AR036598A1 - Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1 - Google Patents

Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1

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Publication number
AR036598A1
AR036598A1 ARP020103508A ARP020103508A AR036598A1 AR 036598 A1 AR036598 A1 AR 036598A1 AR P020103508 A ARP020103508 A AR P020103508A AR P020103508 A ARP020103508 A AR P020103508A AR 036598 A1 AR036598 A1 AR 036598A1
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group
alkyl
whose
amino
substituted
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ARP020103508A
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Josephus H M Lange
Cornelis G Kruse
Jacobus Tipker
Stuivenberg Herman H Van
Arnoldus H J Herremans
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Solvay Pharm Bv
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Abstract

Derivados de 4,5-dihidro-1H-pirazol que son potentes antagonistas de receptores (CB1) de cannabinoides con utilidad para el tratamiento de enfermedades conectadas con desórdenes del sistema cannabinoide. Los compuestos tienen la fórmula general (1) ó (2), en donde: R y R1 representan independientemente fenilo, tienilo o piridilo, cuyos grupos pueden estar sustituidos con 1, 2, ó 3 sustituyentes Y, que pueden ser iguales o diferentes, del grupo alquilo o alcoxi C1-3, hidroxi, halógeno, trifluorometilo, trifluorometiltio, trifluorometoxi, nitro, amino, mono- o dialquil C1-2-amino, mono o dialquil C1-2-amido, alquil C1-3-sulfonilo, dimetilsulfamido, alcoxi C1-3-carbonilo, carboxilo, trifluorometilsulfonilo, ciano, carbamoílo, sulfamoílo y acetilo, o R y/o R1 representa naftilo; R2 representa hidrógeno, hidroxi, alcoxi C1-3, acetiloxi o propioniloxi; R3 representa un átomo de hidrógeno o un grupo alquilo C1-8 ramificado o no ramificado o un grupo cicloalquilo C3-7 cuyo grupo alquilo o gtupo cicloalquilo puede estar sustituido con un grupo hidroxi; R4 representa un átomo de hidrógeno o un grupo molecular alquilo C1-8 ramificado o no ramificado, cicloalquilo C3-8, heteroalquilo C2-10, heterocicloalquilo C3-8 no aromático o heterocicloalquil-alquilo C4-10 no aromático cuyos grupos moleculares pueden contener uno o más heteroátomos del grupo (O, N, S), cuyos grupos moleculares pueden estar sustituidos con un grupo ceto, grupo trifluorometilo, grupo alquilo C1-3, hidroxi, amino, monoalquilamino, o grupo dialquilamino o un átomo de flúor, o R4 representa un grupo amino, hidroxi, fenoxi o benciloxi o R4 representa un grupo alcoxi C1-8, alquenilo C3-8, ramificados o no ramificados, cicloalquenilo C5-8 o cicloalquenilalquilo C6-9 cuyos grupos pueden contener un átomo de azufre, nitrógeno u oxígeno, un grupo ceto o un grupo -SO2- cuyos grupos alcoxi C1-8, alquenilo C3-8, cicloalquenilo C5-8 o cicloalquenilalquilo C6-9 pueden estar sustituidos con un grupo hidroxi, un grupo trifluorometilo, un grupo amino, un grupo monoalquilamino o un grupo dialquilamino o un átomo de flúor, o R4 representa un grupo fenilo, bencilo, piridilo, tienilo, piridilmetilo o fenetilo en donde los anillos aromáticos pueden estar sustituidos con 1, 2 ó 3 de los sustituyentes Y, en donde Y tiene el significado como indicado anteriormente, o R4 representa un grupo NR8R9 con la condición que R3 representa un átomo de hidrógeno o un grupo metilo y en donde R8 y R9 son iguales o diferentes y representan alquilo C1-4 o trifluoroalquilo C2-4 o R8 y R9, junto con el átomo de nitrógeno al cual ellos están unidos, forman un grupo molecular heterocíclico saturado o no saturado que tiene 4 a 8 átomos de anillo cuyo grupo molecular heterocíclico puede contener un átomo de oxígeno o de azufre o un grupo ceto o un grupo -SO2- o un átomo de nitrógeno adicional, cuyo grupo molecular heterocíclico saturado o no saturado puede estar sustituido con un grupo alquilo C1-4 ó R3 y R4, junto con el átomo de nitrógeno al cual ellos están unidos, forman un grupo molecular heterocíclico monocíclico o bicíclico, saturado o no saturado que tiene 4 a 10 átomos de anillo, cuyo grupo molecular heterocíclico puede contener uno o más átomos del grupo (O, N, S) o un grupo ceto o un grupo -SO2-, cuyo grupo molecular puede estar sustituido con un grupo alquilo C1-4, hidroxialquilo, fenilo, tienilo, piridilo, amino, monoalquilaminoalquilo, dialquilaminoalquilo, monoalquilamino, dialquilamino, aminoalquilo, azetidinilo, pirrolidinilo, piperidinilo o hexahidro-1H-azepinilo; R5 y R6 independientemente uno de otro representan un átomo de hidrógeno o un grupo alquilo o alquenilo C1-8 ramificado o no ramificado cuyos grupos pueden contener uno o más heteroátomos del grupo (O, N, S), un grupo ceto o un grupo -SO2- y cuyos grupos pueden estar sustituidos con un grupo hidroxi o amino, o R5 y R6 independientemente uno del otro representan un grupo cicloalquilo C3-8 o un grupo cicloalquenilo C3-8 cuyo grupo puede contener uno o más heteroátomos de anillo del grupo (O, N, S) o el grupo -SO2-, y cuyos grupos pueden estar sustituidos con un grupo hidroxi, alquilo C1-3, el grupo -SO2-, el grupo ceto, el grupo amino, el grupo monoalquil C1-3-amino o el grupo dialquil C1-3-amino, ó R5 representa un grupo naftilo o un grupo fenilo cuyo grupo fenilo puede estar sustituido con 1, 2 ó 3 sustituyentes Y en donde Y tiene el significado como el descripto anteriormente, con la condición que R6 representan un átomo de hidrógeno, o un grupo alquilo C1-5 ramificado o no ramificado cuyo grupo alquilo puede contener uno o más heteroátomos del grupo (O, N, S) o el grupo -SO2- y cuyo grupo alquilo puede estar sustituido con un grupo hidroxi, ceto o amino, o R5 y R6, junto con el átomo de nitrógeno al cual ellos están unidos, forman un grupo alquilo o alquenilo monocíclico, bicíclico o tricíclico el cual puede contener heteroátomos de anillo del grupo (O, N, S), el grupo ceto o el grupo SO2 y cuyo grupo alquilo o alquenilo monocíclico, bicíclico o tricíclico puede estar sustituido con un grupo hidroxi, un grupo alquilo C1-3, un grupo SO2, un grupo ceto, un grupo amino, un grupo monoalquil C1-3-amino, un grupo dialquil C1-3 amino, un grupo pirrolidinilo, un grupo piperidinilo, el cual grupo alquilo o alquenilo monocíclico, bicíclico o tricíclico puede contener un grupo fenilo condensado el cual grupo fenilo condensado puede estar sustituido con 1 ó 2 sustituyentes Y, en donde Y tiene el significado como se describió anteriormente; R7 representa un alquilo C1-3 ramificado o no ramificado, y tautómeros, estereoisómeros, prodrogas y sales de los mismos. Se describen métodos para la preparación de estos compuestos, y composiciones farmacéuticas que contienen uno o más de estos compuestos como un componente activo.
ARP020103508A 2001-09-21 2002-09-18 Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1 AR036598A1 (es)

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AR (1) AR036598A1 (es)
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