JP7269923B2 - 呼吸器疾患治療のためのＥＮａＣ阻害剤としてのビス（ペンタヒドロキシヘキシル）アミノ置換された２－｛［（３－アミノ－ピラジン－２－イル）ホルムアミド］メチル｝－１Ｈ－１，３－ベンゾジアゾール－３－イウム誘導体 - Google Patents

呼吸器疾患治療のためのＥＮａＣ阻害剤としてのビス（ペンタヒドロキシヘキシル）アミノ置換された２－｛［（３－アミノ－ピラジン－２－イル）ホルムアミド］メチル｝－１Ｈ－１，３－ベンゾジアゾール－３－イウム誘導体 Download PDF

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JP7269923B2
JP7269923B2 JP2020521539A JP2020521539A JP7269923B2 JP 7269923 B2 JP7269923 B2 JP 7269923B2 JP 2020521539 A JP2020521539 A JP 2020521539A JP 2020521539 A JP2020521539 A JP 2020521539A JP 7269923 B2 JP7269923 B2 JP 7269923B2
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methyl
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アレクサンダー ヘイ ダンカン
ボーレガード スコフィールド トーマス
ウェント ナオミ
マッカーティー クリーブ
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エンタープライズ セラピューティクス リミテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/12—Mucolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020521539A 2017-10-17 2018-10-17 呼吸器疾患治療のためのＥＮａＣ阻害剤としてのビス（ペンタヒドロキシヘキシル）アミノ置換された２－｛［（３－アミノ－ピラジン－２－イル）ホルムアミド］メチル｝－１Ｈ－１，３－ベンゾジアゾール－３－イウム誘導体 Active JP7269923B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1717051.5 2017-10-17
GBGB1717051.5A GB201717051D0 (en) 2017-10-17 2017-10-17 Compounds
PCT/GB2018/052983 WO2019077340A1 (en) 2017-10-17 2018-10-17 BIS (PENTAHYDROXYHEXYL) AMINO-SUBSTITUTED 2 - {[(3-AMINO-PYRAZIN-2-YL) FORMAMIDO] METHYL} -1H-1,3-BENZODIAZOL-3-IUM DERIVATIVES AS ENAC INHIBITORS FOR TREATMENT OF RESPIRATORY DISEASES

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JP2020537658A JP2020537658A (ja) 2020-12-24
JP2020537658A5 JP2020537658A5 (cg-RX-API-DMAC10.html) 2021-12-09
JP7269923B2 true JP7269923B2 (ja) 2023-05-09

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US (1) US11370778B2 (cg-RX-API-DMAC10.html)
EP (1) EP3697788B1 (cg-RX-API-DMAC10.html)
JP (1) JP7269923B2 (cg-RX-API-DMAC10.html)
GB (1) GB201717051D0 (cg-RX-API-DMAC10.html)
WO (1) WO2019077340A1 (cg-RX-API-DMAC10.html)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220050126A (ko) 2019-06-12 2022-04-22 티엠이엠16에이 리미티드 호흡기 질환을 치료하기 위한 화합물
GB201908453D0 (en) 2019-06-12 2019-07-24 Enterprise Therapeutics Ltd Compounds for treating respiratory disease
TW202237090A (zh) 2020-12-11 2022-10-01 英商Ｔｍｅｍ16Ａ有限公司 治療呼吸道疾病之化合物
KR20250130409A (ko) * 2023-01-11 2025-09-01 젠맵 에이/에스 링커, 약물 링커 및 그의 접합체 및 그의 사용 방법

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011079087A1 (en) 2009-12-23 2011-06-30 Glaxo Group Limited Enac blockers
JP2014518268A (ja) 2011-06-27 2014-07-28 パリオン・サイエンシィズ・インコーポレーテッド ３，５−ジアミノ−６−クロロ−ｎ−（ｎ−（４−（４−（２−（ヘキシル（２，３，４，５，６−ペンタヒドロキシヘキシル）アミノ）エトキシ）フェニル）ブチル）カルバミミドイル）ピラジン−２−カルボキサミド
JP2016503028A (ja) 2012-12-17 2016-02-01 パリオン・サイエンシィズ・インコーポレーテッド 粘膜への水分付与が不十分であることが好都合である疾患の治療に有用なクロロ−ピラジンカルボキサミド誘導体
JP2016503027A (ja) 2012-12-17 2016-02-01 パリオン・サイエンシィズ・インコーポレーテッド ３，５−ジアミノ−６−クロロ−ｎ−（ｎ−（４−フェニルブチル）カルバムイミドイル）ピラジン−２−カルボキサミド化合物
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
WO2018096325A1 (en) 2016-11-22 2018-05-31 Enterprise Therapeutics Limited Benzodiazolium compounds as enac inhibitors

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6858614B2 (en) 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenolic guanidine sodium channel blockers
US6858615B2 (en) 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
US6903105B2 (en) 2003-02-19 2005-06-07 Parion Sciences, Inc. Sodium channel blockers
CA2534568A1 (en) 2003-08-18 2005-03-24 Parion Sciences, Inc. Aliphatic pyrazinoylguanidine sodium channel blockers
EP1670474A4 (en) 2003-08-18 2008-08-06 Parion Sciences Inc CYCLIC PYRAZINOYLGUANIDINE AS SODIUM CHANNEL BLOCKER
US20050090505A1 (en) 2003-08-18 2005-04-28 Johnson Michael R. Methods of reducing risk of infection from pathogens
AU2004266704B2 (en) 2003-08-18 2012-02-23 Parion Sciences, Inc. Capped 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
US8288391B2 (en) 2007-04-03 2012-10-16 Parion Sciences, Inc. Pyrazinoylguanidine compounds for use as taste modulators
EP2332933A1 (en) 2007-05-07 2011-06-15 Novartis AG Epithelial sodium channel (ENaC) inhibitors
WO2009019506A1 (en) 2007-08-03 2009-02-12 Astrazeneca Ab Heterocyclyc sulfonamides having edg-1 antagonistic activity
BRPI0820669A2 (pt) 2007-12-10 2020-08-04 Novartis Ag compostos orgânicos
WO2009139948A1 (en) 2008-02-26 2009-11-19 Johnson Michael R Poly aromatic sodium channel blockers
MX2010012441A (es) 2008-05-13 2010-12-06 Novartis Ag Derivados de acido 3,5-diamino-6-cloro-pirazin-2-carboxilico y su uso como bloqueadores del canal de sodio epitelial para el tratamiento de enfermedades de las vias respiratorias.
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
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
NO2773633T3 (cg-RX-API-DMAC10.html) 2011-11-02 2017-12-30
US8859559B2 (en) 2011-12-20 2014-10-14 Boehringer Ingelheim International Gmbh Substituted pyrazines and their use in the treatment of disease
WO2013181232A2 (en) 2012-05-29 2013-12-05 Michael Ross Johnson Dendrimer like amino amides possessing sodium channel blocker activity for the treatment of dry eye and other mucosal diseases
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
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
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
CA2915633A1 (en) 2013-07-02 2015-01-08 The California Institute For Biomedical Research Compounds for treatment of cystic fibrosis
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
WO2015007519A1 (en) 2013-07-15 2015-01-22 Boehringer Ingelheim International Gmbh Novel benzimidazolium compounds
EP3022197B1 (en) 2013-07-15 2017-09-06 Boehringer Ingelheim International GmbH Novel tetra- and pentasubstituted benzimidazolium compounds
WO2015007516A1 (en) 2013-07-15 2015-01-22 Boehringer Ingelheim International Gmbh Novel 5-substituted benzimidazolium compounds
EP3030555B1 (en) 2013-08-08 2019-01-30 Boehringer Ingelheim International GmbH Novel pyrazine amide compounds
US9932324B2 (en) 2015-01-12 2018-04-03 Boehringer Ingelheim International Gmbh Substituted benzimidazolium compounds useful in the treatment of respiratory diseases
EP3245200B1 (en) 2015-01-12 2021-03-10 Boehringer Ingelheim International GmbH 2-(pyrazin-2-ylcarbonylaminomethyl)benzimidazolium compounds as epithelial sodium channel inhibitors
EP3245202B1 (en) 2015-01-12 2020-03-11 Boehringer Ingelheim International GmbH Tetrasubstituted benzimidazolium compounds useful in the treatment of respiratory diseases
EP3298022B1 (en) 2015-08-20 2019-06-05 Boehringer Ingelheim International GmbH Novel annelated phenoxyacetamides
GB201610854D0 (en) 2016-06-21 2016-08-03 Entpr Therapeutics Ltd Compounds

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011079087A1 (en) 2009-12-23 2011-06-30 Glaxo Group Limited Enac blockers
JP2014518268A (ja) 2011-06-27 2014-07-28 パリオン・サイエンシィズ・インコーポレーテッド ３，５−ジアミノ−６−クロロ−ｎ−（ｎ−（４−（４−（２−（ヘキシル（２，３，４，５，６−ペンタヒドロキシヘキシル）アミノ）エトキシ）フェニル）ブチル）カルバミミドイル）ピラジン−２−カルボキサミド
JP2016503028A (ja) 2012-12-17 2016-02-01 パリオン・サイエンシィズ・インコーポレーテッド 粘膜への水分付与が不十分であることが好都合である疾患の治療に有用なクロロ−ピラジンカルボキサミド誘導体
JP2016503027A (ja) 2012-12-17 2016-02-01 パリオン・サイエンシィズ・インコーポレーテッド ３，５−ジアミノ−６−クロロ−ｎ−（ｎ−（４−フェニルブチル）カルバムイミドイル）ピラジン−２−カルボキサミド化合物
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
WO2018096325A1 (en) 2016-11-22 2018-05-31 Enterprise Therapeutics Limited Benzodiazolium compounds as enac inhibitors

Also Published As

Publication number Publication date
US11370778B2 (en) 2022-06-28
EP3697788B1 (en) 2021-12-15
US20200239442A1 (en) 2020-07-30
EP3697788A1 (en) 2020-08-26
JP2020537658A (ja) 2020-12-24
GB201717051D0 (en) 2017-11-29
WO2019077340A1 (en) 2019-04-25

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