AR049652A1 - Sales cuaternarias antagonistas del receptor ccr2 - Google Patents

Sales cuaternarias antagonistas del receptor ccr2

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Publication number
AR049652A1
AR049652A1 ARP050102614A ARP050102614A AR049652A1 AR 049652 A1 AR049652 A1 AR 049652A1 AR P050102614 A ARP050102614 A AR P050102614A AR P050102614 A ARP050102614 A AR P050102614A AR 049652 A1 AR049652 A1 AR 049652A1
Authority
AR
Argentina
Prior art keywords
halogen
aryl
lower alkyl
optionally substituted
alkoxycarbonyl
Prior art date
Application number
ARP050102614A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR049652A1 publication Critical patent/AR049652A1/es

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    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract

Formas farmacéuticamente aceptables de los mismos, que son antagonistas de CCR2 y son utiles para prevenir, tratar o mejorar los síndromes, trastornos o enfermedades en un sujeto que lo necesita. Reivindicacion 1: Un compuesto de formula (1), y formas farmacéuticamente aceptables del mismo, en la cual: A es carbonilo, tiocarbonilo o sulfonilo; X es un enlace o -CH=CH-; R1 está seleccionado de: a) arilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, alcoxicarbonilo, ciano, halogeno o fenilo opcionalmente sustituido con alquilo inferior, -(CH2)n-CF3, alcoxi inferior, alcoxicarbonilo, ciano o halogeno; b) cicloalquilo C5-15 opcionalmente sustituido con uno o más de alquilo inferior, - (CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; o c) heterociclilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilalquilo inferior, arilo halogeno- sustituido, alcoxicarbonilo, ciano o halogeno; n es 0, 1, 2, 3 o 4; Y es un enlace o -CH2-; X2 es -(CH2)m- donde m es 1 o 2; R2 es -N+(R4R5)-ZR3; Z es -(CH2)p- donde p es 0, 1 o 2; R3 está seleccionado de: a) arilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; b) cicloalquilo C5-15 opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; o c) heterociclilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; donde cuando el heterociclilo está unido a través de un miembro de anillo de átomo de carbono y un miembro de anillo heteroátomico es adyacente a dicho átomo de carbono, entonces p es 1 o 2; R4 y R5, son cada uno individualmente alquilo inferior o alquenilo inferior; alternativamente, R4 y R5 se combinan con el átomo de nitrogeno de formula (1) para formar un anillo heterociclilo de 5 a 9 átomos de anillo en total, que contienen opcionalmente un átomo del anillo, de oxígeno o azufre, donde el átomo de nitrogeno del anillo heterociclilo está sustituido con uno de alquilo inferior o alquenilo inferior para formar una sal cuaternaria, y donde -ZR3 está ausente y el anillo heterociclilo está opcionalmente sustituido con arilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno sustituido, alcoxicarbonilo, ciano o halogeno.
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