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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- 229960001367 tartaric acid Drugs 0.000 description 1
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- YBIANLZYEWCDCW-VIFPVBQESA-N tert-butyl (2s)-2-amino-2-methylbutanoate Chemical compound CC[C@](C)(N)C(=O)OC(C)(C)C YBIANLZYEWCDCW-VIFPVBQESA-N 0.000 description 1
- KTYIEPAXQWLADO-UHFFFAOYSA-N tert-butyl 1-aminocyclopentane-1-carboxylate Chemical compound CC(C)(C)OC(=O)C1(N)CCCC1 KTYIEPAXQWLADO-UHFFFAOYSA-N 0.000 description 1
- 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
- KUYMVWXKHQSIAS-UHFFFAOYSA-N tert-butyl 2-chloroacetate Chemical compound CC(C)(C)OC(=O)CCl KUYMVWXKHQSIAS-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000003554 tetrahydropyrrolyl group Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
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- 125000003396 thiol group Chemical group [H]S* 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
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000013519 translation Methods 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 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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- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—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
- 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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- 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
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- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
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- 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]
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
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- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Pulmonology (AREA)
- Diabetes (AREA)
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- Transplantation (AREA)
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- Neurology (AREA)
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- Pain & Pain Management (AREA)
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- Emergency Medicine (AREA)
- 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 |
|---|---|---|---|
| GB0803748.3 | 2008-02-29 | ||
| GB0803748A GB0803748D0 (en) | 2008-02-29 | 2008-02-29 | Ihibitors of p38 MAP kinase |
| GB0815544A GB0815544D0 (en) | 2008-08-27 | 2008-08-27 | Inhibitors of p38 map kinase |
| GB0815544.2 | 2008-08-27 | ||
| 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 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010548176A Expired - Fee Related JP5555186B2 (ja) | 2008-02-29 | 2009-02-27 | ｐ３８ＭＡＰキナーゼ阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8778953B2 (enExample) |
| EP (1) | EP2245012B1 (enExample) |
| JP (1) | JP5555186B2 (enExample) |
| ES (1) | ES2427892T3 (enExample) |
| WO (1) | WO2009106844A1 (enExample) |
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| HUE033281T2 (en) * | 2006-05-04 | 2017-11-28 | Chroma Therapeutics Ltd | p38 mitogen-activated protein (MAP) kinase inhibitors |
| 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 |
| SI3222616T1 (sl) | 2012-10-17 | 2019-10-30 | Macrophage Pharma Ltd | N-(2-(4-(6-amino-5-(2,4-difluorobenzoil)-2-oksopiridin-1(2H)-IL)-3,5- difluorofenil)etil)-L-alanin in njegov terbutil ester |
| GB201306901D0 (en) * | 2013-04-16 | 2013-05-29 | Chroma Therapeutics Ltd | Combination |
| CN116570594A (zh) | 2016-06-23 | 2023-08-11 | 马里兰大学巴尔的摩分校 | 选择性p38α特异性MAPK抑制剂 |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
| JP7594787B2 (ja) | 2018-12-07 | 2024-12-05 | ユニバーシティ オブ メリーランド、ボルチモア | 非ＡＴＰ／触媒部位ｐ３８マイトジェン活性化プロテインキナーゼ阻害剤 |
| CN116406355B (zh) | 2020-05-18 | 2026-05-15 | Gen1E生命科学公司 | P38α促分裂原活化蛋白激酶抑制剂 |
| AU2021370893B2 (en) | 2020-10-29 | 2024-03-07 | Gen1E Lifesciences Inc. | Crystalline 5-(dimethylamino) -n- (4-(morpholinomethyl)phenyl) naphthalene-1-sulfonamide di-hydrochloride di-hydrate |
| NZ804686A (en) | 2021-03-23 | 2026-03-27 | Gen1E Lifesciences Inc | Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors |
| CN117651698A (zh) * | 2021-07-09 | 2024-03-05 | 新特拉有限公司 | 吡啶酮mk2抑制剂及其用途 |
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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 |
| IL163957A0 (en) * | 2002-03-14 | 2005-12-18 | Bayer Healthcare Ag | Monocyclic aroylpyridinones as antiinflammatory agents |
| EP1633751A1 (en) | 2003-06-16 | 2006-03-15 | Chroma Therapeutics Limited | Carboline and betacarboline derivatives for use as hdac enzyme inhibitors |
| JP2007510621A (ja) | 2003-07-29 | 2007-04-26 | シグニチャー アールアンドディー ホールディングス，エルエルシー． | アミノ酸プロドラッグ |
| EP3075247B1 (en) | 2004-02-02 | 2022-10-12 | BioSight Ltd. | Conjugates for cancer therapy and diagnosis |
| KR101792651B1 (ko) * | 2004-05-14 | 2017-11-20 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 아우로라 키나아제의 억제에 의해 유사분열 진행을 억제하기 위한 화합물 및 그 화합물을 포함하는 약학적 조성물 |
| MX2007013257A (es) * | 2005-05-05 | 2008-01-21 | Chroma Therapeutics Ltd | Conjugados de ester de alfa-aminoacido-farmaco hidrolizables por carboxilesterasa. |
| HUE033281T2 (en) * | 2006-05-04 | 2017-11-28 | Chroma Therapeutics Ltd | p38 mitogen-activated protein (MAP) kinase inhibitors |
| GB0621830D0 (en) | 2006-11-02 | 2006-12-13 | Chroma Therapeutics Ltd | Inhibitors of p38 mitogen-activated protein kinase |
| WO2009060160A1 (en) | 2007-11-07 | 2009-05-14 | Chroma Therapeutics Ltd. | P38 map kinase inhibitors |
-
2009
- 2009-02-27 ES ES09713855T patent/ES2427892T3/es active Active
- 2009-02-27 JP JP2010548176A patent/JP5555186B2/ja not_active Expired - Fee Related
- 2009-02-27 WO PCT/GB2009/000553 patent/WO2009106844A1/en not_active Ceased
- 2009-02-27 EP EP09713855.6A patent/EP2245012B1/en not_active Not-in-force
- 2009-02-27 US US12/867,774 patent/US8778953B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20110034520A1 (en) | 2011-02-10 |
| EP2245012B1 (en) | 2013-07-03 |
| ES2427892T3 (es) | 2013-11-04 |
| US8778953B2 (en) | 2014-07-15 |
| WO2009106844A1 (en) | 2009-09-03 |
| JP2011513288A (ja) | 2011-04-28 |
| EP2245012A1 (en) | 2010-11-03 |
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