ES2549084T3 - Derivados de benzoxazinona - Google Patents

Derivados de benzoxazinona Download PDF

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ES2549084T3
ES2549084T3 ES08836571.3T ES08836571T ES2549084T3 ES 2549084 T3 ES2549084 T3 ES 2549084T3 ES 08836571 T ES08836571 T ES 08836571T ES 2549084 T3 ES2549084 T3 ES 2549084T3
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alkyl
methyl
heteroalkyl
trifluoromethyl
oxo
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Shiho Ishikawa
Takashi Mizutani
Tsuyoshi Nagase
Nagaaki Sato
Hidekazu Takahashi
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MSD KK
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Abstract

Un compuesto representado por la fórmula (I) o una sal farmacéuticamente aceptable del mismo: **Fórmula** en la que R1 representa alquilo C1-6 halogenado o cicloalquilo C3-8 halogenado; R2 representa un sustituyente seleccionado entre un grupo que consiste en los siguientes grupos: **Fórmula** en la que W representa alquileno C1-6, alquenileno C2-6, alquinileno C2-6 o cicloalquileno C3-6, en donde los alquileno, alquenileno, alquinileno o cicloalquileno pueden estar sustituidos con alquilo C1-3 opcionalmente halogenado, alquiloxi C1-3 opcionalmente halogenado, hidroxilo o halógeno; R representa alquilo C1-6 cicloalquilo C3-8, arilo o heteroarilo, en donde los alquilo C1-6 cicloalquilo C3-8, arilo o heteroarilo pueden estar sustituidos con halógeno, alquilo C1-6 opcionalmente halogenado, alquiloxi C1-6 opcionalmente halogenado, alquilsulfonilo C1-6, ciano, fenilo, alquiltio C1-6, hidroxilo, amino, alquilamino C1-6, di alquilamino C1-6, hidroxi-alquilo C1-6, amino-alquilo C1-6, alquilamino C1-6-alquilo C1-6, di-alquilaminoalquilo C1-6, alcoxi C1-6-alquilo C1-6, alquilcarbonilo C1-6, alquilcarbonilamino C1-6, alquilcarbamoílo C1-6, cicloalquilcarbamoílo C3-8, alquilsulfonilamino C1-6 o alquilaminosulfonilo C1-6; R3 representa un átomo de hidrógeno, alquilo C1-6, arilo o heteroarilo; X representa -O-, -C(R4a)(R4b)- o -NR5-; R4a, R4b y R5 representan cada uno independientemente hidrógeno, alquilo C1-6, cicloalquilo C3-8, arilo o heteroarilo, en donde los alquilo C1-6, cicloalquilo C3-8, arilo o heteroarilo pueden estar sustituidos con halógeno, alquilo C1-6 opcionalmente halogenado, alquiloxi C1-6 opcionalmente halogenado, alquilsulfonilo C1-6, ciano, arilo o heteroarilo; Y1 representa -CR6 - o -N-; Y2 representa -CR7 - o -N-; Y3 representa -CR8 - o -N-; Y4 representa -CR9 - o -N-; R6, R7, R8 y R9 representan cada uno independientemente un átomo de hidrógeno, halógeno, ciano, alquilo C1-6 cicloalquilo C3-8, alcoxi C1-6, hidroxilo, hidroxi-alquilo C1-6, amino, alquilamino C1-6, di-alquilamino C1-6, amino alquilo C1-6, alquilamino C1-6-alquilo C1-6, di-alquilamino C1-6-alquilo (C1-6), alcoxi C1-6-alquilo C1-6, heterociclilo, arilo, heteroarilo, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, arilsulfonilo, heteroarilsulfonilo, arilsulfinilo, heteroarilsulfinilo, ariltio, heteroariltio, alquilcarbonilo C1-6, arilcarbonilo, heteroarilcarbonilo, alquilcarbonilamino C1-6, arilcarbonilamino, heteroarilcarbonilamino, alquilcarbamoílo C1-6, cicloalquilcarbamoílo C3-8, heterociclilcarbamoílo, arilcarbamoílo, heteroarilcarbamoílo, alquilsulfonilamino C1-6, arilsulfonilamino, heteroarilsulfonilamino, alquilsulfamoílo C1-6, arilsulfamoílo o heteroarilsulfamoílo, en donde los alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo pueden estar sustituidos con un grupo seleccionado entre el grupo que consiste en halógeno, alquilo C1-6 opcionalmente halogenado, alquiloxi C1-6 opcionalmente halogenado, alquilsulfonilo C1-6 , carboxilo y ciano.

Description

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N-{[6-cloro-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}-N’-piridin-4-ilurea; 4-fluoro-N-{[2-oxo-6-(1H-pirazol-5-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; (4S*)-4-fluoro-N-{[2-oxo-6-(1H-pirazol-5-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-isoxazol-4-il-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(1H-pirazol-4-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; (4S*)-4-fluoro-N-{[2-oxo-6-(1H-pirazol-4-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-(1-metil-1H-pirazol-4-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; (4S*)-4-fluoro-N-{[6-(1-metil-1H-pirazol-4-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-(3-metil-1H-pirazol-5-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-(4-metil-1H-pirazol-5-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(1H-pirrol-2-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[6-(2-furilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(2-tienilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(1H-pirazol-3-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}bencenosulfonamida; ’4-fluoro-N-{[(4S*)-2-oxo-6-(1H-pirazol-3-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}bencenosulfonamida; N-{[2-oxo-6-(1H-pirazol-3-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}piridin-2-sulfonamida; N-{[(4S*)-2-oxo-6-(1H-pirazol-3-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}piridin-2sulfonamida; 4-fluoro-N-({2-oxo-4-(trifluorometilo)-6-[3-(trifluorometilo)-1H-pirazol-5-il]-1,4-dihidro-2H-3,1-benzoxazin-4il}metilo)benzamida; 4-fluoro-N-{[2-oxo-6-(2-oxopirrolidin-1-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; (4S*)-4-fluoro-N-{[2-oxo-6-(2-oxopirrolidin-1-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(propionilamino)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(1H-1,2,4-triazol-5-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; N-{[6-(benzoilamino)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil} -4-fluorobenzamida; 4-fluoro-N-{[2-oxo-6-(2-oxo-1,3-oxazolidin-3-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[(4S*)-2-oxo-6-(2-oxo-1,3-oxazolidin-3-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-(3-metil-2-oxazolidin-1-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(2-oxopiridin-1 (2H)-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(1H-pirazol-1-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[(4S*)-2-oxo-6-(1H-pirazol-1-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-(4-metil-1H-pirazol-1-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-(3-metil-1H-pirazol-1-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; N-{[6-(3-amino-1H-pirazol-1-ilo)-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}-4fluorobenzamida; 4-fluoro-N-{[2-oxo-4-(trifluorometilo)-6-[3-(trifluorometilo)-1H-pirazol-1-il]-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[6-[(3S)-3-hidroxi-2-oxopirrolidin-1-il]-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4il]metil}benzamida; 4-fluoro-N-{[2-oxo-6-(1H-pirazol-5-ilo)-4-(trifluorometilo)-1,2,3,4-tetrahidroquinazolin-4-il]metil}benzamida; 4-fluoro-N-{[(4S*)-2-oxo-6-(1H-pirazol-5-ilo)-4-(trifluorometilo)-1,2,3,4-tetrahidroquinazolin-4-il]metil}benzamida; N-{[6-cloro-2-oxo-4-(trifluorometilo)-1,2,3,4-tetrahidroquinazolin-4-il]metil}4-fluorobenzamida; N-{[(4S*)-6-cloro-2-oxo-4-(trifluorometilo)-1,2,3,4-tetrahidroquinazolin-4-il]metil}4-fluorobenzamida; 4-fluoro-N-{[2-oxo-6-(1H-pirazol-4-ilo)-4-(trifluorometilo)-1,2,3,4-tetrahidroquinazolin-4-il]metil}benzamida; N-{[2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; 4-fluoro-N-{[6-metil-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}benzamida; N-{[2-oxo-6-(1H-pirazol-4-ilo)-4-(trifluorometilo)-1,4-dihidro-2H-3,1-benzoxazin-4-il]metil}piridin-2-sulfonamida; N-biciclo[2,2,1]heptan-2-il-4-{[(4-fluorobenzoíl)amino]metil}-2-oxo-4-(trifluorometilo)-1,4-dihidro-2H-3,1benzoxazin-6-carboxamida; y
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Como el disolvente de reacción, se ilustran THF, dioxano, un disolvente mixto de THF-agua y similares.
Como la temperatura de reacción, se ilustra una temperatura de 0 a 100 ºC, preferentemente, se recomienda una temperatura de 0 a 80 ºC, y generalmente, la reacción se completa en 1 a 24 horas. 5 Etapa 10
El Compuesto 13 se trata con un ácido, mediante lo cual se obtiene el Compuesto 14. Como el ácido, se ilustran un ácido clorhídrico 4 N/dioxano y similares. 10 Como la cantidad usada del ácido, se ilustra una cantidad de 10 a 100 moles por mol del Compuesto 13.
Como la temperatura de reacción, se ilustra una temperatura de 0 a 100 ºC, preferentemente, se recomienda una temperatura de 25 a 80 ºC, y generalmente, la reacción se completa en 6 a 24 horas. 15 Etapa 11
El Compuesto 14 y Compuesto 15 se condensan, mediante lo cual se obtiene un compuesto representado por la fórmula (I-1b).
20 La condensación puede realizarse por un método convencionalmente conocido, y se ilustran un método en que el Compuesto 14 se hace reaccionar con el Compuesto 15 en presencia de un agente de condensación, un método en el que el resto de ácido carboxílico del Compuesto 15 se activa mediante un método convencionalmente conocido para formar un derivado reactivo y después, el derivado y el Compuesto 14 se amidan y similares (véase "Pepuchido
25 Gosei no Kiso to Jikken", Nobuo Izumiya, et al., Maruzen Co., Ltd., 1983).
Como la reacción usando un agente de condensación, por ejemplo, se ilustra el siguiente método.
Es decir, el Compuesto 15 y el Compuesto 14 se condensan usando un agente de condensación en un disolvente de 30 reacción, mediante lo cual se obtiene un compuesto representado por la fórmula (I-1b).
Como la cantidad usada del Compuesto 15, se ilustra una cantidad de 1 a 3 moles por mol del Compuesto 14.
Como el agente de condensación, se ilustran diciclohexilcarbodiimida, 1-etil-3-(3-dimetilaminopropilo)-carbodiimida y 35 similares, y como la cantidad usada del agente de condensación, se ilustra una cantidad de 1 a 3 moles por mol del Compuesto 14.
Además, para el propósito de acelerar la reacción, puede añadirse hidroxibenzotriazol (en lo sucesivo denominado "HOBT") o similares al sistema de reacción. Como la cantidad usada de HOBT, se ilustra una cantidad de 1 a 3 40 moles por mol del Compuesto 14.
Como el disolvente de reacción, se ilustra THF, dioxano, DMF, DMSO, diclorometano o un disolvente mixto de los mismos.
45 Como la temperatura de reacción, se ilustra una temperatura de 20 a 100 ºC, preferentemente, se recomienda una temperatura de 20 a 50 ºC, y generalmente, la reacción se completa en 1 a 24 horas.
Como el Compuesto 15, se ilustran ácido 4-fluorobenzoico y similares.
50 El compuesto así obtenido representado por la fórmula (I-1b) puede aislarse y purificarse por un método de separación y purificación conocido, tal como concentración, concentración al vacío, cristalización, extracción de disolventes, reprecipitation o cromatografía.
Método de Producción 4 55 El Método de Producción 4 es un método para producir un compuesto representado por la fórmula (I-1c).
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N-{3-[(4R*)-6-cloro-2-oxo4-(trifluorometil)-1,4-dihidro2H-3,1-benzoxazin-4-il]propil} -4-fluorobenzamida 17 151 N-{[(4S*)-2-oxo-6-(1H-pirazol-3-il)-4-(trifluorometil)-1,4-dihidro-2H3,1-benzoxazin-4-il]metil}piridin2-sulfonamida 16
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N-{3-[(4R*)-6-cloro-2-oxo4-(trifluorometil)-1,4-dihidro2H-3,1-benzoxazin-4-il] propil}piridin-2-sulfonamida 128 154 (4S*)-4-fluoro-N-{[2-oxo-6-(2oxopirrolidin-1-il)-4-(trifluorometil)-1,4-dihidro-2H3,1-benzoxazin-4il]metil}benzamida 15
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N-{2-[(4R*)-6-cloro-2-oxo4-(trifluorometil)-1,4-dihidro2H-3,1-benzoxazin-4-il] etil}piridin-2-sulfonamida 5.4 173 4-fluoro-N-{[(4S*)-2-oxo-6-(2-oxo1,3-oxazolidin-3-il)-4-(trifluorometil)-1,4-dihidro-2H3,1-benzoxazin-4il]metil}benzamida 108
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N-{[(4S*)-6-cloro-2-oxo4-(trifluorometil)-1,4-dihidro2H-3,1-benzoxazin-4-il] metil}-N’-(4-fluorofenil)urea 18 174 4-fluoro-N-{[6-(3-metil-2oxazolidin-1-il)-2-oxo-4-(trifluorometil)-1,4-dihidro-2H3,1-benzoxazin-4il]metil}benzamida 5,3
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(4S*)-4-fluoro-N-{[2-oxo-6-(1Hpirazol-5-il)-4-(trifluorometil)1,4-dihidro-2H-3,1-benzoxazin4-il]metil}benzamida 2,7 176 4-fluoro-N-{[(4S*)-2-oxo-6-(1Hpirazol-1-il)-4-(trifluorometil)-1,4dihidro-2H-3,1-benzoxazin-4il]metil}benzamida 19
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(4S*)-4-fluoro-N-{[2-oxo-6-(1Hpirazol-4-il)-4-(trifluorometil)1,4-dihidro-2H-3,1-benzoxazin4-il]metil}benzamida 9,6 178 4-fluoro-N-{[6-(3-metil-1H-pirazol1-il)-2-oxo-4-(trifluorometil)-1,4dihidro-2H-3,1-benzoxazin-4il]metil}benzamida 7,3
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(4S*)-4-fluoro-N-{[6-(1-metil1H-pirazol-4-il)-2-oxo4-(trifluorometil)-1,4-dihidro2H-3,1-benzoxazin-4il]metil}benzamida 119 182 4-fluoro-N-{[(4S*)-2-oxo-6-(1Hpirazol-5-il)-4-(trifluorometil)1,2,3,4-tetrahidroquinazolin-4il]metil}benzamida 6,6
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4-fluoro-N-{[6-(2-furil)-2-oxo4-(trifluorometil)-1,4-dihidro2H-3,1-benzoxazin-4-il] metil}benzamida 14 187 N-{[(4S*)-6-cloro-2-oxo4-(trifluorometil)-1,2,3,4tetrahidroquinazolin-4-il]metil}4fluorobenzamida 45
El compuesto representado con la fórmula general (I) se puede administrar por vía oral o por vía parenteral, y mediante la formulación del compuesto en una preparación adecuada para tal ruta de administración, el compuesto se puede usar como un agente de tratamiento para enfermedades cardiovasculares tales como hipertensión, angina 5 de pecho, insuficiencia cardiaca, infarto de miocardio, apoplejía, claudicación, nefropatía diabética, retinopatía diabética, disminución de la visión, anomalía electrolítica y aterosclerosis; enfermedades del sistema nervioso central tales como bulimia y neuropatía diabética; enfermedades metabólicas tales como síndrome metabólico, obesidad, diabetes, resistencia a la insulina, hiperlipidemia, hipercolesterolemia, hipertrigliceridemia, dislipidemia, hígado graso no alcohólico, anomalía en la secreción de hormonas, gota e hígado graso; enfermedades del sistema reproductor
10 tales como trastorno menstrual y disfunción sexual; enfermedades del sistema gastrointestinal tales como disfunción hepática, pancreatitis, colecistitis y reflujo gastroesofágico; enfermedades del sistema respiratorio tales como síndrome de hipoventilación por obesidad (síndrome de Pickwick) y síndrome de apnea del sueño; enfermedades infecciosas causadas por bacterias, hongos o parásitos; neoplasias malignas; enfermedades inflamatorias tales como artritis y úlcera cutánea; y similares.
15 Un aspecto de la divulgación es proporcionar un método para el tratamiento o la prevención de un trastorno, enfermedad o afección causada por la modulación de LCE que incluye la administración de una cantidad terapéutica
o profilácticamente eficaz del compuesto (I) o una sal farmacéuticamente aceptable del mismo de acuerdo con la invención a un sujeto con necesidad del mismo.
20 Otro aspecto de la divulgación es proporcionar un método para el tratamiento o la prevención de síndrome metabólico, hígado graso, hiperlipidemia, dislipidemia, hígado graso no alcohólico, obesidad, diabetes, bulimia, una neoplasia maligna o una enfermedad infecciosa que incluye la administración de una cantidad terapéutica o profilácticamente eficaz del compuesto (I) o una sal farmacéuticamente aceptable del mismo de acuerdo con la
25 invención a un sujeto con necesidad del mismo.
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WO2009044788A1 (ja) 2009-04-09
AU2008308092B2 (en) 2013-07-11
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AU2008308092A1 (en) 2009-04-09
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