CY1121882T1 - Αναστολεις πυραζολυλο κινοξαλινο κινασης - Google Patents

Αναστολεις πυραζολυλο κινοξαλινο κινασης

Info

Publication number
CY1121882T1
CY1121882T1 CY20191100858T CY191100858T CY1121882T1 CY 1121882 T1 CY1121882 T1 CY 1121882T1 CY 20191100858 T CY20191100858 T CY 20191100858T CY 191100858 T CY191100858 T CY 191100858T CY 1121882 T1 CY1121882 T1 CY 1121882T1
Authority
CY
Cyprus
Prior art keywords
kinase inhibitors
compounds
pyrazolyl
quinoxaline kinase
pyrazolyl quinoxaline
Prior art date
Application number
CY20191100858T
Other languages
English (en)
Inventor
Christopher William Murray
Valerio Berdini
Gilbert Ebai Besong
Christopher Charles Frederick Hamlett
Christopher Norbert Johnson
Steven John Woodhead
Michael Reader
David Charles Rees
Patrick René Angibaud
Eddy Jean Edgard Freyne
Tom Cornelis Hortense Govaerts
Johan Erwin Edmond Weerts
Timothy Pietro Suren Perera
Ronaldus Arnodus Hendrika Joseph Gilissen
Berthold Wroblowski
Jean Fernand Armand Lacrampe
Alexandra Papanikos
Olivier Alexis Georges Querolle
Elisabeth Thérèse Jeanne PASQUIER
Isabelle Noëlle Constance PILATTE
Pascal Ghislain André BONNET
Werner Constant Johan Embrechts
Rhalid Akkari
Lieven Meerpoel
Gordon Saxty
Laurence Anne Mevellec
Original Assignee
Astex Therapeutics Limited
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 Limited filed Critical Astex Therapeutics Limited
Publication of CY1121882T1 publication Critical patent/CY1121882T1/el

Links

Classifications

    • 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
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D403/14Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6524Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Otolaryngology (AREA)

Abstract

Η εφεύρεση αναφέρεται σε νέες ενώσεις παραγώγων κινοξαλίνης, σε φαρμακευτικές συνθέσεις που περιλαμβάνουν τις εν λόγω ενώσεις, σε μεθόδους για την παρασκευή των αναφερθεισών ενώσεων και στη χρήση των αναφερθεισών ενώσεων στη θεραπεία νόσων, π.χ. του καρκίνου.
CY20191100858T 2010-04-30 2019-08-09 Αναστολεις πυραζολυλο κινοξαλινο κινασης CY1121882T1 (el)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US32988410P 2010-04-30 2010-04-30
GB201007286A GB201007286D0 (en) 2010-04-30 2010-04-30 New compounds
PCT/GB2011/050851 WO2011135376A1 (en) 2010-04-30 2011-04-28 Pyrazolyl quinazoline kinase inhibitors
EP11724710.6A EP2563775B1 (en) 2010-04-30 2011-04-28 Pyrazolyl quinoxaline kinase inhibitors

Publications (1)

Publication Number Publication Date
CY1121882T1 true CY1121882T1 (el) 2020-10-14

Family

ID=42289929

Family Applications (2)

Application Number Title Priority Date Filing Date
CY20191100858T CY1121882T1 (el) 2010-04-30 2019-08-09 Αναστολεις πυραζολυλο κινοξαλινο κινασης
CY20211101014T CY1124928T1 (el) 2010-04-30 2021-11-23 Αναστολεις πυραζολυλο κινοξαλινο κινασης

Family Applications After (1)

Application Number Title Priority Date Filing Date
CY20211101014T CY1124928T1 (el) 2010-04-30 2021-11-23 Αναστολεις πυραζολυλο κινοξαλινο κινασης

Country Status (35)

Country Link
US (6) US8895601B2 (el)
EP (3) EP3590934B1 (el)
JP (1) JP5639261B2 (el)
KR (2) KR101933843B1 (el)
CN (2) CN102858765B (el)
AP (1) AP3210A (el)
AR (1) AR080982A1 (el)
AU (2) AU2011247047B2 (el)
BR (1) BR112012027509B1 (el)
CA (1) CA2796204C (el)
CL (1) CL2012003048A1 (el)
CR (2) CR20180339A (el)
CY (2) CY1121882T1 (el)
DK (3) DK2563775T3 (el)
EA (2) EA028599B1 (el)
EC (1) ECSP12012318A (el)
ES (3) ES2899937T3 (el)
GB (1) GB201007286D0 (el)
HR (1) HRP20211675T1 (el)
HU (3) HUE033702T2 (el)
IL (1) IL222600A (el)
IN (1) IN2012MN02591A (el)
JO (1) JO3366B1 (el)
LT (3) LT3590934T (el)
ME (1) ME01825B (el)
MX (2) MX365702B (el)
MY (2) MY189427A (el)
NZ (1) NZ602726A (el)
PL (3) PL3590934T3 (el)
PT (3) PT3178818T (el)
RS (3) RS62570B1 (el)
SG (2) SG184966A1 (el)
SI (3) SI2563775T1 (el)
TW (1) TWI545122B (el)
WO (1) WO2011135376A1 (el)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2009008099A (es) 2007-02-01 2009-12-14 Resverlogix Corp Compuestos para la prevencion y tratamiento de enfermedades cardiovasculares.
US9238640B2 (en) 2009-03-18 2016-01-19 Resverlogix Corp. Anti-inflammatory agents
BRPI1014956B8 (pt) 2009-04-22 2021-05-25 Resverlogix Corp agentes anti-inflamatórios
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
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
GB201118654D0 (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
ME02651B (me) 2012-06-13 2017-06-20 Incyte Holdings Corp Substituisana triciklična jedinjenja kao inhibitori fgfr
WO2014011900A2 (en) 2012-07-11 2014-01-16 Blueprint Medicines Inhibitors of the fibroblast growth factor receptor
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
PT2906531T (pt) * 2012-10-15 2018-02-06 Resverlogix Corp Compostos úteis na síntese de compostos de benzamida
WO2014071358A2 (en) 2012-11-05 2014-05-08 Foundation Medicine, Inc. Novel ntrk1 fusion molecules and uses thereof
US9719970B2 (en) 2012-11-30 2017-08-01 Waters Technologies Corporation Methods and apparatus for the analysis of vitamin D metabolites
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
PE20151776A1 (es) * 2013-03-15 2015-12-11 Celgene Avilomics Res Inc Compuestos de heteroarilo y sus usos
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
US9321786B2 (en) 2013-03-15 2016-04-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CA2909207C (en) 2013-04-19 2021-11-02 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GB201307577D0 (en) * 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
CN104163794A (zh) * 2013-10-17 2014-11-26 中国药科大学 2-氨基芳环类血管内皮生长因子受体(vegfr)抑制剂及其制备方法和用途
AU2014339972B9 (en) 2013-10-25 2019-05-30 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
JO3512B1 (ar) * 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
CN105017227B (zh) * 2014-07-08 2018-03-09 四川百利药业有限责任公司 N‑(1h‑吡唑‑5‑基)喹唑啉‑4‑胺类化合物
ES2914072T3 (es) 2014-08-18 2022-06-07 Eisai R&D Man Co Ltd Sal de derivado de piridina monocíclico y su cristal
HRP20220496T1 (hr) * 2014-09-26 2022-05-27 Janssen Pharmaceutica Nv Uporaba fgfr mutantnih genskih panela kod identifikacije pacijenata s rakom koji će reagirati na liječenje s inhibitorom fgfr
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
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
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
JP6903585B2 (ja) 2015-03-13 2021-07-14 レスバーロジックス コーポレイション 補体関連疾患の治療のための組成物および治療方法
TWI703984B (zh) * 2015-04-03 2020-09-11 英商阿斯特克斯治療有限公司 用於癌症治療之fgfr/pd-1組合療法
US10478494B2 (en) * 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
ES2811845T3 (es) 2015-09-23 2021-03-15 Janssen Pharmaceutica Nv Heterociclos tricíclicos para el tratamiento del cáncer
BR112018005625B1 (pt) * 2015-09-23 2023-11-14 Janssen Pharmaceutica N.V Compostos derivados de quinolina, piridopirazina, naftiridina e quinazolinona, composições farmacêuticas que os compreende e uso dos mesmos
CN105596330B (zh) * 2015-12-11 2018-10-16 深圳市坤健创新药物研究院 虚拟筛选化合物在制备激酶抑制剂中的应用和药物
CN107459519A (zh) 2016-06-06 2017-12-12 上海艾力斯医药科技有限公司 稠合嘧啶哌啶环衍生物及其制备方法和应用
US20190192522A1 (en) 2016-09-08 2019-06-27 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor 4 in combination with cyclin-dependent kinase inhibitors
WO2018071348A1 (en) * 2016-10-10 2018-04-19 Development Center For Biotechnology Quinoxaline compounds as type iii receptor tyrosine kinase inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JOP20190280A1 (ar) * 2017-06-02 2019-12-02 Janssen Pharmaceutica Nv مثبطات fgfr2 لعلاج سرطان الأوعية الصفراوية
JP7399846B2 (ja) 2017-08-21 2023-12-18 セルジーン コーポレイション (s)-tert-ブチル4,5-ジアミノ-5-オキソペンタノエートの調製プロセス
US11661411B2 (en) 2017-12-01 2023-05-30 Board Of Regents Of The University Of Nebraska Quinoxaline compounds and uses thereof
CN111712245A (zh) 2018-03-28 2020-09-25 卫材R&D管理有限公司 用于肝细胞癌的治疗剂
JP7491510B2 (ja) * 2018-04-26 2024-05-28 メディシナル バイオコンバージェンス リサーチ センター mTOR阻害剤としての新規化合物及びその用途
WO2019213544A2 (en) 2018-05-04 2019-11-07 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
JP2022501355A (ja) 2018-09-21 2022-01-06 ヤンセン ファーマシューティカ エヌ.ベー. 胆管癌の処置
EP3898615A1 (en) * 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
CN113645974A (zh) 2019-03-29 2021-11-12 詹森药业有限公司 用于治疗尿路上皮癌的fgfr酪氨酸激酶抑制剂
JP2022527482A (ja) 2019-03-29 2022-06-02 ヤンセン ファーマシューティカ エヌ.ベー. 尿路上皮癌の治療のためのfgfrチロシンキナーゼ阻害剤
WO2020208592A1 (en) * 2019-04-12 2020-10-15 Dr. Reddy’S Laboratories Limited Process for preparation of erdafitinib, its purification and amorphous solid dispersion
CN111909044A (zh) * 2019-05-09 2020-11-10 南京爱德程医药科技有限公司 2-(烷基氨基)乙基苯甲酸酯类化合物的合成方法
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI759829B (zh) * 2019-08-23 2022-04-01 財團法人生物技術開發中心 作為第iii型受體酪胺酸激酶抑制劑之雜環吡唑衍生物
WO2021058798A1 (en) 2019-09-26 2021-04-01 Janssen Pharmaceutica Nv Use of fgfr inhibitors in fgfr-genetically altered cancers to enhance patient response to immune checkpoint inhibitors in sequential treatment settings
JOP20220083A1 (ar) 2019-10-14 2023-01-30 Incyte Corp حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN110790677B (zh) * 2019-11-05 2022-04-29 浙江工业大学 一种金刚烷甲酰胺类化合物及其制备方法和应用
JP2023505258A (ja) 2019-12-04 2023-02-08 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
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CN113024518A (zh) * 2019-12-09 2021-06-25 武汉九州钰民医药科技有限公司 一种厄达替尼的制备方法
CN113024517A (zh) * 2019-12-09 2021-06-25 武汉九州钰民医药科技有限公司 一种制备厄达替尼的方法
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021146163A1 (en) * 2020-01-17 2021-07-22 Beta Pharma, Inc. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors
TW202140012A (zh) 2020-02-12 2021-11-01 比利時商健生藥品公司 用於治療尿路上皮癌的fgfr酪胺酸激酶抑制劑和抗pd1藥劑
CN115103678A (zh) 2020-02-12 2022-09-23 詹森药业有限公司 用于治疗高风险非肌层浸润性膀胱癌的fgfr酪氨酸激酶抑制剂
US20240010632A1 (en) 2020-08-17 2024-01-11 Teva Pharmaceuticals International Gmbh Solid state forms of erdafitinib salts and processes for preparation of erdafitinib
CN112920167B (zh) * 2020-08-19 2022-08-26 四川大学华西医院 靶向fgfr和hdac的双靶点抑制剂及其制备方法和应用、药物组合物及药剂
EP4210702A1 (en) 2020-09-14 2023-07-19 JANSSEN Pharmaceutica NV Fgfr inhibitor combination therapies
AU2022277796A1 (en) 2021-05-19 2024-01-18 Janssen Pharmaceutica Nv Fgfr tyrosine kinase inhibitors for the treatment of advanced solid tumors
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
WO2022271612A1 (en) 2021-06-22 2022-12-29 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
TW202333720A (zh) 2021-10-12 2023-09-01 美商塔里斯生物醫學有限責任公司 用於膀胱內施用的厄達替尼調配物及系統
WO2023081923A1 (en) 2021-11-08 2023-05-11 Frequency Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
TW202400174A (zh) * 2022-02-18 2024-01-01 美商塔里斯生物醫學有限責任公司 用於膀胱內施用的Erdafitinib調配物及滲透系統
CN115108926B (zh) * 2022-04-02 2023-06-20 上海工程技术大学 一种用于制备厄达替尼的中间体化合物及制备方法

Family Cites Families (128)

* 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
WO1994026723A2 (en) 1993-05-14 1994-11-24 Genentech, Inc. 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
EP1001945B1 (en) 1997-05-28 2011-03-02 Aventis Pharmaceuticals Inc. QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p56lck TYROSINE KINASES
US6235740B1 (en) 1997-08-25 2001-05-22 Bristol-Myers Squibb Co. Imidazoquinoxaline protein tyrosine kinase inhibitors
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
WO2000042026A1 (en) 1999-01-15 2000-07-20 Novo Nordisk A/S Non-peptide glp-1 agonists
AP2002002479A0 (en) 1999-09-15 2002-06-30 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
ES2295441T3 (es) 2001-12-18 2008-04-16 MERCK & CO., INC. Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato.
MXPA04006260A (es) 2001-12-24 2005-03-31 Astrazeneca Ab Derivados de quinazolina sustituidos como inhibidores de cinasas aurora.
JP2003213463A (ja) 2002-01-17 2003-07-30 Sumitomo Chem Co Ltd 金属腐食防止剤および洗浄液
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
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
KR20110050745A (ko) 2002-10-03 2011-05-16 탈자진 인코포레이티드 혈관항상성 유지제 및 그의 사용 방법
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
EP1590341B1 (en) 2003-01-17 2009-06-17 Warner-Lambert Company LLC 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
WO2004110350A2 (en) 2003-05-14 2004-12-23 Torreypines Therapeutics, Inc. Compouds and uses thereof in modulating amyloid beta
MXPA05012645A (es) 2003-05-23 2006-02-08 Zentaris Gmbh Piridopirazinas novedosas y su uso como moduladores de cinasa.
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
US7511145B2 (en) 2003-08-01 2009-03-31 Genelabs Technologies, Inc. Bicyclic heteroaryl derivatives
AU2004283479A1 (en) 2003-10-17 2005-05-06 4 Aza Bioscience Nv Heterocycle-substituted pteridine derivatives and their use in therapy
EP2762475A1 (en) 2003-11-07 2014-08-06 Novartis Vaccines and Diagnostics, Inc. Pharmaceutically acceptable salts of quinolinone compounds and their medical use
SG150533A1 (en) 2003-11-20 2009-03-30 Janssen Pharmaceutica Nv 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2- quinoxalinones as poly(adp-ribose) polymerase inhibitors
JP2007512275A (ja) 2003-11-24 2007-05-17 エフ.ホフマン−ラ ロシュ アーゲー ピラゾリルおよびイミダゾリルピリミジン
AU2004303602C1 (en) 2003-12-23 2009-05-28 Astex Therapeutics Limited 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
CN101048388A (zh) 2004-08-31 2007-10-03 阿斯利康(瑞典)有限公司 喹唑啉酮衍生物及其作为B-Raf抑制剂的用途
KR100875408B1 (ko) 2004-10-14 2008-12-23 에프. 호프만-라 로슈 아게 Cdk1 항증식성 활성을 갖는 1,5-나프티리딘 아졸리디논
JP2008516939A (ja) 2004-10-15 2008-05-22 アストラゼネカ アクチボラグ 化学化合物
ES2425567T3 (es) 2004-12-24 2013-10-16 Spinifex Pharmaceuticals Pty Ltd Método de tratamiento o profilaxis
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
EP1881986A2 (en) 2005-05-12 2008-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1881981A1 (en) 2005-05-18 2008-01-30 Wyeth 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of tpl2 kinase and methods of making and using the same
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
NZ565749A (en) 2005-08-26 2010-12-24 Serono Lab Pyrazine derivatives and use as PI3K inhibitors
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
CA2628039A1 (en) 2005-11-11 2007-05-18 Aeterna Zentaris Gmbh Novel 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
RS55630B1 (sr) 2005-12-21 2017-06-30 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
WO2007125405A2 (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
EP2029600B1 (de) 2006-05-24 2012-03-14 Boehringer Ingelheim International GmbH Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
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
EP2081928B1 (en) 2006-11-10 2014-02-26 Bristol-Myers Squibb Company Pyrrolo-pyridine kinase inhibitors
JP2008127446A (ja) 2006-11-20 2008-06-05 Canon Inc 1,5−ナフチリジン化合物及び有機発光素子
CN102123712B (zh) 2006-12-13 2014-03-19 默沙东公司 使用igf1r抑制剂治疗癌症的方法
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
US8895745B2 (en) * 2006-12-22 2014-11-25 Astex Therapeutics Limited Bicyclic heterocyclic compounds as FGFR inhibitors
JP2010514693A (ja) 2006-12-22 2010-05-06 ノバルティス アーゲー Pdk1阻害のためのキナゾリン
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
JP2010526823A (ja) * 2007-05-10 2010-08-05 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キナーゼ阻害物質としてのキノキサリン誘導体
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
KR101251933B1 (ko) 2007-06-20 2013-04-09 미쓰비시 타나베 파마 코퍼레이션 신규한 말론산술폰아미드 유도체 및 그 의약 용도
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
EP2173338A1 (en) 2007-07-06 2010-04-14 OSI Pharmaceuticals, Inc. Combination anti-cancer therapy
AR068054A1 (es) 2007-08-08 2009-11-04 Smithkline Beecham Corp Compuestos de pirrolopirimidina
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
WO2009021083A1 (en) * 2007-08-09 2009-02-12 Smithkline Beecham Corporation Quinoxaline derivatives as pi3 kinase inhibitors
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
BRPI0820544A2 (pt) 2007-11-16 2015-06-16 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase
EP2282739A2 (en) 2008-05-05 2011-02-16 Schering Corporation Sequential administration of chemotherapeutic agents for treatment of cancer
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
EP2356116A1 (en) 2008-11-20 2011-08-17 OSI Pharmaceuticals, Inc. Substituted pyrroloý2,3-b¨-pyridines and-pyrazines
AU2010206161B2 (en) 2009-01-21 2014-08-07 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
HUE061262T2 (hu) 2009-06-12 2023-05-28 Abivax Splicing mechanizmust gátló új kémiai molekulák splicing hibákból betegségek kezelésére
DK2473504T3 (en) 2009-09-03 2015-03-16 Bioenergenix Heterocyclic Compounds for Inhibition of Passover
EP2473498A1 (en) 2009-09-04 2012-07-11 Bayer Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
US20110123545A1 (en) 2009-11-24 2011-05-26 Bristol-Myers Squibb Company Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases
EP2332939A1 (en) 2009-11-26 2011-06-15 Æterna Zentaris GmbH Novel Naphthyridine derivatives and the use thereof as kinase inhibitors
EP2560966B1 (en) 2010-03-30 2021-01-06 Verseon International Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
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
UY33883A (es) 2011-01-31 2012-08-31 Novartis Ag Novedosos derivados heterocíclicos
JP2014510265A (ja) 2011-02-02 2014-04-24 アムジェン インコーポレイテッド Igf−1rの阻害に関する方法および組成物
WO2012148540A1 (en) 2011-02-23 2012-11-01 Intellikine, Llc Combination of kanase inhibitors and uses threof
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
WO2012149014A1 (en) 2011-04-25 2012-11-01 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
JP6002223B2 (ja) 2011-08-26 2016-10-05 ニューファーマ, インコーポレイテッド 特定の化学的実体、組成物、および方法
CN115403531A (zh) 2011-09-14 2022-11-29 润新生物公司 作为激酶抑制剂的化学实体、组合物及方法
WO2013043935A1 (en) 2011-09-21 2013-03-28 Neupharma, Inc. Certain chemical entites, compositions, and methods
WO2013052699A2 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118652D0 (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
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
WO2013061305A1 (en) 2011-10-28 2013-05-02 Novartis Ag Novel purine derivatives and their use in the treatment of disease
GB201118654D0 (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.
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
WO2014113729A2 (en) 2013-01-18 2014-07-24 Foundation Mecicine, Inc. Methods of treating cholangiocarcinoma
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP3027623A4 (en) 2013-08-02 2017-03-01 Ignyta, Inc. METHODS OF TREATING VARIOUS CANCERS USING AN AXL/cMET INHIBITOR ALONE OR IN COMBINATION WITH OTHER AGENTS
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
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
KR20170137717A (ko) 2015-02-19 2017-12-13 바이오클린 테라퓨틱스, 인크. 암의 치료를 위한 방법, 조성물, 및 키트
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
US20150105368A1 (en) 2015-04-16
LT3178818T (lt) 2019-08-12
EP3590934A1 (en) 2020-01-08
US10519137B2 (en) 2019-12-31
CL2012003048A1 (es) 2013-04-19
US20220135544A1 (en) 2022-05-05
EP2563775A1 (en) 2013-03-06
ME01825B (me) 2014-12-20
JO3366B1 (ar) 2019-03-13
EA023222B8 (ru) 2017-04-28
ECSP12012318A (es) 2013-02-28
AU2011247047B2 (en) 2017-01-19
EA201291143A1 (ru) 2013-05-30
ES2899937T3 (es) 2022-03-15
EP3178818A1 (en) 2017-06-14
TWI545122B (zh) 2016-08-11
EA028599B1 (ru) 2017-12-29
IL222600A0 (en) 2012-12-31
CR20120576A (es) 2013-03-04
WO2011135376A1 (en) 2011-11-03
PT3178818T (pt) 2019-09-05
EA201500278A1 (ru) 2015-09-30
GB201007286D0 (en) 2010-06-16
JP5639261B2 (ja) 2014-12-10
CA2796204C (en) 2020-08-25
US9850228B2 (en) 2017-12-26
CN104725362A (zh) 2015-06-24
SI2563775T1 (sl) 2017-05-31
AU2017202512A1 (en) 2017-05-04
TW201204714A (en) 2012-02-01
BR112012027509A8 (pt) 2021-11-03
IL222600A (en) 2016-02-29
DK2563775T3 (en) 2017-03-27
EA023222B1 (ru) 2016-05-31
PT3590934T (pt) 2021-11-25
LT3590934T (lt) 2021-12-27
LT2563775T (lt) 2017-04-10
RS55863B1 (sr) 2017-08-31
CA2796204A1 (en) 2011-11-03
HUE033702T2 (en) 2017-12-28
PL3590934T3 (pl) 2022-02-07
US9464071B2 (en) 2016-10-11
AP2012006490A0 (en) 2012-10-31
HRP20211675T1 (hr) 2022-02-18
PL2563775T3 (pl) 2017-07-31
ES2621461T3 (es) 2017-07-04
CN102858765B (zh) 2015-04-01
EP3590934B1 (en) 2021-08-25
PT2563775T (pt) 2017-04-18
RS59196B1 (sr) 2019-10-31
US20130072457A1 (en) 2013-03-21
HUE045893T2 (hu) 2020-01-28
CR20180339A (es) 2018-11-12
KR101889565B1 (ko) 2018-08-17
US20180127397A1 (en) 2018-05-10
NZ602726A (en) 2014-05-30
KR20130108076A (ko) 2013-10-02
JP2013528580A (ja) 2013-07-11
AU2011247047A1 (en) 2013-01-10
EP3178818B1 (en) 2019-05-22
EP2563775B1 (en) 2017-01-04
AU2017202512B2 (en) 2018-07-26
BR112012027509B1 (pt) 2022-07-05
HUE056999T2 (hu) 2022-04-28
AR080982A1 (es) 2012-05-23
AP3210A (en) 2015-04-30
KR20180093134A (ko) 2018-08-20
SG10201708578QA (en) 2017-11-29
SI3590934T1 (sl) 2022-03-31
US8895601B2 (en) 2014-11-25
MY191669A (en) 2022-07-06
CN102858765A (zh) 2013-01-02
MX2012012414A (es) 2013-02-26
SI3178818T1 (sl) 2019-09-30
IN2012MN02591A (el) 2015-06-12
KR101933843B1 (ko) 2018-12-28
MX365702B (es) 2019-06-11
PL3178818T3 (pl) 2019-11-29
US20200131153A1 (en) 2020-04-30
CY1124928T1 (el) 2023-01-05
RS62570B1 (sr) 2021-12-31
ES2742409T3 (es) 2020-02-14
CN104725362B (zh) 2017-04-12
US20160311800A1 (en) 2016-10-27
MY189427A (en) 2022-02-11
DK3590934T3 (da) 2021-11-08
SG184966A1 (en) 2012-11-29
DK3178818T3 (da) 2019-07-22
BR112012027509A2 (pt) 2017-08-08

Similar Documents

Publication Publication Date Title
CY1124928T1 (el) Αναστολεις πυραζολυλο κινοξαλινο κινασης
CY1124436T1 (el) Δικυκλικες ετεροκυκλικες ενωσεις και χρησεις αυτων στη θεραπεια
CY1124311T1 (el) Παρεμποδιστες dna-pk
CY1120318T1 (el) Υποκατεστημενες βενζυλινδαζολες για χρηση ως αναστολεις κινασης bub1 στη θεραπευτικη αντιμετωπιση υπερπολλαπλασιαστικων ασθενειων
CY1122966T1 (el) 5-βρωμο-2,6-δι-(1η-πυραζολ-1-υλ)πυριμιδιν-4-αμινη για χρηση στη θεραπευτικη αγωγη καρκινου
CY1121170T1 (el) Νεες ενωσεις ως ρυθμιστες πρωτεϊνικων κινασων
CY1124068T1 (el) Στερεες μορφες ενος εκλεκτικου αναστολεα cdk4/6
CY1124729T1 (el) Φαρμακοτεχνικες μορφες του ενζαλουταμιδιου
CY1125436T1 (el) Αναστολεις dna-pk
CY1124307T1 (el) Φαρμακευτικη συνθεση, μεθοδοι θεραπειας και χρησεις αυτων
CY1121793T1 (el) Εκλεκτικοι αναστολεις pi3k δελτα
CY1122186T1 (el) Μεθοδοι θεραπειας καρκινου
CY1122786T1 (el) Δοσολογικα σχηματα για ενωσεις κατηγοριας εχινοκανδινης
CY1122247T1 (el) Αγωγη καρκινων με τη χρηση τροποποιητων ισομορφης κινασης ρι3
CY1120939T1 (el) Συνδυασμος ρεγοραφενιμπης και ακετυλοσαλικυλικου οξεος για τη θεραπευτικη αντιμετωπιση του ορθοκολικου καρκινου
CY1124000T1 (el) Υποκατεστημενες 5-φθορο-1η-πυραζολοπυριδινες σε κρυσταλλικη μορφη
CY1118379T1 (el) Αναστολεις ιου ηπατιτιδας c
CY1118061T1 (el) Δικυκλικα παραγωγα heterocyclyl σαν καταστολεις κινασης (kinase) fgfr για θεραπευτικη χρηση
CY1122098T1 (el) Παραγωγα ισοχρωμενιου ως αναστολεις κινασων φωσφοϊνοσιτιδης-3
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
EA201600204A1 (ru) Производные хиназолина, фармацевтическая композиция на их основе и их применение для профилактики или лечения опухоли
CY1114988T1 (el) Βενζοδιαζεπινη αναστολεας bromodomain
CY1123490T1 (el) Συνθεσεις που προερχονται απο χιτοζανη
EA201391106A1 (ru) Новые гетероциклические производные
EA201591166A1 (ru) Ингибиторы аутотаксина