ES2572481T3 - Derivado de triacina y composición farmacéutica que tiene una actividad analgésica que contiene la misma - Google Patents

Derivado de triacina y composición farmacéutica que tiene una actividad analgésica que contiene la misma

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ES2572481T3
ES2572481T3 ES11816413T ES11816413T ES2572481T3 ES 2572481 T3 ES2572481 T3 ES 2572481T3 ES 11816413 T ES11816413 T ES 11816413T ES 11816413 T ES11816413 T ES 11816413T ES 2572481 T3 ES2572481 T3 ES 2572481T3
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Hiroyuki Kai
Takayuki Kameyama
Tohru Horiguchi
Kentaro Asahi
Takeshi Endoh
Yasuhiko Fujii
Takuya Shintani
Ken'ichiroh Nakamura
Sae Jikihara
Tsuyoshi Hasegawa
Miho Oohara
Yukio Tada
Toshikatsu Maki
Akira Iida
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Shionogi and Co Ltd
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Abstract

Un compuesto de la fórmula (VIII):**Fórmula** en el que Z1 y Z2 son cada uno independientemente un átomo de oxígeno, un átomo de azufre o >=N-Rx; Rx es un átomo de hidrógeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, un grupo heterocíclico no aromático sustituido o no sustituido, arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido; Rc es un átomo de hidrógeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, acilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, un grupo heterocíclico no aromático sustituido o no sustituido, arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido; R4a y R4b son cada uno independientemente un átomo de hidrógeno o alquilo sustituido o no sustituido, o R4a y R4b ligados al mismo átomo de carbono se toman juntos para formar oxo o tioxo; n es un número entero de 1 a 4; R2 es cicloalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, un grupo heterocíclico no aromático sustituido o no sustituido, arilo sustituido o no sustituido o heteroarilo sustituido o no sustituido; -X- es -O-, -S-, -N(R5)- o (CR5aR5b)-; -L- es -O-, -S-, -N(R5')- o -(CR5a'-R5b')-; R5 y R5' son cada uno independientemente un átomo de hidrógeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, o acilo sustituido o no sustituido; R5a, R5b, R6a' y R5b' son cada uno independientemente un átomo de hidrógeno, halógeno, hidroxi, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, alquiloxi sustituido o no sustituido, alquiniloxi sustituido o no sustituido o alqueniloxi sustituido o no sustituido; el anillo D es un anillo de benceno, un anillo de piridina, un anillo de pirimidina, un anillo de piracina o un anillo de piridacina; el átomo de carbono a y el átomo de carbono b son átomos de carbono que constituyen el anillo D; el anillo B es un anillo heterocíclico aromático; s y s' son cada uno independientemente un número entero de 0 a 3; y R9 y R9' son cada uno independientemente halógeno, hidroxi, carboxi, ciano, nitro, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, alquiloxi sustituido o no sustituido, alqueniloxi sustituido o no sustituido, alquiniloxi sustituido o no sustituido, alquiltio sustituido o no sustituido, alqueniltio sustituido o no sustituido, alquiniltio sustituido o no sustituido, acilo sustituido o no sustituido, alquiloxicarbonilo sustituido o no sustituido, alqueniloxicarbonilo sustituido o no sustituido, alquiniloxicarbonilo sustituido o no sustituido, carbamoílo sustituido o no sustituido, amino sustituido o no sustituido, sulfamoílo sustituido o no sustituido, sulfonilo sustituido, sulfinilo sustituido, cicloalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, un grupo heterocíclico no aromático sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, cicloalquiloxi sustituido o no sustituido, cicloalqueniloxi sustituido o no sustituido, heterocicliloxi no aromático sustituido o no sustituido, ariloxi sustituido o no sustituido o heteroariloxi sustituido o no sustituido; o su sal farmacéuticamente aceptable o un solvato del mismo, en donde sustituyentes permisibles para "alquilo sustituido", "alquenilo sustituido", "alquinilo sustituido", "alquiloxi sustituido", "alqueniloxi sustituido", "alquiniloxi sustituido ", "alquiltio sustituido", "alqueniltio sustituido ", "alquiniltio sustituido", "alquiloxicarbonilo sustituido", "alqueniloxicarbonilo sustituido" y "alquiniloxicarbonilo sustituido" incluyen uno o más sustituyentes iguales o diferentes seleccionados del grupo que consiste en: hidroxi, carboxi, halógeno, haloalquiloxi, cicloalquilo, cicloalquenilo, metoxi, etoxi, propoxi, butoxi, alqueniloxi, alquiloxicarbonilo, nitro, nitroso, amino, alquilamino, acilamino, arilalquilamino, hidroxiamino, alquilsulfonilamino, alquilsulfinilamino, imino, hidroxiimino, alquilimino, alquiloxiimino, acilimino, azido, arilo, arilalquilo, arilalquiloxi, un grupo heterocíclico no aromático, heteroarilo, heteroarilalquilo, ciano, isociano, isocianato, tiocianato, isotiocianato, mercapto, alquiltio, alquilsulfonilo, carbamoílo, alquilcarbamoílo, sulfamoílo, alquilsulfamoílo, acilo, formiloxi, tioformilo, tiocarboxi, ditiocarboxi, tiocarbamoílo, sulfino, sulfo, hidracino, azido, ureido, amidino, guanidino, ftalimido, trialquilsililo y oxo, sustituyentes para "acilo sustituido" se seleccionan de los sustituyentes que se definen anteriormente para "alquilo sustituido", un grupo hidrocarbonado monovalente de cadena lineal o ramificada de un número de carbonos de 1 a 15, un alquenilo lineal o ramificado de un número de carbonos de 2 a 15 y un alquinilo lineal o ramificado de un número de carbonos de 2 a 15, si R en el acilo (R-C(>=O)-) es cicloalquilo, cicloalquenilo, un grupo heterocíclico no aromático, arilo o heteroarilo, entonces cada anillo puede estar sustituido con alquilo, haloalquilo, alquenilo, alquinilo, alquiloxi, halógeno, sustituyentes para "carbamoílo sustituido" y "sulfamoílo sustituido" son uno o más grupos iguales o diferentes seleccionados del grupo que consiste en: hidroxi, carboxi, halógeno, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, alquiloxicarbonilo, amino, alquilamino, acilamino, arilalquilamino, hidroxiamino, arilo, ciano, isociano, isocianato, tiocianato, isotiocianato y acilo, sustituyentes para "amino sustituido" son uno o más grupos iguales o diferentes seleccionados del grupo que consiste en: alquilo, haloalquilo, hidroxialquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, alquiloxi, haloalquiloxi, alqueniloxi, alquiloxicarbonilo, alquiloxicarbonilalquilo, amino, alquilamino, acilamino, arilalquilamino, hidroxiamino, imino, hidroxiimino, alquilimino, alquiloxiimino, acilimino, arilo, arilalquilo, ariloxi, un grupo heterocíclico no aromático, heteroarilo, heteroarilalquilo, heterocicliloxi no aromático, heteroariloxi, hidroxi, halógeno, ciano, acilo, alquilsulfonilo, alquilsulfinilo, carbamoílo, alquilcarbamoílo, alquilcarbamoilalquilo, carbamoilalquilo, carboxialquilo, sulfamoílo, alquilsulfamoílo, alquilsulfamoilalquilo y sulfamoilalquilo, sustituyentes para "cicloalquilo sustituido", "cicloalquenilo sustituido", "arilo sustituido", "heteroarilo sustituido" y "un grupo heterocíclico no aromático sustituido" son uno o más grupos iguales o diferentes seleccionados del grupo que consiste en: alquilo, haloalquilo, haloalquiloxi, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, alquiloxi, alqueniloxi, alquiloxicarbonilo, nitro, nitroso, amino, alquilamino, acilamino, arilalquilamino, hidroxiamino, amino sustituido con uno o dos sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Y mencionado posteriormente, imino, hidroxiimino, alquilimino, alquiloxiimino, acilimino, azido, arilo, arilalquilo, carbocicliloxi no aromático no sustituido, carbocicliloxi no aromático sustituido con uno o más sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Z mencionado posteriormente, carbociclilalquiloxi no aromático no sustituido, carbociclilalquiloxi no aromático sustituido con uno o más sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Z mencionado posteriormente, ariloxi no sustituido, ariloxi sustituido con uno o más sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Z mencionado posteriormente, arilalquiloxi no sustituido, arilalquiloxi sustituido con uno o más sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Z mencionado posteriormente, un grupo heterocíclico no aromático, heteroarilo, heteroarilalquilo, heterocicliloxi no aromático no sustituido, heterocicliloxi no aromático sustituido con uno o más sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Z mencionado posteriormente, heteroariloxi no sustituido, heteroariloxi sustituido con uno o más sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Z mencionado posteriormente, ciano, isociano, isocianato, tiocianato, isotiocianato, mercapto, alquiltio, alquilsulfonilo, carbamoílo sustituido o no sustituido, alquilcarbamoílo sustituido o no sustituido, sulfamoílo, alquilsulfamoílo, hidroxi, carboxi, halógeno, acilo, formiloxi, tioformilo, tiocarboxi, ditiocarboxi, tiocarbamoílo, sulfino, sulfo, hidracino, azido, ureido, amidino, guanidino, ftalimido y oxo, un Grupo de Sustituyentes Y incluye hidroxialquilo, alquiloxicarbonilo, alquiloxicarbonilalquilo, alquilsulfonilo, alquilsulfinilo, carbamoílo, alquilcarbamoílo, alquilcarbamoilalquilo, carbamoilalquilo, carboxialquilo, sulfamoílo, alquilsulfamoílo, alquilsulfamoilalquilo y sulfamoilalquilo, un Grupo de Sustituyentes Z incluye halógeno, hidroxi, carboxi, ciano, nitro, alquilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, alquenilo, alquinilo, alquiloxi, alqueniloxi, alquiniloxi, alquiltio, alqueniltio, alquiniltio, acilo, alquiloxicarbonilo, alqueniloxicarbonilo, alquiniloxicarbonilo, carbamoílo, alquilcarbamoílo, haloalquilcarbamoílo, hidroxialquilcarbamoílo, cianocarbamoílo, amino, acilamino, amino sustituido con uno o dos sustituyentes iguales o diferentes seleccionados del Grupo de Sustituyentes Y anterior, sulfamoílo, metilsulfonilo, metilsulfinilo, cicloalquilo, cicloalquenilo, un grupo heterocíclico no aromático, arilo, heteroarilo, cicloalquiloxi, cicloalqueniloxi, heterocicliloxi no aromático, ariloxi y heteroariloxi.
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TWI637949B (zh) 2013-06-14 2018-10-11 塩野義製藥股份有限公司 胺基三衍生物及含有其等之醫藥組合物

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