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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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Argentina
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group
alkyl
whose
amino
substituted
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ARP020103508A
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English (en)
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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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Publication of AR036598A1 publication Critical patent/AR036598A1/es

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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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US (2) US6974810B2 (es)
EP (1) EP1429762A1 (es)
JP (1) JP4313672B2 (es)
KR (1) KR100950430B1 (es)
CN (2) CN101195604A (es)
AR (1) AR036598A1 (es)
AU (1) AU2002333853B2 (es)
BR (1) BR0208253A (es)
CA (1) CA2442245C (es)
HR (1) HRP20030913A2 (es)
HU (1) HUP0402113A3 (es)
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MX (1) MXPA03009439A (es)
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NZ (1) NZ528280A (es)
PL (1) PL367814A1 (es)
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UA (1) UA77441C2 (es)
WO (1) WO2003026648A1 (es)
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