JP2011513288A5 - - Google Patents
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- Publication number
- JP2011513288A5 JP2011513288A5 JP2010548176A JP2010548176A JP2011513288A5 JP 2011513288 A5 JP2011513288 A5 JP 2011513288A5 JP 2010548176 A JP2010548176 A JP 2010548176A JP 2010548176 A JP2010548176 A JP 2010548176A JP 2011513288 A5 JP2011513288 A5 JP 2011513288A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- optionally substituted
- group
- phenyl
- 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.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000002619 bicyclic group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- -1 bicyclo [2.2.1] hept-2-yl Chemical group 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 125000002843 carboxylic acid group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004185 ester group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 claims 1
- 125000006554 (C4-C8) cycloalkenyl group Chemical group 0.000 claims 1
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 claims 1
- 125000006334 2,4-difluoro benzoyl group Chemical group [H]C1=C([H])C(C(*)=O)=C(F)C([H])=C1F 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 108090000371 Esterases Proteins 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 235000008206 alpha-amino acids Nutrition 0.000 claims 1
- 150000001371 alpha-amino acids Chemical class 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- MDEJDVFJIGMTIC-UHFFFAOYSA-N cyclopentyl 2-[2-[4-[2-amino-3-(2,4-difluorobenzoyl)-6-oxopyridin-1-yl]-3,5-difluorophenyl]ethylamino]-2-methylpropanoate Chemical compound C1CCCC1OC(=O)C(C)(C)NCCC(C=C1F)=CC(F)=C1N(C(C=C1)=O)C(N)=C1C(=O)C1=CC=C(F)C=C1F MDEJDVFJIGMTIC-UHFFFAOYSA-N 0.000 claims 1
- 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
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003884 phenylalkyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 150000003568 thioethers Chemical class 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
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 | ||
| 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 true JP2011513288A5 (https=) | 2012-04-12 |
| JP5555186B2 JP5555186B2 (ja) | 2014-07-23 |
Family
ID=40585513
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 (https=) |
| EP (1) | EP2245012B1 (https=) |
| JP (1) | JP5555186B2 (https=) |
| ES (1) | ES2427892T3 (https=) |
| WO (1) | WO2009106844A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2605727T3 (es) * | 2006-05-04 | 2017-03-16 | Chroma Therapeutics Limited | Inhibidores de MAP cinasa p38 |
| 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 |
| HUE046132T2 (hu) | 2012-10-17 | 2020-02-28 | Macrophage Pharma Ltd | N-[2-{4-[6-amino-5-(2,4-difluor-benzoil)-2-oxopiridin-1(2H)-il]-3,5-difluor-fenil}etil]-l-alanin és annak tercbutil-észtere |
| GB201306901D0 (en) * | 2013-04-16 | 2013-05-29 | Chroma Therapeutics Ltd | Combination |
| WO2017223284A1 (en) | 2016-06-23 | 2017-12-28 | University Of Maryland, Baltimore | 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 |
| AU2019392904B9 (en) * | 2018-12-07 | 2022-12-22 | University Of Maryland, Baltimore | Non-ATP/catalytic site p38 mitogen activated protein kinase inhibitors |
| EP4153303A1 (en) | 2020-05-18 | 2023-03-29 | GEN1E Lifesciences Inc. | P38alpha mitogen-activated protein kinase inhibitors |
| EP4237415A1 (en) | 2020-10-29 | 2023-09-06 | GEN1E Lifesciences Inc. | Crystalline 5-(dimethylamino)-n-(4-(morpholinomethyl)phenyl) naphthalene-1-sulfonamide di-hydrochloride di-hydrate |
| WO2022204046A1 (en) | 2021-03-23 | 2022-09-29 | Gen1E Lifesciences Inc. | Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| MXPA04008822A (es) * | 2002-03-14 | 2004-11-26 | Bayer Healthcare Ag | Aroilpiridinonas monociclicas. |
| US20060235012A1 (en) | 2003-06-16 | 2006-10-19 | Chroma Therapeutics Limited | Carboline and betacarboline derivatives for use as hdac enzyme inhibitors |
| CN101123878A (zh) | 2003-07-29 | 2008-02-13 | 信号研发控股有限责任公司 | 氨基酸前药 |
| EP3075247B1 (en) | 2004-02-02 | 2022-10-12 | BioSight Ltd. | Conjugates for cancer therapy and diagnosis |
| ES2540987T3 (es) * | 2004-05-14 | 2015-07-15 | Millennium Pharmaceuticals, Inc. | Métodos para preparar inhibidores de la aurora cinasa |
| BRPI0610368A8 (pt) | 2005-05-05 | 2015-09-08 | Glaxosmithkline Ip Dev Ltd | Modulação de enzima e de receptor |
| ES2605727T3 (es) * | 2006-05-04 | 2017-03-16 | Chroma Therapeutics Limited | Inhibidores de MAP cinasa p38 |
| GB0621830D0 (en) | 2006-11-02 | 2006-12-13 | Chroma Therapeutics Ltd | Inhibitors of p38 mitogen-activated protein kinase |
| EP2220044A1 (en) | 2007-11-07 | 2010-08-25 | Chroma Therapeutics Limited | P38 map kinase inhibitors |
-
2009
- 2009-02-27 US US12/867,774 patent/US8778953B2/en active Active
- 2009-02-27 EP EP09713855.6A patent/EP2245012B1/en not_active Not-in-force
- 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 ES ES09713855T patent/ES2427892T3/es active Active
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