ES2301859T3 - Nuevos derivados de piridazin-3(2h)-ona. - Google Patents

Nuevos derivados de piridazin-3(2h)-ona. Download PDF

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ES2301859T3
ES2301859T3 ES03782471T ES03782471T ES2301859T3 ES 2301859 T3 ES2301859 T3 ES 2301859T3 ES 03782471 T ES03782471 T ES 03782471T ES 03782471 T ES03782471 T ES 03782471T ES 2301859 T3 ES2301859 T3 ES 2301859T3
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mono
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Vittorio Dal Piaz
Izquierdo Nuria Aguilar
Maria Antonia Buil Albero
Marta Carrascal Riera
Jordi Gracia Ferrer
Maria Paola Giovannoni
Claudia Vergelli
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Almirall SA
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Abstract

Un derivado de piridazin-3(2H)-ona de fórmula (I): (Ver fórmula) en la que R1 representa un grupo seleccionado de: * un grupo alquilo C1-C4 que está opcionalmente sustituido con uno o más; y * grupos de fórmula -(CH2)n-R6 en la que n es un número entero que varía de 1 a 3 y R6 representa un grupo cicloalquilo C3-C6, R2 es un átomo de hidrógeno, R3 representa un grupo arilo C5-C14 monocíclico o policíclico o un grupo heteroarilo de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, que está opcionalmente sustituido con uno o más, por ejemplo 1, 2, 3 ó 4 sustituyentes seleccionados de: * átomos de halógeno; * grupos alquilo C1-C20 y alquileno C1-C6, que están opcionalmente sustituidos con uno o más sustituyentes seleccionados de átomos de halógeno; y grupos fenilo, hidroxi, hidroxialquilo C1-C10, alcoxi C1-C10, ariloxi C5-C14, (alquil C1-C10)tio, oxo, amino, mono- o di-(alquil C1-C10)amino, acilamino, hidroxicarbonilo, (alcoxi C1-C10)carbonilo, carbamoilo, mono- o di-(alquil C1-C10)carbamoilo * grupos fenilo, hidroxi, hidroxialquilo C1-C10, alcoxi C1-C10, cicloalcoxi C3-C7, nitro, ariloxi C5-C14, (alquil C1-C10)tio, (alquil C1-C10)sulfinilo, (alquil C1-C10)sulfonilo, (alquil C1-C10)sulfamoilo, acilo, amino, mono- o di(alquil C1-C10)amino, acilamino, hidroxicarbonilo, (alcoxi C1-C10)carbonilo, carbamoilo, mono- o di(alquil C1-C10)carbamoilo, ureido, N''-(alquil C1-C10)ureido, N'',N''-di(alquil C1-C10)ureido, (alquil C1-C10)sulfamido, aminosulfonilo, mono- o di(alquil C1-C10)aminosulfonilo, ciano, difluorometoxi o trifluorometoxi; R5 representa un grupo -COOR7 o un grupo arilo C5-C14 monocíclico o policíclico o un grupo heteroarilo de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, que está opcionalmente sustituido con uno o más sustituyentes seleccionados de: * átomos de halógeno; * grupos alquilo C1-C20 y alquileno C2-C20, que están opcionalmente sustituidos con uno o más sustituyentes seleccionados de átomos de halógeno y grupos fenilo, hidroxi, hidroxialquilo C1-C10, alcoxi C1-C10, ariloxi C5-C14, (alquil C1-C10)tio, oxo, amino, mono- o di-(alquil C1-C10)amino, acilamino, hidroxicarbonilo, (alcoxi C1-C10)carbonilo, carbamoilo, mono- o di(alquil C1-C10)carbamoilo; y * grupos fenilo, hidroxi, (alquileno C1-C6)dioxi, alcoxi C1-C10, cicloalcoxi C3-C7, nitro, (alquil C1-C10)tio, (alquil C1-C10)sulfinilo, (alquil C1-C10)sulfonilo, (alquil C1-C10)sulfamoilo, amino, mono- o di(alquil C1-C10)amino, acilamino, nitro, acilo, hidroxicarbonilo, (alcoxi C1-C10)carbonilo, carbamoilo, mono- o di(alquil C1-C10)carbamoilo, ureido, N''-(alquil C1-C10)ureido, N'',N''-di(alquil C1-C10)ureido, (alquil C1-C10)sulfamido, aminosulfonilo, mono- o di(alquil C1-C10)aminosulfonilo, ciano, difluorometoxi o trifluorometoxi; en el que R7 representa un alquilo C1-C20 que está opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halógeno y grupos hidroxi, alcoxi C1-C10, ariloxi C5-C14, (alquil C1-C10)tio, oxo, amino, mono- o di(alquil C1-C10)amino, acilamino, hidroxicarbonilo, (alcoxi C1-C10)carbonilo, carbamoilo, mono- o di-(alquil C1-C10)carbamoilo o un grupo de fórmula -(CH2)m-R11 en la que m es un número entero de 0 a 4 y R11 representa: * un grupo cicloalquilo C3-C7 o cicloalquenilo C3-C7; * un grupo arilo C5-C14, que está opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halógeno y grupos alquilo C1-C20, hidroxi, alcoxi C1-C10, (alquileno C1-C6)dioxi, (alquil C1-C10)tio, amino, mono- o di(alquil C1-C10)amino, nitro, acilo, hidroxicarbonilo, (alcoxi C1-C10)carbonilo, carbamoilo, mono- o di-(alquil C1-C10)carbamoilo, ciano, trifluorometilo, difluorometoxi o trifluorometoxi; * o un anillo de 3 a 7 miembros que comprende de 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno y azufre, anillo que puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halógeno y grupos alquilo C1-C20, hidroxi, alcoxi C1-C10, (alquileno C1-C6)dioxi, amino, mono- o di(alquil C1-C10)amino, nitro, ciano o trifluorometilo; y R4 representa * un grupo alquilo que tiene de 1 a 6 átomos de carbono y que está opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halógeno y grupo hidroxi; * un grupo mono-(alquil C1-C4)amino o di-(alquil C1-C4)amino no sustituido; * un grupo alquilo C1-C4 que está no sustituido o sustituido con uno o más sustituyentes seleccionados de grupos hidroxi, alcoxi C1-C4, amino, mono(alquil C1-C4)amino y di(alquil C1-C4)amino; * un grupo fenil(alquilo C1-C4)- no sustituido; o * un grupo de fórmula -(CH2)p-R12 en la que p es 2 y R12 representa un radical seleccionado de fenilo, piridilo y tienilo opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halógeno y grupos alquilo C1-C20, hidroxi, alcoxi C1-C10, (alquileno C1-C6)dioxi, amino, mono- o di(alquil C1-C10)amino, nitro, ciano y trifluorometilo, siendo cada resto acilo en R3, R5 y R11 un radical C2-C20 unido a un radical carbonilo; asi como los N-óxidos obtenibles de los radicales heteroarilo presentes en la estructura cuando dichos radicales comprenden átomos de nitrógeno y sus sales farmacéuticamente aceptables, con la condición de que cuando R5 no es un grupo heteroarilo opcionalmente sustituido ni un grupo COOR7, entonces R3 es un grupo heteroarilo opcionalmente sustituido.
ES03782471T 2002-12-26 2003-12-22 Nuevos derivados de piridazin-3(2h)-ona. Expired - Lifetime ES2301859T3 (es)

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