MX366166B - Derivados de quinazolinona utiles como moduladores de cinasa del receptor del factor de crecimiento del fibroblasto (fgfr). - Google Patents

Derivados de quinazolinona utiles como moduladores de cinasa del receptor del factor de crecimiento del fibroblasto (fgfr).

Info

Publication number
MX366166B
MX366166B MX2015014471A MX2015014471A MX366166B MX 366166 B MX366166 B MX 366166B MX 2015014471 A MX2015014471 A MX 2015014471A MX 2015014471 A MX2015014471 A MX 2015014471A MX 366166 B MX366166 B MX 366166B
Authority
MX
Mexico
Prior art keywords
relates
compounds
signals
toys
cancer
Prior art date
Application number
MX2015014471A
Other languages
English (en)
Other versions
MX2015014471A (es
Inventor
René Angibaud Patrick
Sophie Poncelet Virginie
Meerpoel Lieven
Noëlle Constance Pilatte Isabelle
Alexis Georges Querolle Olivier
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 MX2015014471A publication Critical patent/MX2015014471A/es
Publication of MX366166B publication Critical patent/MX366166B/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/91Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms
    • C07D239/82Oxygen atoms with an aryl radical attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Toys (AREA)

Abstract

La presente invención se refiere a nuevos compuestos derivados de quinazolinona, a composiciones farmacéuticas que comprenden tales compuestos, a procesos para la preparación de tales compuestos y al uso de tales compuestos en el tratamiento de enfermedades, por ejemplo, cáncer.
MX2015014471A 2013-04-26 2014-04-25 Derivados de quinazolinona utiles como moduladores de cinasa del receptor del factor de crecimiento del fibroblasto (fgfr). MX366166B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1307577.5A GB201307577D0 (en) 2013-04-26 2013-04-26 New compounds
PCT/GB2014/051288 WO2014174307A1 (en) 2013-04-26 2014-04-25 Quinazolinone derivatives useful as fgfr kinase modulators

Publications (2)

Publication Number Publication Date
MX2015014471A MX2015014471A (es) 2016-06-28
MX366166B true MX366166B (es) 2019-07-01

Family

ID=48626899

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015014471A MX366166B (es) 2013-04-26 2014-04-25 Derivados de quinazolinona utiles como moduladores de cinasa del receptor del factor de crecimiento del fibroblasto (fgfr).

Country Status (14)

Country Link
US (1) US9493426B2 (es)
EP (1) EP2989092B1 (es)
JP (1) JP6419784B2 (es)
KR (1) KR102341202B1 (es)
CN (1) CN105324378B (es)
AU (1) AU2014259151B2 (es)
BR (1) BR112015026830B1 (es)
CA (1) CA2910142C (es)
DK (1) DK2989092T3 (es)
ES (1) ES2650312T3 (es)
GB (1) GB201307577D0 (es)
MX (1) MX366166B (es)
RU (1) RU2701517C2 (es)
WO (1) WO2014174307A1 (es)

Families Citing this family (48)

* 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
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
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
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
BR112016008276B1 (pt) 2013-10-25 2021-03-02 Novartis Ag derivados bicíclicos de piridila fundidos ao anel, seus usos e seu intermediário, e composição farmacêutica
MA39784B1 (fr) 2014-03-26 2021-03-31 Astex Therapeutics Ltd Combinaisons des inhibiteurs du fgfr et du cmet destinées au traitement du cancer
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
AU2015238305B2 (en) 2014-03-26 2020-06-18 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
WO2016054483A1 (en) 2014-10-03 2016-04-07 Novartis Ag Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JO3695B1 (ar) 2015-02-10 2020-08-27 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n- (3.5- ثنائي ميثوكسي فينيل)-n-(1-ميثيل إيثيل)-n- 3-( ميثيل-h1-بيرازول-4-يل) كينوكسالين-6-يل) إيثان- 1.2-ثنائي الأمين)
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG11201706287PA (en) 2015-02-20 2017-09-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
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
KR102703498B1 (ko) * 2015-09-23 2024-09-04 얀센 파마슈티카 엔브이 신규 화합물
CN108137546B (zh) * 2015-09-23 2021-07-27 詹森药业有限公司 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途
EP3508482B1 (en) * 2016-09-01 2020-12-16 Nanjing Transthera Biosciences Co. Ltd. Inhibitors of fibroblast growth factor receptor and use thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
ES3061844T3 (en) 2018-05-04 2026-04-07 Incyte Corp Salts of an fgfr inhibitor
MX2020011718A (es) 2018-05-04 2021-02-15 Incyte Corp Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
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
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
CN110903253B (zh) * 2019-12-13 2020-12-25 西安交通大学医学院第一附属医院 一种喹唑啉酮类化合物及其制备方法和应用
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP7630801B2 (ja) * 2020-07-13 2025-02-18 国立大学法人富山大学 Nr4a1拮抗薬を用いた鎮痛薬
CN112279834B (zh) * 2020-12-29 2021-04-09 北京鑫开元医药科技有限公司 一种fgfr4抑制剂、制备方法、药物组合物及其应用
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
CN115260164B (zh) * 2021-05-01 2024-03-26 杭州星鳌生物科技有限公司 新型4(3h)-喹唑啉酮类似物的制备方法、结构组成及其在抗肿瘤药物中的应用
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR102862736B1 (ko) 2022-12-07 2025-09-22 부산대학교 산학협력단 신규 2-((트랜스-4-(4-아릴옥시)사이클로헥실)아미노)퀴나졸리논 유도체 및 이의 제조방법

Family Cites Families (104)

* 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
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
AU742739B2 (en) 1997-05-28 2002-01-10 Aventis Pharmaceuticals Inc. Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56 lck 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
JP2002534512A (ja) 1999-01-15 2002-10-15 ノボ ノルディスク アクティーゼルスカブ 非ペプチドglp−1アゴニスト
KR20020027649A (ko) 1999-09-15 2002-04-13 로즈 암스트롱, 크리스틴 에이. 트러트웨인 카이나제 억제제로서의 프테리딘온
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
ES2295441T3 (es) 2001-12-18 2008-04-16 MERCK & CO., INC. Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato.
KR101029281B1 (ko) 2001-12-24 2011-04-18 아스트라제네카 아베 오로라 키나제의 억제제로서 치환된 퀴나졸린 유도체
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
US20040097725A1 (en) 2002-07-10 2004-05-20 Norman Herron Charge transport compositions and electronic devices made with such compositions
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
BR0315053A (pt) 2002-10-03 2005-08-09 Targegen Inc Agentes vasculostáticos , composição, artigo e processo de preparação dos mesmos
AR043059A1 (es) 2002-11-12 2005-07-13 Bayer Pharmaceuticals Corp Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
EP1620413A2 (en) 2003-04-30 2006-02-01 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
DE10323345A1 (de) 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
ME00541B (me) 2003-05-23 2011-10-10 Zentaris Gmbh NOVI PIRIDOPIRAZINI I NJlUHOVA UPOTREBA KAO MODULATORA KlNAZA
WO2005007099A2 (en) 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
AU2004259000A1 (en) 2003-07-21 2005-02-03 Bethesda Pharmaceuticals, Inc. Design and synthesis of optimized ligands for PPAR
TWI347940B (en) 2003-11-07 2011-09-01 Novartis Ag Methods for synthesizing quinolinone compounds
AU2004295058B9 (en) 2003-11-20 2011-06-30 Janssen Pharmaceutica N.V. 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors
BRPI0416853A (pt) 2003-11-24 2007-02-13 Hoffmann La Roche pirazolila e imidazolila pirimidinas
NZ547696A (en) 2003-12-23 2009-12-24 Astex Therapeutics Ltd Pyrazole derivatives as protein kinase modulators
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
MX2007002434A (es) * 2004-08-31 2007-05-04 Astrazeneca Ab Derivados de quinazolinona y su uso como inhibidores de b-raf.
WO2006066361A1 (en) 2004-12-24 2006-06-29 The University Of Queensland Method of treatment or prophylaxis
EP1848704A4 (en) 2005-02-14 2011-05-11 Bionomics Ltd Novel tubulin polymerisation inhibitors
WO2006092430A1 (de) 2005-03-03 2006-09-08 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
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
AU2006313701B2 (en) 2005-11-11 2012-05-31 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
HUE030390T2 (en) 2005-12-21 2017-05-29 Janssen Pharmaceutica Nv Triazolopyridazines as tyrosine kinase modulators
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
US20100016293A1 (en) 2006-07-03 2010-01-21 Rogier Adriaan Smits Quinazolines and Related Heterocyclic Compounds, 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
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
WO2008079988A2 (en) 2006-12-22 2008-07-03 Novartis Ag Quinazolines for pdk1 inhibition
EP2114941B1 (en) 2006-12-22 2015-03-25 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
PE20090288A1 (es) 2007-05-10 2009-04-03 Smithkline Beecham Corp Derivados de quinoxalina como inhibidores de la pi3 quinasa
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
EP2154965A4 (en) 2007-05-29 2011-08-17 Glaxosmithkline Llc 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
WO2008156142A1 (ja) * 2007-06-20 2008-12-24 Mitsubishi Tanabe Pharma Corporation 新規なマロン酸スルホンアミド誘導体およびその医薬用途
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
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
MX2010005300A (es) 2007-11-16 2010-06-25 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas y 4-pirazolil-n-heteroarilpir imidin-2-aminas como inhibidores de cinasas janus.
JP5351254B2 (ja) 2008-05-23 2013-11-27 ノバルティス アーゲー キノキサリン−およびキノリン−カルボキシアミド誘導体
WO2010059771A1 (en) 2008-11-20 2010-05-27 Osi Pharmaceuticals, Inc. Substituted pyrrolo[2,3-b]-pyridines and-pyrazines
CA2750047A1 (en) 2009-01-21 2010-07-29 Basilea Pharmaceutica Ag Novel 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
FI2440546T3 (fi) 2009-06-12 2023-03-30 Abivax Ennenaikaisen vanhenemisen ja erityisesti progerian hoitamiseen hyödyllisiä yhdisteitä
EA021275B9 (ru) 2009-09-03 2015-08-31 Байоэнердженикс Гетероциклические соединения, содержащая их фармацевтическая композиция и их применение для лечения pask-опосредованного заболевания
JP5728683B2 (ja) 2009-09-04 2015-06-03 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン
EP2332939A1 (en) 2009-11-26 2011-06-15 Æterna Zentaris GmbH Novel Naphthyridine derivatives and the use thereof as kinase inhibitors
JP6155187B2 (ja) 2010-03-30 2017-06-28 ヴァーセオン コーポレイション トロンビンの阻害剤としての多置換芳香族化合物
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
US9096590B2 (en) 2010-05-24 2015-08-04 Intellikine Llc Substituted benzoxazoles as PI3 kinase inhibitors
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
CA2825605C (en) 2011-01-31 2019-05-07 Novartis Ag Heterocyclic derivatives
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
CN107245056A (zh) 2011-08-26 2017-10-13 润新生物公司 化学实体、组合物及方法
EP2755657B1 (en) 2011-09-14 2017-11-29 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9249110B2 (en) 2011-09-21 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
AU2012318580A1 (en) 2011-10-04 2014-05-22 Gilead Calistoga Llc Novel quinoxaline inhibitors of PI3K
PH12014500912A1 (en) 2011-10-28 2014-06-09 Novartis Ag Novel purine derivatives and their use in the treatment of disease
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
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
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
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
AU2015238305B2 (en) 2014-03-26 2020-06-18 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
MA39784B1 (fr) 2014-03-26 2021-03-31 Astex Therapeutics Ltd Combinaisons des inhibiteurs du fgfr et du cmet destinées au traitement du cancer
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JO3695B1 (ar) 2015-02-10 2020-08-27 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n- (3.5- ثنائي ميثوكسي فينيل)-n-(1-ميثيل إيثيل)-n- 3-( ميثيل-h1-بيرازول-4-يل) كينوكسالين-6-يل) إيثان- 1.2-ثنائي الأمين)

Also Published As

Publication number Publication date
RU2015150417A (ru) 2017-06-06
DK2989092T3 (da) 2017-11-13
BR112015026830A2 (pt) 2017-07-25
MX2015014471A (es) 2016-06-28
GB201307577D0 (en) 2013-06-12
AU2014259151A1 (en) 2015-11-26
KR102341202B1 (ko) 2021-12-20
BR112015026830A8 (pt) 2019-12-24
WO2014174307A1 (en) 2014-10-30
EP2989092B1 (en) 2017-08-30
CA2910142A1 (en) 2014-10-30
RU2015150417A3 (es) 2018-03-29
US9493426B2 (en) 2016-11-15
AU2014259151B2 (en) 2018-03-15
US20160075666A1 (en) 2016-03-17
RU2701517C2 (ru) 2019-09-27
CN105324378A (zh) 2016-02-10
EP2989092A1 (en) 2016-03-02
CN105324378B (zh) 2017-10-24
KR20160003035A (ko) 2016-01-08
JP2016521276A (ja) 2016-07-21
ES2650312T3 (es) 2018-01-17
BR112015026830B1 (pt) 2022-11-16
CA2910142C (en) 2021-08-10
JP6419784B2 (ja) 2018-11-07

Similar Documents

Publication Publication Date Title
MX2015014471A (es) Derivados de quinazolinona utiles como moduladores de cinasa del receptor del factor de crecimiento del fibroblasto (fgfr).
PH12020550901A1 (en) Macrocyclic compounds for treating disease
CA2999253C (en) Heterocyclic compounds and uses thereof
MX2022001755A (es) Compuestos de dinucleotidos ciclicos y metodos de uso.
PH12014501542B1 (en) Substituted pyrrolidine -2- carboxamides
MX2019001125A (es) Inhibidores de cinasa macrociclica.
PH12016500024A1 (en) Bromodomain inhibitor
WO2014194254A9 (en) Treatment of cancers using pi3 kinase isoform modulators
MX2015011984A (es) Inhibidores de bromodominio de dihidro-pirrolopiridinona.
HK1223911A1 (zh) 磷脂醯肌醇3-激酶抑制剂
HK1217292A1 (zh) 基於k- ras的突变状态治疗癌症的方法
WO2015010078A3 (en) Substituted 6,5-fused bicyclic heteroaryl compounds
MX362215B (es) Derivados 2-aminopirido-[4,3-d]pirimidin-5-ona y su uso como inhibidores de wee-1.
HK1217294A1 (zh) 4'-氟-2'-甲基取代的核苷衍生物
MY197626A (en) Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
PH12018501084B1 (en) Heterocyclic compounds as immunomodulators
GEP20156318B (en) Heteroaryl derivatives as alpha7 nachr modulators
MX368903B (es) Compuestos terapéuticos y sus usos en el tratamiento de enfermedades proliferativas.
NZ717825A (en) Hemisulfate salt of 5,10-methylene-(6r)-tetrahydrofolic acid
AU2017269673A1 (en) Pyridine dicarboxamide derivatives as bromodomain inhibitors
SG10201900541QA (en) Derivatives of xanthone compounds
WO2014194053A3 (en) Carbohydrate compounds for nutritional and therapeutic use
CY1121238T1 (el) Παραγωγα παντοθενικου για την αντιμετωπιση νευρολογικων διαταραχων
ZA201808562B (en) Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer
CA3010771A1 (en) Combination therapy with an iron compound and a citrate compound

Legal Events

Date Code Title Description
FG Grant or registration