CA2854217C - Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof - Google Patents

Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof Download PDF

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Publication number
CA2854217C
CA2854217C CA2854217A CA2854217A CA2854217C CA 2854217 C CA2854217 C CA 2854217C CA 2854217 A CA2854217 A CA 2854217A CA 2854217 A CA2854217 A CA 2854217A CA 2854217 C CA2854217 C CA 2854217C
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Prior art keywords
alkyl
compound
acid
phenyl
amino
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Expired - Fee Related
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CA2854217A
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English (en)
French (fr)
Other versions
CA2854217A1 (en
Inventor
Armin Heckel
Sara Frattini
Dieter Hamprecht
Joerg Kley
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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Publication of CA2854217A1 publication Critical patent/CA2854217A1/en
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Publication of CA2854217C publication Critical patent/CA2854217C/en
Expired - Fee Related legal-status Critical Current
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Infusion, Injection, And Reservoir Apparatuses (AREA)
  • Hydrogenated Pyridines (AREA)
CA2854217A 2011-11-02 2012-10-29 Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof Expired - Fee Related CA2854217C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11187553.0 2011-11-02
EP11187553 2011-11-02
PCT/EP2012/071352 WO2013064450A1 (en) 2011-11-02 2012-10-29 Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof

Publications (2)

Publication Number Publication Date
CA2854217A1 CA2854217A1 (en) 2013-05-10
CA2854217C true CA2854217C (en) 2019-12-31

Family

ID=47073464

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2854217A Expired - Fee Related CA2854217C (en) 2011-11-02 2012-10-29 Substituted pyrazinoylguanidine compounds and their use as epithelial sodium channel blockers, medicaments containing said compounds and processes for the preparation thereof

Country Status (34)

Country Link
US (4) US8759349B2 (https=)
EP (1) EP2773633B1 (https=)
JP (1) JP6091513B2 (https=)
KR (1) KR102006612B1 (https=)
CN (2) CN104024244B (https=)
AP (1) AP2014007670A0 (https=)
AU (1) AU2012331274B2 (https=)
BR (1) BR112014010583A2 (https=)
CA (1) CA2854217C (https=)
CL (1) CL2014001047A1 (https=)
CO (1) CO6940429A2 (https=)
CY (1) CY1120974T1 (https=)
DK (1) DK2773633T3 (https=)
EA (1) EA025158B9 (https=)
EC (1) ECSP14001929A (https=)
ES (1) ES2645744T3 (https=)
GE (2) GEP20186880B (https=)
HR (1) HRP20171614T1 (https=)
HU (1) HUE034929T2 (https=)
IL (1) IL232035A (https=)
LT (1) LT2773633T (https=)
ME (1) ME02905B (https=)
MX (1) MX348522B (https=)
NO (1) NO2773633T3 (https=)
PE (1) PE20141607A1 (https=)
PH (1) PH12014500970B1 (https=)
PL (1) PL2773633T3 (https=)
PT (1) PT2773633T (https=)
RS (1) RS56498B1 (https=)
SG (1) SG11201401907TA (https=)
SI (1) SI2773633T1 (https=)
TN (1) TN2014000180A1 (https=)
UA (1) UA115868C2 (https=)
WO (1) WO2013064450A1 (https=)

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EP3219705B1 (en) 2005-12-28 2020-03-11 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
KR102006612B1 (ko) * 2011-11-02 2019-08-02 베링거 인겔하임 인터내셔날 게엠베하 헤테로사이클릭 화합물, 상기 화합물을 포함하는 약제, 이의 용도, 및 이의 제조 방법
AU2014284268A1 (en) * 2013-07-02 2016-01-07 The California Institute For Biomedical Research Compounds for treatment of cystic fibrosis
EP3019492B1 (en) 2013-07-08 2017-09-06 Boehringer Ingelheim International GmbH Amiloride-type compounds as inhibitors in epithelial sodium channels for the treatment of diseases of the lungs and airways
CN107250113B (zh) 2014-10-07 2019-03-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调节蛋白的调节剂的共晶
CA2965467A1 (en) 2014-10-24 2016-04-28 Ono Pharmaceutical Co., Ltd. Kcnq2-5 channel activator
HK1246718A1 (zh) * 2015-01-07 2018-09-14 斯克利普斯研究所 用於治疗囊性纤维化的化合物
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
JP2023541601A (ja) 2020-09-10 2023-10-03 プレシリックス・ナームローゼ・ベンノートシヤープ Fapに対する抗体フラグメント
CN112107580A (zh) * 2020-09-29 2020-12-22 北京鑫开元医药科技有限公司 一种脾酪氨酸激酶抑制剂的制剂组合物及其制备方法
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
CA3251753A1 (en) 2022-05-02 2023-11-09 Precirix N.V. PRE-TARGETTING
WO2024243025A1 (en) * 2023-05-19 2024-11-28 Ikena Oncology, Inc. Naphthyl-substituted pyrido[4,3-d]pyrimidines and related compounds and their use in treating medical conditions

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NL6812003A (https=) 1967-09-07 1969-03-11
US3953476A (en) 1971-12-27 1976-04-27 Merck & Co., Inc. 3-Amino-5-sulfonylbenzoic acids
KR20020038694A (ko) 1999-07-19 2002-05-23 프란시스 제이 메이어 소듐 채널 차단제의 콘쥬게이트 및 그 이용방법
JP2003520042A (ja) 2000-01-24 2003-07-02 アイシス・ファーマシューティカルス・インコーポレーテッド 誘導性一酸化窒素シンターゼ発現のアンチセンスモジュレーション
US7956059B2 (en) 2004-08-18 2011-06-07 Parion Sciences, Inc. Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
US20080124276A1 (en) * 2006-07-24 2008-05-29 Lifeline Cell Technology Synthetic cornea from retinal stem cells
DE602008005140D1 (de) * 2007-05-07 2011-04-07 Novartis Ag Organische verbindungen
MX2010006421A (es) 2007-12-10 2010-06-25 Novartis Ag Compuestos organicos.
CA2723938A1 (en) * 2008-05-13 2009-11-19 Novartis Ag 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of airway diseases
JP2011522860A (ja) 2008-06-10 2011-08-04 ノバルティス アーゲー 上皮性ナトリウムチャネルブロッカーとしてのピラジン誘導体
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
CN103687488B (zh) 2011-06-27 2015-06-10 帕里昂科学公司 化学和代谢稳定的具有钠通道阻滞剂活性的二肽
KR102006612B1 (ko) * 2011-11-02 2019-08-02 베링거 인겔하임 인터내셔날 게엠베하 헤테로사이클릭 화합물, 상기 화합물을 포함하는 약제, 이의 용도, 및 이의 제조 방법
CA2854221A1 (en) 2011-11-02 2013-05-10 Boehringer Ingelheim International Gmbh Novel process for the preparation of acylguanidines and acylthioureas

Also Published As

Publication number Publication date
JP2014534222A (ja) 2014-12-18
HK1196819A1 (zh) 2014-12-24
EP2773633A1 (en) 2014-09-10
US8759349B2 (en) 2014-06-24
IL232035A0 (en) 2014-05-28
NO2773633T3 (https=) 2017-12-30
CN104024244A (zh) 2014-09-03
US9920035B2 (en) 2018-03-20
ECSP14001929A (es) 2015-11-30
PT2773633T (pt) 2017-11-14
US20130109697A1 (en) 2013-05-02
IL232035A (en) 2017-05-29
CN106279110B (zh) 2019-12-10
AU2012331274A1 (en) 2014-04-03
CA2854217A1 (en) 2013-05-10
US20180194747A1 (en) 2018-07-12
US20140228374A1 (en) 2014-08-14
CL2014001047A1 (es) 2014-11-07
TN2014000180A1 (en) 2015-09-30
DK2773633T3 (da) 2017-11-13
MX2014005166A (es) 2014-05-28
AP2014007670A0 (en) 2014-05-31
BR112014010583A2 (pt) 2020-04-22
HRP20171614T1 (hr) 2017-12-01
JP6091513B2 (ja) 2017-03-08
EA025158B1 (ru) 2016-11-30
WO2013064450A1 (en) 2013-05-10
NZ622469A (en) 2016-08-26
PL2773633T3 (pl) 2018-01-31
AU2012331274B2 (en) 2017-06-08
GEAP201813485A (en) 2018-04-10
HUE034929T2 (en) 2018-03-28
ES2645744T3 (es) 2017-12-07
PH12014500970B1 (en) 2017-10-06
GEP20186880B (en) 2018-07-25
EA201400521A1 (ru) 2014-09-30
EP2773633B1 (en) 2017-08-02
UA115868C2 (uk) 2018-01-10
CO6940429A2 (es) 2014-05-09
CN106279110A (zh) 2017-01-04
SG11201401907TA (en) 2014-05-29
KR102006612B1 (ko) 2019-08-02
PE20141607A1 (es) 2014-11-23
CY1120974T1 (el) 2019-12-11
EA025158B9 (ru) 2018-03-30
LT2773633T (lt) 2017-11-10
RS56498B1 (sr) 2018-01-31
MX348522B (es) 2017-06-16
US20150336933A1 (en) 2015-11-26
KR20140085498A (ko) 2014-07-07
CN104024244B (zh) 2016-09-14
PH12014500970A1 (en) 2014-06-09
SI2773633T1 (sl) 2017-11-30
ME02905B (me) 2018-10-20

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EEER Examination request

Effective date: 20171030

MKLA Lapsed

Effective date: 20211029