CN110214141B - 作为ENaC抑制剂的苯并二唑鎓化合物 - Google Patents

作为ENaC抑制剂的苯并二唑鎓化合物 Download PDF

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Publication number
CN110214141B
CN110214141B CN201780084165.3A CN201780084165A CN110214141B CN 110214141 B CN110214141 B CN 110214141B CN 201780084165 A CN201780084165 A CN 201780084165A CN 110214141 B CN110214141 B CN 110214141B
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amino
methyl
pyrrolo
pyrazin
carboxamido
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Chinese (zh)
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CN110214141A (zh
Inventor
C·麦卡锡
J·D·哈格雷夫
D·A·哈伊
T·B·斯科菲尔德
N·温特
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Enterprise Therapeutics Ltd
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Enterprise Therapeutics Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/12Mucolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201780084165.3A 2016-11-22 2017-11-22 作为ENaC抑制剂的苯并二唑鎓化合物 Active CN110214141B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1619694.1 2016-11-22
GBGB1619694.1A GB201619694D0 (en) 2016-11-22 2016-11-22 Compounds
PCT/GB2017/053499 WO2018096325A1 (en) 2016-11-22 2017-11-22 Benzodiazolium compounds as enac inhibitors

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CN110214141A CN110214141A (zh) 2019-09-06
CN110214141B true CN110214141B (zh) 2022-05-31

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US (4) US10941149B2 (enExample)
EP (1) EP3544981B1 (enExample)
JP (1) JP6980014B2 (enExample)
KR (1) KR102517273B1 (enExample)
CN (1) CN110214141B (enExample)
AU (1) AU2017364308B2 (enExample)
CA (1) CA3043132A1 (enExample)
DK (1) DK3544981T3 (enExample)
EA (1) EA039607B1 (enExample)
ES (1) ES2890226T3 (enExample)
GB (1) GB201619694D0 (enExample)
HU (1) HUE055692T2 (enExample)
IL (1) IL266745B (enExample)
MA (1) MA46878A (enExample)
MX (1) MX389496B (enExample)
PL (1) PL3544981T3 (enExample)
PT (1) PT3544981T (enExample)
TW (1) TWI756305B (enExample)
WO (1) WO2018096325A1 (enExample)
ZA (1) ZA201902710B (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201610854D0 (en) 2016-06-21 2016-08-03 Entpr Therapeutics Ltd Compounds
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
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
CN118852442A (zh) 2023-04-26 2024-10-29 上海麦科思生物医药有限公司 抗ptk7抗体及其用途
GB202406247D0 (en) 2024-05-03 2024-06-19 Enterprise Therapeutics Ltd Compounds and pharmaceutical compositions

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101142194A (zh) * 2005-03-14 2008-03-12 特兰斯泰克制药公司 吲哚衍生物,组合物及用作β-分泌酶抑制剂的方法
WO2016113167A1 (en) * 2015-01-12 2016-07-21 Boehringer Ingelheim International Gmbh Substituted benzimidazolium compounds useful in the treatment of respiratory diseases

Family Cites Families (47)

* 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
CA2534569A1 (en) 2003-08-18 2005-02-24 Parion Sciences, Inc. Cyclic pyrazinoylguanidine sodium channel blockers
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
AU2004271945A1 (en) 2003-08-18 2005-03-24 Parion Sciences, Inc. Aliphatic pyrazinoylguanidine sodium channel blockers
US7745442B2 (en) 2003-08-20 2010-06-29 Parion Sciences, Inc. Methods of reducing risk of infection from pathogens
WO2005042497A2 (en) * 2003-10-28 2005-05-12 Vertex Pharmaceuticals, Incorporated Benzimidazoles useful as modulators of ion channels
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
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
WO2009019506A1 (en) 2007-08-03 2009-02-12 Astrazeneca Ab Heterocyclyc sulfonamides having edg-1 antagonistic activity
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
TW201204353A (en) * 2010-06-08 2012-02-01 Vertex Pharma Formulations of (R)-1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
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
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
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
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
JP6667538B2 (ja) 2015-01-12 2020-03-18 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 呼吸器系疾患の治療に有用な置換ベンズイミダゾリウム化合物
WO2016113169A1 (en) 2015-01-12 2016-07-21 Boehringer Ingelheim International Gmbh Tetra- and pentasubstituted 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
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
GB201610854D0 (en) * 2016-06-21 2016-08-03 Entpr Therapeutics Ltd Compounds
GB201619694D0 (en) * 2016-11-22 2017-01-04 Entpr Therapeutics Ltd Compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101142194A (zh) * 2005-03-14 2008-03-12 特兰斯泰克制药公司 吲哚衍生物,组合物及用作β-分泌酶抑制剂的方法
WO2016113167A1 (en) * 2015-01-12 2016-07-21 Boehringer Ingelheim International Gmbh Substituted benzimidazolium compounds useful in the treatment of respiratory diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Novel small molecule epithelial sodium channel inhibitors as potential therapeutics in cystic fibrosis - a patent evaluation;SCHOENBERGER,等;《EXPERT OPIN. THER. PATENTS》;20131231;第23卷(第10期);第1383-1389页 *

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IL266745A (en) 2019-07-31
US12371436B2 (en) 2025-07-29
US10941149B2 (en) 2021-03-09
MX389496B (es) 2025-03-20
KR20190084076A (ko) 2019-07-15
ES2890226T3 (es) 2022-01-18
TWI756305B (zh) 2022-03-01
KR102517273B1 (ko) 2023-04-03
WO2018096325A1 (en) 2018-05-31
PL3544981T3 (pl) 2021-12-20
US20210147432A1 (en) 2021-05-20
CA3043132A1 (en) 2018-05-31
GB201619694D0 (en) 2017-01-04
MA46878A (fr) 2019-10-02
JP2019535747A (ja) 2019-12-12
CN110214141A (zh) 2019-09-06
US20250304590A1 (en) 2025-10-02
NZ753048A (en) 2024-09-27
EP3544981A1 (en) 2019-10-02
BR112019009864A2 (pt) 2019-08-27
EA201991253A1 (ru) 2019-11-29
AU2017364308A1 (en) 2019-05-23
PT3544981T (pt) 2021-09-23
TW201833111A (zh) 2018-09-16
JP6980014B2 (ja) 2021-12-15
EA039607B1 (ru) 2022-02-16
AU2017364308B2 (en) 2021-03-11
DK3544981T3 (da) 2021-09-20
US20190315757A1 (en) 2019-10-17
MX2019005934A (es) 2019-11-12
IL266745B (en) 2021-12-01
US11739094B2 (en) 2023-08-29
ZA201902710B (en) 2021-10-27
EP3544981B1 (en) 2021-06-23
US20240067653A1 (en) 2024-02-29
HUE055692T2 (hu) 2021-12-28

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