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EA201001772A1 - Производные 3,5-диамино-6-хлорпиразин-2-карбоновой кислоты и их применение в качестве блокаторов эпителиальных натриевых каналов для лечения заболеваний дыхательных путей - Google Patents

Производные 3,5-диамино-6-хлорпиразин-2-карбоновой кислоты и их применение в качестве блокаторов эпителиальных натриевых каналов для лечения заболеваний дыхательных путей

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Publication number
EA201001772A1
EA201001772A1 EA201001772A EA201001772A EA201001772A1 EA 201001772 A1 EA201001772 A1 EA 201001772A1 EA 201001772 A EA201001772 A EA 201001772A EA 201001772 A EA201001772 A EA 201001772A EA 201001772 A1 EA201001772 A1 EA 201001772A1
Authority
EA
Eurasian Patent Office
Prior art keywords
application
diseases
treatment
chlorpyrazin
blocators
Prior art date
Application number
EA201001772A
Other languages
English (en)
Inventor
Стивен Пол Коллингвуд
Кэтрин Хаушем
Томас Антони Хант
Original Assignee
Новартис Аг
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201001772A1 publication Critical patent/EA201001772A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 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
    • C07D403/02—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В заявке описано соединение формулы Iв свободной форме или в форме соли или сольвата, в которой R, R, R, R, R, R, R, Rи Rобладают значениями, указанными в описании, применимое для лечения заболеваний, которые реагируют на блокирование эпителиальных натриевых каналов. В заявке также описаны фармацевтические композиции, которые содержат эти соединения, и способы получения этих соединений.
EA201001772A 2008-05-13 2009-05-11 Производные 3,5-диамино-6-хлорпиразин-2-карбоновой кислоты и их применение в качестве блокаторов эпителиальных натриевых каналов для лечения заболеваний дыхательных путей EA201001772A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08156060 2008-05-13
PCT/EP2009/055657 WO2009138378A1 (en) 2008-05-13 2009-05-11 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of arway diseases

Publications (1)

Publication Number Publication Date
EA201001772A1 true EA201001772A1 (ru) 2011-06-30

Family

ID=39627401

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201001772A EA201001772A1 (ru) 2008-05-13 2009-05-11 Производные 3,5-диамино-6-хлорпиразин-2-карбоновой кислоты и их применение в качестве блокаторов эпителиальных натриевых каналов для лечения заболеваний дыхательных путей

Country Status (12)

Country Link
US (1) US8664228B2 (ru)
EP (1) EP2285785B1 (ru)
JP (1) JP2011520831A (ru)
KR (1) KR20110011621A (ru)
CN (1) CN102015662A (ru)
AU (1) AU2009248179A1 (ru)
BR (1) BRPI0912542A2 (ru)
CA (1) CA2723938A1 (ru)
EA (1) EA201001772A1 (ru)
ES (1) ES2394241T3 (ru)
MX (1) MX2010012441A (ru)
WO (1) WO2009138378A1 (ru)

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US6858615B2 (en) 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
AR070527A1 (es) 2008-02-26 2010-04-14 Johnson Michael R Bloqueadores poliaromaticos del canal de sodio
EP2300010B1 (en) * 2008-06-10 2015-03-04 Novartis AG Pyrazine derivatives as epithelial sodium channel blockers
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
US9050339B2 (en) 2010-09-17 2015-06-09 Novartis Ag Pyrazine derivatives as ENaC blockers
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
WO2013038386A1 (en) * 2011-09-16 2013-03-21 Novartis Ag Heterocyclic compounds for the treatment of cystic fibrosis
CN106279110B (zh) * 2011-11-02 2019-12-10 勃林格殷格翰国际有限公司 杂环化合物、含有所述化合物的药物及其用途和其制备方法
US20130109856A1 (en) 2011-11-02 2013-05-02 Boehringer Ingelheim International Gmbh Novel process for the preparation of acylguanidines and acylthioureas
US8859559B2 (en) 2011-12-20 2014-10-14 Boehringer Ingelheim International Gmbh Substituted pyrazines and their use in the treatment of disease
EP2861577B1 (en) 2012-05-25 2017-01-04 Boehringer Ingelheim International GmbH Tertiary amines, medicaments containing said amines, use thereof and processes for the preparation thereof
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
BR112015012420A8 (pt) * 2012-11-28 2017-10-24 Gruenenthal Gmbh amino-arilcarboxamidas substituídas como moduladores de kcnq2/3
CN104995178B (zh) 2012-12-17 2018-06-26 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
AP2015008556A0 (en) 2012-12-17 2015-06-30 Parion Sciences Inc Chloro-pyrazine carboxamide derivatives useful forthe treatment of diseases favoured by insufficien t mucosal hydration
US9102633B2 (en) 2013-12-13 2015-08-11 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
UY36034A (es) 2014-03-18 2015-09-30 Astrazeneca Ab Derivados de 3,5-diamino-6-cloro-pirazina-2-carboxamida y sales farmaceuticamente aceptables de estos
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
GB201808093D0 (en) 2018-05-18 2018-07-04 Enterprise Therapeutics Ltd Compounds
US20240308954A1 (en) * 2021-03-12 2024-09-19 Biomedcode Hellas Sa Anti-inflammatory carboxamide derivatives

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4550111A (en) * 1982-01-29 1985-10-29 Imperial Chemical Industries Plc Alkanolamine derivatives
US4803206A (en) * 1988-03-07 1989-02-07 Schering Corporation Antihypertensive acylpyrazines
JP2007502827A (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 脂肪族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
EP1786427A4 (en) * 2004-08-18 2009-11-11 Michael R Johnson BLOCKERS OF SODIUM CHANNELS OF PYRAZINOYLGUANIDINE WITH AMIDE AND ALIPHATIC ESTER

Also Published As

Publication number Publication date
CN102015662A (zh) 2011-04-13
JP2011520831A (ja) 2011-07-21
ES2394241T3 (es) 2013-01-23
US20110059989A1 (en) 2011-03-10
EP2285785A1 (en) 2011-02-23
US8664228B2 (en) 2014-03-04
MX2010012441A (es) 2010-12-06
WO2009138378A1 (en) 2009-11-19
EP2285785B1 (en) 2012-09-05
KR20110011621A (ko) 2011-02-08
AU2009248179A1 (en) 2009-11-19
CA2723938A1 (en) 2009-11-19
BRPI0912542A2 (pt) 2015-10-13

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