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AR034269A1 - Nuevos 7-azaindoles, su uso como inhibidores de la fosfodiesterasa 4 y el procedimiento para su preparacion, los medicamentos que los contienen y su preparacion - Google Patents

Nuevos 7-azaindoles, su uso como inhibidores de la fosfodiesterasa 4 y el procedimiento para su preparacion, los medicamentos que los contienen y su preparacion

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Publication number
AR034269A1
AR034269A1 ARP010105014A ARP010105014A AR034269A1 AR 034269 A1 AR034269 A1 AR 034269A1 AR P010105014 A ARP010105014 A AR P010105014A AR P010105014 A ARP010105014 A AR P010105014A AR 034269 A1 AR034269 A1 AR 034269A1
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AR
Argentina
Prior art keywords
alkyl
aryl
mono
polysubstituted
unsubstituted
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ARP010105014A
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English (en)
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Elbion Ag
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Priority claimed from DE10053275A external-priority patent/DE10053275A1/de
Application filed by Elbion Ag filed Critical Elbion Ag
Publication of AR034269A1 publication Critical patent/AR034269A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

Se describen 7-azaindoles de fórmula (1), en la cual: n puede ser 1 ó 2; y R1 es a) alquilo C1-10, de cadena recta o ramificada, insustituido o mono o polisustituido con -OH, -SH, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NH-arilo C6-14, -N(arilo C6-14)2, -N(alquil C1-6)(arilo C6-14), -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo C1-6, -O-arilo C6-14, -S-alquilo C1-6, -S-arilo C6-14, -SO3H, -SO2-alquilo C1-6, -SO2-arilo C6-14, -OSO2alquilo C1-6, -OSO2arilo C6-14, -COOH, -C(O)alquilo C1-5, con carbociclos mono, bi o tricíclicos saturados o mono o poliinsaturados con 3-14 miembros del anillo, con heterociclos mono, bi o tricíclicos saturados o mono o poliinsaturados con 5-15 miembros del anillo y 1-6 heteroátomos que preferentemente son N, O y S, donde los grupos arilo C6-14 y los sustituyentes carbocíclicos y heterocíclicos pueden estar, a su vez, insustituidos o mono o polisustituidos con R4; ó b) alquenilo C2-10, mono o poliinsaturado, de cadena recta o ramificada, insustituido o mono o polisustituido con -OH, -SH, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NH-arilo C6-14, -N(arilo C6-14)2, -N(alquil C1-6)(arilo C6-14), -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo C1-6, -O-arilo C6-14, -S-alquilo C1-6, -S-arilo C6-14, -SO3H, -SO2-alquilo C1-6, -SO2-arilo C6-14, -OSO2alquilo C1-6, -OSO2arilo C6-14, -COOH, -C(O)alquilo C1-5, con carbociclos mono, bi o tricíclicos saturados o mono o poliinsaturados con 3-14 miembros del anillo, con heterociclos mono, bi o tricíclicos saturados o mono o poliinsaturados con 5-15 miembros del anillo y 1-6 heteroátomos que preferentemente son N, O y S, donde los grupos arilo C6-14 y los sustituyentes carbocíclicos y heterocíclicos pueden estar, a su vez, insustituidos o mono o polisustituidos con R4; R2 y R3 pueden ser iguales o diferentes, donde sólo uno de los dos puede ser hidrógeno, y R2 y R3 pueden ser, además, a) alquilo C1-5, insustituido o mono o polisustituido con -OH, -SH, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo C1-6, -S-alquilo C1-6, -fenilo, y -piridilo; b) fenilo, insustituido o mono o polisustituido con -OH, -SH, -NH2, -NH-alquilo C1-3, -N(alquilo C1-3)2, -NO2, -CN, -COOH, -COOalquilo C1-3, -F, -Cl, -Br, -O-alquilo C1-3, y -S-alquilo C1-3; c) piridilo, insustituido o mono o polisustituido con -NO2, -CN, -COOH, -COOalquilo C1-3, -Cl, -Br, -O-alquilo C1-3, y -S-alquilo C1-3; así como d) un compuesto seleccionado de las fórmulas (2) a (5); además el grupo -NR2R3 puede ser un resto seleccionado de las fórmulas (6) a (9); y R4 es -H, -OH, -SH, -NH2, -NHalquilo C1-6, -N(alquilo C1-6)2, -NHarilo C6-14, -N(arilo C6-14)2, -N(alquil C1-6)(arilo C6-14), -NCOalquilo C1-6, -NO2, -CN, -COOH, -COOalquilo C1-6, -(CO)alquilo C1-6, -(CS)alquilo C1-6, -F, -Cl, -Br, -I, -O-alquilo C1-6, -O-arilo C6-14, -S-alquilo C1-6, -S-arilo C6-14, -SOalquilo C1-6, y -SO2alquilo C1-6. También se describen las sales fisiológicamente tolerables de los compuestos de fórmula (1), el procedimiento para prepararlas, el uso de las mismas para preparar medicamentos, los medicamentos que las contienen y su preparación. Los compuestos de fórmula (1) son útiles como inhibidores de la fosfodiesterasa 4 y, por tanto, son útiles para tratar inflamaciones de las articulaciones, incluyendo artritis y artritis reumatoidea, y para tratar infecciones virales y parasitárias.
ARP010105014A 2000-10-27 2001-10-26 Nuevos 7-azaindoles, su uso como inhibidores de la fosfodiesterasa 4 y el procedimiento para su preparacion, los medicamentos que los contienen y su preparacion AR034269A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10053275A DE10053275A1 (de) 2000-10-27 2000-10-27 Neue 7-Azaindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
US24434200P 2000-10-30 2000-10-30

Publications (1)

Publication Number Publication Date
AR034269A1 true AR034269A1 (es) 2004-02-18

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ARP010105014A AR034269A1 (es) 2000-10-27 2001-10-26 Nuevos 7-azaindoles, su uso como inhibidores de la fosfodiesterasa 4 y el procedimiento para su preparacion, los medicamentos que los contienen y su preparacion

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US7354948B2 (en) * 2002-11-06 2008-04-08 Celgene Corporation Methods for treatment of chronic uveitis using cyclopropyl-n-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindoline-4-yl}carboxamide
DE10318610A1 (de) * 2003-04-24 2004-11-11 Elbion Ag 7-Azaindole und deren Verwendung als Therapeutika
US20050054691A1 (en) * 2003-08-29 2005-03-10 St. Jude Children's Research Hospital Carboxylesterase inhibitors
BRPI0414313A (pt) * 2003-09-11 2006-11-07 Kemia Inc inibidores de citocinas
AU2005325271A1 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. PDE4B inhibitors and uses therefor
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