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
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- 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
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- 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
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- 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
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- 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
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US169503P | 1999-12-07 | ||
| US16950309P | 2009-04-15 | 2009-04-15 | |
| GB0906470 | 2009-04-15 | ||
| GBGB0906470.0A GB0906470D0 (en) | 2009-04-15 | 2009-04-15 | New compounds |
| 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 |
|---|---|---|---|---|
| US8513276B2 (en) | 2006-12-22 | 2013-08-20 | Astex Therapeutics Limited | Imidazo[1,2-a]pyridine compounds for use in treating cancer |
| HRP20150642T1 (hr) | 2006-12-22 | 2015-08-14 | Astex Therapeutics Limited | BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a |
| 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 |
| RS58514B1 (sr) | 2012-06-13 | 2019-04-30 | Incyte Holdings Corp | Supstituisana triciklična jedinjenja kao inhibitori 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 |
| JP6430383B2 (ja) * | 2012-09-28 | 2018-11-28 | ヴァンダービルト ユニバーシティーＶａｎｄｅｒｂｉｌｔ Ｕｎｉｖｅｒｓｉｔｙ | 選択的ｂｍｐ阻害剤としての縮合複素環化合物 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
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| GB0906470D0 (en) | 2009-05-20 |
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| AU2010238290B2 (en) | 2015-12-17 |
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| RS54166B1 (sr) | 2015-12-31 |
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| AU2010238290A1 (en) | 2011-12-08 |
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| WO2010119285A1 (en) | 2010-10-21 |
| US8722687B2 (en) | 2014-05-13 |
| CA2757326C (en) | 2018-06-12 |
| SI2419428T1 (sl) | 2015-10-30 |
| JP2012524056A (ja) | 2012-10-11 |
| US20120041000A1 (en) | 2012-02-16 |
| EP2419428B1 (en) | 2015-05-13 |
| EP2419428A1 (en) | 2012-02-22 |
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