AR042461A1 - Analogos 2-sustituidos de quinazolin-4-il - amina. composiciones farmaceuticas - Google Patents

Analogos 2-sustituidos de quinazolin-4-il - amina. composiciones farmaceuticas

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Publication number
AR042461A1
AR042461A1 ARP030104607A ARP030104607A AR042461A1 AR 042461 A1 AR042461 A1 AR 042461A1 AR P030104607 A ARP030104607 A AR P030104607A AR P030104607 A ARP030104607 A AR P030104607A AR 042461 A1 AR042461 A1 AR 042461A1
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Argentina
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8alkyl
substituted
amino
independent substituents
alkyl
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ARP030104607A
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Neurogen Corp
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Abstract

Certeza de que lo provisto son análogos sustitutos de 2-quinazolina-4-ilamina. Tales compuestos son ligandos que pueden ser usados para modular la actividad específica del receptor in vivo o in vitro, y son particularmente útiles en el tratamiento de condiciones asociadas con la activación del receptor patológico en humanos, animales companeros domésticos y animales de ganado. Son provistas composiciones farmacéuticas y métodos para el uso de ellas para tratar tales afecciones, como son estos métodos para tratar tales ligandos para estudios de localización del receptor. Reivindicación 1: Un compuesto de la fórmula (1) o una forma farmacéutica aceptable de esto, donde: X, V, W, Y y Z son cada cual independiente de N o de CR1, con la condición que al menos uno de V y X es N. R1 es seleccionado independiente de cada acontecimiento de H, halógeno, hidróxido, ciano, amino, C1-6 alquil, halo C1-6 alquil, C1-6alcóxido,halo C1-6alcóxido carbónico y mono- y di-(C1-6 alquil)amino; R es -O-R7 o -(R4)-N-R3; R7 es (I) H, (II) C1-8alquil, C1-8alquenil, C1-8alquinil, C1-8alcanol, C3-8alcanone, C2-8éter alquil, C6-10aril C0-8alquil o (5 a 10 miembros heterocíclicos)C0-8alquilo, cada uno de estos es sustituido con 0 a 4 sustituyentes independientes escogidos de Rb, o (III) tomados juntos con un R5 o R6 para formar de 4- a 10- miembros heterocíclicos que es sustituido con 0 a 4 sustituyentes independientes escogidos de Rb; R3 y R4 son: cada uno seleccionado independiente de a) H, b) C1-8alquil, C2-8alquenil, C2-8alquinil, C2-8alcanone, C2-8alcanoil, C2-8éter alquil, C6-10aril C0-8alquil, (5- a 10- miembros heterocíclicos) C0-8alquil y -(SO2)C1-8alquil, cada uno de estos es sustituido con 0 a 4 sustituyentes independientes escogidos de Rb; y c) grupos que son tomados junto con un R5 o R6 para formar de 4- a 10- miembros heterocíclicos que es sustituido con 0 a 4 sustituyentes independientes escogidos de Rb; o tomados juntos para formar de 4 a 10 miembros heterocíclicos que es sustituido de 0 a 4 sustituyentes independientes escogidos de Rb; R5 o R6 son, independientes de cada acontecimiento: (1) Cada H independiente, C1-8 alquil sustituido de 0 a 2 sustituyentes independientes escogidos de Rb, o tomados cada uno con R3, R4 o R7 para formar un grupo de 4- a 10- miembros heterocíclicos que es sustituido con 0 a 4 sustituyentes independientes escogidos de Rb; (2) tomados juntos para formar un grupo aceto; o (3) tomados juntos para formar anillos de 3 a 7 miembros carbocíclicos o heterocíclico que es sustituido con 0 a 4 sustituyentes independientes escogidos de Rb; n es 1, 2, o 3; Ar1 y Ar2 son seleccionados independientes de grupos arilos de 6- a 10 miembros y 5- 10- miembros heterocíclicos, cada uno de estos es sustituidos con 0 a 3 sustituyentes independientes seleccionados de grupos de la fórmula LRa; L es seleccionado independiente de cada acontecimiento de un enlace, O, S(O)C(=O), OC(=O), C(=O)O, O-C(=O)O, N( Rx ), C(=O)N(Rx), N(Rx)C(=O)N(Rx)S(O)m, S(O)mN(Rx) y N[S(O)mRx]S(O)m; donde m es seleccionado independiente de cada acontecimiento de 0, 1, y 2; y Rx es seleccionada independiente de cada acontecimiento de H y C1-8 alquil; Ra es seleccionado independiente de cada acontecimiento d: 1) H, halógeno, ciano y nitro; y 2) C1-8alquil, C2-8alquenil, C2-8alquinil, C2-8éter alquil, (4 a 10 miembros heterocíclicos) C0-8 alquil y mono- y di-(C1-8alquil)amino, cada uno de estos es sustituidos con 0 a 4 sustituyentes independientes seleccionados de hidróxido, halógeno, amino, ciano, nitro, oxo, -COOH, C1-4alquil, C1-4alcóxido, halo C1-4alquil, halo C1-4alcóxido, hidróxido C1-4alquil, y mono- y di-(C1-6alquil)amino, y Rb es escogido independiente de cada uno de los acontecimientos de: 1) hidróxido, halógeno, amino, aminocarbonílico, ciano, nitro, oxo y -COOH; y 2) C1-8alquil, C1-8haloalquil, C1-8alcóxido, C1-8haloalcóxido, C1-8alcanoil, C2-8alcoxicarbonil, C2-8alcanoilóxido, C1-8alquitio, C2-8éter alquil, fenil C0-8alquil, fenil C0-8alcóxido, mono- y di-(C1-6alquil)amino amino C0-6alquil,-(SO2)C1-8alquil y (4- a 7- miembros heterocíclicos) (C0-8alquil); cada uno de estos es sustituidos con 0 a 3 sustituyentes independientes escogidos de hidróxido, halógeno, amino, ciano, C1-4 alquil, C1-4alcóxido, hidróxido C1-4alquil, halo C1-4alquil, y mono- y di-(C1-4alquil)amino.
ARP030104607A 2002-12-13 2003-12-12 Analogos 2-sustituidos de quinazolin-4-il - amina. composiciones farmaceuticas AR042461A1 (es)

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MXPA05006123A (es) 2005-09-30
TW200418480A (en) 2004-10-01
KR20050084292A (ko) 2005-08-26
CN1726205A (zh) 2006-01-25
PE20040935A1 (es) 2005-01-01
US7432275B2 (en) 2008-10-07
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CA2509233A1 (en) 2004-07-01
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