AR048341A1 - Moduladores cannabinoides de tetrahidro-indazol - Google Patents

Moduladores cannabinoides de tetrahidro-indazol

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Publication number
AR048341A1
AR048341A1 ARP050101196A ARP050101196A AR048341A1 AR 048341 A1 AR048341 A1 AR 048341A1 AR P050101196 A ARP050101196 A AR P050101196A AR P050101196 A ARP050101196 A AR P050101196A AR 048341 A1 AR048341 A1 AR 048341A1
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Argentina
Prior art keywords
hydroxy
halogen
positions
optionally substituted
alkylene
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ARP050101196A
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Janssen Pharmaceutica Nv
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Publication of AR048341A1 publication Critical patent/AR048341A1/es

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Abstract

La presente trata de moduladores cannabinoides de tetrahidroindazol, y un método para usarlo en el tratamiento, mejoramiento o prevencion de un sindrome, desorden o enfermedad intermediado por un receptor cannabinoide. Reivindicacion 1: Un compuesto que tiene una estructura de acuerdo con la formula (1): en la cual la línea punteada entre las posiciones 2-3 y las posiciones 3a-7a en la formula (1) representan ubicaciones para los dos dobles enlaces presentes cuando X1R1 está presente; las líneas punteadas entre las posiciones 3-3a y las posiciones 7a-1 en la formula (1) representan ubicaciones para los dos dobles enlaces presentes cuando está presente X2R2; la línea punteada entre las posiciones 7 y X4R4 en la formula (1) representa la ubicacion para un doble enlace; X1 está ausente o es alquileno inferior; X2 está ausente o es alquileno inferior; donde unicamente están presentes uno de X1R1 y X2R2; X3 está ausente, o es alquileno inferior, alquilideno inferior o -NH- ; cuando la línea punteada entre las posiciones 7 y X4R4 está ausente, X4 está ausente o es alquileno inferior; cuando la línea punteada entre las posiciones 7 y X4R4 está presente, X4 está ausente; X5 está ausente o es alquileno inferior; R1 está seleccionado del grupo que consiste en arilo, cicloalquilo C3-12, o heterociclilo, cualquiera de los cuales está opcionalmente sustituido en una o más posiciones con halogeno, alquilo inferior, hidroxi o alcoxi inferior; R2 está seleccionado del grupo que consiste en arilo, cicloalquilo C3-12, o heterociclilo, cualquiera de los cuales está opcionalmente sustituido en una o más posiciones con halogeno, alquilo inferior, hidroxi o alcoxi inferior; R3 es como se muestra en el grupo de formulas (2), cuando la línea punteada entre las posiciones 7 y X4R4 está ausente, R4 es H, hidroxi, alquilo inferior, alcoxi inferior, halogeno, arilo opcionalmente sustituido en una o más posiciones con hidroxi, alquilo inferior, alcoxi inferior o halogeno, heterociclilo opcionalmente sustituido en una o más posiciones con hidroxi, alquilo inferior, alcoxi inferior o halogeno, o cicloalquilo C3-12 opcionalmente sustituido en una o más posiciones con hidroxi, alquilo inferior, alcoxi inferior o halogeno; cuando la línea punteada entre las posiciones 7 y X4R4 está presente, R4 es CH-arilo es donde arilo está opcionalmente sustituido en una o más posiciones con hidroxi, alquilo inferior, alcoxi inferior o halogeno; o CH-heterociclilo en donde el heterociclilo está opcionalmente sustituido en una o más posiciones con hidroxi, alquilo inferior, alcoxi inferior o halogeno; R5 es H, hidroxi, alquilo inferior, alcoxi inferior, hidroxi-alquileno inferior-carboxi, alcoxicarbonilo, ariloxicarbonilo, aril-alcoxicarbonilo, NHR10, C(O)NR11R11a, -O-C(O)-R12, oxo, o -C(O)R13; R6 está ausente, o es -CH(R6a)-; R6a es H, alquilo inferior, o arilo opcionalmente sustituido con uno o más de halogeno, hidroxi, alcoxi inferior, carboxi o alcoxicarbonilo; R7 es alcoxi inferior, arilo opcionalmente sustituido con uno más hidroxi, halogeno, alquilo inferior, carboxi, alcoxicarbonilo, alcoxi inferior, hidroxi-alquileno-, -NH(R6a), ariloxi, arilalcoxi, o aril-alquileno inferior, cicloalquilo C3-12 opcionalmente sustituido con uno o mas hidroxi, halogeno, alquilo inferior, alquilo inferior-aminocarbonilo, carboxi, alcoxicarbonilo, alcoxi inferior, alcoxi inferior-alquileno inferior, hidroxi-alquileno-, ariloxi, arilalcoxi, arilalcoxi-alquileno inferior- opcionalmente sustituido en el arilo con uno o más hidroxi, halogeno o alquilo inferior, o aril-alquileno inferior, heterociclilo opcionalmente sustituido con uno o más hidroxi, halogeno, alquilo inferior, carboxi, alcoxicarbonilo, alcoxi inferior, alcoxi inferior-alquileno inferior-, hidroxi-alquileno-, ariloxi o arilalcoxi; R8, R8a, R9 y R9a, son cada uno individualmente H, alquilo inferior, -NHR15, arilo opcionalmente sustituido con uno o más hidroxi, halogeno, -NH(R6a), -SO2-NH(R6a), alquilo inferior, carboxi, alcoxicarbonilo, alcoxi inferior, hidroxi-alquileno-, ariloxi o arilalcoxi, cicloalquilo C3-12 opcionalmente sustituido con uno o más hidroxi, halogeno, amino, alquilo inferior, carboxi, alcoxicarbonilo, alcoxi inferior, hidroxi-alquileno-, ariloxi, arilalcoxi, o alquileno inferior, o heterociclilo opcionalmente sustituido con uno o más hidroxi, halogeno, amino, alquilo inferior, carboxi, alcoxicarbonilo, alcoxi inferior, hidroxi- alquileno-, ariloxi o arilalcoxi; R10 es H, alcoxicarbonilo C1-10 opcionalmente sustituido en una o más posiciones con hidroxi, halogeno o arilo, -C(O)CF3, -SO2-NR14R14a, -C(O)-heterociclilo opcionalmente sustituido en una o más posiciones con hidroxi, halogeno, o arilo, -C(O)NR14R14a, -SO2-arilo, -SO2R14, o SO2NR14R14a, R11, R11a, R12, R13, R14 y R14a y R15 son cada uno individualmente H, alquilo C1-10, heterociclilo, cicloalquilo C3-12, o arilo opcionalmente sustituido con alquilo inferior, hidroxi, alcoxi, halogeno-SO2-N(R6a)2, heterociclilo o aril-alquileno inferior-; Z1 está ausente, -NH-, o es alquileno inferior opcionalmente sustituido en una o más posiciones con halogeno, hidroxi,. alcoxi inferior, carboxi o alcoxicarbonilo inferior; Z2 está ausente, o es alquileno inferior opcionalmente sustituido en una o más posiciones con arilo, cicloalquilo, halogeno, hidroxi, alquilo inferior, alcoxi inferior, carboxi, alcoxicarbonilo o arilo, o una sal, isomero, profármaco, metabolito o polimorfo farmacéuticamente aceptable del mismo.
ARP050101196A 2004-03-24 2005-03-28 Moduladores cannabinoides de tetrahidro-indazol AR048341A1 (es)

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US (2) US7452997B2 (es)
EP (1) EP1735286B1 (es)
JP (1) JP4825792B2 (es)
CN (1) CN1956964B (es)
AR (1) AR048341A1 (es)
AT (1) ATE540027T1 (es)
AU (1) AU2005228868B2 (es)
BR (1) BRPI0509207A (es)
CA (1) CA2561305C (es)
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