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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C07D239/82—Oxygen atoms with an aryl radical attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
GB201118675D0 (en) 2011-10-28 2011-12-14 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
GB201118656D0 (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
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
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
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
EP3200786B1 (en) 2014-10-03 2019-08-28 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
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
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
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
ES2904513T3 (es) * 2015-09-23 2022-04-05 Janssen Pharmaceutica Nv 1,4-Benzodiazepinas biheteroarilo sustituidas y usos de las mismas para el tratamiento del cáncer
EP3353177B1 (en) * 2015-09-23 2020-06-03 Janssen Pharmaceutica NV Tricyclic heterocycles for the treatment of cancer
CN107793395B (zh) * 2016-09-01 2021-01-05 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂及其用途
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
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
WO2021146424A1 (en) 2020-01-15 2021-07-22 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
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
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
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220155A1 (en) 2021-06-09 2022-12-15 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
EP0951541B1 (en) 1995-07-31 2005-11-30 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
ES2235331T3 (es) 1997-05-28 2005-07-01 Aventis Pharmaceuticals Inc Compuestos quinolina y quinoxalina que inhiben el factor de crecimiento derivado de plaquetas y/o tirosina quinasas p561ck.
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
EP1147094A1 (en) 1999-01-15 2001-10-24 Novo Nordisk A/S Non-peptide glp-1 agonists
CN1373763A (zh) 1999-09-15 2002-10-09 沃尼尔·朗伯公司 作为激酶抑制剂的蝶啶酮
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
RU2323215C2 (ru) 2001-12-24 2008-04-27 Астразенека Аб Замещенные производные хиназолина как ингибиторы ауроракиназы
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
DE602004021558D1 (de) 2003-01-17 2009-07-30 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
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.
DE10323345A1 (de) 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
AU2004240747B2 (en) 2003-05-23 2008-01-03 Zentaris Gmbh Novel pyridopyrazines and use thereof as kinase modulators
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
EP1682529A4 (en) 2003-11-07 2010-06-30 Novartis Vaccines & Diagnostic PROCESS FOR SYNTHESIS OF CHINOLINONE 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
WO2005054231A1 (en) 2003-11-24 2005-06-16 F.Hoffmann-La Roche Ag Pyrazolyl and imidazolyl pyrimidines
US8247576B2 (en) 2003-12-23 2012-08-21 Astex Therapeutics Limited 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
US20090118261A1 (en) * 2004-08-31 2009-05-07 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
CN102049048B (zh) 2004-12-24 2013-12-25 西芬克斯医药有限公司 治疗或预防的方法
CA2597447C (en) 2005-02-14 2014-03-25 Bionomics Limited Novel tubulin polymerisation inhibitors
US9271963B2 (en) 2005-03-03 2016-03-01 Universitat Des Saarlandes Selective inhibitors of human corticosteroid synthases
US20090156617A1 (en) 2005-05-12 2009-06-18 Northrup Alan B Tyrosine kinase inhibitors
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
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
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
RS55630B1 (sr) 2005-12-21 2017-06-30 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
ATE549338T1 (de) 2006-05-24 2012-03-15 Boehringer Ingelheim Int 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
WO2008076278A2 (en) 2006-12-13 2008-06-26 Schering Corporation Methods of cancer treatment with igf1r inhibitors
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US20100216767A1 (en) 2006-12-22 2010-08-26 Mina Aikawa Quinazolines for pdk1 inhibition
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
TW200902008A (en) 2007-05-10 2009-01-16 Smithkline Beecham Corp 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
US20100179143A1 (en) 2007-05-29 2010-07-15 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
BRPI0813105A2 (pt) * 2007-06-20 2015-08-04 Mitsubishi Tanabe Pharma Corp Derivado de sulfonamida de ácido malônico e uso faramacêutico do mesmo
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
JP2010535804A (ja) 2007-08-09 2010-11-25 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害薬としてのキノキサリン誘導体
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
US8309718B2 (en) 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
AU2009248774B2 (en) 2008-05-23 2012-05-31 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
JP2012509342A (ja) 2008-11-20 2012-04-19 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換ピロロ［２，３−ｂ］−ピリジンおよび−ピラジン
CA2750047A1 (en) 2009-01-21 2010-07-29 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
JP2012516847A (ja) 2009-02-02 2012-07-26 メルク・シャープ・エンド・ドーム・コーポレイション Ａｋｔ活性の阻害剤
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
MX353776B (es) 2009-06-12 2018-01-29 Abivax Compuestos utiles para tratar cancer.
ES2534226T3 (es) 2009-09-03 2015-04-20 Bioenergenix Compuestos heterocíclicos para la inhibición de PASK
US9340528B2 (en) 2009-09-04 2016-05-17 Bayer Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
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
US8513421B2 (en) 2010-05-19 2013-08-20 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2011149937A1 (en) 2010-05-24 2011-12-01 Intellikine, Inc. Heterocyclic compounds and uses thereof
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
AU2012213080B2 (en) 2011-01-31 2014-03-27 Novartis Ag Novel heterocyclic derivatives
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
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
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
EP2763994A4 (en) 2011-10-04 2015-08-26 Gilead Calistoga Llc NEW QUINOXALINE INHIBITORS OF THE PI3K PATH
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
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
PH12014500912A1 (en) 2011-10-28 2014-06-09 Novartis Ag Novel purine derivatives and their use in the treatment of disease
GB201118675D0 (en) 2011-10-28 2011-12-14 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
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
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
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

Also Published As

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

Similar Documents

Publication Publication Date Title
MX366166B (es) Derivados de quinazolinona utiles como moduladores de cinasa del receptor del factor de crecimiento del fibroblasto (fgfr).
WO2014096812A3 (en) Interacting toys
PH12020550901A1 (en) Macrocyclic compounds for treating disease
CA2999253C (en) Heterocyclic compounds and uses thereof
PH12014501542A1 (en) Substituted pyrrolidine -2- carboxamides
MX2016002544A (es) Compuestos utiles como inmunomoduladores.
MX2019001125A (es) Inhibidores de cinasa macrociclica.
WO2014194254A8 (en) Treatment of cancers using pi3 kinase isoform modulators
MX367897B (es) Derivados de piridazinona macrociclicos.
MX2015011984A (es) Inhibidores de bromodominio de dihidro-pirrolopiridinona.
MX2015017964A (es) Inhibidores de bromodominio.
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
GEP20156318B (en) Heteroaryl derivatives as alpha7 nachr modulators
MX368903B (es) Compuestos terapéuticos y sus usos en el tratamiento de enfermedades proliferativas.
MX2015011193A (es) Compuestos antivirales.
NZ745811A (en) Hemisulfate salt of 5,10-methylene-(6r)-tetrahydrofolic acid
AU2017269673A1 (en) Pyridine dicarboxamide derivatives as bromodomain inhibitors
HK1217092A1 (zh) 治疗性化合物及其用途
MX2019005855A (es) Formulaciones que se pueden pulverizar.
ZA202301066B (en) Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer
CY1121238T1 (el) Παραγωγα παντοθενικου για την αντιμετωπιση νευρολογικων διαταραχων
CA3010771A1 (en) Combination therapy with an iron compound and a citrate compound
PH12015500399A1 (en) Azaindolines
WO2014194053A3 (en) Carbohydrate compounds for nutritional and therapeutic use

Legal Events

Date Code Title Description
FG Grant or registration