AR039554A1 - Compuestos derivados de aminopirimidina y aminopiridina, su empleo, un metodo para su preparacion, composiciones que los comprenden, y compuestos intermediarios - Google Patents

Compuestos derivados de aminopirimidina y aminopiridina, su empleo, un metodo para su preparacion, composiciones que los comprenden, y compuestos intermediarios

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AR039554A1
AR039554A1 ARP020104262A ARP020104262A AR039554A1 AR 039554 A1 AR039554 A1 AR 039554A1 AR P020104262 A ARP020104262 A AR P020104262A AR P020104262 A ARP020104262 A AR P020104262A AR 039554 A1 AR039554 A1 AR 039554A1
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alkyl
cycloalkyl
hydrogen
aryl
independently
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Ronald Charles Hawley
Sharada Shenvi Labadie
Eric Brian Sjogren
Francisco Xavier Talamas
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Hoffmann La Roche
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/14Heterocyclic 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 three or more hetero rings

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Abstract

Compuestos derivados de aminopirimidina y aminopiridina que tienen la fórmula (1), en la cual: uno de V ó X es N y el otro es CRa, ó ambos V y X son CRa (donde cada Ra es independientemente hidrógeno, alquilo (C1-6), cicloalquilo (C3-7) ó cicloalquil (C3-7)-alquilo (C1-6); Y es O, S ó NR; donde R es hidrógeno, CN, NO2, (alquilo C1-10), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), alquenilo (C3-10) ó alquinilo (C2-10); Z es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-6)-alquilo (C1-6), alquenilo (C2-6), alquinilo (C2-6) ó N(R2)(R3); R1 es hidrógeno, alquilo (C1-10), alquenilo (C3-10), alquinilo (C2-10), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), heteroalquilo (C1-10), heterociclilo, heterociclil-alquilo (C1-6), arilo, aril-alquilo (C1-4), aril-heteroalquilo (C1-4), heteroaril-alquilo (C1-4), heteroaril-heteroalquilo (C1-4), C(O)R11 ó alquileno (C1-6)-C(O)R11; R11 es hidrógeno, alquilo (C1-6) ó NR12R13 (donde R12 y R13 son independientemente hidrógeno, alquilo (C1-6) ó heteroalquilo (C1-6)); R2 y R3 son independientemente hidrógeno, alquilo (C1-10), alquenilo (C3-10), alquinilo (C2-10), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6) ó heteroalquilo (C1-10), ó R2 y R3 pueden combinarse para formar un anillo heterocíclico de 5-7 miembros; R4 es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), alquenilo (C2-6) ó alquinilo (C2-6); A es hidrógeno, alquilo (C1-10), alquenilo (C3-10), alquinilo (C2-10), haloalquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), heteroalquilo (C1-10), heterociclilo, heterociclil-alquilo (C1-6), cicloalquilo (C3-7) heterosustituido, arilo, aril-alquilo (C1-4), aril-heteroalquilo (C1-4), heteroarilo, heteroaril-alquilo (C1-4), heteroaril-heteroalquilo (C1-4) ó RaRbNC(=X)- donde Ra y Rb son independientemente hidrógeno, alquilo (C1-4) ó arilo y X es O ó S; B es un anillo aromático de cinco o seis miembros sustituido o no sustituido, que contiene al menos un átomo de nitrógeno, y entre 0 y 3 heteroátomos adicionales, donde los sustituyentes del anillo B se seleccionan entre halógeno, CF3, CF3O, alquilo (C1-6), amino, alquilamino (C1-6), di-alquilamino (C1-6), ciano, nitro, sulfonamido, acilo, acilamino y carboxamido; U es -NR5-, -O- ó -S-; y, R5 es hidrógeno ó alquilo (C1-6); y sales farmacéuticamente aceptables de los mismos; donde el término "heteroalquilo" se refiere a un radical alquilo (C1-6) con uno, dos o tres sustituyentes independientemente seleccionados entre ciano, -ORa, -NRbRc, y -S(O)nRd (donde n es un entero que oscila entre 0 y 2); entendiendo que el punto de unión del radical heteroalquilo es a través de un átomo de carbono del radical heteroalquilo, y Ra es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo, aril-alquilo (C1-6), alcoxicarbonilo (C1-6), ariloxicarbonilo, carboxamido, ó mono- o di-alquil (C1-6) carbamoilo, Rb es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo ó aril-alquilo (C1-6), Rc es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo, aril-alquilo (C1-6), alcoxicarbonilo (C1-6), ariloxicarbonilo, carboxamido, mono- o di-alquil (C1-6) carbamoilo, alquilsulfonilo (C1-6), -C(O)R', ó -S(O)nR' (donde n es un entero que oscila entre 0 y 2; donde R' es hidrógeno, alquilo (C1-6) ó arilo), Rd es hidrógeno (siempre y cuando n sea 0), alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo, aril-alquilo (C1-6), amino, monoalquilamino (C1-6), dialquilamino (C1-6), ó hidroxialquilo (C1-6); el término "heteroarilo" se refiere a un radical monocíclico o bicíclico monovalente que tiene entre 5 y 12 átomos en el anillo, que tiene al menos un anillo aromático que contiene uno, dos o tres heteroátomos en el anillo seleccionados entre N, O, ó S, y el resto de los átomos del anillo son C, entendiendo que el punto de unión del radical heteroarilo será en un anillo aromático, y el anillo heteroarilo está opcionalmente sustituido en forma independiente por uno a cuatro sustituyentes seleccionados entre alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), halo, nitro, ciano, hidroxi, alcoxi (C1-6), amino, acilamino, monoalquilamino (C1-6), dialquilamino (C1-6), haloalquilo (C1-6), haloalcoxi (C1-6), heteroalquilo (C1-6), -COR (donde R es hidrógeno, alquilo (C1-6), fenilo ó fenilalquilo (C1-6)), -(CR'R")n-COOR (donde n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), y R es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), fenilo ó fenilalquilo (C1-6)), ó -(CR'R")n-CONRaRb (donde n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), y Ra y Rb son, independientemente uno del otro, hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-(alquilo C1-6), fenilo ó fenilalquilo (C1-6)); el término "heterociclilo" se refiere a un radical cíclico no aromático saturado o insaturado que tiene entre 3 y 8 átomos en el anillo, donde uno o dos átomos del anillo son heteroátomos seleccionados entre O, NR (donde R es independientemente hidrógeno, alquilo (C1-6), ó cualquiera de los sustituyentes que se mencionan más adelante), ó S(O)n (donde n es un entero que oscila entre 0 y 2), y el resto de los átomos del anillo son C, donde uno o dos átomos de C pueden ser reemplazados opcionalmente por un grupo carbonilo, y el anillo de heterociclilo puede estar opcionalmente sustituido en forma independiente por uno, dos o tres sustituyentes seleccionados entre alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), aril-alquilo (C1-6), halo, nitro, ciano, cianoalquilo (C1-6), hidroxi, alcoxi (C1-6), amino, monoalquilamino (C1-6), dialquilamino (C1-6), haloalquilo (C1-6), haloalcoxi (C1-6), -(CR'R")n-COR (donde n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), R es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), fenilo, ó fenilalquilo (C1-6)), -(CR'R")n-COOR (donde n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), y R es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), fenilo ó fenilalquilo (C1-6)), -(CR'R")n-C(=Q)NRaRb (donde Q es O ó S, n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), y Ra y Rb son, independientemente uno del otro, hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquilo (C3-7)-alquilo (C1-6), heteroalquilo (C1-6), fenilo ó fenilalquilo (C1-6)), ó -(CR'R")n1-S(O)nRd (donde n1 es un entero que oscila entre 0 y 5, Rd es hidrógeno (siempre y cuando n sea 0), alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo, aril-alquilo (C1-6), amino, monoalquilamino (C1-6), dialquilamino (C1-6), ó hidroxialquilo (C1-6), y n es un entero que oscila entre 0 y 2); el término "arilo" se refiere a un radical de hidrocarburo aromático monocíclico o bicíclico monovalente que tiene entre 6 y 10 átomos en el anillo, que está opcionalmente sustituido independientemente por uno a cuatro sustituyentes seleccionados entre alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), fenilo, halo, nitro, ciano, cianoalquilo (C1-6), hidroxi, alcoxi (C1-6), amino, acilamino, monoalquilamino (C1-6), dialquilamino (C1-6), haloalquilo (C1-6), haloalcoxi (C1-6), heteroalquilo (C1-6), COR (donde R es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), fenilo ó fenilalquilo (C1-6)), -S(O)n-Rd (donde n es un entero que oscila entre 0 y 2, y cuando n es 0, Rd es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), ó cicloalquil (C3-7)-alquilo (C1-6), y cuando n es 1 ó 2, Rd es alquilo (C1-6), cicloalquilo (C3-7), cicloalquilo (C3-7)-alquilo (C1-6), amino, acilamino, monoalquilamino (C1-6), ó dialquilamino (C1-6)), -NS(O)2Rf (donde Rf es alquilo (C1-6) ó arilo), -NHCORe (donde Re es amino, alquilamino (C1-6), dialquilamino (C1-6) ó alcoxi (C1-4)), -(CR'R")n-COOR (donde n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), y R es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquilo (C3-7)-alquilo (C1-6), fenilo ó fenilalquilo (C1-6)), -(CR'R")nS(O)n-Rd (donde n es un entero que oscila entre 0 y 2, y cuando n es 0, Rd es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), ó cicloalquil (C3-7)-alquilo (C1-6), y cuando n es 1 ó 2, Rd es alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), amino, acilamino, monoalquilamino (C1-6), ó dialquilamino (C1-6)), -(CR'R")n-CONRaRb (donde n es un entero que oscila entre 0 y 5, R' y R" son independientemente hidrógeno ó alquilo (C1-6), y Ra y Rb son, independientemente uno del otro, hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), fenilalcoxi (C1-4) ó fenilalquilo (C1-6)) ó cualesquiera dos átomos de carbono adyacentes están sustituidos por -O(CH2)nO- (donde n es 1 ó 2); el término "acilo" se refiere al grupo -C(O)R', donde R' es hidrógeno, alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo y aril-alquilo (C1-6); el término "cicloalquilo heterosustituido" se refiere a un grupo cicloalquilo (C3-7) en donde uno, dos o tres átomos de hidrógeno se reemplazan por sustituyentes seleccionados independientemente entre el grupo que comprende ciano, cianometilo, hidroxi, hidroximetilo, alcoxi (C1-6), amino, acilamino, monoalquilamino (C1-6), dialquilamino (C1-6), -SOnR (donde n es un entero que oscila entre 0 y 2 y cuando n es 0, R es hidrógeno ó alquilo (C1-6) y cuando n es 1 ó 2, R es alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), arilo, aril-alquilo (C1-6), heteroarilo, amino, acilamino, monoalquilamino (C1-6), dialquilamino (C1-6), ó hidroxialquilo (C1-6)) ó -NHSO2R d
ARP020104262A 2001-11-07 2002-11-07 Compuestos derivados de aminopirimidina y aminopiridina, su empleo, un metodo para su preparacion, composiciones que los comprenden, y compuestos intermediarios AR039554A1 (es)

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