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AR033643A1 - Compuestos que inhiben la adhesion de leucocitos intermediada por vla-4, composiciones farmaceuticas que los comprenden, el uso de dichas composiciones para la manufactura de medicamentos y un metodo in vitro para adherir vla-4 en una muestra biologica - Google Patents

Compuestos que inhiben la adhesion de leucocitos intermediada por vla-4, composiciones farmaceuticas que los comprenden, el uso de dichas composiciones para la manufactura de medicamentos y un metodo in vitro para adherir vla-4 en una muestra biologica

Info

Publication number
AR033643A1
AR033643A1 ARP000100286A ARP000100286A AR033643A1 AR 033643 A1 AR033643 A1 AR 033643A1 AR P000100286 A ARP000100286 A AR P000100286A AR P000100286 A ARP000100286 A AR P000100286A AR 033643 A1 AR033643 A1 AR 033643A1
Authority
AR
Argentina
Prior art keywords
substituted
heteroaryl
heterocyclic
aryl
group
Prior art date
Application number
ARP000100286A
Other languages
English (en)
Original Assignee
Wyeth Corp
Elan Pharm Inc
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 Wyeth Corp, Elan Pharm Inc filed Critical Wyeth Corp
Publication of AR033643A1 publication Critical patent/AR033643A1/es

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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
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Abstract

Se describen compuestos que se unen a VLA-4 que comprenden la fórmula (1) o (2), en donde en la fórmula (1), R1 y R2, conjuntamente con el átomo de carbono y W al cual están unidos respectivamente, se unen para formar un grupo arilo, cicloalquenilo, heteroarilo o heterocíclico que tiene por lo menos 5 átomos en el grupo arilo, cicloalquenilo, heteroarilo o heterocíclico y opcionalmente contienen o adicionalmente contienen en el caso de los grupos heteroarilo y heterocíclico, uno a tres heteroátomos seleccionados del grupo que consiste en oxígeno, nitrógeno y azufre y donde el grupo heteroarilo o heterocíclico es monocíclico; en la fórmula (2), R1 y R2, conjuntamente con el átomo de carbono y W' al cual están unidos respectivamente, se unen para formar un grupo cicloalquilo, cicloalquenilo o heterocíclico que tiene por los menos 5 átomos en el grupo cicloalquilo, cicloalquenilo o heterocíclico y que contiene opcionalmente o contiene adicionalmente en el caso del grupo heterocíclico uno a tres heteroátomos seleccionados del grupo que consiste en oxígeno, nitrógeno y azufre, y donde el grupo heterocíclico es monocíclico; y donde además, dicho grupo arilo, cicloalquilo, cicloalquenilo, heteroarilo o heterocíclico de la fórmula (1) o (2) está opcionalmente substituido en cualquier átomo del anillo capaz de substitución con 1-3 substituyentes seleccionados del grupo que consiste en alquilo, alquilo substituido, alcoxi, alcoxi substituido, acilo, acilamino, tiocarbonilamino, aciloxi, amino, amino substituido, amidino, alquilamidino, tioamidino, aminoacilo, aminocarbonilamino, aminotiocarbonilamino, aminocarboniloxi, arilo, arilo substituido, ariloxi, ariloxi substituido, ariloxiarilo, ariloxiarilo substituido, ciano, halógeno, hidroxilo, nitro, oxo, carboxilo, cicloalquilo, cicloalquilo substituido, guanidino, guanidino sulfona, tiol, tioalquilo, tioalquilo substituido, tioarilo, tioarilo substituido, tiocicloalquilo, tiocicloalquilo substituido, tioheteroarilo, tioheteroarilo substituido, tioheterocíclico, tioheterocíclico substituido, heteroarilo, heteroarilo substituido, heterocíclico, heterocíclico substituido, cicloalcoxi, cicloalcoxi substituido, heteroariloxi, heteroariloxi substituido, heterocicliloxi, heterocicliloxi substituido, oxicarbonilamino, oxitiocarbonilamino, -OS(O)2-alquilo, -OS(O)2-alquilo substituido, -OS(O)2-arilo, -OS(O)2-arilo substituido, -OS(O)2-heteroarilo, -OS(O)2-heteroarilo substituido, -OS(O)2-heterocíclico, -OS(O)2-heterocíclico substituido, -OSO2-NRR donde cada R es independientemente hidrógeno o alquilo; -NRS(O)2-alquilo, -NRS(O)2-alquilo substituido, -NRS(O)2-arilo, -NRS(O)2-arilo substituido, -NRS(O)2-heteroarilo, -NRS(O)2-heteroarilo substituido, -NRS(O)2-heterocíclico, -NRS(O)2-heterocíclico substituido, -NRS(O)2-NR-alquilo, -NRS(O)2-NR-alquilo substituido, -NRS(O)2-NR-arilo, -NRS(O)2-NR-arilo substituido, -NRS(O)2-NR-heteroarilo, -NRS(O)2-NR-heteroarilo substituido, -NRS(O)2-NR-heterocíclico, -NRS(O)2-NR-heterocíclico substituido donde cada R es hidrógeno o alquilo; -N[S(O)2-R']2 y -N[S(O)2-NR']2 donde cada R' está independientemente seleccionado del grupo que consiste en alquilo, alquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterocíclico y heterocíclico substituido; donde R3 es -(CH2)x-Ar-R9, donde Ar es arilo, arilo substituido, heteroarilo, y heteroarilo substituido; R9 está seleccionado del grupo que consiste en acilo, acilamino, aciloxi, amidino, alquilamidino, aminoacilo, aminocarbonilamino, aminotiocarbonilamino, aminocarboniloxi, guanidino, guanidino sulfona, oxicarbonilamino, oxitiocarbonilamino, tioamidino y tiocarbonilamino; x es un entero de 0 a 4; R3' es hidrógeno; Q está seleccionado del grupo que consiste en -O-, -S-, -S(O)-, -S(O)2 y -NR4-; R4 está seleccionado del grupo que consiste en hidrógeno, alquilo, alquilo substituido, alquenilo, alquenilo substituido, cicloalquilo, cicloalquilo substituido, cicloalquenilo, cicloalquenilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterocíclico y heterocíclico substituido u opcionalmente R4 y R1 ó R4 y R2 conjuntamente con los átomos a los cuales están unidos, se unen para formar un grupo heteroarilo, heteroarilo substituido, un heterocíclico o un heterocíclico substituido; W está seleccionado del grupo que consiste en nitrógeno y carbono; y W' está seleccionado del grupo que consiste en nitrógeno, carbono, oxígeno, azufre, S(O), y S(O)2; X está seleccionado del grupo que consiste en hidroxilo, alcoxi, alcoxi substituido, alquenoxi, alquenoxi substituido, cicloalcoxi, cicloalcoxi substituido, cicloalquenoxi, cicloalquenoxi substituido, ariloxi, ariloxi substituido, heteroariloxi, heteroariloxi substituido, heterocicliloxi, heterocicliloxi substituido, y -NR''R'' donde cada R'' está independientemente seleccionada del grupo que consiste en hidrógeno, alquilo, alquilo substituido, alquenilo, alquenilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterocíclico y heterocíclico substituido; y los enantiómeros, diaestereómeros y sus sales farmacéuticamente aceptables; con la condición de que: (i) el compuesto de la fórmula (1) o (2) tiene una afinidad de adhesión para VLA-4 expresada mediante la Cl50 de aproximadamente 15 microm o menos; y (ii)en la fórmula (1) y (2), R1 y R2, conjuntamente con el átomo de carbono y W al cual están unidos respectivamente, no forman un anillo piridazina substituido o no substituido. Algunos de estos compuestos también inhiben la adhesión de leucocitos y, en particular, la adhesión de leucocitos intermediada por VLA-4. Dichos compuestos son útiles en el tratamiento de enfermedades inflamatorias en mamíferos, por ejemplo, en seres humanos, que sufren de asma, enfermedad de Alzheimer, ateroesclerosis, demencia causada por SIDA, diabetes, enfermedad intestinal inflamatoria, artritis reumatoidea, transplante de piel, metástasis de tumores o isquemia de miocardio. Los compuestos pueden también administrarse para el tratamiento de enfermedades cerebrales tales como esclerosis múltiple. También se describen composiciones farmacéuticas que comprenden dichos compuestos de fórmula (1) y (2) y el uso de dichas composiciones para la manufactura de un medicamento. También se describe un método in vitro para adherir VLA-4 en una muestra biológica que comprende contactar la muestra biológica con un compuesto bajo condiciones en las cuales dicho compuesto se une a VLA-4.
ARP000100286A 1999-01-22 2000-01-24 Compuestos que inhiben la adhesion de leucocitos intermediada por vla-4, composiciones farmaceuticas que los comprenden, el uso de dichas composiciones para la manufactura de medicamentos y un metodo in vitro para adherir vla-4 en una muestra biologica AR033643A1 (es)

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