JP2010526800A5 - - Google Patents
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- JP2010526800A5 JP2010526800A5 JP2010506999A JP2010506999A JP2010526800A5 JP 2010526800 A5 JP2010526800 A5 JP 2010526800A5 JP 2010506999 A JP2010506999 A JP 2010506999A JP 2010506999 A JP2010506999 A JP 2010506999A JP 2010526800 A5 JP2010526800 A5 JP 2010526800A5
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- JP
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- Prior art keywords
- optionally substituted
- alkyl
- group
- substituents
- optionally
- 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.)
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- 229910052760 oxygen Inorganic materials 0.000 claims 52
- 125000000217 alkyl group Chemical group 0.000 claims 45
- 125000001424 substituent group Chemical group 0.000 claims 45
- 229910052717 sulfur Inorganic materials 0.000 claims 37
- 229910052757 nitrogen Inorganic materials 0.000 claims 34
- 125000005842 heteroatom Chemical group 0.000 claims 33
- 229910052736 halogen Inorganic materials 0.000 claims 31
- 150000002367 halogens Chemical class 0.000 claims 30
- 125000004093 cyano group Chemical group *C#N 0.000 claims 27
- 125000000623 heterocyclic group Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 18
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- -1 NR c Inorganic materials 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000002015 acyclic group Chemical group 0.000 claims 12
- 125000003282 alkyl amino group Chemical group 0.000 claims 12
- 125000001153 fluoro group Chemical group F* 0.000 claims 12
- 125000004432 carbon atom Chemical group C* 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000002619 bicyclic group Chemical group 0.000 claims 8
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 7
- 125000002252 acyl group Chemical group 0.000 claims 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 7
- 229930195733 hydrocarbon Natural products 0.000 claims 7
- 150000002430 hydrocarbons Chemical class 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 7
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 5
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 4
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 150000001408 amides Chemical class 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- MIXJMLGVZCBRIX-UHFFFAOYSA-N 2,5-diphenyl-1,3-oxazole-4-carboxamide Chemical compound NC(=O)C=1N=C(C=2C=CC=CC=2)OC=1C1=CC=CC=C1 MIXJMLGVZCBRIX-UHFFFAOYSA-N 0.000 claims 3
- JCNYVYGICSWKQM-UHFFFAOYSA-N 2-(4-methylphenyl)-5-phenyl-1,3-oxazole-4-carboxamide Chemical compound C1=CC(C)=CC=C1C1=NC(C(N)=O)=C(C=2C=CC=CC=2)O1 JCNYVYGICSWKQM-UHFFFAOYSA-N 0.000 claims 3
- AHLPYPYPMMOUDM-UHFFFAOYSA-N 2-phenyl-5-(3,4,5-trimethoxyphenyl)-1,3-oxazole-4-carboxamide Chemical compound COC1=C(OC)C(OC)=CC(C2=C(N=C(O2)C=2C=CC=CC=2)C(N)=O)=C1 AHLPYPYPMMOUDM-UHFFFAOYSA-N 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- JUOPGNVRTKZCPM-UHFFFAOYSA-N 2,4-diphenyl-1h-imidazole-5-carboxamide Chemical compound NC(=O)C=1N=C(C=2C=CC=CC=2)NC=1C1=CC=CC=C1 JUOPGNVRTKZCPM-UHFFFAOYSA-N 0.000 claims 2
- RGFVVYIVBCLQJQ-UHFFFAOYSA-N 2-(4-fluorophenyl)-4-(4-methoxyphenyl)-1h-imidazole-5-carboxamide Chemical compound C1=CC(OC)=CC=C1C1=C(C(N)=O)N=C(C=2C=CC(F)=CC=2)N1 RGFVVYIVBCLQJQ-UHFFFAOYSA-N 0.000 claims 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 2
- QJBYSTKTNPHHEY-UHFFFAOYSA-N 2-phenyl-5-thiophen-2-yl-1h-imidazole-4-carboxamide Chemical compound NC(=O)C=1N=C(C=2C=CC=CC=2)NC=1C1=CC=CS1 QJBYSTKTNPHHEY-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 102000003989 Aurora kinases Human genes 0.000 claims 2
- 108090000433 Aurora kinases Proteins 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 2
- 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 claims 2
- 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 238000003763 carbonization Methods 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Chemical group 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 229910052789 astatine Inorganic materials 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91719107P | 2007-05-10 | 2007-05-10 | |
| GB0709031.9 | 2007-05-10 | ||
| US60/917,191 | 2007-05-10 | ||
| GBGB0709031.9A GB0709031D0 (en) | 2007-05-10 | 2007-05-10 | Pharmaceutical compounds |
| US98727307P | 2007-11-12 | 2007-11-12 | |
| US60/987,273 | 2007-11-12 | ||
| PCT/GB2008/001612 WO2008139161A1 (en) | 2007-05-10 | 2008-05-09 | Oxazole tyrosine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010526800A JP2010526800A (ja) | 2010-08-05 |
| JP2010526800A5 true JP2010526800A5 (enExample) | 2011-06-23 |
| JP5555620B2 JP5555620B2 (ja) | 2014-07-23 |
Family
ID=38219198
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506999A Active JP5555620B2 (ja) | 2007-05-10 | 2008-05-09 | オキサゾールチロシンキナーゼ阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US8378095B2 (enExample) |
| EP (1) | EP2170849B1 (enExample) |
| JP (1) | JP5555620B2 (enExample) |
| CN (1) | CN101796038B (enExample) |
| GB (1) | GB0709031D0 (enExample) |
| WO (1) | WO2008139161A1 (enExample) |
Families Citing this family (55)
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| GB0709031D0 (en) | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
| KR20150036210A (ko) | 2007-06-13 | 2015-04-07 | 인사이트 코포레이션 | 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염 |
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| US8420695B2 (en) * | 2008-07-09 | 2013-04-16 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
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| LT2899191T (lt) | 2009-04-30 | 2017-10-25 | Glaxo Group Limited | Oksazolo pakeistieji indazolai kaip pi3-kinazės inhibitoriai |
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| SI2432472T1 (sl) | 2009-05-22 | 2019-11-29 | Incyte Holdings Corp | 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK |
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| EP2712290A4 (en) * | 2011-05-19 | 2014-11-19 | Univ Leland Stanford Junior | ANTIPROLIFERATIVE COMPOUNDS AND METHOD FOR THEIR USE |
| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| EP2727920B1 (en) | 2011-07-29 | 2016-11-02 | FUJIFILM Corporation | 1,5-naphthyridine derivative or salt thereof |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
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| GB201202027D0 (en) * | 2012-02-06 | 2012-03-21 | Sareum Ltd | Pharmaceutical compounds |
| EP3040336B1 (en) | 2012-03-02 | 2020-04-08 | Sareum Limited | Compounds for use in treating tyk2 kinase mediated conditions |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| PH12020551186B1 (en) | 2012-11-15 | 2024-03-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| RS62867B1 (sr) | 2013-03-06 | 2022-02-28 | Incyte Holdings Corp | Postupci i intermedijeri za dobijanje inhibitora jak |
| SMT202000315T1 (it) | 2013-08-07 | 2020-07-08 | Incyte Corp | Forme di dosaggio a rilascio prolungato per un inibitore di jak1 |
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| CN104974095B (zh) * | 2015-06-30 | 2017-09-15 | 浙江大学 | 2,4,5‑多取代咪唑类化合物及制备方法 |
| CN105601580B (zh) * | 2015-11-29 | 2017-11-14 | 陈玉玲 | 一种噁唑类医药中间体化合物的合成方法 |
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| US11331313B2 (en) | 2017-05-22 | 2022-05-17 | Whitehead Institute For Biomedical Research | KCC2 expression enhancing compounds and uses thereof |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| SG11202007164UA (en) | 2018-01-30 | 2020-08-28 | Incyte Corp | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| EP3749697A4 (en) | 2018-02-05 | 2021-11-03 | Bio-Rad Laboratories, Inc. | CHROMATOGRAPHY RESIN WITH LIGAND MIXED MODE ANIONIC / HYDROPHOBIC EXCHANGE |
| WO2019164996A1 (en) * | 2018-02-21 | 2019-08-29 | Southern Research Institute | 2-aminoaryl-5-aryloxazole analogs for the treatment of neurodegenerative diseases |
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| US11718593B2 (en) | 2018-05-17 | 2023-08-08 | Southern Research Institute | 2,5-aryl-thiazole analogs for the treatment of neurodegenerative diseases |
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| GB0504753D0 (en) | 2005-03-08 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| JP5222561B2 (ja) | 2005-10-07 | 2013-06-26 | キッセイ薬品工業株式会社 | 含窒素芳香族複素環化合物およびそれを含有する医薬組成物 |
| DK200600313A (da) | 2006-03-03 | 2006-03-13 | Novo Nordisk As | Treating type 2 diabetes or metabolic syndrome with an interleukin 1beta inhibitor or an interleukin 1beta synthesis or release inhibitor |
| ES2352320T3 (es) | 2006-05-12 | 2011-02-17 | Ab Science | Nuevo procedimiento para la síntesis de compuestos de 2-aminoxazol. |
| WO2008024980A2 (en) | 2006-08-24 | 2008-02-28 | Serenex, Inc. | Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives |
| GB0709031D0 (en) | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
-
2007
- 2007-05-10 GB GBGB0709031.9A patent/GB0709031D0/en not_active Ceased
-
2008
- 2008-05-09 US US12/599,653 patent/US8378095B2/en active Active
- 2008-05-09 WO PCT/GB2008/001612 patent/WO2008139161A1/en not_active Ceased
- 2008-05-09 EP EP08750551.7A patent/EP2170849B1/en active Active
- 2008-05-09 CN CN200880024256.9A patent/CN101796038B/zh active Active
- 2008-05-09 JP JP2010506999A patent/JP5555620B2/ja active Active
-
2012
- 2012-12-05 US US13/705,659 patent/US20130102592A1/en not_active Abandoned
-
2014
- 2014-06-03 US US14/294,263 patent/US8921544B2/en active Active
- 2014-10-31 US US14/529,902 patent/US9187465B2/en active Active
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