AR051675A1 - Derivados de 3-fenil-pirazol como moduladores del receptor 5-ht2a de la serotonina utiles para el tratamiento de trastornos relacionados con este - Google Patents

Derivados de 3-fenil-pirazol como moduladores del receptor 5-ht2a de la serotonina utiles para el tratamiento de trastornos relacionados con este

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AR051675A1
AR051675A1 ARP050104844A ARP050104844A AR051675A1 AR 051675 A1 AR051675 A1 AR 051675A1 AR P050104844 A ARP050104844 A AR P050104844A AR P050104844 A ARP050104844 A AR P050104844A AR 051675 A1 AR051675 A1 AR 051675A1
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Argentina
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alkoxy
alkyl
cycloalkyl
alkenyl
group
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Arena Pharm Inc
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Abstract

Los compuestos y sus composiciones farmacéuticas están dirigidos hacia métodos utiles en el tratamiento de la agregacion plaquetaria, arteriopatía, coronaria, infarto de miocardio, accidente isquémico transitorio, angina, accidente cerebrovascular, fibrilacion auricular, reduccion del riesgo de formacion de coágulos sanguíneos, asma o sus síntomas, agitacion o un síntoma, trastornos de la conducta, psicosis farmacogena, psicosis excitativa, síndrome de Gilles de la Tourette, trastorno maníaco, psicosis orgánico o sin especificacion, trastorno psicotico, psicosis, esquizofrenia agua, esquizofrenia cronica, esquizofrenia sin especificacion y trastornos relacionados, y trastornos del sueno, trastornos relacionados con la diabetes, leucoencefalopatía multifocal progresiva y semejantes. Reivindicacion 1: Un compuesto de formula (1), o una sal farmacéuticamente aceptable, hidrato o solvato de dicho compuesto; en donde: V es O, S, S(=O), S(=O)2 o NR10; W es C1-4 alquileno opcionalmente sustituido con 1 a 8 sustituyentes seleccionados independientemente entre el grupo integrado por C1-3 alquilo, C1-4 alcoxilo, carboxilo, ciano, C1-3 haloalquilo, halogeno y oxo, o W está ausente; X es C(=O), C(=S) o está ausente; Y es O, NR11 o está ausente; Z es C1-4 alquileno o C3-6 cicloalquileno, cada uno opcionalmente sustituido con 1 a 8 sustituyentes seleccionados independientemente entre el grupo integrado por C1-3 alquilo, C1-4 alcoxilo, carboxilo, ciano, C1-3 haloalquilo, halogeno, hidroxilo y oxo, o Z está ausente; R1 se selecciona del grupo integrado por H, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo y C3-7 cicloalquilo; R2 se selecciona del grupo integrado por H, C1-6 acilo, C1-6 aciloxilo, C2-6 alquenilo, C1-6 alcoxilo, C1-6 alquilo, C1-6 alquilcarboxamida, C2-6 alquinilo, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio, C1-6 alquilureilo, amino, C1-6 alquilamino, C2-8 dialquilamino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-7 cicloalquilo, C2-8 dialquilcarboxamida, C2-8 dialquilsulfonamida, halogeno, C1-6 haloalcoxilo, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, hidroxilo, tiol, nitro y sulfonamida; R3 se selecciona del grupo integrado por H, C2-6 alquenilo, C1-6 alquilo, C1-6 alquilcarboxamida, C2-6 alquinilo, C1-6 alquilsulfonamida, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-7 cicloalquilo, C2-8 dialquilcarboxamida, halogeno, heteroarilo y fenilo; y en donde cada grupo C2-6 alquenilo, C1-6 alquilo, C2-6 alquinilo, C1-6 alquilsulfonamida, C3-7 cicloalquilo, heteroarilo y fenilo está opcionalmente sustituido con 1 a 5 sustituyentes seleccionados independientemente entre el grupo integrado por C1-5 acilo, C1-5 aciloxilo, C2-6 alquenilo, C1-4 alcoxilo, C1-8 alquilo, C1-6 alquilamino, C2-8 dialquilamino, C1-4 alquilcarboxamida, C2-6 alquinilo C1-4 alqulsulfonamida, C1-4 alquilsulfinilo, C1-4 alquilsulfonilo, C1-4 alquiltio, C1-4 alquilureilo, amino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-6 cicloalquilo, C2-6 dialquilcarboxamida, halogeno, C1-4 haloalcoxilo, C1-4 haloalquilo, C1-4 haloalquilsulfinilo, C1-4 haloalquilsulfonilo, C1-4 haloalquiltio, hidroxilo, nitro y sulfonamida; R4 es heterociclo, heterociclo, o heteroarilo, cada uno independientemente sustituido con sustituyentes seleccionados independientemente entre el grupo integrado por C1-6 acilo, C1-12 aciloxilo, C2-6 alquenilo, C1-4 alcoxilo,C1-6 alcoxicarbonilamino, C1-6 alquilo, C1-6 alquilamino, C2-8 dialquilamino, C1-4 alquilcarboxamida, C2-6 alquinilo, C1-4 alquilsulfonamida, C1-4 alquilsulfonilo, C1-4 alquilsulfonilo, C1-4 alquiltio, C1-4 alquilureilo, amino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-6 cicloalquilo, C3-7 cicloalquilcarbonilo, C2-6 dialquicarboxamida, formilo, halogeno, C1-4 haloalcoxilo, C1-4 haloalquilo, C1-4 haloalquilsulfinilo, C1-4 haloalquilsulfonilo, C1-4 haloalquiltio, heteroarilo, hidroxilo, nitro, fenilo y sulfonamida; en donde cada C1-5 acilo, C1-5 aciloxilo, C1-4 alcoxilo, C1-6 alquilo, C1-4 alquilcarboxamida, amino, carbo-C1-6-alcoxilo y heteroarilo está opcionalmente sustituido con sustituyentes seleccionados independientemente entre el grupo integrado por C1-6 alquilo, C1-5 acilo, C1-4 alcoxilo, C1-6 alquilamino, C2-8 dialquilamino, C1-4 alquilcarboxamida, C1-4 alquilsulfonilo, amino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-6 cicloalquilo, halogeno, C1-4 haloalcoxilo, C1-4 haloalquilo, hidroxilo y fenilo; R5, R6, y R7 se seleccionan independientemente del grupo integrado por H, C1-6 acilo, C1-6 aciloxilo, C2-6 alquenilo, C1-6 alcoxilo, C1-6 alquilo, C1-6 alquilcarboxamida, C2-6 alquinilo, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio, C1-6 alquilureilo, amino, C1-6 alquilamino, C2-8 dialquilamino, C1-6 alquilimino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-7 cicloalquilo, C2-8 dialquilcarboxamida, C2-8 dialquilsulfonamida, halogeno, C1-6 haloalcoxilo, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, heterociclo, hidroxilo, tiol, nitro, fenoxilo y fenilo; R8 es C1-8 alquilo, C2-6 alquenilo, arilo, C3-7 cicloalquilo o heteroarilo, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente entre el grupo integrado por C1-6 acilo, C1-6 aciloxilo, C2-6 alquenilo, C1-6 alcoxilo, C1-6 alquilo, C1-6 alquilcarboxamida, C2-6 alquinilo, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio, C1-6 alquilureilo, amino, C1-6 alquilamino, C2-8 dialquilamino, C1-6 alquilimino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-7 cicloalquilo, C2-8 dialquilcarboxamida, C2-8 dialquilsulfonamida, halogeno, C1-6 haloalcoxilo, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, heterociclo, hidroxilo, tiol, nitro, fenoxilo y fenilo, o dos sustituyentes adyacentes junto con dicho arilo o dicho heteroarilo forman un C5-7 cicloalquilo que opcionalmente comprende 1 a 2 átomos de oxígeno y opcionalmente está sustituido con F, Cl o Br; y en donde cada C2-6 alquenilo, C1-6 alquilo, C2-6 alquinilo, C1-6 alquilamino, C1-6 alquilimino, C2-8 dialquilamino, heterociclo y fenilo está opcionalmente sustituido con 1 a 5 sustituyentes seleccionados independientemente entre el grupo integrado por C1-6 acilo, C1-6 aciloxilo, C2-6 alquenilo, C1-6 alcoxilo, C1-6 alquilo, C1-6 alquilcarboxamida, C2-6 alquinilo, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio, C1-6 alquilureilo, amino, C1-6 alquilamino, C2-8 dialquilamino, carbo-C1-6-alcoxilo, carboxamida, carboxilo, ciano, C3-7 cicloalquilo, C2-8 dialquilcarboxamida, halogeno, C1-6 haloalcoxilo, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, hidroxilo, tiol y nitro; y R9, R10 y R11 son independientemente H o C1-8 alquilo; siempre que dicho compuesto no sea N-[4-oxiranilmetoxi-3-(2H-pirazol-3-il)-fenil]-acetamida.
ARP050104844A 2004-11-19 2005-11-17 Derivados de 3-fenil-pirazol como moduladores del receptor 5-ht2a de la serotonina utiles para el tratamiento de trastornos relacionados con este AR051675A1 (es)

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