JP2015526455A5 - - Google Patents
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- Publication number
- JP2015526455A5 JP2015526455A5 JP2015527915A JP2015527915A JP2015526455A5 JP 2015526455 A5 JP2015526455 A5 JP 2015526455A5 JP 2015527915 A JP2015527915 A JP 2015527915A JP 2015527915 A JP2015527915 A JP 2015527915A JP 2015526455 A5 JP2015526455 A5 JP 2015526455A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- ring
- group
- replaced
- cycloalkyl
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- -1 pyridine-N-oxydyl Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000002837 carbocyclic group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 229940122524 Cathepsin C inhibitor Drugs 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000027004 Eosinophilic disease Diseases 0.000 claims 1
- 208000017189 Gastrointestinal inflammatory disease Diseases 0.000 claims 1
- 229940122236 Histamine receptor antagonist Drugs 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 102100022364 Polyunsaturated fatty acid 5-lipoxygenase Human genes 0.000 claims 1
- 101710156627 Polyunsaturated fatty acid 5-lipoxygenase Proteins 0.000 claims 1
- 102000009389 Prostaglandin D receptors Human genes 0.000 claims 1
- 108050000258 Prostaglandin D receptors Proteins 0.000 claims 1
- 102000002255 Secretory Proteinase Inhibitory Proteins Human genes 0.000 claims 1
- 108010000303 Secretory Proteinase Inhibitory Proteins Proteins 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 239000003591 leukocyte elastase inhibitor Substances 0.000 claims 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims 1
- 244000000010 microbial pathogen Species 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12181541 | 2012-08-23 | ||
| EP12181541.9 | 2012-08-23 | ||
| PCT/EP2013/067427 WO2014029832A1 (en) | 2012-08-23 | 2013-08-22 | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015526455A JP2015526455A (ja) | 2015-09-10 |
| JP2015526455A5 true JP2015526455A5 (enExample) | 2016-10-13 |
| JP6278416B2 JP6278416B2 (ja) | 2018-02-14 |
Family
ID=46963419
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015527915A Active JP6278416B2 (ja) | 2012-08-23 | 2013-08-22 | 置換４−ピリドン及びそれらの好中球エラスターゼ活性阻害薬としての使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20140057920A1 (enExample) |
| EP (1) | EP2888249B1 (enExample) |
| JP (1) | JP6278416B2 (enExample) |
| WO (1) | WO2014029832A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9458113B2 (en) | 2014-07-31 | 2016-10-04 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9657015B2 (en) | 2014-07-31 | 2017-05-23 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9475779B2 (en) | 2014-07-31 | 2016-10-25 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9290457B2 (en) | 2014-07-31 | 2016-03-22 | Boehringer Ingelheim International Gmbh | Substituted dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9440930B2 (en) | 2014-07-31 | 2016-09-13 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US20220354833A1 (en) | 2019-09-17 | 2022-11-10 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| ES2962498T3 (es) | 2020-04-16 | 2024-03-19 | Mereo Biopharma 4 Ltd | Métodos que implican el inhibidor de elastasa de neutrófilos alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina |
| US11804467B2 (en) * | 2020-06-25 | 2023-10-31 | Micron Technology, Inc. | Radiative heat collective bonder and gangbonder |
| CN112920124B (zh) * | 2021-01-29 | 2024-03-01 | 安徽医科大学 | 一种嘧啶-2,4-二胺类化合物及其制备方法与应用 |
| US20240382472A1 (en) | 2021-10-20 | 2024-11-21 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4844732A (en) * | 1985-10-24 | 1989-07-04 | Daicel Chemical Industries Ltd. | Pyridine-3-carboxamide derivatives |
| WO2001068652A1 (en) | 2000-03-17 | 2001-09-20 | Novo Nordisk A/S | Condensed imidazoles as histamine h3 receptor ligands |
| US7211595B2 (en) | 2000-11-30 | 2007-05-01 | Abbott Laboratories | Farnesyltransferase inhibitors |
| TW200500341A (en) * | 2002-11-12 | 2005-01-01 | Astrazeneca Ab | Novel compounds |
| SE0302486D0 (sv) | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
| SE0302487D0 (sv) | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
| GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
| TW200700392A (en) * | 2005-03-16 | 2007-01-01 | Astrazeneca Ab | Novel compounds |
| EP1907383A1 (en) | 2005-06-30 | 2008-04-09 | Prosidion Limited | Gpcr agonists |
| TW200808771A (en) | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
| TW200808763A (en) | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds I |
| WO2009058076A1 (en) | 2007-11-02 | 2009-05-07 | Astrazeneca Ab | 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase |
| EP2217591A4 (en) | 2007-11-06 | 2011-10-26 | Astrazeneca Ab | CERTAIN 2-PYRAZINONE DERIVATIVES AND THEIR USE AS NEUTROPHILES ELASTASE INHIBITORS |
| PT2235002E (pt) * | 2008-01-23 | 2013-01-30 | Bristol Myers Squibb Co | Compostos de 4-piridinona e a sua utilização para o tratamento do cancro |
| US20090281089A1 (en) | 2008-04-11 | 2009-11-12 | Genentech, Inc. | Pyridyl inhibitors of hedgehog signalling |
| TW201036957A (en) | 2009-02-20 | 2010-10-16 | Astrazeneca Ab | Novel salt 628 |
| EP2261211A1 (en) | 2009-05-20 | 2010-12-15 | Université de Lille 2 Droit et Santé | 1,4-dihydropyridine derivatives and their uses |
| CA2773618A1 (en) | 2009-10-02 | 2011-04-07 | Astrazeneca Ab | 2-pyridone compounds used as inhibitors of neutrophil elastase |
| WO2011110852A1 (en) | 2010-03-10 | 2011-09-15 | Astrazeneca Ab | Polymorphic forms of 6- [2- (4 -cyanophenyl) - 2h - pyrazol - 3 - yl] - 5 -methyl - 3 - oxo - 4 - (trifluoromethyl - phenyl) 3,4-dihydropyrazine-2-carboxylic acid ethylamide |
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2013
- 2013-08-20 US US13/971,374 patent/US20140057920A1/en not_active Abandoned
- 2013-08-22 JP JP2015527915A patent/JP6278416B2/ja active Active
- 2013-08-22 WO PCT/EP2013/067427 patent/WO2014029832A1/en not_active Ceased
- 2013-08-22 EP EP13756033.0A patent/EP2888249B1/en active Active
-
2015
- 2015-09-02 US US14/843,254 patent/US9340507B2/en active Active