PE20090733A1 - Derivados de pirazina como bloqueadores de los canales de sodio epitelial - Google Patents

Derivados de pirazina como bloqueadores de los canales de sodio epitelial

Info

Publication number
PE20090733A1
PE20090733A1 PE2008000782A PE2008000782A PE20090733A1 PE 20090733 A1 PE20090733 A1 PE 20090733A1 PE 2008000782 A PE2008000782 A PE 2008000782A PE 2008000782 A PE2008000782 A PE 2008000782A PE 20090733 A1 PE20090733 A1 PE 20090733A1
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PE
Peru
Prior art keywords
bis
diil
azan
methylen
alkyl
Prior art date
Application number
PE2008000782A
Other languages
English (en)
Inventor
Robin Alec Fairhurst
Rebecca Butler
Paul Joseph Oakley
Sthephen Paul Collingwood
Nichola Smith
Emily Stanley
Perez Maria Ines Rodriguez
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20090733A1 publication Critical patent/PE20090733A1/es

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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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE PIRAZINA DE FORMULA (I), DONDE M1 Y M2 SON UNA ESTRUCTURA DE FORMULA (a); R1, R2, R3 Y R4 SON H, ALQUILO C1-C8, HALOALQUILO C1-C8, ALCOXILO C1-C8, ENTRE OTROS; T ES H, HALOGENO, ALQUILO C1-C8, HALOALCOXILO C1-C8, ENTRE OTROS; L1 Y L2 SE SELECCIONAN DE (i) y (ii); R5, R5a Y R6 SON H, ALQUILO C1-C8, CN, ENTRE OTROS; W1 Y W2 SON ALQUILENO C2-C8; X1 Y X2 SON UN GRUPO HETEROCICLICO DE 4 A 14 MIEMBROS; Y1 Y Y2 SON ALQUILENO C0-C8 O ALQUILO C1-C8-AMINO; A ES UN GRUPO CARBOCICLICO AROMATICO DE 6 A 15 MIEMBROS, -C(=O), -CO-(ALQUILENO C1-C8)-CO-, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N,N-(1,1'-(1,4-FENILEN-BIS-(METILEN))-BIS-(AZAN-DIIL)-BIS-(OXO-METILEN)-BIS-(PIPERIDIN-4,1-DIIL))-BIS-(AZAN-DIIL)-BIS-(IMINO-METILEN)-BIS-(3,5-DIAMINO-6-CLORO-PIRAZIN-2-CARBOXAMIDA), N,N-(1,1'-(1,4-FENILEN-BIS-(AZAN-DIIL))-BIS-(OXO-METILEN)-BIS-(PIPERIDIN-4,1-DIIL))-BIS-(AZAN-DIIL)-BIS-(IMINO-METILEN)-BIS-(3,5-DIAMINO-6-CLORO-PIRAZIN-2-CARBOXAMIDA), N,N-(1,1'-(CILOHEXAN-1,3-DIIL-BIS-(METILEN))-BIS-(AZAN-DIIL)-BIS-(OXO-METILEN)-BIS-(PIPERIDIN-4,1-DIIL))-BIS-(AZAN-DIIL)-BIS-(IMINO-METILEN)-BIS-(3,5-DIAMINO-6-CLORO-PIRAZIN-2-CARBOXAMIDA), ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON BLOQUEADORES DEL CANAL DE SODIO EPITELIAL (ENaC) Y SON UTILES EN EL TRATAMIENTO DE FIBROSIS QUISTICA, DISQUINESIA CILIAR PRIMARIA, BROQUITIS CRONICA, CARCINOMA PULMONAR, ENTRE OTROS
PE2008000782A 2007-05-07 2008-05-05 Derivados de pirazina como bloqueadores de los canales de sodio epitelial PE20090733A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07107654 2007-05-07

Publications (1)

Publication Number Publication Date
PE20090733A1 true PE20090733A1 (es) 2009-07-17

Family

ID=38581916

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000782A PE20090733A1 (es) 2007-05-07 2008-05-05 Derivados de pirazina como bloqueadores de los canales de sodio epitelial

Country Status (32)

Country Link
US (1) US8318935B2 (es)
EP (2) EP2155721B1 (es)
JP (1) JP5244904B2 (es)
KR (1) KR20100005730A (es)
CN (1) CN101687851B (es)
AR (1) AR066458A1 (es)
AT (1) ATE499363T1 (es)
AU (1) AU2008248598B2 (es)
BR (1) BRPI0811562A2 (es)
CA (1) CA2685546A1 (es)
CL (1) CL2008001301A1 (es)
CO (1) CO6290667A2 (es)
CR (1) CR11091A (es)
DE (1) DE602008005140D1 (es)
EA (1) EA200901489A1 (es)
EC (1) ECSP099718A (es)
ES (1) ES2361595T3 (es)
GT (1) GT200900289A (es)
HK (1) HK1141285A1 (es)
HN (1) HN2009003214A (es)
IL (1) IL201828A0 (es)
MA (1) MA31400B1 (es)
MX (1) MX2009012077A (es)
NZ (1) NZ580737A (es)
PE (1) PE20090733A1 (es)
PL (1) PL2155721T3 (es)
PT (1) PT2155721E (es)
SV (1) SV2009003406A (es)
TN (1) TN2009000469A1 (es)
TW (1) TWI351402B (es)
WO (1) WO2008135557A1 (es)
ZA (1) ZA200907491B (es)

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WO2008135557A1 (en) 2008-11-13
EP2155721B1 (en) 2011-02-23
JP2010526118A (ja) 2010-07-29
KR20100005730A (ko) 2010-01-15
MX2009012077A (es) 2009-11-19
CR11091A (es) 2009-12-17
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CO6290667A2 (es) 2011-06-20
ZA200907491B (en) 2010-07-28
ECSP099718A (es) 2009-12-28
CA2685546A1 (en) 2008-11-13
CN101687851B (zh) 2013-02-27
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AU2008248598B2 (en) 2011-11-17
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EA200901489A1 (ru) 2010-04-30
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