AR034555A1 - Compuestos de 1,4-dihidropiridina como antagonistas de bradicinina; composicion farmaceutica, compuesto intermediario, procedimiento para preparar dichos compuestos - Google Patents

Compuestos de 1,4-dihidropiridina como antagonistas de bradicinina; composicion farmaceutica, compuesto intermediario, procedimiento para preparar dichos compuestos

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AR034555A1
AR034555A1 ARP010103819A ARP010103819A AR034555A1 AR 034555 A1 AR034555 A1 AR 034555A1 AR P010103819 A ARP010103819 A AR P010103819A AR P010103819 A ARP010103819 A AR P010103819A AR 034555 A1 AR034555 A1 AR 034555A1
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alkyl
alkoxy
amino
acyl
cycloalkyl
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Pfizer
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Abstract

Compuestos de fórmula (1), en la que: A es independientemente halo; Y es -(CH2)m-, -C(O)- ó -S(O)-; R1 y R2 son independientemente alquilo C1-4; R3 se selecciona entre (a) azaciclo-, azabiciclo- o azatriciclo-alquilo C7-14, en los que el átomo de nitrógeno tiene opcionalmente un sustituyente seleccionado entre alquilo C1-4, bencilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halo y alquilo C1-4 sustituido con halo, alcoxi C1-4-carbonilo opcionalmente sustituido con uno o dos átomos de halógeno y acilo C1-6; (b) hidrógeno, alquilo C1-7 opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre hidroxi, amino, alquil C1-4-amino, dialquil C1-4-amino, piridilo, carbamoílo, pirrolidinilcarbonilo, alquil C1-4-aminocarbonilo, piperidinilcarbonilo, morfolinocarbonilo, 2-oxopirrolidinilo, alquil C1-4-sulfonilamino, ciano, acil C1-6-amino, 1,1-dioxoisotiazolinilo, 2-oxo-1,3-oxazolidinilo, morfolino, alquil C1-4-2-oxopirrolidinilo, piperidinilo y oxo-piperidinilo; (c) piperidinilo opcionalmente sustituido en el átomo de nitrógeno con alquilo C1-4 o alcoxi C1-4-carbonilo; (d) cicloalquilo, bicicloalquilo o tricicloalquilo C5-14, estando el cicloalquilo, bicicloalquilo o tricicloalquilo C5-14 opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre oxo, hidroxi, amino, alquil C1-4-amino, di-alquil C1-4-amino, alcoxi C1-4-benzamido, morfolino y oxopirrolidinilo; (e) bicicloalquenilo C7-10, benzo-cicloalquilo C5-7 o heterociclilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre alquilo C1-4 y halo, y (f) alquil C1-6-cicloalquilo C3-7, estando el radical cicloalquilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados independientemente entre ciano, amino-alquilo C1-4, alquil C1-4-amino-alquilo C1-4-, acil C1-6-amino-alquilo C1-4-, alquil C1-4-sulfonilamino-alquilo C1-4, amino, oxopirrolidinilo, cicloalquil C4-7-amino-alquilo C1-4, di-alquil C1-4-amino-alquilo C1-4, hidroxilo, carbamoílo, acil C1-6(alquil C1-4)amino, acil C1-6(alquil C1-4)amino-alquilo C1-4, di-alquil C1-4-amino, pirrolidinil-alquilo C1-4, oxo-pirrolidinil-alquilo C1-4 y di-alquil C1-4-amino-alquilo C1-4; R4 es fenilo sustituido en la posición 2 con un sustituyente seleccionado entre (a) alquilo C1-4 sustituido con uno, dos, o tres sustituyentes seleccionados independientemente entre amino, amino-alcoxi C2-4, tiofenilo, alquil C1-4-tiofenilo, di-alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino, di-alquil C1-4-amino, hidroxi, alcoxi C1-4, piperazinilo, oxopirrolidinilo, pirrolidinilo, alquilenodioxi C2-4, aciloxi C1-6, oxo, morfolino, alquil C1-4-aminocarbonil-acil C1-6-amino, alcoxi C1-4-carbonil-acil C1-6-amino, alcoxi C1-4-carbonilpiperazinilo, acil C1-6-piperazinilo, tioalquilo C1-4, heterociclil-alcoxi C1-4, (di-alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4, (alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4 y (amino)(cicloalquil C3-7)alcoxi C2-4; (b) alquilo C5-7 opcionalmente sustituido con uno, dos, o tres sustituyentes seleccionados independientemente entre amino, amino-alcoxi C2-4, tiofenilo, alquil C1-4-tiofenilo, di-alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino, di-alquil C1-4-amino, hidroxi, alcoxi C1-4, piperazinilo, oxopirrolidinilo, pirrolidinilo, alquileno-dioxi C2-4, aciloxi C1-6, oxo, morfolino, alquil C1-4-aminocarbonil-acil C1-6-amino, alcoxi C1-4-carbonil-acil C1-6-amino, alcoxi C1-4-carbonilpiperazinilo, acil C1-6-piperazinilo, tioalquilo C1-4, heterociclil-alcoxi C1-4, (di-alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4, (alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4 y (amino)(cicloalquil C3-7)alcoxi C2-4; (c) alcoxi C1-4 o tioalquilo C1-4, estando sustituido el alcoxi C1-4 o el tioalquilo C1-4 con uno, dos, o tres sustituyentes seleccionados independientemente entre amino, amino-alcoxi C2-4, tiofenilo, alquil C1-4-tiofenilo, di-alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino, di-alquil C1-4-amino, hidroxi, alcoxi C1-4, piperazinilo, oxopirrolidinilo, pirrolidinilo, alquilenodioxi C2-4, aciloxi C1-6, oxo, morfolino, alquil C1-4-aminocarbonil-acil C1-6-amino, alcoxi C1-4-carbonil-acil C1-6-amino, alcoxi C1-4-carbonilpiperazinilo, acil C1-6-piperazinilo, tioalquilo C1-4, heterociclil-alcoxi C1-4, (di-alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4, (alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4 y (amino)(cicloalquil C3-7)alcoxi C2-4; (d) alcoxi C5-7 o tioalquilo C5-7, estando los grupos alcoxi C5-7 o tioalquilo C5-7 opcionalmente sustituidos con uno, dos, o tres sustituyentes seleccionados independientemente entre amino, amino-alcoxi C2-4, tiofenilo, alquil C1-4-tiofenilo, di-alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino-alcoxi C2-4, alquil C1-4-amino, di-alquil C1-4-amino, hidroxi, alcoxi C1-4, piperazinilo, oxopirrolidinilo, pirrolidinilo, alquilenodioxi C2-4, aciloxi C1-6, oxo, morfolino, alquil C1-4-aminocarbonil-acil C1-6-amino, alcoxi C1-4-carbonilacil C1-6-amino, alcoxi C1-4-carbonilpiperazinilo, acil C1-6-piperazinilo, tioalquilo C1-4, heterociclil-alcoxi C1-4, (di-alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4, (alquil C1-4-amino)(cicloalquil C3-7)alcoxi C2-4 y (amino)(cicloalquil C3-7)alcoxi C2-4; (e) amino, alquil C1-4-amino, acil C1-6-amino, aminoacetilamino, alquil C1-4-sulfonilamino, alquil C1-4-sulfonilamino sustituido con halo, alquil C1-4-amino sustituido con halo, o alcoxi C1-4-carbonilaminoacetilamino; (f) piperazinilcarbonilo, morfolinocarbonilo, nitro, ciano, hidroxi, alquil C1-4-sulfonilo, alquil C1-4-sulfinilo o di-alquil C1-4-aminosulfenilo; (g) tioalquilo C1-4, tioacilo C1-6, amino-tioacilo C1-6, alquil C1-4-tiosulfonilo, tioalquilo C1-4 sustituido con halo o alcoxi C1-4-aminotioacetilo; (h) alquenilo C2-7 o alquinilo C2-7, estando los grupos alquenilo C2-7 o alquinilo C2-7 opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados independientemente entre amino, alquil C1-3-amino, di-alquil C1-4-amino, hidroxi, alcoxi C1-4, piperazinilo, oxopirrolidinilo, pirrolidinilo, alquilenodioxi C2-4, halo, aciloxi C1-6, oxo, morfolino, alquil C1-4-aminocarbonilacil C1-6-amino, alcoxi C1-4-carbonil-acil C1-6-amino, alcoxi C1-4-carbonilpiperazinilo, acil C1-6-piperazinilo y tioalquilo C1-4; y (i) azacicloalquilo C7-14 opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre oxo y alquilo C1-4; R5 es hidrógeno o alquilo C1-4; m es 0, 1 ó 2; y n es 0, 1, 2, 3, 4, ó 5; o una sal farmacéuticamente aceptable del mismo. También se refiere a composiciones de los mismos en el tratamiento y prevención de la inflamación, asma, rinitis alérgica, dolor y otros trastornos. Se describen también intermediarios y procesos útiles para la preparación de estos compuestos.
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