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AR050425A1 - Antagonistas multivalentes de vla-4 que comprende fracciones polimericas. composiciones farmaceuticas - Google Patents

Antagonistas multivalentes de vla-4 que comprende fracciones polimericas. composiciones farmaceuticas

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Publication number
AR050425A1
AR050425A1 ARP050102848A ARP050102848A AR050425A1 AR 050425 A1 AR050425 A1 AR 050425A1 AR P050102848 A ARP050102848 A AR P050102848A AR P050102848 A ARP050102848 A AR P050102848A AR 050425 A1 AR050425 A1 AR 050425A1
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AR
Argentina
Prior art keywords
substituted
alkyl
optionally
group
aryl
Prior art date
Application number
ARP050102848A
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English (en)
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Elan Pharm Inc
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Publication date
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Publication of AR050425A1 publication Critical patent/AR050425A1/es

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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract

Se presentan compuestos que se unen a VLA-4. algunos de estos compuestos también inhiben la adhesion leucocitaria y, particularmente, la adhesion leucocitaria mediada por VLA-4. estos compuestos son usados en el tratamiento de enfermedades inflamatorios en un paciente mamífero, por ejemplo, humanos, tales como asma, enfermedad de Alzheimer, ateroesclerosis, demencia por SIDA, diabetes, enfermedad intestinal inflamatoria, artritis reumatoide, transplantes de tejidos, metástasis tumorales e isquemia miocárdica. Los compuestos también pueden administrarse para el tratamiento de enfermedades cerebrales inflamatorias, tal como la esclerosis multiple. Reivindicacion 1: Un conjugado de la formula (1), B es una fraccion polimérica biocompatible opcionalmente unido en forma covalente a una molécula central de cadena ramificada; q es de aprox. 2 hasta aprox. 100; A en cada ocurrencia es independientemente un compuesto de formula (2), o una sal farmacéuticamente aceptable de los mismos componentes, donde J se selecciona de: a) un grupo de formula (3), donde R31 es un enlace covalente con la fraccion polimérica que opcionalmente comprende un ligador, o R31 es -H, R31', -NH2, -NHR31' o -N(R31')2, -'NC3- 6cíclico, -OR31', -SR31' donde cada R31' es independientemente un C1-6 alquílico lineal o ramificado opcionalmente sustituido o C1-6 alquílico opcionalmente sustituido, C3-6 cicloalquílico opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido; y R32 es un enlace covalente con la fraccion polimérica que opcionalmente comprende un ligador, o R32 es -H, -NO2, haloalquilo o el grupo -N(MR41)R42 donde M es un enlace covalente, -C(O)- o -SO2-, R41 es R41', N(R41')2, o -OR41'; donde cada R41' es independientemente hidrogeno, un C1-6 alquilo lineal o ramificado opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heterocíclico opcionalmente sustituido o un heteroarilo opcionalmente sustituido, donde las sustituciones opcionales son haluro, C1-6 alquilo, o -OC1-6alquilo; y R42 es hidrogeno o R41'; y b) un grupo de formula (4), donde R se selecciona de un grupo que consiste en un enlace covalente con la fraccion polimérica, amino, hidroxilo, amino sustituido, alquilo, alquiloxi, ariloxi, heteroariloxi, heterocicliloxi, tiol, ariltio, heteroariltio, heterocicliltio y alquilo sustituido, donde cada amino, amino, sustituido, alquilo y alquilo sustituido esta opcionalmente unido en forma covalente a la fraccion polimérica donde, en cada caso, la fraccion polimérica comprende opcionalmente un ligador que se une covalentemente a la fraccion polimérica; Ar1 se selecciona de un grupo formado por aril, aril sustituido, heteroarilo y heteroarilo sustituido donde cada arilo, arilo sustituido, heteroarilo y heteroarilo sustituido está opcionalmente unido en forma covalente a la fraccion polimérica donde la fraccion polimérica comprende opcionalmente un ligador que une la fraccion polimérica a Ar1; Ar2 se selecciona de un grupo formado por arilo, arilo sustituido, heteroarilo y heteroarilo sustituido donde cada arilo, arilo sustituido, heteroarilo y heteroarilo sustituido está opcionalmente unido en forma covalente a la fraccion polimérica donde la fraccion polimérica comprende opcionalmente un ligador que une la fraccion polimérica a Ar2; X se selecciona del grupo formado por -NR1-, -O-, S-S, -SO-, -SO2 y -CH2- opcionalmente sustituido donde R1 se selecciona del grupo formado por hidrogeno y alquilo; T se selecciona de: a) un grupo de formula (5), donde Y se selecciona de un grupo formado por -O- y -NR1- donde R1 se selecciona del grupo formado por hidrogeno y alquilo; W se selecciona del grupo formado por un enlace covalente unido a una fraccion polimérica que opcionalmente comprende un ligador y -NR2R3 donde R2 y R3 son seleccionados independientemente en el grupo formado por hidrogeno, alquilo, alquilo sustituido y donde R2 y R3, junto con el átomo de nitrogeno allí enlazado, forman un anillo heterocíclico o un anillo heterocíclico sustituido en donde cada alquilo, alquilo sustituido, heterocíclico y heterocíclico sustituido está opcionalmente unido en forma covalente a una fraccion polimérica que además comprende opcionalmente un ligador; m es un entero igual a 0, 1 o 2; n es un entero igual a 0, 1 o 2; y b) un grupo de formula (6), donde G es un arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido con anillo de 5 o 6 miembros conteniendo 0 a 3 nitrogenos, donde dicho arilo o heteroarilo opcionalmente comprende también un enlace covalente con la fraccion polimérica que opcionalmente comprende un ligador; R6 es un enlace covalente con una fraccion polimérica que opcionalmente comprende un ligador, o R6 es -H, alquilo, alquilo sustituido o -CH2C(O)R17, donde R17 es -OH, OR18, o -NHR18, donde R18 es alquilo, alquilo sustituido, arilo o arilo sustituido; R55 se selecciona del grupo compuesto por amino, amino sustituido, alcoxi, alcoxi sustituido, cicloalcoxi, cicloalcoxi sustituido, ariloxi y ariloxi sustituido, y -OH; con tal de que: A es al menos uno de R, Ar1, Ar2, y T contenga un enlace covalente con la fraccion polimérica; B es cuando R esté unido covalentemente a la fraccion polimérica, n sea uno y X no sea -O-, -S-, -SO-, o -SO2-; C es cuando X sea -O- o -NR1-, entonces m sea dos; y D es el conjugado de la formula (1) tenga un peso molecular menor que 100,000.
ARP050102848A 2004-07-08 2005-07-08 Antagonistas multivalentes de vla-4 que comprende fracciones polimericas. composiciones farmaceuticas AR050425A1 (es)

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US58697504P 2004-07-08 2004-07-08

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AR050425A1 true AR050425A1 (es) 2006-10-25

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US (4) US7794700B2 (es)
EP (4) EP1765412A2 (es)
JP (1) JP2008505927A (es)
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CA2573245C (en) 2013-10-01
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