AR037950A1 - Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear - Google Patents

Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear

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AR037950A1
AR037950A1 ARP020105038A ARP020105038A AR037950A1 AR 037950 A1 AR037950 A1 AR 037950A1 AR P020105038 A ARP020105038 A AR P020105038A AR P020105038 A ARP020105038 A AR P020105038A AR 037950 A1 AR037950 A1 AR 037950A1
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Argentina
Prior art keywords
substituted
cycloalkenyl
cycloalkyl
alkyl
heterocycle
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ARP020105038A
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English (en)
Inventor
Mark E Salvati
James Aaron Balog
Dacia A Pickering
Soren Giese
Aberra Fura
Ramesh N Patel
Ronald L Hanson
Jacques Y Roberge
James R Corte
Steven H Spergel
Raj Misra
Hai-Yun Xiao
Wenying Li
Toomas Mitt
Richard A Rampulla
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Bristol Myers Squibb Co
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Publication of AR037950A1 publication Critical patent/AR037950A1/es

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Abstract

Método de preparación y método de uso de tales compuestos en el tratamiento de condiciones asociados con el receptor de la hormona nuclear tal como el cáncer y padecimientos inmunes, y composiciones farmacéuticas que contienen tales compuestos. Reivindicación 1: Un compuesto de la siguiente fórmula (1), en donde los símbolos tienen los siguientes significados y son, cada vez que se presentan, seleccionados independientemente: G es un grupo arilo o heterociclo, donde el grupo es mono- o policíclico, y el cual está opcionalmente sustituido en una o más posiciones; Z1 es O, S, NH, o NR6; Z2 es O, S, NH, o NR6; A1 es CR7 o N; A2 es CR7 o N; Y es J-J'-J'' donde J es (CR7R7')n y n=0-3, J' es un enlace u O, S, S=O, SO2, NH, NR7, CR7R7', R2P=O, R2P=S, R2OP=O, R2NHP=O, OP=OOR2, OP=ONHR2, OSO2, NHNH, NHNR6, NR6NH, N=N, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, o heterociclo o heterociclo sustituido, y J'' es (CR7R7')n y n=0-3, donde Y no es enlace; y W' es CR7CR7'-CR7C7', CR7R7'-C=O, C=O-C=O, CR7R7'-C=CH2, C=CH2-C=CH2, CR7R7'-C=NR1, C=NR1-C=NR1, NR9-CR7R7', N=CR8, N=N, NR9-NR9', cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, o arilo o arilo sustituido, en donde cuando W' no es NR9-CR7R7', N=CR8, N=N, NR9-NR9', o heterociclo o heterociclo sustituido, entonces J' deberá ser O, S, S=O, SO2, NH, NR7, OP=OOR2, OP=ONHR2, OSO2, NHNH, NHNR6, NR6NH, o N=N; cuando W es CR7R7'-CR7R7', los sustituyentes R7 y R7', cada que se presentan, pueden tomarse juntos para formar un sistema de anillo heterocíclico sustituido o no sustituido o carbocíclico sustituido o no sustituido que puede formarse por cualquier combinación de R7 y R7' enlazado al mismo átomo de carbono; Q1 es H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilalquilo o arilalquilo sustituido, alquinilo o alquinilo sustituido, arilo o arilo sustituido, heterociclo (por ejemplo heteroarilo) o heterociclo sustituido (por ejemplo heteroarilo), halo, CN, R1OC=O, R4C=O, R5R6NC=O, HOCR7R7', nitro, R1OCH2, R1O, NH2, C=OSR1, SO2R1 o NR4R5; Q2 es H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilalquilo o arilalquilo sustituido, alquinilo o alquinilo sustituido, arilo o arilo sustituido, heterociclo (por ejemplo heteroarilo) o heterociclo sustituido (por ejemplo heteroarilo sustituido), halo, CN, R1OC=O, R4C=O, R5R6NC=O, HOCR7R7', nitro, R1OCH2, R1O, NH2, C=OSR1, SO2R1, o NR4R5; L es un enlace, (CR7R7')n, NH, NR5, NH(CR7R7')n, o NR5(CR7R7')n, donde n=0-3; R1 y R1' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido; R2 es alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido; R3 y R3' con cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, halo, CN, hidroxilamina, hidroxamida, alcoxi o alcoxi sustituido, amino, NR1R2, tiol, alquiltio o alquiltio sustituido; R4 es H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, R1C=O, R1OC=O, R1NHC=O, SO2OR1, o SO2R1, SO2NR1R1'; R5 es alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, R1C=O, R1NHC=O, SO2R1, SO2OR1, o SO2NR1R1'; R6 es alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, CN, OH, OR1, R1C=O, R1NHC=O, SO2R1, SO2OR1, o SO2NR1R1'; R7 y R7' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, halo, CN, OR4, nitro, hidroxilamina, hidroxamida, amino, NHR4, NR2R5, NR5R5, NOR1, tiol, alquiltio o alquiltio sustituido, HOC=O, R1C=O, R1(C=O)O, R1OC=O, R1NHC=O, NH2C=O, SO2R1, SOR1, PO3R1R1', R1R1'NC=O, C=OSR1, SO2R1, SO2OR1, o SO2NR1R1', o, en donde A1 o A2 contiene un grupo R7 y W contiene un grupo R7, los grupos R7 de A1 o A2 y W forman juntos un anillo heterocíclico; R8 y R8' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, nitro, halo, CN, OR1, amino, NHR4, NR2R5, NOR1, alquiltio o alquiltio sustituido, C=OSR1, R1OC=O, R1C=O, R1NHC=O, R1R1'NC=O, SO2OR1, S=OR1, SO2R1, PO3R1R1', o SO2NR1R1'; R9 y R9' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, CN, OH, OR1, R1C=O, R1OC=O, R1NHC=O, SO2R1, SO2OR1, o SO2NR1R1'; con la condición de que: (1) cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es -CH2-CH2-, y A1 y A2 son CH, entonces G-L no es fenilo, fenilo monosustituido o fenilo que está sustituido con dos o más de los siguientes grupos: metoxi, halo, NO2, metilo, CH3-S-, OH, CO2H, trifluorometilo, -C(O)-C6H5, NH2, 4-7-epoxi, hexahidro-1H-isoindol-1,3(2H)diona, o -C(O)-CH3; (2) cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es CH2-CH2, y uno de A1 y A2 es CH y el otro es CR7, entonces G-L no es fenilo no sustituido; (3) cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es CH2-CH2, y uno de A1 y A2 es CH y el otro es C-CH3, entonces G-L no es fenilo sustituido con cloro y/o metilo; (4) cuando Y' es -O- o -S-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es CH2-CH2, y uno de A1 y A2 es CH y el otro es CH o C-alquilo, entonces G-L no es piperazin-alquilo N-sustituido o imidazolidin-alquilo N-sustituido; (5) cuando Y' es -O-; Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W'es CH2-CH2, y A1 y A2 son CH, entonces G-L no es oxazol o triazol; (6) cuando Y' es -O-; Q1 y Q2 son hidrógeno o metilo, Z1 y Z2 son O, W' es CH2-CH2, y A1 y A2 son CH o C-CH3, entonces G-L no es tiazol o tiazol sustituido; (7) cuando Y' contiene un grupo J' seleccionado de S, S=O, SO2, NH, NR7, R2P=O, R2P=S, R2OP=O, R2NHP=O, OP=OOR2, OP=ONHR2, OSO2, NHNH, NHR6, NR6NH o N=N, W' es CR7R7'-CR7R7', y Z1 y Z2 son O, entonces G-L no es fenilo no sustituido; (8) cuando y es NR7, W' es fenilo no sustituido o sustituido, y Q1 y Q2 son hidrógeno, entonces Z1 Y Z2 no son O; (9)cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es dihidroisoxazol que porta un grupo fenilo opcionalmente sustituido, A1 y A2 son CH, entonces G-L no es fenilo no sustituido o diclorofenilo; (10) cuando Y' es O, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es óxido de etileno, y A1 y A2 son CH, entonces G-L no es metilfenilo o clorofenilo; (11) cuando Y' es NR7-CR7R7', W' es CR8=CR8', Q1 y Q2 son hidrógeno, A1 y A2 son CH, C-CH3, -C-CH2-
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