ES2323952T3 - 3-aminopirazol triciclicos sustituidos en n como inhibidores receptores de pdfg. - Google Patents

3-aminopirazol triciclicos sustituidos en n como inhibidores receptores de pdfg. Download PDF

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ES2323952T3
ES2323952T3 ES03728909T ES03728909T ES2323952T3 ES 2323952 T3 ES2323952 T3 ES 2323952T3 ES 03728909 T ES03728909 T ES 03728909T ES 03728909 T ES03728909 T ES 03728909T ES 2323952 T3 ES2323952 T3 ES 2323952T3
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benzofused
nhalkyl
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Chih Yung Ho
Bengt Anders Brunmark
Stuart Emanuel
Jr Robert A Galemmo
Dana L Johnson
Donald W Ludovici
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D495/04—Ortho-condensed systems

Abstract

Un compuesto de Fórmula (I): ** ver fórmula** donde, n es un número entero de 1 a 4; R1 se selecciona del grupo que consiste en hidrógeno, alquilo inferior, -OH, alcoxi, -oxo, -NH2, -NH(alquilo) y -N (alquilo)2; ** ver fórmula** se selecciona del grupo que consiste en un arilo, un heteroarilo monocíclico de cinco a seis miembros, un heteroarilo benzofusionado de nueve a diez miembros, un grupo heterocicloalquilo benzofusionado de nueve a diez miembros, y un grupo cicloalquilo benzofusionado de nueve a diez miembros; donde el grupo heteroarilo benzofusionado, heterocicloalquilo benzofusionado o cicloalquilo benzofusionado está anclado a la molécula de manera que el anillo de fenilo está unido directamente a la porción ** ver fórmula** de la molécula; p es un número entero de 0 a 2; R2 se selecciona del grupo que consiste en ** ver fórmula** y -X-A1-Y-A2; donde, X e Y están cada uno independientemente ausentes o se seleccionan del grupo que consiste en -O-, -NH-, -N(alquil)-, -S-, -SO-, -SO2-, -OC(=O), -C(=O)O-, -NH(=O)-, -N(alquil)C(=O)-, -C(=O)NH-, -C(=O)N(alquil)-, -OC(=O)O-, -NHC(=O)O-, -OC(=O)NH-, -N(alquil)C(=O)O-, -OC(=O)N(alquil)-, -NHC(=O)NH-, -NHC(=O)N(alquil)-, -N(alquil)C(=O)NH-, -N(alquil)C(=O)N(alquil)-, -NHSO2-, -SO2NH-, -N(alquil)SO2- y -SO2N(alquil)-; A1 está ausente o se selecciona entre alquilo o alquenilo; A2 se selecciona entre alquilo, alquenilo, o H; donde, cuando A1 o A2 es alquilo o alquenilo, el grupo alquilo o alquenilo puede estar sustituido opcionalmente con uno o más grupos seleccionados independientemente entre halógeno, ciano, hidroxi, alcoxi, tio, alcoxi halogenado, -OC(=O) alquilo, -OC(=O)Oalquilo, amino, alquilamino, -NHC(=O)alquilo, -N(alquil)C(=O)alquilo, dialquilamino, -NHC(=O) NH2, -NHC(=O)NHalquilo, -N(alquil)C(=O)NHalquilo, -N(alquil)C(=O)NH2, -OC(=O)NHalquilo, -NHC(=O)Oalquilo, -N(alquil)C(=O)Oalquilo, -NHSO2alquilo, -N(alquil)SO2alquilo, tioalquilo, tioalquilo halogenado, -SO2alquilo, -SO2alquilo halogenado, -NHC(=O)N(alquilo)2, -N(alquil)C(=O)N(alquilo)2 o -OC(=O)N(alquilo)2; ** ver fórmula** se selecciona del grupo que consiste en un arilo, un cicloalquilo, un carbociclo parcialmente insaturado, un heteroarilo, un heterocicloalquilo, un cicloalquilo benzofusionado de nueve a diez miembros, y un heterocicloalquilo benzofusionado de nueve a diez miembros; donde, el arilo, cicloalquilo, carbociclo parcialmente insaturado, heteroarilo, heterocicloalquilo, cicloalquilo benzofusionado, o heterocicloalquilo benzofusionado, está sustituido opcionalmente con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxi, amino, tio, nitro, ciano, alquilo, alquilo halogenado, alcoxi, alcoxi halogenado, alquilamino, -NHC(=O)alquilo, -N(alquil)C(=O)alquilo, o dialquilamino, -NHC(=O)NH2, -NHC(=O)NHalquilo, -N(alquil)C(=O)NHalquilo, -OC(=O)NHalquilo, -NHC(=O)Oalquilo, -N(alquil)C(=O)Oalquilo, -NHSO2alquilo, -N(alquil)SO2alquilo, tioalquilo, tioalquilo halogenado, -SO2alquilo, -SO2alquilo halogenado, -NHC(=O)N(alquilo)2, -N(alquil)C(=O)N(alquilo)2 o -OC(=O)N(alquilo)2; q es un número entero de 0 a 4; R3 se selecciona del grupo que consiste en halógeno, hidroxi, amino, tio, nitro, ciano, alquilo, alquilo halogenado, alcoxi, alquiloxi halogenado, alquilamino, -NHC(=O)alquilo, -N(alquil)C(=O)alquilo, o dialquilamino, -NHC(=O) NH2, -NHC(=O)NHalquilo, -N(alquil)C(=O)NHalquilo, -OC(=O)NHalquilo, -NHC(=O)Oalquilo, -N(alquil)C(=O) Oalquilo, -NHSO2alquilo, -N(alquil)SO2alquilo, tioalquilo, tioalquilo halogenado, -SO2alquilo, -SO2alquilo halogenado, -NHC(=O)N(alquilo)2, -N(alquil)C(=O)N(alquilo)2 y -OC(=O)N(alquilo)2; siempre que la suma de p y q sea un número entero de 0 a 4; L1 está ausente o se selecciona del grupo que consiste en alquilo; ** ver fórmula** se selecciona del grupo que consiste en un arilo, un cicloalquilo, un carbociclo parcialmente insaturado, un heteroarilo, un heterocicloalquilo, un cicloalquilo benzofusionado de nueve a diez miembros, y un heterocicloalquilo benzofusionado de nueve a diez miembros; o uno de sus isómeros ópticos, enantiómeros, diastereómeros, racematos, o sales farmacéuticamente aceptables; donde "alquilo" significa un grupo alquilo de cadena lineal o ramificada que tiene de 1 a 10 átomos de carbono; "alcoxi" y "alquiloxi" significan un radical éter de oxígeno de dicho grupo alquilo; "alquilo inferior" significa un grupo alquilo de cadena lineal o ramificada que tiene de 1 a 4 átomos de carbono; "alcoxi inferior" y "alquiloxi inferior" significan un radical éter de oxígeno de dicho grupo alquilo inferior; "arilo" significa fenilo, naftilo o fluorenilo; "heteroarilo" significa una estructura anular aromática monocíclica o bicíclica de cinco a diez miembros que contiene átomos de carbono y al menos un heteroátomo seleccionado del grupo que consiste en O, N y S; "cicloalquilo" significa un sistema anular saturado, de tres a diez miembros; "heterocicloalquilo" significa una estructura anular saturada o parcialmente insaturada, monocíclica o bicíclica de cinco a diez miembros que contiene átomos de carbono y al menos un heteroátomo seleccionado del grupo que consiste en O, N y S; y "carbociclo parcialmente insaturado" significa un sistema anular parcialmente insaturado, de cinco a diez miembros que contiene al menos un enlace insaturado.
ES03728909T 2002-05-15 2003-05-13 3-aminopirazol triciclicos sustituidos en n como inhibidores receptores de pdfg. Expired - Lifetime ES2323952T3 (es)

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