2014MN00988A (instruction)
PH12016501898B1 (en) Quinoxaline derivatives useful as fgfr kinase modulators
MX2015006152A (es) Compuestos de aminopirimidina como inhibidores de mutantes de egfr que contienen t7 9 0m.
PH12012500497A1 (en) Substituted (heteroarylmethyl) thiohydantoins as anticancer drugs
PH12014502772A1 (en) Substituted tricyclic compounds as fgfr inhibitors
PH12014502757B1 (en) Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
MX346147B (es) Compuestos de 3-aril-5-substituido-isoquinolin-1-ona y su uso terapeutico.
MX354024B (es) Uso de array-380 y ar00440993 para el tratamiento de cancer de cerebro.
WO2012162513A3 (en) Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase i inhibitors
IN2014DN03010A (instruction)
IN2013MU03118A (instruction)
UA110793C2 (uk) Піразолілхіноксалінові інгібітори кінази