AR076373A1 - N-pirazolil carboxamidas como inhibidores de canales de calcio - Google Patents

N-pirazolil carboxamidas como inhibidores de canales de calcio

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Publication number
AR076373A1
AR076373A1 ARP100101334A ARP100101334A AR076373A1 AR 076373 A1 AR076373 A1 AR 076373A1 AR P100101334 A ARP100101334 A AR P100101334A AR P100101334 A ARP100101334 A AR P100101334A AR 076373 A1 AR076373 A1 AR 076373A1
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AR
Argentina
Prior art keywords
alkyl
group
halogen
formula
alkoxy
Prior art date
Application number
ARP100101334A
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English (en)
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Glaxo Group Ltd
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Publication date
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Publication of AR076373A1 publication Critical patent/AR076373A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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Abstract

Se refiere a compuestos de amida, a procedimientos para su preparacion, a composiciones farmacéuticas que contienen estos compuestos y a su uso en el tratamiento de trastornos, afecciones o trastornos tales como trastornos alérgicos, trastornos inflamatorios y trastornos del sistema inmune. Reivindicacion 1: Un compuesto de formula (1) o un profármaco del mismo en la que Ra es un grupo de formula (2) en la que R1a es alquilo C1-6, CF3, OCF3, alcoxi C1-6 o R1a es un grupo L1-Z1 en el que L1 es O, CH2, OCH2 o CH2O y Z1 es cicloalquilo C3-7 o arilo; o Ra es un grupo de formula (3) en la que R2a es halogeno, alquilo C1-6, CF3 u OCH2Ph; y R3a es halogeno, alquilo C1-6, alcoxi C1-6, hidroxi, cicloalquilo C3-7, CO2alquiIo C1-4 o R3a es un grupo L2-Z2 en el que L2 es O, CH2 u O(CH2)n en el que n es un numero entero de 1-7; y Z2 es hidroxi, metoxi, CO2alquilo C1-4, cicloalquilo C3-7, arilo o heteroarilo; o Ra es un grupo de formula (4) en la que R4a es halogeno, alquilo C1-6, alcoxi C1-6, CF3 u OCH2Ph; y R5a es halogeno, alquilo C1-6, hidroxi, alcoxi C1-6 opcionalmente sustituido con metoxi, o R5a es un grupo L3-Z3 en el que L3 es un enlace sencillo, O, CH2, OCH2 o CH2O y Z3 es cicloalquilo C3-7, arilo o heteroarilo; Ra es un grupo de formula (5) en la que R6a es CI, Br, alquilo C1-6 o CF3; y R7a es halogeno, alquilo C1-6, CF3, OCF3, OCHF2, alcoxi C1-6 o R7a es un grupo L4-Z4 en el que L4 es OCH2 y Z4 es cicloalquilo C3-7; Rb es un grupo de formula (6) en la que Y es CH o N, R1b es halogeno, alquilo C1-6 o CF3; R2b es H, halogeno, alquilo C1-6 o alcoxi C1-6 o una sal del mismo sujeto a la condicion de que no sea un compuesto seleccionado entre 2,6-Difluoro-N-{1-[(2-metilfenil)metil]-1H-pirazol-3-il}benzamida; 2-Fluoro-N-{1-[(2-metilfenil)metil]-1H-pirazol-3-iI}benzamida; 2,6-Dicloro-N-{1-[(2-metilfenil)metil]-1H-pirazol-3-il}benzamida; 2-Metil-N-{1-[(2-metilfenil]-1H-pirazol-3-il}benzamida; y 2-Bromo-N-[1-{(2,5-diclorofenil)metil]-1H-pirazol-3-iI}benzamida.
ARP100101334A 2009-04-24 2010-04-22 N-pirazolil carboxamidas como inhibidores de canales de calcio AR076373A1 (es)

Applications Claiming Priority (2)

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US17228509P 2009-04-24 2009-04-24
US29580110P 2010-01-18 2010-01-18

Publications (1)

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AR076373A1 true AR076373A1 (es) 2011-06-08

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ARP100101334A AR076373A1 (es) 2009-04-24 2010-04-22 N-pirazolil carboxamidas como inhibidores de canales de calcio

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US (2) US8399436B2 (es)
EP (1) EP2421835A1 (es)
JP (1) JP2012524755A (es)
AR (1) AR076373A1 (es)
TW (1) TW201103892A (es)
UY (1) UY32571A (es)
WO (1) WO2010122089A1 (es)

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EP2421835A1 (en) 2012-02-29
WO2010122089A1 (en) 2010-10-28
US8399436B2 (en) 2013-03-19
TW201103892A (en) 2011-02-01
US20100273744A1 (en) 2010-10-28

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