ES2354569T3 - Antagonistas del receptor de histamina-3. - Google Patents

Antagonistas del receptor de histamina-3. Download PDF

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ES2354569T3
ES2354569T3 ES06765575T ES06765575T ES2354569T3 ES 2354569 T3 ES2354569 T3 ES 2354569T3 ES 06765575 T ES06765575 T ES 06765575T ES 06765575 T ES06765575 T ES 06765575T ES 2354569 T3 ES2354569 T3 ES 2354569T3
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Travis T. Wager
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Pfizer Products Inc
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Pfizer Products Inc
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Abstract

Un compuesto de fórmula Ia o Ib **Fórmula** o una sal farmacéuticamente aceptable del mismo, o el isómero cis, el isómero trans, o una mezcla de isómeros cis y trans, en las que: R1 se selecciona entre el grupo que consiste en OR4 y NR2R3; cada uno de R2 y R3 se selecciona independientemente entre el grupo que consiste en hidrógeno; alquilo C1-C8 opcionalmente sustituido con 1 a 4 halógenos; grupo alquilo C1-C4 opcionalmente sustituido con un sustituyente seleccionado entre el grupo que consiste en OH, de uno a cuatro alquilo C1-C4, cicloalquilo C3-C7, dialquilamino C1-C4, arilo C6-C14 opcionalmente sustituido con un halógeno o ariloxi C6-C10 opcionalmente sustituido con uno a dos halógenos, y heteroarilo de 5-10 miembros opcionalmente sustituido con un grupo arilo C6-C10 y opcionalmente sustituido con uno a tres grupos alquilo C1-C4; cicloalquilo C3-C7; arilo C6-C14; heterocicloalquilo de 3-8 miembros opcionalmente sustituido con uno o más grupos alquilcarbonilo C1-C4; arilsulfonilo C6-C10 opcionalmente sustituido con uno o más alquilo C1-C2; heteroarilo de 5-10 miembros; aril C6-C14-alquileno C0-C4-O-alquilo C0-C4, en el que cada alquilo C0-C4 y cada alquileno C0-C4 está opcionalmente sustituido con uno a cuatro alquilo C1-C4; -C(=O)R3, -S(O)2R3'; en el que R3' se selecciona entre el grupo que consiste en hidrógeno, alquilo (C1-C4), alquenilo (C1-C4), arilo, heteroarilo, cicloalquilo (C3-C7), cicloheteroalquilo (C3-C7), y en el que cada hidrógeno en R3' puede estar opcionalmente sustituido independientemente con halo, alquilo (C1-C4), alquenilo (C2-C4) y -S(O)2CH3; en el que R3 25 puede seleccionarse adicionalmente entre el grupo que consiste en arilcarbonil C6-C14-arilo C6-C14; arilcarbonil C6-C14-heterocicloalquilo de 3-8 miembros; cicloalquilcarbonil C3- C8-arilo C6-C14; cicloalquilcarbonil C3-C8-heterocicloalquilo de 3-8 miembros; heterocicloalquilcarbonilo de 3- 8 miembros-arilo C6-C14; y heterocicloalquilcarbonil de 3-8 miembros-heterocicloalquilo 3-8 miembros; o R3 y R2 junto con el nitrógeno del grupo NR2R3 forman un primer anillo alifático de 5, 6 ó 7 miembros, en el que uno de los carbonos en el primer anillo alifático de 5, 6 ó 7 miembros está reemplazado opcionalmente por O, S, NR2' o CO, y el primer anillo alifático de 5, 6 ó 7 miembros está condensado con un arileno C6-C10 y está opcionalmente sustituido en un carbono del anillo con un sustituyente seleccionado entre el grupo que consiste en heteroarilo de 5-10 miembros opcionalmente sustituido con uno o más halógenos y opcionalmente sustituido con uno o más alquilo C1-C2, alcoxi C1-C4 opcionalmente sustituido con uno o más alcoxi C1-C2 y opcionalmente sustituido con uno o más dialquilaminocarbonilo C1-C4, y uno o dos alquilo C1-C4 opcional e independientemente sustituidos con uno o más alcoxi C1-C2; en las que R2' es hidrógeno; alquilo C1-C8 opcionalmente sustituido con 1 a 4 halógenos; heteroarilo de 5-10 miembros opcionalmente sustituido con un sustituyente seleccionado entre el grupo qu5 e consiste en halógeno, alquilo C1-C4, alcoxi C1-C2, arilo C6-C10, alquilaminocarbonilo C1-C4, y ciano; grupo alquilo C1-C4 opcionalmente sustituido con un sustituyente seleccionado entre el grupo que consiste en alcoxi C1-C2-carbonilo, heteroarilo de 5-10 miembros opcionalmente sustituido con uno o más alquilo C1- C2, de uno a cuatro alquilo C1-C4, cicloalquilo C3-C7 y arilo C6-C14; arilo C6-C10 opcionalmente sustituido con uno o dos alquilo C1-C2; alquilcarbonilo C1-C4; o aril C6-C14-alquileno C0-C4-O-alquilo C0-C4, en el que cada alquilo C0-C4 y cada alquileno C0-C4 está opcionalmente sustituido con uno a cuatro alquilo C1-C4; alquilsulfonilo C1-C4 R4 es hidrógeno o metilo; cada uno de R5 y R6 se selecciona independientemente entre el grupo que consiste en hidrógeno; grupo alquilo C1-C4 opcionalmente sustituido con un sustituyente seleccionado entre el grupo que consiste en OH, alquilo C1-C3, alcoxi C1-C3; o R5 y R6 junto con el nitrógeno al que están unidos forman una amina cíclica de 3-7 miembros opcionalmente sustituida con uno o más alquilo C1-C4; R7 es independientemente hidrógeno o metilo; n es 1, 2 ó 3; m es 1, 2 ó 3; Z se selecciona independientemente entre el grupo que consiste en hidrógeno, halógeno, alquilo C1-C4, alcoxi C1-C4 y -C(H)=CH2; o en la que, cuando m es 2 y ambos Z son -C(H)=CH2, ambos Z junto con 2 carbonos adyacentes o el anillo de fenilo de fórmula I forman un anillo aromático de 6 miembros condensado con dicho anillo de fenilo.
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