JP2019519616A5 - - Google Patents
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- Publication number
- JP2019519616A5 JP2019519616A5 JP2019520504A JP2019520504A JP2019519616A5 JP 2019519616 A5 JP2019519616 A5 JP 2019519616A5 JP 2019520504 A JP2019520504 A JP 2019520504A JP 2019520504 A JP2019520504 A JP 2019520504A JP 2019519616 A5 JP2019519616 A5 JP 2019519616A5
- Authority
- JP
- Japan
- Prior art keywords
- heterocyclyl
- carbocyclyl
- alkyl
- heteroaryl
- aryl
- 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
- 150000001875 compounds Chemical class 0.000 claims description 55
- 125000000217 alkyl group Chemical group 0.000 claims description 34
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 125000001424 substituent group Chemical group 0.000 claims description 17
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 125000002947 alkylene group Chemical group 0.000 claims description 9
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 125000004122 cyclic group Chemical group 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 150000001450 anions Chemical class 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000003386 piperidinyl group Chemical group 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims description 4
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims description 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 4
- -1 R 5 Chemical compound 0.000 claims description 4
- 125000004450 alkenylene group Chemical group 0.000 claims description 4
- 125000004419 alkynylene group Chemical group 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000005647 linker group Chemical group 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 208000023504 respiratory system disease Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 2
- 239000003153 chemical reaction reagent Substances 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 230000008878 coupling Effects 0.000 claims description 2
- 238000010168 coupling process Methods 0.000 claims description 2
- 238000005859 coupling reaction Methods 0.000 claims description 2
- 230000000155 isotopic effect Effects 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000004014 thioethyl group Chemical group [H]SC([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004055 thiomethyl group Chemical group [H]SC([H])([H])* 0.000 claims description 2
- 238000011200 topical administration Methods 0.000 claims description 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 239000000126 substance Substances 0.000 description 11
- 125000001054 5 membered carbocyclic group Chemical group 0.000 description 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 description 1
- 125000002837 carbocyclic group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1610854.0 | 2016-06-21 | ||
| GBGB1610854.0A GB201610854D0 (en) | 2016-06-21 | 2016-06-21 | Compounds |
| PCT/GB2017/051815 WO2017221008A1 (en) | 2016-06-21 | 2017-06-21 | Compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019519616A JP2019519616A (ja) | 2019-07-11 |
| JP2019519616A5 true JP2019519616A5 (cg-RX-API-DMAC7.html) | 2020-08-06 |
| JP7012078B2 JP7012078B2 (ja) | 2022-02-10 |
Family
ID=56895059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019520504A Active JP7012078B2 (ja) | 2016-06-21 | 2017-06-21 | 化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10759785B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3472154B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP7012078B2 (cg-RX-API-DMAC7.html) |
| GB (1) | GB201610854D0 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2017221008A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201619694D0 (en) * | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
| GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
| GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
| GB201908453D0 (en) | 2019-06-12 | 2019-07-24 | Enterprise Therapeutics Ltd | Compounds for treating respiratory disease |
| EP3983389A1 (en) | 2019-06-12 | 2022-04-20 | Tmem16A Limited | Compounds for treating respiratory disease |
| GB201910608D0 (en) * | 2019-07-24 | 2019-09-04 | Enterprise Therapeutics Ltd | Compounds |
| EP4052760B1 (en) | 2019-10-31 | 2024-03-13 | FUJIFILM Corporation | Pyrazine derivative or salt thereof, and use of same |
| EP4190402B1 (en) | 2020-07-30 | 2025-08-27 | FUJIFILM Corporation | Nitrogen-containing heterocyclic compound or salt thereof, use thereof, and intermediate thereof |
| WO2022123314A1 (en) | 2020-12-11 | 2022-06-16 | Tmem16A Limited | Benzimidazole derivatives for treating respiratory disease |
| WO2022159028A2 (en) * | 2021-01-25 | 2022-07-28 | Phamri Norden Ab | Method of treating a skin disorder |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
| US6858614B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenolic guanidine sodium channel blockers |
| US6903105B2 (en) | 2003-02-19 | 2005-06-07 | Parion Sciences, Inc. | Sodium channel blockers |
| US20050090505A1 (en) * | 2003-08-18 | 2005-04-28 | Johnson Michael R. | Methods of reducing risk of infection from pathogens |
| EP2465852A1 (en) | 2003-08-18 | 2012-06-20 | Parion Sciences, Inc. | Capped pyrazinoylguanidine sodium channel blockers |
| WO2005025496A2 (en) | 2003-08-18 | 2005-03-24 | Parion Sciences, Inc. | Aliphatic pyrazinoylguanidine sodium channel blockers |
| JP2007502829A (ja) | 2003-08-18 | 2007-02-15 | パリオン・サイエンシィズ・インコーポレーテッド | 環状ピラジノイルグアニジンナトリウムチャネルブロッカー |
| US7745442B2 (en) | 2003-08-20 | 2010-06-29 | Parion Sciences, Inc. | Methods of reducing risk of infection from pathogens |
| US7399766B2 (en) | 2004-08-18 | 2008-07-15 | Parion Sciences, Inc. | Soluble amide & ester pyrazinoylguanidine sodium channel blockers |
| US7807834B2 (en) | 2005-08-03 | 2010-10-05 | Parion Sciences, Inc. | Capped pyrazinoylguanidine sodium channel blockers |
| GB0526240D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| GB0526244D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| EP2049043B1 (en) | 2006-07-24 | 2018-10-10 | International Stem Cell Corporation | Synthetic cornea from retinal stem cells |
| WO2008124491A1 (en) | 2007-04-03 | 2008-10-16 | Parion Sciences, Inc. | Pyrazinoylguanidine compounds for use taste modulators |
| PT2155721E (pt) | 2007-05-07 | 2011-05-09 | Novartis Ag | Compostos org?nicos |
| NZ585789A (en) | 2007-12-10 | 2012-03-30 | Novartis Ag | Pyrazine-2-carboxamide derivatives to treat diseases mediated by blockade of the epithelial sodium channel |
| AR070527A1 (es) | 2008-02-26 | 2010-04-14 | Johnson Michael R | Bloqueadores poliaromaticos del canal de sodio |
| KR20110011621A (ko) | 2008-05-13 | 2011-02-08 | 노파르티스 아게 | ３，５―디아미노―６―클로로―피라진―２―카르복실산 유도체 및 기도 질환의 치료를 위한 상피 나트륨 채널 차단제로서의 이들의 용도 |
| 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 |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| US8372845B2 (en) | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
| AR086745A1 (es) | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida |
| DK2773633T3 (da) | 2011-11-02 | 2017-11-13 | Boehringer Ingelheim Int | Heterocykliske forbindelser, medikamenter indeholdende forbindelserne, anvendelse deraf og fremgangsmåder til fremstilling deraf. |
| US8859559B2 (en) | 2011-12-20 | 2014-10-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
| AU2013267504B2 (en) | 2012-05-29 | 2017-11-02 | Parion Sciences, Inc. | Dendrimer like amino amides possessing sodium channel blocker activity for the treatment of dry eye and other mucosal diseases |
| 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 |
| ES2674665T3 (es) | 2012-12-17 | 2018-07-03 | Parion Sciences, Inc. | Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida |
| CN108658876A (zh) | 2012-12-17 | 2018-10-16 | 帕里昂科学公司 | 3,5-二氨基-6-氯-n-(n-(4-苯基丁基)甲脒基)吡嗪-2-甲酰胺化合物 |
| HUE032891T2 (hu) | 2012-12-17 | 2017-11-28 | Parion Sciences Inc | Klórpirazin-karboxamid-származékok nem kielégítõ nyálkahártya-hidratáció által elõsegített megbetegedések kezelésére |
| WO2014177469A1 (en) | 2013-04-30 | 2014-11-06 | Boehringer Ingelheim International Gmbh,M | Diaminopyrazine compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
| JP2016525508A (ja) | 2013-07-02 | 2016-08-25 | ザ カリフォルニア インスティテュート フォー バイオメディカル リサーチ | 嚢胞性線維症の処置のための化合物 |
| WO2015003958A1 (en) | 2013-07-08 | 2015-01-15 | Boehringer Ingelheim International Gmbh | Amiloride-type compounds as inhibitors in epithelial sodium channels for the treatment of diseases of the lungs and airways |
| WO2015007517A1 (en) | 2013-07-15 | 2015-01-22 | Boehringer Ingelheim International Gmbh | Novel tetra- and pentasubstituted benzimidazolium compounds |
| EP3022196B1 (en) | 2013-07-15 | 2017-09-06 | Boehringer Ingelheim International GmbH | Novel benzimidazolium compounds |
| JP6461948B2 (ja) * | 2013-07-15 | 2019-01-30 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規５−置換ベンゾイミダゾリウム化合物 |
| EP3030555B1 (en) | 2013-08-08 | 2019-01-30 | Boehringer Ingelheim International GmbH | Novel pyrazine amide compounds |
| WO2016113167A1 (en) | 2015-01-12 | 2016-07-21 | Boehringer Ingelheim International Gmbh | Substituted benzimidazolium compounds useful in the treatment of respiratory diseases |
| WO2017028926A1 (en) | 2015-08-20 | 2017-02-23 | Boehringer Ingelheim International Gmbh | Novel annelated benzamides |
| BR112018001035A2 (pt) * | 2015-08-20 | 2018-12-04 | Boehringer Ingelheim International Gmbh | compostos de fenoxiacetamidas aneladas, sal farmaceuticamente aceitável, seu método de síntese, combinação de medicamento e uso dos mesmos |
| GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
-
2016
- 2016-06-21 GB GBGB1610854.0A patent/GB201610854D0/en not_active Ceased
-
2017
- 2017-06-21 EP EP17734416.5A patent/EP3472154B1/en active Active
- 2017-06-21 JP JP2019520504A patent/JP7012078B2/ja active Active
- 2017-06-21 WO PCT/GB2017/051815 patent/WO2017221008A1/en not_active Ceased
- 2017-06-21 US US16/312,158 patent/US10759785B2/en active Active
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