AR034547A1 - Derivados de indolin-2-ona, su utilizacion, procedimiento para su preparacion, composicion farmaceutica que lo contiene, medicamento que consiste en dicho derivado, y un producto que contiene dicho derivado y un antagonista de los receptores de la vasopresina - Google Patents

Derivados de indolin-2-ona, su utilizacion, procedimiento para su preparacion, composicion farmaceutica que lo contiene, medicamento que consiste en dicho derivado, y un producto que contiene dicho derivado y un antagonista de los receptores de la vasopresina

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AR034547A1
AR034547A1 ARP010101541A ARP010101541A AR034547A1 AR 034547 A1 AR034547 A1 AR 034547A1 AR P010101541 A ARP010101541 A AR P010101541A AR P010101541 A ARP010101541 A AR P010101541A AR 034547 A1 AR034547 A1 AR 034547A1
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Argentina
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alkyl
atom
alkoxy
pyrrolidinyl
piperidinyl
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ARP010101541A
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English (en)
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Georges Garcia
Gal Claudine Serradeil-Le
Gerard Vallette
Lodc Foulon
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Sanofi Aventis
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Publication of AR034547A1 publication Critical patent/AR034547A1/es

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Abstract

Derivado de indolin-2-ona en forma de enantiómero puro o de mezcla de enantiómeros de fórmula (1) en la cual: R0 representa un grupo elegido entre fórmula (2) en la cual: Z1 representa un átomo de cloro, bromo, yodo o flúor, alquilo C1-4, alcoxi C1-4 o trifluorometilo; Z2 representa un átomo de hidrógeno, de cloro, bromo, yodo o flúor, alquilo C1-4, cicloalquilo C3-5, alcoxi C1-4, cicloalcoxi C3-5, o polifluoroalquilo C1-4; R5 representa T1W en el cual T1 representa -(CH2)m, m puede ser igual a 0 o 1; W representa un átomo de hidrógeno, hidroxicarbonilo (o carboxilo), alcoxicarbonilo C1-4, 1,3-dioxolan-2-ilo, 1,3-dioxan-2-ilo, o bien W representa un grupo -NR6R7 en el cual R6 y R7 representan independientemente entre sí, un átomo de hidrógeno, alquilo C1-4, alquilsulfonilo C1-4 o fenilsulfonilo en el cual fenilo puede ser mono, di o trisustituido por Z5; o bien R6 y R7 forman con el átomo de nitrógeno al cual están unidos morfolinilo eventualmente sustituido por alquilo o un oxo, o bien R6 y R7 forman con el átomo de nitrógeno al cual están unidos piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3; o bien R6 y R7 forman con el átomo de nitrógeno al cual están unidos pirrolidinilo o piperidinilo, y dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z4; o bien W representa un grupo -NR8COR9 en el cual R8 representa un átomo de hidrógeno o alquilo C1-4 y R9 representa un átomo de hidrógeno, alquilo C1-4, bencilo, piridilo, fenilo, y dicho fenilo puede ser mono, di o trisustituido por Z5; o bien R9 representa un grupo -NR10R11 en el cual R10 y R11 representan independientemente entre sí, un átomo de hidrógeno o un alquilo C1-4, o bien R10 y R11 forman con el átomo de nitrógeno al cual están unidos, pirrolidinilo, piperidinilo, o morfolinilo eventualmente sustituido por alquilo C1-4, o bien R9 representa pirrolidin-2-ilo o 3-ilo, piperidin-2-ilo, 3-ilo o 4-ilo, dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z7; o bien R9 representa un grupo -T2-R12 o -T2-COR12 en el cual T2 representa -(CH2)n-, n puede ser igual a 1, 2, 3 y 4 y R12 representan alcoxi C1-4 o -NR10R11, R10 y R11 son tal como se los ha definido anteriormente; o bien W representa un grupo -CONR13R14 en el cual R13 representa un átomo de hidrógeno, alquilo C1-4, cicloalquilo C3-7, un mono- o polifluoro C1-4 alquilo, y R14 representa un átomo de hidrógeno, alquilo C1-4, fenilo eventualmente sustituido por Z5, -T4-R15 en el cual T4 represente -(CH2)q- con q igual a 1, 2, 3 o 4 y R15 representa hidroxilo, alcoxi C1-4, alcoxicarbonilo C1-4, alcoxicarbonilamino C1-4, fenilo eventualmente mono-, disustituido por Z5, un pirid-2-ilo, 3-ilo o 4-ilo, -NR16R17 en el cual R16 y R17 representan independientemente entre sí, un átomo de hidrógeno, o un alquilo C1-4, o bien R16 y R17 forman con el átomo de nitrógeno al cual están unidos morfolinilo eventualmente mono o disustituido por alquilo C1-4, o bien R16 y R17 forman con el átomo de nitrógeno al cual están unidos piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3, o bien R16 y R17 forman con el átomo de nitrógeno al cual están unidos pirrolidinilo o piperidinilo, dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z5 y se entiende que cuando q = 1, R15 es diferente de hidroxilo, alcoxi C1-4, alcoxicarbonilamino C1-4, -NR16R17; o bien R13 y R14 forman con el átomo de nitrógeno al cual están unidos un grupo morfolinilo eventualmente mono o disustituido por un grupo alquilo C1-4, piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3; o bien R13 y R14 forman con el átomo de nitrógeno al cual están unidos azetidinilo, pirrolidinilo o piperidinilo, hexahidroazepinilo, dichos grupos pirrolidinilo, piperidinilo y hexahidroazepinilo están eventualmente mono o disustituidos por Z8; o bien W representa un grupo OR18, en el cual R18 representa un átomo de hidrógeno, alquilo C1-4, alcoxi C1-4 alquilo C1-4 o -T3-R19 en el cual T3 representa -(CH2)p-, p puede ser igual a 2, 3 y R19 se elige entre los grupos hidroxilo, trifenilmetoxi, -NR20R21 en el cual R20 representa un átomo de hidrógeno o alquilo C1-4 y R21 representa un átomo de hidrógeno, alquilo C1-4, tetrahidrofuranilmetilo o tetrahidropiranilmetilo, o bien R20 y R21 forman con el átomos de nitrógeno al cual están unidos, morfolinilo eventualmente mono o disustituido por alquilo C1-4, piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3 o bien R20 y R21 forman con el átomo de nitrógeno al cual están unidos, pirrolidinilo o piperidinilo, dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z5; Z3 representa alquilo, piridilo o fenilo C1-4, alquilcarbonilo C1-4, alcoxicarbonilo C1-4; Z4 representa un oxo, un átomo de flúor, hidroxilo, alquilo C1-4, bencilo, amino, alquilamino C1-4, di C1-4 alquilamino, alcoxi C1-4, alcoxicarbonilo C1-4, alcoxicarbonilamino C1-4; Z5 representa un átomo de cloro, bromo, yodo o flúor, hidroxilo alquilo C1-4, o alcoxi C1-4; Z7 representa un átomo de flúor, hidroxilo, hidroxialquilo C1-4, alquilo C1-4, alcoxi C1-4, alquilcarbonilo C1-4; Z8 representa un átomo de flúor, hidroxilo alquilo C1-4, cicloalquilo C3-6, bencilo, amino, alquilamino C1-4, dialquilamino C1-4, alcoxicarbonilo C1-4, alcoxicarbonilamino C1-4, cicloalcoxi C3-6, hidroxicarbonilo, hidroxialquilo C1-4 o alcoxi C1-4 alquilo C1-4, alcoxi C1-4, -CONR23R24 en el cual R23 y R24 representan independientemente entre sí, un átomo de hidrógeno, alquilo C1-4, mono o polifluoroalquilo C1-4 o bien R23 y R24 forman con el átomo de nitrógeno al cual están unidos, pirrolidinilo o piperidinilo, dichos grupos pirrolidinilo o piperidinilo están eventualmente sustituidos por Z3, difluorometilideno; o R0 representa un grupo elegido entre fórmula (3)Z6 representa un átomo de cloro o alquilo C1-4 o alcoxi C1-4; R1 representa alquilo C1-4 que presenta eventualmente un doble o un triple enlace, alcoxicarbonilo C1-4; feniloxicarbonilo o un grupo T1-R22 en el cual T1 es tal como se ha definido anteriormente y R22 representa un grupo hidroxilo o alcoxi C1-4; R2 y R4 representan independientemente entre sí, un átomo de hidrógeno, de cloro o de flúor, alquilo C1-4 o alcoxi C1-4; R3 representa un átomo de cloro o de flúor, hidroxilo, alquilo C1-4, alcoxi C1-4, carbamoílo C1-4, alquilcarbonilamino C1-4, nitro, ciano, trifluorometilo, amino, cicloalquilamino C3-6, alquilamino C1-4, dialquilamino C1-4, trialquilamonio C1-4, A-, A- son un anión; pirrolidin-1-ilo, piperidin-1-ilo, piperazin-1-ilo, morfolin-4-ilo o hexahidroazepin-1-ilo; X e Y representan independientemente entre sí, un átomo de hidrógeno, de cloro, bromo, yodo o flúor o alcoxi C1-4 o trifluorometoxi; así como sus sales farmacéuticamente aceptables, solvatos e hidratos. El compuesto de fórmula (1) es afín con los receptores de la oxitocina. Su utilización, procedimiento para su preparación, composición farmacéutica que lo contiene, medicamento que consiste en el compuesto de fórmula (1), y un producto que contiene el compuesto de fórmula (1), y un producto que contiene el compuesto de fórmula (1) antagonista de los receptores de la oxitocina y un antagonista de los receptores de la vasopresina.
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