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 (enExample) | 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 (enExample) |
| EP (1) | EP3030555B1 (enExample) |
| JP (1) | JP6449880B2 (enExample) |
| WO (1) | WO2015018754A1 (enExample) |
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 |
| AU2017314083B2 (en) | 2016-08-15 | 2020-12-10 | Bayer Aktiengesellschaft | Condensed bicyclic heterocycle derivatives as pest control agents |
| GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
| GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
| BR112020009361A2 (pt) | 2017-11-17 | 2020-10-13 | Cellix Bio Private Limited | composto de fórmula i, composição farmacêutica para tratar um distúrbio ocular ou complicações do mesmo, método de síntese de composto, método de tratamento de um distúrbio ocular ou complicações do mesmo em um indivíduo que precisa do mesmo e uso de um composto |
| GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101312968A (zh) * | 2005-09-23 | 2008-11-26 | 记忆药物公司 | 吲唑、苯并噻唑、苯并异噻唑、苯并异噁唑、吡唑并吡啶、异噻唑并吡啶及其制备和用途 |
| CN101679266B (zh) * | 2007-03-01 | 2015-05-06 | 诺华股份有限公司 | Pim激酶抑制剂及其应用方法 |
| CA2680366C (en) * | 2007-03-09 | 2016-06-21 | University Health Network | Inhibitors of carnitine palmitoyltransferase and treating cancer |
| KR20110040818A (ko) * | 2008-06-10 | 2011-04-20 | 노파르티스 아게 | 상피 나트륨 채널 차단제로서의 피라진 유도체 |
| 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 |
| WO2014044849A1 (en) * | 2012-09-24 | 2014-03-27 | 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 JP JP2016532337A patent/JP6449880B2/ja active Active
- 2014-08-01 WO PCT/EP2014/066606 patent/WO2015018754A1/en not_active Ceased
- 2014-08-07 US US14/453,642 patent/US9096548B2/en active Active
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