AR062741A1 - Metodo para aumentar la hidratacion de la mucosa y la evacuacion de l a mucosa mediante tratamiento con bloquadores de los canales del sodio y osmolitos - Google Patents

Metodo para aumentar la hidratacion de la mucosa y la evacuacion de l a mucosa mediante tratamiento con bloquadores de los canales del sodio y osmolitos

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Publication number
AR062741A1
AR062741A1 ARP070103971A ARP070103971A AR062741A1 AR 062741 A1 AR062741 A1 AR 062741A1 AR P070103971 A ARP070103971 A AR P070103971A AR P070103971 A ARP070103971 A AR P070103971A AR 062741 A1 AR062741 A1 AR 062741A1
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Argentina
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chor8
independently
nr7r10
ch2or8
ch2ch2o
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ARP070103971A
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English (en)
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Hirsh Andrew J
Boucher Richard C
Johnson Michael R
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Application filed by Hirsh Andrew J, Boucher Richard C, Johnson Michael R filed Critical Hirsh Andrew J
Publication of AR062741A1 publication Critical patent/AR062741A1/es

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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/12—Mucolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • 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
    • A61P27/04—Artificial tears; Irrigation solutions
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

Métodos y composiciones para tratar enfermedades mejoradas por una mayor depuracion mucociliar e hidratacion de la mucosa administrando una cantidad eficaz de un bloqueador de los canales de sodio segun lo definido en la presente y un osmolito a un sujeto que necesita una mayor depuracion mucociliar e hidratacion de la mucosa. Reivindicacion 14: Una composicion que comprende (a) un bloqueador de los canales de sodio representado por la formula (1) en la cual X es H, halogeno, trifluormetilo, alquilo inferior, fenilo sin sustituir o sustituido, alquilo inferior-tio, fenil-alquilo inferior-tio, alquilo inferior-sulfonilo, o fenil-alquilo inferior-sulfonilo; Y es H, hidroxilo, mercapto, alcoxi inferior, alquilo inferior-tio, halogeno, alquilo inferior, arilo mononuclear sin sustituir o sustituido, o -N(R2)2; R1 es H o alquilo inferior; cada R2 es, independientemente, -R7, -(CH2)m-OR8, -(CH2)m-NR7R10, -(CH2)n(CHOR8)(CHOR8)n-CH2OR8, -(CH2CH2O)m-R8, -(CH2CH2O)m-CH2CH2NR7R10, -(CH2)n- C(=O)NR7R10, -(CH2)n-Zg-R7, -(CH2)m-NR10-CH2(CHOR8)(CHOR8)n-CH2OR8, -(CH2)n-CO2R7, o como en formula (2); R3 y R4 son en forma individual e independientemente, H, un grupo representado por la formula (3), alquilo inferior, hidroxi alquilo inferior, fenilo, fenilalquilo inferior, (halofenil)-alquilo inferior, (alquilfenilalquilo)-inferior, (alcoxifenilo)inferior-alquilo inferior, naftil-alquilo inferior, o piridil-alquilo inferior, con la condicion de que por lo menos uno de R3 y R4 es un grupo representado por la formula (3) en la cual cada RL es, independientemente -R7, -(CH2)n-OR8, -O-(CH2)m-OR8, -(CH2)n-NR7R10, -O-(CH2)m-NR7R10, (CH2)n(CHOR8)(CHOR8)n-CH2OR8, -O-(CH2)m(CHOR8)(CHOR8)n-CH2OR8, -(CH2CH2O)m-R8, -O-(CH2CH2O)m-R8, -(CH2CH2O)m- CH2CH2NR7R10, -O-(CH2CH2O)m-CH2CH2NR7R10, -(CH2)n-C(=O)NR7R10, -O-(CH2)m-C(=O)NR7R10, -(CH2)n-(Z)g-R7, -O-(CH2)m-(Z)g-R7, -(CH2)n-NR10-CH2(CHOR8)(CHOR8)n-CH2OR8, -O-(CH2)m-NR10-CH2(CHOR8)(CHOR8)n-CH2OR8, -(CH2)n-CO2R7, -O-(CH2)m-CO2R7, -OSO3H, -O- glucuronido, -O-glucosa, formulas (4) o (2), cada o es, independientemente, un numero entero del 0 al 10; cada p es un numero entero del 0 al 10; con la condicion de que la suma de o y p en cada cadena contigua sea del 1 al 10; cada x es, independientemente, O, NR10, C(=O), CHOH, C(=N-R10), CHNR7R10, o representa un enlace simple; cada R5 es, independientemente, -(CH2)m-OR8, -O-(CH2)m-OR8, -(CH2)n-NR7R10, -O-(CH2)m-NR7R10, (CH2)n(CHOR8)(CHOR8)n-CH2OR8, -O-(CH2)m(CHOR8)(CHOR8)n- CH2OR8, -(CH2CH2O)m-R8, -O-(CH2CH2O)m-R8, -(CH2CH2O)m-CH2CH2NR7R10, -O-(CH2CH2O)m-CH2CH2NR7R10, -(CH2)n-C(=O)NR7R10, -O-(CH2)m-C(=O)NR7R10, -(CH2)n-(Z)g-R7, -O-(CH2)m-(Z)g-R7, -(CH2)n-NR10-CH2(CHOR8)(CHOR8)n-CH2OR8, -O-(CH2)m-NR10-CH2(CHOR8)(CHOR8)n- CH2OR8, -(CH2)n-CO2R7, -O-(CH2)m-CO2R7, -OSO3H, -O-glucuronido, -O-glucosa, formulas (4), (2),o (5); cada R6 es, independientemente -R7, -OR11, -N(R7)2, -(CH2)m-OR8, -O-(CH2)m-OR8, -(CH2)n-NR7R10, -O-(CH2)m-NR7R10, (CH2)n(CHOR8)(CHOR8)n-CH2OR8, -O- (CH2)m(CHOR8)(CHOR8)n-CH2OR8, -(CH2CH2O)m-R8, -O-(CH2CH2O)m-R8, -(CH2CH2O)m-CH2CH2NR7R10, -O-(CH2CH2O)m-CH2CH2NR7R10, -(CH2)n-C(=O)NR7R10, -O-(CH2)m-C(=O)NR7R10, -(CH2)n-(Z)g-R7, -O-(CH2)m-(Z)g-R7, -(CH2)n-NR10-CH2(CHOR8)(CHOR8)n-CH2OR8, -O-(CH2)m- NR10-CH2(CHOR8)(CHOR8)n-CH2OR8, -(CH2)n-CO2R7, -O-(CH2)m-CO2R7, -OSO3H, -O-glucuronido, -O-glucosa, formulas (4) o (2), en la cual cuando dos R6 son -OR11 y están ubicados en forma adyacente entre sí en un anillo de fenilo, las porciones alquilo de los dos R6 pueden estar enlazadas entre sí para formar un grupo metilendioxi, cada R7 es, independientemente, H o alquilo inferior; cada R8 es, independientemente, H, alquilo inferior, -C(=O)-R11, glucuronido, 2-tetrahidropiranilo, o formula (5); cada R9 es, independientemente -CO2R7, -CON(R7)2, -SO2CH3, o -C(=O)R7; cada R10 es, independientemente, H, -SO2CH3, -CO2R7, -C(=O)NR7R9, -C(=O)R7, o -CH2-(CHOH)n-CH2OH; cada Z es, independientemente, CHOH, C(=O), CHNR7R10, C=NR10, o NR10; cada R11 es, independientemente, alquilo inferior; cada g es, independientemente, un numero entero del 1 al 6; cada m es, independientemente, un numero entero del 1 al 7; cada n es, independientemente, un numero entero del 0 al 7; cada Q es, independientemente, C-R5, C-R6, o un átomo de N, donde como mucho tres Q en un anillo son átomos de N y por lo menos una Q es C-R5; o su sal farmacéuticamente aceptable, incluyendo a todos los enantiomeros, diastereomeros y mezclas racémicas de los mismos; y (b) un compuesto osmoticamente activo. Reivindicacion 17: La composicion de acuerdo con la reivindicacion 14, donde el bloqueador de los canales de sodio representado por la formula (1) es como en el grupo de formulas (6).
ARP070103971A 2006-09-07 2007-09-07 Metodo para aumentar la hidratacion de la mucosa y la evacuacion de l a mucosa mediante tratamiento con bloquadores de los canales del sodio y osmolitos AR062741A1 (es)

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US84517106P 2006-09-18 2006-09-18

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US (1) US8058278B2 (es)
EP (1) EP2059237A4 (es)
JP (1) JP2010502738A (es)
KR (1) KR20090065508A (es)
AR (1) AR062741A1 (es)
AU (1) AU2007294547A1 (es)
BR (1) BRPI0716884A2 (es)
CA (1) CA2663041A1 (es)
EA (1) EA200970258A1 (es)
MX (1) MX2009002602A (es)
TW (1) TW200817343A (es)
WO (1) WO2008031028A2 (es)

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TW200817343A (en) 2008-04-16
WO2008031028A2 (en) 2008-03-13
MX2009002602A (es) 2009-05-28
AU2007294547A2 (en) 2009-03-19
AU2007294547A1 (en) 2008-03-13
BRPI0716884A2 (pt) 2013-10-15
WO2008031028A3 (en) 2008-11-13
CA2663041A1 (en) 2008-03-13
EA200970258A1 (ru) 2009-08-28
US8058278B2 (en) 2011-11-15
EP2059237A2 (en) 2009-05-20
KR20090065508A (ko) 2009-06-22
US20080090841A1 (en) 2008-04-17
JP2010502738A (ja) 2010-01-28

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