JP2007519695A5 - - Google Patents
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- Publication number
- JP2007519695A5 JP2007519695A5 JP2006550298A JP2006550298A JP2007519695A5 JP 2007519695 A5 JP2007519695 A5 JP 2007519695A5 JP 2006550298 A JP2006550298 A JP 2006550298A JP 2006550298 A JP2006550298 A JP 2006550298A JP 2007519695 A5 JP2007519695 A5 JP 2007519695A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- compound
- heterocyclyl
- formula
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 239000001301 oxygen Substances 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical group FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- -1 6- {5-[(cyclopropylamino) carbonyl] -2-methylphenyl} -1,2-benzisoxazol-3-yl Chemical group 0.000 claims 2
- 102000004127 Cytokines Human genes 0.000 claims 2
- 108090000695 Cytokines Proteins 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- NTEZQSHKEITMIG-UHFFFAOYSA-N 3-[1-[(4-benzylmorpholin-2-yl)methyl]indazol-5-yl]-n-cyclopropyl-5-fluoro-4-methylbenzamide Chemical compound CC1=C(F)C=C(C(=O)NC2CC2)C=C1C(C=C1C=N2)=CC=C1N2CC(OCC1)CN1CC1=CC=CC=C1 NTEZQSHKEITMIG-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 150000004820 halides Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- MLFRDKXWLJIRPF-UHFFFAOYSA-N n-cyclopropyl-3-fluoro-4-methyl-5-[1-(oxan-2-ylmethyl)indazol-5-yl]benzamide Chemical compound CC1=C(F)C=C(C(=O)NC2CC2)C=C1C(C=C1C=N2)=CC=C1N2CC1CCCCO1 MLFRDKXWLJIRPF-UHFFFAOYSA-N 0.000 claims 1
- VRGMJONHCOCFRD-UHFFFAOYSA-N n-cyclopropyl-3-fluoro-4-methyl-5-[1-(oxolan-2-ylmethyl)indazol-5-yl]benzamide Chemical compound CC1=C(F)C=C(C(=O)NC2CC2)C=C1C(C=C1C=N2)=CC=C1N2CC1CCCO1 VRGMJONHCOCFRD-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0402140.8A GB0402140D0 (en) | 2004-01-30 | 2004-01-30 | Novel compounds |
| PCT/GB2005/000281 WO2005073219A1 (en) | 2004-01-30 | 2005-01-27 | Fused heteroaryl derivatives for use as p38 kinase inhibitors in the treatment of i.a. rheumatoid arthritis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007519695A JP2007519695A (ja) | 2007-07-19 |
| JP2007519695A5 true JP2007519695A5 (https=) | 2008-03-13 |
Family
ID=31971800
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006550298A Pending JP2007519695A (ja) | 2004-01-30 | 2005-01-27 | Ｉ．Ａ．関節リウマチの治療においてｐ３８キナーゼ阻害剤として使用するための縮合ヘテロアリール誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US7687532B2 (https=) |
| EP (1) | EP1745038A1 (https=) |
| JP (1) | JP2007519695A (https=) |
| GB (1) | GB0402140D0 (https=) |
| WO (1) | WO2005073219A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0124939D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124934D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124941D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124938D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124933D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| ATE375980T1 (de) | 2002-02-12 | 2007-11-15 | Smithkline Beecham Corp | Nicotinamide und deren verwendung als p38 inhibitoren |
| GB0217757D0 (en) | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Novel compounds |
| GB0318814D0 (en) * | 2003-08-11 | 2003-09-10 | Smithkline Beecham Corp | Novel compounds |
| GB0402143D0 (en) * | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| GB0402137D0 (en) * | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| GB0402138D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| GB0612026D0 (en) | 2006-06-16 | 2006-07-26 | Smithkline Beecham Corp | New use |
| ES2301380B1 (es) | 2006-08-09 | 2009-06-08 | Laboratorios Almirall S.A. | Nuevos derivados de 1,7-naftiridina. |
| EP1900729A1 (en) * | 2006-09-15 | 2008-03-19 | Novartis AG | Benzoxazoles and oxazolopyridines being useful as Janus kinases inhibitors |
| WO2008055842A1 (en) | 2006-11-09 | 2008-05-15 | F. Hoffmann-La Roche Ag | Substituted 6-phenyl-pyrido [2,3-d] pyrimidin-7-one derivatives as kinase inhibitors and methods for using the same |
| ES2320955B1 (es) | 2007-03-02 | 2010-03-16 | Laboratorios Almirall S.A. | Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida. |
| ES2329639B1 (es) | 2007-04-26 | 2010-09-23 | Laboratorios Almirall S.A. | Nuevos derivados de 4,8-difenilpoliazanaftaleno. |
| EP1992344A1 (en) | 2007-05-18 | 2008-11-19 | Institut Curie | P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation |
| EP2108641A1 (en) | 2008-04-11 | 2009-10-14 | Laboratorios Almirall, S.A. | New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors |
| EP2113503A1 (en) | 2008-04-28 | 2009-11-04 | Laboratorios Almirall, S.A. | New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors |
| AR074199A1 (es) | 2008-11-20 | 2010-12-29 | Glaxosmithkline Llc | Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer. |
| EP2322176A1 (en) | 2009-11-11 | 2011-05-18 | Almirall, S.A. | New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives |
| MX2012013197A (es) | 2010-05-12 | 2013-04-03 | Abbvie Inc | Inhibidores de indazol de cinasa. |
| JP2014166961A (ja) * | 2011-06-20 | 2014-09-11 | Dainippon Sumitomo Pharma Co Ltd | 新規インダゾール誘導体 |
| RU2014144951A (ru) | 2012-04-10 | 2016-06-10 | Сумитомо Дайниппон Фарма Ко., Лтд. | Новое 1-замещенное производное индазола |
| EP3233840B1 (en) | 2014-12-16 | 2018-11-21 | Eudendron S.r.l. | Heterocyclic derivatives modulating activity of certain protein kinases |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| BR112020006677A2 (pt) | 2017-10-05 | 2020-10-06 | Fulcrum Therapeutics, Inc. | uso de inibidores p38 para reduzir a expressão de dux4 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003500403A (ja) | 1999-05-21 | 2003-01-07 | サイオス，インコーポレーテッド | ｐ３８キナーゼのインヒビターとしてのインドール型誘導体 |
| PE20020506A1 (es) | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
| FR2824827B1 (fr) * | 2001-05-17 | 2004-02-13 | Fournier Lab Sa | Nouveaux derives de 5-phenyl-1h-indole antagoniste des recepteurs de l'interleukine-8 |
| GB0124848D0 (en) | 2001-10-16 | 2001-12-05 | Celltech R&D Ltd | Chemical compounds |
| GB0124941D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124934D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124938D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124936D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124931D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124932D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124939D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124933D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| ATE375980T1 (de) * | 2002-02-12 | 2007-11-15 | Smithkline Beecham Corp | Nicotinamide und deren verwendung als p38 inhibitoren |
| GB0209891D0 (en) * | 2002-04-30 | 2002-06-05 | Glaxo Group Ltd | Novel compounds |
| MXPA04011417A (es) * | 2002-05-17 | 2005-02-14 | Pharmacia Italia Spa | Derivados de aminoindazol activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden. |
| GB0217757D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Novel compounds |
| US7396943B2 (en) * | 2003-03-07 | 2008-07-08 | Eli Lilly And Company | Opioid receptor antagonists |
| GB0308186D0 (en) * | 2003-04-09 | 2003-05-14 | Smithkline Beecham Corp | Novel compounds |
| GB0308201D0 (en) * | 2003-04-09 | 2003-05-14 | Smithkline Beecham Corp | Novel compounds |
| GB0308185D0 (en) * | 2003-04-09 | 2003-05-14 | Smithkline Beecham Corp | Novel compounds |
| GB0318814D0 (en) * | 2003-08-11 | 2003-09-10 | Smithkline Beecham Corp | Novel compounds |
| GB0402143D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| GB0402137D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| GB0402138D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| US20080051416A1 (en) * | 2004-10-05 | 2008-02-28 | Smithkline Beecham Corporation | Novel Compounds |
| GB0512429D0 (en) * | 2005-06-17 | 2005-07-27 | Smithkline Beecham Corp | Novel compound |
-
2004
- 2004-01-30 GB GBGB0402140.8A patent/GB0402140D0/en not_active Ceased
-
2005
- 2005-01-27 US US10/587,614 patent/US7687532B2/en not_active Expired - Fee Related
- 2005-01-27 EP EP05702034A patent/EP1745038A1/en not_active Withdrawn
- 2005-01-27 JP JP2006550298A patent/JP2007519695A/ja active Pending
- 2005-01-27 WO PCT/GB2005/000281 patent/WO2005073219A1/en not_active Ceased
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