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)
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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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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

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  • 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)
  • Hydrogenated Pyridines (AREA)
  • Infusion, Injection, And Reservoir Apparatuses (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)

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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 (cg-RX-API-DMAC7.html)
EP (1) EP2773633B1 (cg-RX-API-DMAC7.html)
JP (1) JP6091513B2 (cg-RX-API-DMAC7.html)
KR (1) KR102006612B1 (cg-RX-API-DMAC7.html)
CN (2) CN106279110B (cg-RX-API-DMAC7.html)
AP (1) AP2014007670A0 (cg-RX-API-DMAC7.html)
AU (1) AU2012331274B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014010583A2 (cg-RX-API-DMAC7.html)
CA (1) CA2854217C (cg-RX-API-DMAC7.html)
CL (1) CL2014001047A1 (cg-RX-API-DMAC7.html)
CO (1) CO6940429A2 (cg-RX-API-DMAC7.html)
CY (1) CY1120974T1 (cg-RX-API-DMAC7.html)
DK (1) DK2773633T3 (cg-RX-API-DMAC7.html)
EA (1) EA025158B9 (cg-RX-API-DMAC7.html)
EC (1) ECSP14001929A (cg-RX-API-DMAC7.html)
ES (1) ES2645744T3 (cg-RX-API-DMAC7.html)
GE (1) GEP20186880B (cg-RX-API-DMAC7.html)
HR (1) HRP20171614T1 (cg-RX-API-DMAC7.html)
HU (1) HUE034929T2 (cg-RX-API-DMAC7.html)
IL (1) IL232035A (cg-RX-API-DMAC7.html)
LT (1) LT2773633T (cg-RX-API-DMAC7.html)
ME (1) ME02905B (cg-RX-API-DMAC7.html)
MX (1) MX348522B (cg-RX-API-DMAC7.html)
NO (1) NO2773633T3 (cg-RX-API-DMAC7.html)
PE (1) PE20141607A1 (cg-RX-API-DMAC7.html)
PH (1) PH12014500970B1 (cg-RX-API-DMAC7.html)
PL (1) PL2773633T3 (cg-RX-API-DMAC7.html)
PT (1) PT2773633T (cg-RX-API-DMAC7.html)
RS (1) RS56498B1 (cg-RX-API-DMAC7.html)
SG (1) SG11201401907TA (cg-RX-API-DMAC7.html)
SI (1) SI2773633T1 (cg-RX-API-DMAC7.html)
TN (1) TN2014000180A1 (cg-RX-API-DMAC7.html)
UA (1) UA115868C2 (cg-RX-API-DMAC7.html)
WO (1) WO2013064450A1 (cg-RX-API-DMAC7.html)

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HUE032813T2 (en) 2005-12-28 2017-11-28 Vertex Pharma Solid forms of N- [2,4-bis (1,1-dimethyl ethyl) -5-hydroxyphenyl] -1,4-dihydro-4-oxoquinoline-3-carboxamide
PL2773633T3 (pl) * 2011-11-02 2018-01-31 Boehringer Ingelheim Int Związki heterocykliczne, leki zawierające wymienione związki, ich zastosowanie i procesy ich wytwarzania
KR20160054460A (ko) * 2013-07-02 2016-05-16 더 캘리포니아 인스티튜트 포 바이오메디칼 리써치 낭성 섬유증의 치료를 위한 화합물
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
EP3204358B1 (en) 2014-10-07 2018-09-19 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
SG11201703284XA (en) 2014-10-24 2017-06-29 Ono Pharmaceutical Co 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
AU2021341508A1 (en) 2020-09-10 2023-05-25 Precirix N.V. Antibody fragment against fap
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
IL318992A (en) 2022-05-02 2025-04-01 Precirix N V Cancer treatment through advance directives
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 (cg-RX-API-DMAC7.html) 1967-09-07 1969-03-11
US3953476A (en) 1971-12-27 1976-04-27 Merck & Co., Inc. 3-Amino-5-sulfonylbenzoic acids
AU774865B2 (en) 1999-07-19 2004-07-08 University Of North Carolina At Chapel Hill, The Conjugates of sodium channel blockers and methods of using the same
WO2001052902A1 (en) 2000-01-24 2001-07-26 Isis Pharmaceuticals, Inc. Antisense modulation of inducible nitric oxide synthase expression
WO2006023573A2 (en) 2004-08-18 2006-03-02 Johnson Michael R Aliphatic amide & ester pyrazinoylguanidine sodium channel blockers
GB0526244D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
WO2008013557A1 (en) * 2006-07-24 2008-01-31 International Stem Cell Corporation Synthetic cornea from retinal stem cells
ATE499363T1 (de) * 2007-05-07 2011-03-15 Novartis Ag Organische verbindungen
NZ585789A (en) 2007-12-10 2012-03-30 Novartis Ag Pyrazine-2-carboxamide derivatives to treat diseases mediated by blockade of the epithelial sodium channel
EP2285785B1 (en) * 2008-05-13 2012-09-05 Novartis AG 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of arway diseases
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IL232035A0 (en) 2014-05-28
EA025158B9 (ru) 2018-03-30
MX2014005166A (es) 2014-05-28
HUE034929T2 (en) 2018-03-28
KR20140085498A (ko) 2014-07-07
JP2014534222A (ja) 2014-12-18
PH12014500970B1 (en) 2017-10-06
CA2854217A1 (en) 2013-05-10
AP2014007670A0 (en) 2014-05-31
US20180194747A1 (en) 2018-07-12
SG11201401907TA (en) 2014-05-29
JP6091513B2 (ja) 2017-03-08
GEP20186880B (en) 2018-07-25
DK2773633T3 (da) 2017-11-13
US20150336933A1 (en) 2015-11-26
EP2773633A1 (en) 2014-09-10
ME02905B (me) 2018-10-20
PT2773633T (pt) 2017-11-14
KR102006612B1 (ko) 2019-08-02
UA115868C2 (uk) 2018-01-10
PH12014500970A1 (en) 2014-06-09
MX348522B (es) 2017-06-16
SI2773633T1 (sl) 2017-11-30
RS56498B1 (sr) 2018-01-31
TN2014000180A1 (en) 2015-09-30
ECSP14001929A (es) 2015-11-30
AU2012331274A1 (en) 2014-04-03
IL232035A (en) 2017-05-29
EP2773633B1 (en) 2017-08-02
US20130109697A1 (en) 2013-05-02
BR112014010583A2 (pt) 2020-04-22
NZ622469A (en) 2016-08-26
PL2773633T3 (pl) 2018-01-31
ES2645744T3 (es) 2017-12-07
LT2773633T (lt) 2017-11-10
CL2014001047A1 (es) 2014-11-07
NO2773633T3 (cg-RX-API-DMAC7.html) 2017-12-30
US20140228374A1 (en) 2014-08-14
CN106279110B (zh) 2019-12-10
CN104024244A (zh) 2014-09-03
EA201400521A1 (ru) 2014-09-30
CY1120974T1 (el) 2019-12-11
AU2012331274B2 (en) 2017-06-08
HK1196819A1 (zh) 2014-12-24
US9920035B2 (en) 2018-03-20
PE20141607A1 (es) 2014-11-23
CN104024244B (zh) 2016-09-14
CN106279110A (zh) 2017-01-04
EA025158B1 (ru) 2016-11-30
WO2013064450A1 (en) 2013-05-10
CO6940429A2 (es) 2014-05-09
HRP20171614T1 (hr) 2017-12-01
US8759349B2 (en) 2014-06-24

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