ES2613538T3 - Derivados de arilamida como bloqueadores de TTX-S - Google Patents

Derivados de arilamida como bloqueadores de TTX-S Download PDF

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ES2613538T3
ES2613538T3 ES11834032T ES11834032T ES2613538T3 ES 2613538 T3 ES2613538 T3 ES 2613538T3 ES 11834032 T ES11834032 T ES 11834032T ES 11834032 T ES11834032 T ES 11834032T ES 2613538 T3 ES2613538 T3 ES 2613538T3
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independently selected
alkyl
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Tatsuya Yamagishi
Kiyoshi Kawamura
Yoshimasa Arano
Mikio Morita
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Raqualia Pharma Inc
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Abstract

Un compuesto de la siguiente fórmula (II)**Fórmula** en la que R1 se selecciona independientemente entre el grupo que consiste en -CF3, -CHF2, -OCF3, - OCHF2, -OCH2CHF2, -OCH2CF3, -OCF2CHF2, -OCF2CF3, -OCH2CH2CF3, - OCH(CH3)CF3, -OCH2C(CH3)F2, -OCH2CF2CHF2, - OCH2CF2CF3, -OCH2CH2OCH2CF3, - NHCH2CF3, -SCF3, -SCH2CF3, -CH2CF3, 10 -CH2CH2CF3, -CH2OCH2CF3 y - OCH2CH2OCF3; R2 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) hidroxilo, (4) -On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (5) -On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (6) - On-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (7) -On-fenilo o -On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (8) -On-grupo heterocíclico, donde el grupo heterocíclico está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (9) -(C>=O)-NR7R8, (10) -NR7R8, (11) -S(O)2-NR7R8, (12) -NR7- S(O)2R8, (13) -S(O)t-R7, donde t es 0, 1 o 2, (14) - NR7(C>=O)R8, (15) -CN y (16) -NO2; en la que n es 0 o 1, cuando n es 0, está presente un enlace químico en el lugar de -On-; p es 1, 2, 3 o 4; cuando p es dos o más de dos, R2 puede ser igual o diferente; R3 y R4 son independientemente hidrógeno o alquilo C1-6 que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo y -O-alquilo C1-6, ni R3 ni R4 son alquilo C1-6 al mismo tiempo. R5 se selecciona entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) hidroxilo, (4) -(C>=O)m-Ol-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (5) -Ol-perfluoroalquilo (C1-3), (6) -(C>=O)m-Ol-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (7) -(C>=O)m-Ol-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (8) - (C>=O)m-Ol-fenilo o -(C>=O)m-Ol-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (9) -(C>=O)m-Ol-grupo heterocíclico, donde el grupo heterocíclico está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (10) -(C>=O)-NR7R8, (11) -NR7R8, (12) -S(O)2-NR7R8, (13) -S(O)t-R7, donde t es 0, 1 o 2, (14) -CO2H, (15) -CN y (16) -NO2; en la que I es 0 o 1 y m es 0 o 1; cuando I es 0 o m es 0, está presente un enlace químico en el lugar de -Ol- o -(C>=O)m- y cuando I es 0 y m es 0, está presente un enlace químico en el lugar de - (C>=O)m-Ol-; R6 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) hidroxilo, (3) halógeno, (4) -alquilo C1-6, (5) -cicloalquilo C3-6, (6) - O-alquilo C1-6, (7) - O(C>=O)-alquilo C1-6, (8) -NH-alquilo C1-6, (9) fenilo, (10) grupo heterocíclico y (11) -CN; R7 y R8 son independientemente hidrógeno, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-7 o arilo, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, alquilo C1-6 y -O-alquilo C1-6; o R7 forman un anillo de 4 a 7 miembros con R8 que puede contener un átomo de nitrógeno, un átomo de oxígeno, un átomo de azufre o un doble enlace, en la que el anillo de 4 a 7 miembros está opcionalmente sustituido con 1 a 6 sustituyentes seleccionados independientemente entre el grupo que consiste en: (1) hidrógeno, (2) hidroxilo, (3) halógeno, (4) alquilo C1-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (5) cicloalquilo C3-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (6) -O-alquilo C1-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, y (7) -Ocicloalquilo C3-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6; X es un átomo de nitrógeno o un átomo de carbono; Z es un átomo de nitrógeno o un átomo de carbono; Y es hidrógeno o alquilo C1-6; R9 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) -On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (4) - On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5 y (5) -Onalquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5; en la que n es 0 o 1, cuando n es 0, está presente un enlace químico en el lugar de -On-; q es 1, 2 o 3; cuando q es dos o más de dos, R9 puede ser igual o diferente; R10 es independientemente hidrógeno, alquilo C1-6, alquenilo C2-6 o cicloalquilo C3-7, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, alquilo C1-6, -O-alquilo C1-6, -cicloalquilo C3-7 y -O-cicloalquilo C3-7; o una sal farmacéuticamente aceptable del mismo.
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