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 |
|---|---|---|---|
| GBGB1610854.0A GB201610854D0 (en) | 2016-06-21 | 2016-06-21 | Compounds |
| GB1610854.0 | 2016-06-21 | ||
| 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 (enExample) | 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 (enExample) |
| EP (1) | EP3472154B1 (enExample) |
| JP (1) | JP7012078B2 (enExample) |
| GB (1) | GB201610854D0 (enExample) |
| WO (1) | WO2017221008A1 (enExample) |
Families Citing this family (11)
| 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 |
| GB201801355D0 (en) | 2018-01-26 | 2018-03-14 | 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 |
| AU2020290049A1 (en) | 2019-06-12 | 2022-02-03 | 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 |
| JP7598380B2 (ja) | 2020-07-30 | 2024-12-11 | 富士フイルム株式会社 | 含窒素複素環化合物またはその塩、その利用、およびその中間体 |
| JP2023552638A (ja) | 2020-12-11 | 2023-12-18 | ティーエムイーエム１６エー リミテッド | 呼吸器疾患を治療するためのベンゾイミダゾール誘導体 |
| 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 |
| AU2004266704B2 (en) | 2003-08-18 | 2012-02-23 | Parion Sciences, Inc. | Capped pyrazinoylguanidine sodium channel blockers |
| AU2004271945A1 (en) | 2003-08-18 | 2005-03-24 | Parion Sciences, Inc. | Aliphatic pyrazinoylguanidine sodium channel blockers |
| US20050090505A1 (en) | 2003-08-18 | 2005-04-28 | Johnson Michael R. | Methods of reducing risk of infection from pathogens |
| CA2534569A1 (en) | 2003-08-18 | 2005-02-24 | Parion Sciences, Inc. | Cyclic pyrazinoylguanidine sodium channel blockers |
| 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 |
| EP2484308A1 (en) | 2006-07-24 | 2012-08-08 | 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 |
| US8318935B2 (en) | 2007-05-07 | 2012-11-27 | Novartis Ag | Organic compounds 75074 |
| EP2231280B1 (en) | 2007-12-10 | 2016-08-10 | Novartis AG | Amiloride-like Pyrazine-carboxamides as ENaC blockers |
| EP2257296B1 (en) | 2008-02-26 | 2014-05-07 | Parion Sciences, Inc. | Poly aromatic sodium channel blockers |
| CN102015662A (zh) | 2008-05-13 | 2011-04-13 | 诺瓦提斯公司 | 3,5-二氨基-6-氯-吡嗪-2-甲酸衍生物和它们作为上皮钠通道阻断剂用于治疗气道疾病的用途 |
| BRPI0915018A2 (pt) | 2008-06-10 | 2015-10-27 | Novartis Ag | compostos orgânicos |
| 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 |
| SI2773633T1 (sl) | 2011-11-02 | 2017-11-30 | Boehringer Ingelheim International Gmbh | Heterociklične spojine, zdravila, ki vsebujejo te spojine, njihova uporaba in postopki za njihovo pripravo |
| US8859559B2 (en) | 2011-12-20 | 2014-10-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
| EA201990616A3 (ru) | 2012-05-29 | 2019-12-30 | Парион Сайэнс, Инк. | Дендримероподобные аминоамиды, обладающие активностью блокаторов натриевых каналов, для лечения сухости глаз и других заболеваний слизистых оболочек |
| US8841309B2 (en) | 2012-09-24 | 2014-09-23 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
| CN105073717B (zh) | 2012-12-17 | 2018-05-22 | 帕里昂科学公司 | 可用于治疗由黏膜水化不足造成的疾病的氯-吡嗪甲酰胺衍生物 |
| 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 |
| EP2991981B1 (en) | 2013-04-30 | 2017-03-01 | Boehringer Ingelheim International GmbH | Diaminopyrazine compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof |
| CN105518000B (zh) | 2013-07-02 | 2018-09-14 | 加州生物医学研究所 | 用于治疗囊性纤维化的化合物 |
| JP6449870B2 (ja) | 2013-07-08 | 2019-01-09 | 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 | 肺および気道の疾患を処置するための上皮性ナトリウムチャネルの阻害剤としてのアミロライド型化合物 |
| EP3022197B1 (en) | 2013-07-15 | 2017-09-06 | Boehringer Ingelheim International GmbH | Novel tetra- and pentasubstituted benzimidazolium compounds |
| JP6461134B2 (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 | 新規ベンゾイミダゾリウム化合物 |
| EP3022198B1 (en) * | 2013-07-15 | 2019-09-11 | Boehringer Ingelheim International GmbH | Novel 5-substituted benzimidazolium compounds |
| WO2015018754A1 (en) | 2013-08-08 | 2015-02-12 | Boehringer Ingelheim International Gmbh | Novel pyrazine amide compounds |
| US10155749B2 (en) | 2015-01-12 | 2018-12-18 | Boehringer Ingelheim International Gmbh | Substituted benzimidazolium compounds useful in the treatment of respiratory diseases |
| JP6620171B2 (ja) * | 2015-08-20 | 2019-12-11 | 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 | 新規縮環フェノキシアセトアミド |
| CN108135897B (zh) | 2015-08-20 | 2021-07-27 | 勃林格殷格翰国际有限公司 | 稠合的苯甲酰胺 |
| 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 JP JP2019520504A patent/JP7012078B2/ja active Active
- 2017-06-21 WO PCT/GB2017/051815 patent/WO2017221008A1/en not_active Ceased
- 2017-06-21 EP EP17734416.5A patent/EP3472154B1/en active Active
- 2017-06-21 US US16/312,158 patent/US10759785B2/en active Active
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