ES2545215T3 - Derivados de imidazo[1,2-a]piridina como inhibidores del FGFR quinasa para uso en terapia - Google Patents
Derivados de imidazo[1,2-a]piridina como inhibidores del FGFR quinasa para uso en terapia Download PDFInfo
- Publication number
- ES2545215T3 ES2545215T3 ES10718660.3T ES10718660T ES2545215T3 ES 2545215 T3 ES2545215 T3 ES 2545215T3 ES 10718660 T ES10718660 T ES 10718660T ES 2545215 T3 ES2545215 T3 ES 2545215T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- compound
- cycloalkyl
- cycloalkenyl
- alkynyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
Links
- 108091008794 FGF receptors Proteins 0.000 title 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 title 1
- 150000005234 imidazo[1,2-a]pyridines Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 71
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract description 16
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract description 14
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract description 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract description 13
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract description 13
- -1 -O- ( CH2) n-ORd Chemical group 0.000 abstract description 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract description 13
- 239000001257 hydrogen Substances 0.000 abstract description 13
- 125000003545 alkoxy group Chemical group 0.000 abstract description 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract description 5
- 125000004438 haloalkoxy group Chemical group 0.000 abstract description 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 6
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 6
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 13
- 210000004027 cell Anatomy 0.000 description 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 9
- 238000000034 method Methods 0.000 description 7
- OZFAFGSSMRRTDW-UHFFFAOYSA-N (2,4-dichlorophenyl) benzenesulfonate Chemical compound ClC1=CC(Cl)=CC=C1OS(=O)(=O)C1=CC=CC=C1 OZFAFGSSMRRTDW-UHFFFAOYSA-N 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- 239000012591 Dulbecco’s Phosphate Buffered Saline Substances 0.000 description 6
- 102000029749 Microtubule Human genes 0.000 description 4
- 108091022875 Microtubule Proteins 0.000 description 4
- 229920004890 Triton X-100 Polymers 0.000 description 4
- 239000013504 Triton X-100 Substances 0.000 description 4
- 210000004688 microtubule Anatomy 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 238000003556 assay Methods 0.000 description 3
- 206010020772 Hypertension Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 230000008034 disappearance Effects 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000011534 incubation Methods 0.000 description 2
- 239000003068 molecular probe Substances 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- PRDFBSVERLRRMY-UHFFFAOYSA-N 2'-(4-ethoxyphenyl)-5-(4-methylpiperazin-1-yl)-2,5'-bibenzimidazole Chemical compound C1=CC(OCC)=CC=C1C1=NC2=CC=C(C=3NC4=CC(=CC=C4N=3)N3CCN(C)CC3)C=C2N1 PRDFBSVERLRRMY-UHFFFAOYSA-N 0.000 description 1
- 241000283707 Capra Species 0.000 description 1
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 description 1
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 101001047090 Homo sapiens Potassium voltage-gated channel subfamily H member 2 Proteins 0.000 description 1
- 101000851007 Homo sapiens Vascular endothelial growth factor receptor 2 Proteins 0.000 description 1
- 241001529936 Murinae Species 0.000 description 1
- 102100022807 Potassium voltage-gated channel subfamily H member 2 Human genes 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 description 1
- 238000003927 comet assay Methods 0.000 description 1
- 231100000170 comet assay Toxicity 0.000 description 1
- 125000001352 cyclobutyloxy group Chemical group C1(CCC1)O* 0.000 description 1
- 230000001086 cytosolic effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000007850 fluorescent dye Substances 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 230000001631 hypertensive effect Effects 0.000 description 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 description 1
- 238000010166 immunofluorescence Methods 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- 238000000386 microscopy Methods 0.000 description 1
- 230000008880 microtubule cytoskeleton organization Effects 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 230000004526 pharmaceutical effect Effects 0.000 description 1
- 238000006116 polymerization reaction Methods 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 230000000452 restraining effect Effects 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000026683 transduction Effects 0.000 description 1
- 238000010361 transduction Methods 0.000 description 1
- 238000012800 visualization Methods 0.000 description 1
- MBMQEIFVQACCCH-QBODLPLBSA-N zearalenone Chemical compound O=C1O[C@@H](C)CCCC(=O)CCC\C=C\C2=CC(O)=CC(O)=C21 MBMQEIFVQACCCH-QBODLPLBSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Transplantation (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16950309P | 2009-04-15 | 2009-04-15 | |
| GBGB0906470.0A GB0906470D0 (en) | 2009-04-15 | 2009-04-15 | New compounds |
| US169503P | 2009-04-15 | ||
| GB0906470 | 2009-04-15 | ||
| PCT/GB2010/050618 WO2010119285A1 (en) | 2009-04-15 | 2010-04-15 | Imidazo [1,2-a]pyridine derivatives as fgfr kinase inhibitors for use in therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2545215T3 true ES2545215T3 (es) | 2015-09-09 |
Family
ID=40750626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10718660.3T Active ES2545215T3 (es) | 2009-04-15 | 2010-04-15 | Derivados de imidazo[1,2-a]piridina como inhibidores del FGFR quinasa para uso en terapia |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8722687B2 (https=) |
| EP (1) | EP2419428B1 (https=) |
| JP (1) | JP5646598B2 (https=) |
| AU (1) | AU2010238290B2 (https=) |
| CA (1) | CA2757326C (https=) |
| DK (1) | DK2419428T3 (https=) |
| ES (1) | ES2545215T3 (https=) |
| GB (1) | GB0906470D0 (https=) |
| HR (1) | HRP20150825T1 (https=) |
| HU (1) | HUE027494T2 (https=) |
| PL (1) | PL2419428T3 (https=) |
| PT (1) | PT2419428E (https=) |
| RS (1) | RS54166B1 (https=) |
| SI (1) | SI2419428T1 (https=) |
| SM (1) | SMT201500200B (https=) |
| WO (1) | WO2010119285A1 (https=) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008078091A1 (en) | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| CN101679409B (zh) | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| UA111382C2 (uk) | 2011-10-10 | 2016-04-25 | Оріон Корпорейшн | Інгібітори протеїнкінази |
| WO2013138341A1 (en) * | 2012-03-15 | 2013-09-19 | Regents Of The University Of Minnesota | Topk inhibiting compounds |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| CN102786543B (zh) * | 2012-07-24 | 2016-04-27 | 上海瑞博化学有限公司 | 咪唑并[1，2-a]吡啶-6-硼酸频哪醇酯及其衍生物的制备方法 |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| KR102092988B1 (ko) * | 2012-09-28 | 2020-03-25 | 벤더르빌트 유니버시티 | 선택성 bmp 저해제로써 융합된 헤테로 고리 화합물들 |
| 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 |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| KR102344105B1 (ko) | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모노시클릭 피리딘 유도체의 염 및 이의 결정 |
| JP6585167B2 (ja) * | 2014-10-03 | 2019-10-02 | ノバルティス アーゲー | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
| WO2016060937A1 (en) * | 2014-10-13 | 2016-04-21 | R4 Ventures Llc | Real time individual electronic enclosure cooling system |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | 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 |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| ES2887148T3 (es) | 2015-03-25 | 2021-12-21 | Nat Cancer Ct | Agente terapéutico contra el cáncer de vías biliares |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| EP3362455A1 (en) | 2015-10-16 | 2018-08-22 | AbbVie Inc. | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
| US11780848B2 (en) | 2015-10-16 | 2023-10-10 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof |
| US12365689B2 (en) | 2015-10-16 | 2025-07-22 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US12414945B2 (en) | 2015-12-17 | 2025-09-16 | Eisai R&D Management Co., Ltd. | Therapeutic agent for breast cancer |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| WO2019178383A1 (en) | 2018-03-14 | 2019-09-19 | Vanderbilt University | Inhibition of bmp signaling, compounds, compositions and uses thereof |
| SG11202007591RA (en) | 2018-03-28 | 2020-09-29 | Eisai R&D Man Co Ltd | Therapeutic agent for hepatocellular carcinoma |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| 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 |
| KR102753831B1 (ko) * | 2019-07-26 | 2025-01-14 | 씨젠테크 (쑤저우, 차이나) 컴퍼니 리미티드 | Fgfr 및 vegfr 이중 억제제로서의 피리딘 유도체 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | 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 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| WO2021146424A1 (en) * | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| KR102537615B1 (ko) * | 2020-02-25 | 2023-05-30 | 주식회사 종근당 | 히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물 |
| KR102537616B1 (ko) | 2020-02-25 | 2023-05-26 | 주식회사 종근당 | 히스톤 탈아세틸화 효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물 |
| CA3206502A1 (en) * | 2021-01-26 | 2022-08-04 | Zhengxia CHEN | Crystal form of methylpyrazole-substituted pyridoimidazole compound and preparation method therefor |
| 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 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202432120A (zh) * | 2023-02-01 | 2024-08-16 | 韓商安康尼克治療有限公司 | 注射用組合物、包含其之醫藥調配物以及製備該組合物之方法 |
Family Cites Families (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5554630A (en) | 1993-03-24 | 1996-09-10 | Neurosearch A/S | Benzimidazole compounds |
| DE69524598T2 (de) | 1994-06-20 | 2002-07-11 | Takeda Chemical Industries, Ltd. | Kondensierte imidazolderivate, ihre herstellung und verwendung |
| AU5348396A (en) | 1995-05-01 | 1996-11-21 | Fujisawa Pharmaceutical Co., Ltd. | Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivati ves and their use as bone resorption inhibitors |
| WO1998004689A1 (en) | 1995-07-31 | 1998-02-05 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate disease |
| US6218529B1 (en) | 1995-07-31 | 2001-04-17 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer |
| WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| HU228962B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo triazines, pharmaceutical compositions containing them and use of the compounds |
| CA2291709A1 (en) | 1997-05-30 | 1998-12-03 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| US5990146A (en) | 1997-08-20 | 1999-11-23 | Warner-Lambert Company | Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation |
| WO2000012089A1 (en) | 1998-08-31 | 2000-03-09 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| US6465484B1 (en) | 1997-09-26 | 2002-10-15 | Merck & Co., Inc. | Angiogenesis inhibitors |
| EP1049699B1 (en) | 1998-01-28 | 2004-04-21 | Bristol-Myers Squibb Pharma Company | Pyrazolotriazines as crf antagonists |
| US6245759B1 (en) | 1999-03-11 | 2001-06-12 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| WO2001000214A1 (en) | 1999-06-30 | 2001-01-04 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| AU5636900A (en) | 1999-06-30 | 2001-01-31 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| JP2003503351A (ja) | 1999-06-30 | 2003-01-28 | メルク エンド カムパニー インコーポレーテッド | Ｓｒｃキナーゼ阻害化合物 |
| JP2001057292A (ja) | 1999-08-20 | 2001-02-27 | Toray Ind Inc | 発光素子 |
| GB9919778D0 (en) | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
| GB9921150D0 (en) | 1999-09-07 | 1999-11-10 | Merck Sharp & Dohme | Therapeutic agents |
| WO2001021634A1 (en) | 1999-09-21 | 2001-03-29 | Lion Bioscience Ag | Benzimidazole derivatives and combinatorial libraries thereof |
| GB9927687D0 (en) | 1999-11-23 | 2000-01-19 | Merck Sharp & Dohme | Therapeutic agents |
| AU2001237401B2 (en) | 2000-03-01 | 2006-11-09 | Janssen Pharmaceutica N.V. | 2,4-disubstituted thiazolyl derivatives |
| KR20020081424A (ko) | 2000-03-09 | 2002-10-26 | 아벤티스 파마 도이칠란트 게엠베하 | Ｐｐａｒ 매개인자의 치료학적 용도 |
| US20020041880A1 (en) | 2000-07-05 | 2002-04-11 | Defeo-Jones Deborah | Method of treating cancer |
| CA2417942C (en) | 2000-08-04 | 2010-06-29 | Warner-Lambert Company | 2-(4-pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones |
| WO2002034748A1 (fr) | 2000-10-24 | 2002-05-02 | Sankyo Company, Limited | Derives d'imidazopyridine |
| GB0027561D0 (en) | 2000-11-10 | 2000-12-27 | Merck Sharp & Dohme | Therapeutic agents |
| US20070004713A1 (en) | 2000-12-07 | 2007-01-04 | Bernard Barlaam | Therapeutic benimidazole compounds |
| US20020107262A1 (en) | 2000-12-08 | 2002-08-08 | 3M Innovative Properties Company | Substituted imidazopyridines |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| EP1423388B1 (en) | 2001-02-20 | 2008-12-03 | AstraZeneca AB | 2-arylamino-pyrimidines for the treatment of gsk3-related disorders |
| SE0100567D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
| SE0100568D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
| TWI248936B (en) | 2001-03-21 | 2006-02-11 | Merck Sharp & Dohme | Imidazo-pyrimidine derivatives as ligands for GABA receptors |
| DE10117183A1 (de) | 2001-04-05 | 2002-10-10 | Gruenenthal Gmbh | Verwendung von substituierten Imidazo[1,2-a]-pyridinverbindungen als Arzneimittel |
| US7074801B1 (en) | 2001-04-26 | 2006-07-11 | Eisai Co., Ltd. | Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof |
| WO2003007955A2 (en) | 2001-07-20 | 2003-01-30 | Cancer Research Technology Limited | Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer |
| GB0128499D0 (en) | 2001-11-28 | 2002-01-23 | Merck Sharp & Dohme | Therapeutic agents |
| US6900208B2 (en) | 2002-03-28 | 2005-05-31 | Bristol Myers Squibb Company | Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders |
| JP2003295882A (ja) | 2002-04-02 | 2003-10-15 | Canon Inc | 音声合成用テキスト構造、音声合成方法、音声合成装置及びそのコンピュータ・プログラム |
| EP1505068A4 (en) | 2002-04-23 | 2008-03-19 | Shionogi & Co | PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND INHIBITOR OF NAD (P) H OXIDASE CONTAINING SAID DERIVATIVE |
| JP2004002826A (ja) | 2002-04-24 | 2004-01-08 | Sankyo Co Ltd | 高分子イミダゾピリジン誘導体 |
| WO2003092595A2 (en) | 2002-05-02 | 2003-11-13 | Merck & Co., Inc | Tyrosine kinase inhibitors |
| NZ537156A (en) | 2002-05-23 | 2007-06-29 | Cytopia Pty Ltd | Kinase inhibitors |
| GB0212049D0 (en) | 2002-05-24 | 2002-07-03 | Merck Sharp & Dohme | Therapeutic agents |
| GB0212048D0 (en) | 2002-05-24 | 2002-07-03 | Merck Sharp & Dohme | Therapeutic agents |
| US7196111B2 (en) | 2002-06-04 | 2007-03-27 | Schering Corporation | Pyrazolo[1,5a]pyrimidine compounds as antiviral agents |
| US7196090B2 (en) | 2002-07-25 | 2007-03-27 | Warner-Lambert Company | Kinase inhibitors |
| ATE378336T1 (de) | 2002-09-19 | 2007-11-15 | Schering Corp | Imidazopyridine als hemmstoffe cyclin abhängiger kinasen |
| GB0223349D0 (en) | 2002-10-08 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic agents |
| WO2004035579A1 (ja) | 2002-10-15 | 2004-04-29 | Takeda Pharmaceutical Company Limited | イミダゾピリジン誘導体、その製造法および用途 |
| US7550470B2 (en) | 2002-12-11 | 2009-06-23 | Merck & Co. Inc. | Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors |
| AU2003298942A1 (en) | 2002-12-11 | 2004-06-30 | Merck And Co., Inc. | Tyrosine kinase inhibitors |
| US7826979B2 (en) | 2003-02-14 | 2010-11-02 | Vertex Pharmaceuticals Incorporated | Method of modeling complex formation between a query ligan and a target molecule |
| US7476670B2 (en) | 2003-02-18 | 2009-01-13 | Aventis Pharma S.A. | Purine derivatives, method for preparing, pharmaceutical compositions and novel use |
| US7157460B2 (en) | 2003-02-20 | 2007-01-02 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| US7893096B2 (en) | 2003-03-28 | 2011-02-22 | Novartis Vaccines And Diagnostics, Inc. | Use of small molecule compounds for immunopotentiation |
| US7442709B2 (en) | 2003-08-21 | 2008-10-28 | Osi Pharmaceuticals, Inc. | N3-substituted imidazopyridine c-Kit inhibitors |
| AU2004268949A1 (en) | 2003-08-21 | 2005-03-10 | Osi Pharmaceuticals, Inc. | N-substituted benzimidazolyl C-kit inhibitors |
| DE602004020073D1 (de) | 2003-08-21 | 2009-04-30 | Osi Pharm Inc | 3-substituierte imidazopyridinderivate als c-kit-inhibitoren |
| BRPI0417345A (pt) | 2003-12-03 | 2007-03-13 | Cytopia Res Pty Ltd | compostos inibidores de quìnase baseados em azola, composições e seus usos |
| EP1711496A4 (en) | 2004-01-28 | 2009-02-11 | Smithkline Beecham Corp | THIAZOLE COMPOUNDS |
| TW200530236A (en) | 2004-02-23 | 2005-09-16 | Chugai Pharmaceutical Co Ltd | Heteroaryl phenylurea |
| CN1950372A (zh) | 2004-05-10 | 2007-04-18 | 万有制药株式会社 | 咪唑并吡啶化合物 |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| US7718801B2 (en) | 2004-08-31 | 2010-05-18 | Banyu Pharmaceutical Co., Ltd. | Substituted imidazole derivative |
| CN101083985A (zh) | 2004-09-21 | 2007-12-05 | 幸讬制药公司 | 用于炎症及免疫相关用途的化合物 |
| WO2006038001A1 (en) | 2004-10-06 | 2006-04-13 | Celltech R & D Limited | Aminopyrimidine derivatives as jnk inhibitors |
| EP1831206B1 (en) | 2004-12-01 | 2011-08-24 | OSI Pharmaceuticals, Inc. | N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library |
| US20080167314A1 (en) | 2004-12-28 | 2008-07-10 | Osamu Uchikawa | Condensed Imidazole Compound And Use Thereof |
| US20100160324A1 (en) | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| DOP2006000051A (es) | 2005-02-24 | 2006-08-31 | Lilly Co Eli | Inhibidores de vegf-r2 y métodos |
| AU2006218403A1 (en) | 2005-03-03 | 2006-09-08 | Sirtris Pharmaceuticals, Inc. | Fused heterocyclic compounds and their use as sirtuin modulators |
| NZ562468A (en) | 2005-04-05 | 2009-10-30 | Pharmacopeia Inc | Purine and imidazopyridine derivatives for immunosuppression |
| FR2884821B1 (fr) | 2005-04-26 | 2007-07-06 | Aventis Pharma Sa | Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation |
| US7572807B2 (en) | 2005-06-09 | 2009-08-11 | Bristol-Myers Squibb Company | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| WO2007036732A1 (en) | 2005-09-30 | 2007-04-05 | Astrazeneca Ab | Imidazo [1,2-a] pyridine having anti-cell-proliferation activity |
| US8119643B2 (en) | 2006-03-20 | 2012-02-21 | Synta Pharmaceuticals Corp. | Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses |
| US8163777B2 (en) | 2006-03-23 | 2012-04-24 | Synta Pharmaceuticals Corp. | Benzimidazolyl-pyridine compounds for inflammation and immune-related uses |
| ITVA20060041A1 (it) | 2006-07-05 | 2008-01-06 | Dialectica Srl | Uso di composti derivati amminotiazolici, di loro composizioni farmaceutiche, nel trattamento di malattie caratterizzate dalla anormale repressione della trascrizione genica, particolarmente il morbo di huntington |
| TW200811134A (en) | 2006-07-12 | 2008-03-01 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| EP1882475A1 (en) | 2006-07-26 | 2008-01-30 | Novartis AG | Method of treating disorders mediated by the fibroblast growth factor receptor |
| US7737149B2 (en) | 2006-12-21 | 2010-06-15 | Astrazeneca Ab | N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof |
| WO2008078091A1 (en) * | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| US8131527B1 (en) | 2006-12-22 | 2012-03-06 | Astex Therapeutics Ltd. | FGFR pharmacophore compounds |
| CN101679409B (zh) * | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| US7977336B2 (en) | 2006-12-28 | 2011-07-12 | Banyu Pharmaceutical Co. Ltd | Aminopyrimidine derivatives as PLK1 inhibitors |
| EP2137184B1 (en) | 2007-04-03 | 2013-05-08 | Array Biopharma, Inc. | Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors |
| JP5539864B2 (ja) | 2007-06-12 | 2014-07-02 | アカオゲン，インコーポレーテッド | 抗菌剤 |
| EP2170882A1 (en) | 2007-06-26 | 2010-04-07 | Gilead Colorado, Inc. | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0810902D0 (en) * | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
-
2009
- 2009-04-15 GB GBGB0906470.0A patent/GB0906470D0/en not_active Ceased
-
2010
- 2010-04-15 WO PCT/GB2010/050618 patent/WO2010119285A1/en not_active Ceased
- 2010-04-15 SI SI201030994T patent/SI2419428T1/sl unknown
- 2010-04-15 ES ES10718660.3T patent/ES2545215T3/es active Active
- 2010-04-15 EP EP20100718660 patent/EP2419428B1/en active Active
- 2010-04-15 PL PL10718660T patent/PL2419428T3/pl unknown
- 2010-04-15 DK DK10718660.3T patent/DK2419428T3/en active
- 2010-04-15 JP JP2012505239A patent/JP5646598B2/ja not_active Expired - Fee Related
- 2010-04-15 CA CA2757326A patent/CA2757326C/en active Active
- 2010-04-15 US US13/264,596 patent/US8722687B2/en active Active
- 2010-04-15 HR HRP20150825TT patent/HRP20150825T1/hr unknown
- 2010-04-15 PT PT107186603T patent/PT2419428E/pt unknown
- 2010-04-15 RS RS20150533A patent/RS54166B1/sr unknown
- 2010-04-15 AU AU2010238290A patent/AU2010238290B2/en not_active Ceased
- 2010-04-15 HU HUE10718660A patent/HUE027494T2/en unknown
-
2015
- 2015-08-18 SM SM201500200T patent/SMT201500200B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PT2419428E (pt) | 2015-09-21 |
| JP2012524056A (ja) | 2012-10-11 |
| EP2419428B1 (en) | 2015-05-13 |
| US20120041000A1 (en) | 2012-02-16 |
| JP5646598B2 (ja) | 2014-12-24 |
| SMT201500200B (it) | 2015-10-30 |
| US8722687B2 (en) | 2014-05-13 |
| SI2419428T1 (sl) | 2015-10-30 |
| AU2010238290A1 (en) | 2011-12-08 |
| HUE027494T2 (en) | 2016-10-28 |
| WO2010119285A1 (en) | 2010-10-21 |
| AU2010238290B2 (en) | 2015-12-17 |
| HRP20150825T1 (hr) | 2015-09-11 |
| CA2757326A1 (en) | 2010-10-21 |
| RS54166B1 (sr) | 2015-12-31 |
| CA2757326C (en) | 2018-06-12 |
| GB0906470D0 (en) | 2009-05-20 |
| DK2419428T3 (en) | 2015-08-10 |
| EP2419428A1 (en) | 2012-02-22 |
| PL2419428T3 (pl) | 2015-10-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2545215T3 (es) | Derivados de imidazo[1,2-a]piridina como inhibidores del FGFR quinasa para uso en terapia | |
| ES2905539T3 (es) | Compuestos bicíclicos para diagnóstico y terapia | |
| AU2009298004B2 (en) | Pyrazolo Pyridine Compounds as NADPH Oxidase Inhibitors | |
| CA2820362C (en) | Substituted pyrazolopyrimidines as glucocerebrosidase activators | |
| RU2669367C2 (ru) | Модуляторы натриевого канала для лечения боли | |
| ES2580781T3 (es) | Derivados heterociclilos bicíclicos como inhibidores de FGFR quinasa para uso terapéutico | |
| AR067093A1 (es) | N-(2-(hetaril) arilsulfonamidas y n-(2-( heteraril) hetaril) arilsulfonamidas | |
| CN106132934B (zh) | 治疗炎性病症的苯并咪唑衍生物及其医药组合物 | |
| CA2496633A1 (en) | Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein | |
| CN107530353A (zh) | Melk的三环激酶抑制剂和使用方法 | |
| NL1031473C2 (nl) | Cyclopentapyridine- en tetrahydrochinolinederivaten. | |
| AR050788A1 (es) | Compuestos de aminoheteroarilo enantiomericamente puros como inhibidores de proteina quinasa | |
| WO2010117787A2 (en) | Inhibiting eph b-3 kinase | |
| CA2388593A1 (en) | Bicyclic and tricyclic heteroaromatic compounds | |
| ES2259419T3 (es) | Imidazo(1,2-a)piridinas. | |
| CN110172051A (zh) | IRE-1α抑制剂 | |
| JP5856086B2 (ja) | 薬物製造のためのイソキノロン類の使用、新規なイソキノロン類およびそれらの合成方法 | |
| CN110981868B (zh) | 咪唑并吡啶类化合物、包含该化合物的药物组合物及其制备方法和用途 | |
| BR112019011924A2 (pt) | derivados de bis-heteroarila bicíclicos como moduladores de agregação de proteína | |
| Griebel et al. | Behavioural profiles in the mouse defence test battery suggest anxiolytic potential of 5-HT1A receptor antagonists | |
| Deau et al. | Rational design, pharmacomodulation, and synthesis of dual 5-hydroxytryptamine 7 (5-HT7)/5-hydroxytryptamine 2A (5-HT2A) receptor antagonists and evaluation by [18F]-PET imaging in a primate brain | |
| Ilatovskaya et al. | Single-channel analysis of TRPC channels in the podocytes of freshly isolated glomeruli | |
| BRPI0717106A2 (pt) | Compostos para o tratamento de distúrbios metabólicos | |
| CN101031338B (zh) | 治疗认知障碍的组合物和方法 | |
| BR112013007073A2 (pt) | derivados do cromeno; composição farmacêutica; utilização de um composto da fórmula i e processo de preparação de um composto da fórmula i |