JP2016529248A5 - - Google Patents
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- Publication number
- JP2016529248A5 JP2016529248A5 JP2016532337A JP2016532337A JP2016529248A5 JP 2016529248 A5 JP2016529248 A5 JP 2016529248A5 JP 2016532337 A JP2016532337 A JP 2016532337A JP 2016532337 A JP2016532337 A JP 2016532337A JP 2016529248 A5 JP2016529248 A5 JP 2016529248A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- optionally
- membered heterocyclyl
- independently selected
- 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 53
- 125000001424 substituent group Chemical group 0.000 claims 48
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000003386 piperidinyl group Chemical group 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 125000002757 morpholinyl group Chemical group 0.000 claims 16
- 125000004193 piperazinyl group Chemical group 0.000 claims 16
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 16
- -1 trifluoroacetate ion Chemical class 0.000 claims 11
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- PNHZYFXCSQLDHY-UHFFFAOYSA-N 1,2,3,5-tetrahydroimidazo[1,2-a]pyrazine Chemical compound C1C=NC=C2NCCN21 PNHZYFXCSQLDHY-UHFFFAOYSA-N 0.000 claims 8
- 125000002883 imidazolyl group Chemical group 0.000 claims 8
- 125000001041 indolyl group Chemical group 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims 8
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 8
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 206010006451 bronchitis Diseases 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 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 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 3
- 230000000172 allergic effect Effects 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims 2
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical compound C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 206010052613 Allergic bronchitis Diseases 0.000 claims 1
- 206010001889 Alveolitis Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009137 Chronic sinusitis Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims 1
- 241000233866 Fungi Species 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 229940122696 MAP kinase inhibitor Drugs 0.000 claims 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims 1
- 102100029438 Nitric oxide synthase, inducible Human genes 0.000 claims 1
- 101710089543 Nitric oxide synthase, inducible Proteins 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 206010037423 Pulmonary oedema Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 1
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 1
- 201000009267 bronchiectasis Diseases 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 1
- 229940000425 combination drug Drugs 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 239000002713 epithelial sodium channel blocking agent Substances 0.000 claims 1
- 201000001155 extrinsic allergic alveolitis Diseases 0.000 claims 1
- 244000000013 helminth Species 0.000 claims 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 208000022098 hypersensitivity pneumonitis Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 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
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- 208000037916 non-allergic rhinitis Diseases 0.000 claims 1
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 208000015768 polyposis Diseases 0.000 claims 1
- 208000005333 pulmonary edema Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 239000000021 stimulant Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 239000003848 thrombocyte activating factor antagonist Substances 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13179737.5 | 2013-08-08 | ||
| EP13179737 | 2013-08-08 | ||
| PCT/EP2014/066606 WO2015018754A1 (en) | 2013-08-08 | 2014-08-01 | Novel pyrazine amide compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016529248A JP2016529248A (ja) | 2016-09-23 |
| JP2016529248A5 true JP2016529248A5 (cg-RX-API-DMAC7.html) | 2017-09-14 |
| JP6449880B2 JP6449880B2 (ja) | 2019-01-09 |
Family
ID=48917461
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016532337A Active JP6449880B2 (ja) | 2013-08-08 | 2014-08-01 | 新規ピラジンアミド化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9096548B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3030555B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6449880B2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2015018754A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201610854D0 (en) | 2016-06-21 | 2016-08-03 | Entpr Therapeutics Ltd | Compounds |
| CN109996799B (zh) | 2016-08-15 | 2022-07-19 | 拜耳作物科学股份公司 | 作为害虫防治剂的稠合双环杂环衍生物 |
| GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
| GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
| JP7006990B2 (ja) | 2017-11-17 | 2022-02-10 | セリックス バイオ プライヴェート リミテッド | 眼障害の処置のための組成物及び方法 |
| GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009509964A (ja) * | 2005-09-23 | 2009-03-12 | メモリー・ファーマシューティカルズ・コーポレイション | インダゾール類、ベンゾチアゾール類、ベンゾイソオキサゾール類、ピラゾロピリジン類、イソチアゾロピリジン類、およびそれらの製造と用途 |
| CA2679659C (en) * | 2007-03-01 | 2016-01-19 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| CA2680366C (en) * | 2007-03-09 | 2016-06-21 | University Health Network | Inhibitors of carnitine palmitoyltransferase and treating cancer |
| AU2009256645A1 (en) * | 2008-06-10 | 2009-12-17 | Novartis Ag | Pyrazine derivatives as epithelial sodium channel blockers |
| WO2011028740A1 (en) * | 2009-09-03 | 2011-03-10 | Glaxo Group Limited | ENaC BLOCKERS |
| WO2011079087A1 (en) * | 2009-12-23 | 2011-06-30 | Glaxo Group Limited | Enac blockers |
| AU2012321111A1 (en) * | 2011-10-31 | 2013-05-16 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
| US8859559B2 (en) * | 2011-12-20 | 2014-10-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
| EP2897940B1 (en) * | 2012-09-24 | 2019-05-01 | Boehringer Ingelheim International GmbH | Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
-
2014
- 2014-08-01 EP EP14745155.3A patent/EP3030555B1/en active Active
- 2014-08-01 WO PCT/EP2014/066606 patent/WO2015018754A1/en not_active Ceased
- 2014-08-01 JP JP2016532337A patent/JP6449880B2/ja active Active
- 2014-08-07 US US14/453,642 patent/US9096548B2/en active Active