JP5555186B2 - ｐ３８ＭＡＰキナーゼ阻害剤 - Google Patents
ｐ３８ＭＡＰキナーゼ阻害剤 Download PDFInfo
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- JP5555186B2 JP5555186B2 JP2010548176A JP2010548176A JP5555186B2 JP 5555186 B2 JP5555186 B2 JP 5555186B2 JP 2010548176 A JP2010548176 A JP 2010548176A JP 2010548176 A JP2010548176 A JP 2010548176A JP 5555186 B2 JP5555186 B2 JP 5555186B2
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- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 title description 36
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 title description 36
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title description 3
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 39
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- VUMMFAUQEGRHCK-UHFFFAOYSA-N cyclopentyl 2-[2-[4-[2-amino-3-(2,4-difluorobenzoyl)-6-oxopyridin-1-yl]phenyl]ethylamino]-2-methylpropanoate Chemical compound C1CCCC1OC(=O)C(C)(C)NCCC(C=C1)=CC=C1N(C(C=C1)=O)C(N)=C1C(=O)C1=CC=C(F)C=C1F VUMMFAUQEGRHCK-UHFFFAOYSA-N 0.000 claims 1
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- IFCKTPNRSKNSMH-UHFFFAOYSA-N tert-butyl 2-[2-[4-[2-amino-3-(2,4-difluorobenzoyl)-6-oxopyridin-1-yl]phenyl]ethylamino]-2-methylpropanoate Chemical compound C1=CC(CCNC(C)(C)C(=O)OC(C)(C)C)=CC=C1N1C(=O)C=CC(C(=O)C=2C(=CC(F)=CC=2)F)=C1N IFCKTPNRSKNSMH-UHFFFAOYSA-N 0.000 description 1
- IDUCCWPJHLCUCT-UHFFFAOYSA-N tert-butyl 2-[3-[4-[2-amino-3-(2,4-difluorobenzoyl)-6-oxopyridin-1-yl]-3,5-difluorophenoxy]propylamino]-2-methylpropanoate Chemical compound FC1=CC(OCCCNC(C)(C)C(=O)OC(C)(C)C)=CC(F)=C1N1C(=O)C=CC(C(=O)C=2C(=CC(F)=CC=2)F)=C1N IDUCCWPJHLCUCT-UHFFFAOYSA-N 0.000 description 1
- OGFBTFZTWVAAMG-UHFFFAOYSA-N tert-butyl 2-[[2-[4-[2-amino-3-(2,4-difluorobenzoyl)-6-oxopyridin-1-yl]phenyl]acetyl]amino]-2-methylpropanoate Chemical compound C1=CC(CC(=O)NC(C)(C)C(=O)OC(C)(C)C)=CC=C1N1C(=O)C=CC(C(=O)C=2C(=CC(F)=CC=2)F)=C1N OGFBTFZTWVAAMG-UHFFFAOYSA-N 0.000 description 1
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
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- XUIIKFGFIJCVMT-UHFFFAOYSA-N thyroxine-binding globulin Natural products IC1=CC(CC([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-UHFFFAOYSA-N 0.000 description 1
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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Classifications
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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Landscapes
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- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0803748A GB0803748D0 (en) | 2008-02-29 | 2008-02-29 | Ihibitors of p38 MAP kinase |
| GB0803748.3 | 2008-02-29 | ||
| GB0815544.2 | 2008-08-27 | ||
| GB0815544A GB0815544D0 (en) | 2008-08-27 | 2008-08-27 | Inhibitors of p38 map kinase |
| PCT/GB2009/000553 WO2009106844A1 (en) | 2008-02-29 | 2009-02-27 | Inhibitors of p38 map kinase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011513288A JP2011513288A (ja) | 2011-04-28 |
| JP2011513288A5 JP2011513288A5 (enExample) | 2012-04-12 |
| JP5555186B2 true JP5555186B2 (ja) | 2014-07-23 |
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| JP2010548176A Expired - Fee Related JP5555186B2 (ja) | 2008-02-29 | 2009-02-27 | ｐ３８ＭＡＰキナーゼ阻害剤 |
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| Country | Link |
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| US (1) | US8778953B2 (enExample) |
| EP (1) | EP2245012B1 (enExample) |
| JP (1) | JP5555186B2 (enExample) |
| ES (1) | ES2427892T3 (enExample) |
| WO (1) | WO2009106844A1 (enExample) |
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| JP5340918B2 (ja) * | 2006-05-04 | 2013-11-13 | クロマ セラピューティクス リミテッド | ｐ３８ＭＡＰキナーゼ阻害剤 |
| GB0803747D0 (en) * | 2008-02-29 | 2008-04-09 | Martin | Enzyme and receptor modulation |
| GB0903480D0 (en) | 2009-02-27 | 2009-04-08 | Chroma Therapeutics Ltd | Enzyme Inhibitors |
| GB201211310D0 (en) | 2012-06-26 | 2012-08-08 | Chroma Therapeutics Ltd | CSF-1R kinase inhibitors |
| CA2888928C (en) | 2012-10-17 | 2020-05-26 | Chroma Therapeutics Ltd | Tert-butyl n-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2h)-yl]-3,5- difluorophenyl}ethyl]-l-alaninate or a salt, hydrate or solvate thereof |
| GB201306901D0 (en) * | 2013-04-16 | 2013-05-29 | Chroma Therapeutics Ltd | Combination |
| AU2017281222B2 (en) | 2016-06-23 | 2022-06-16 | The Usa As Represented By The Department Of Veterans Affairs; Dept. Of Veterans Affairs Office Of General Counsel - Pag Iv (024) | Non-catalytic substrate-selective P38α-specific MAPK inhibitors with endothelial-stabilizing and anti-inflammatory activity, and methods of use thereof |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
| WO2020118194A1 (en) * | 2018-12-07 | 2020-06-11 | University Of Maryland, Baltimore | NON-ATP/CATALYTIC SITE p38 MITOGEN ACTIVATED PROTEIN KINASE INHIBITORS |
| CN116406355A (zh) | 2020-05-18 | 2023-07-07 | Gen1E生命科学公司 | P38α促分裂原活化蛋白激酶抑制剂 |
| US11390581B2 (en) | 2020-10-29 | 2022-07-19 | Gen1E Lifesciences Inc. | Crystalline 5-(dimethylamino)-n-(4-(morpholinomethyl)phenyl)naphthalene-1-sulfonamide di-hydrochloride di-hydrate |
| CN117120422A (zh) | 2021-03-23 | 2023-11-24 | Gen1E生命科学公司 | 取代的萘基P38α丝裂原活化的蛋白激酶抑制剂 |
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| US5331006A (en) | 1990-08-31 | 1994-07-19 | Warner-Lambert Company | Amino acid analogs as CCK antagonists |
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
| US6448256B1 (en) | 1999-05-24 | 2002-09-10 | University Of Massachusetts | Antibiotic prodrugs |
| JP2005526068A (ja) * | 2002-03-14 | 2005-09-02 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | 抗炎症剤としての単環式アロイルピリジノン類 |
| US20060235012A1 (en) | 2003-06-16 | 2006-10-19 | Chroma Therapeutics Limited | Carboline and betacarboline derivatives for use as hdac enzyme inhibitors |
| KR20120116991A (ko) | 2003-07-29 | 2012-10-23 | 시그너쳐 알 앤드 디 홀딩스, 엘엘씨 | 아미노산 프로드럭 |
| EP1718145A4 (en) | 2004-02-02 | 2012-03-07 | Biosight Ltd | CONJUGATES FOR CANCER THERAPY AND DIAGNOSIS |
| DE602005003951T4 (de) | 2004-05-14 | 2012-10-11 | Millennium Pharmaceuticals, Inc. | Verbindungen und verfahren zur inhibierung der mitotischen progression durch hemmung von aurorakinase |
| EP1877098B1 (en) * | 2005-05-05 | 2013-04-24 | Chroma Therapeutics Limited | Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase |
| JP5340918B2 (ja) * | 2006-05-04 | 2013-11-13 | クロマ セラピューティクス リミテッド | ｐ３８ＭＡＰキナーゼ阻害剤 |
| GB0621830D0 (en) | 2006-11-02 | 2006-12-13 | Chroma Therapeutics Ltd | Inhibitors of p38 mitogen-activated protein kinase |
| JP2011503042A (ja) | 2007-11-07 | 2011-01-27 | クロマ セラピューティクス リミテッド | ｐ３８ＭＡＰキナーゼ阻害剤 |
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2009
- 2009-02-27 US US12/867,774 patent/US8778953B2/en active Active
- 2009-02-27 JP JP2010548176A patent/JP5555186B2/ja not_active Expired - Fee Related
- 2009-02-27 EP EP09713855.6A patent/EP2245012B1/en not_active Not-in-force
- 2009-02-27 WO PCT/GB2009/000553 patent/WO2009106844A1/en not_active Ceased
- 2009-02-27 ES ES09713855T patent/ES2427892T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20110034520A1 (en) | 2011-02-10 |
| ES2427892T3 (es) | 2013-11-04 |
| WO2009106844A1 (en) | 2009-09-03 |
| US8778953B2 (en) | 2014-07-15 |
| EP2245012B1 (en) | 2013-07-03 |
| JP2011513288A (ja) | 2011-04-28 |
| EP2245012A1 (en) | 2010-11-03 |
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