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AR049344A1 - Inhibidores de la 11-beta-hidroxi esteroide deshidrogenasa de tipo 1 - Google Patents

Inhibidores de la 11-beta-hidroxi esteroide deshidrogenasa de tipo 1

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Publication number
AR049344A1
AR049344A1 ARP050102153A ARP050102153A AR049344A1 AR 049344 A1 AR049344 A1 AR 049344A1 AR P050102153 A ARP050102153 A AR P050102153A AR P050102153 A ARP050102153 A AR P050102153A AR 049344 A1 AR049344 A1 AR 049344A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
aryl
cycloalkyl
cr8r9
Prior art date
Application number
ARP050102153A
Other languages
English (en)
Original Assignee
Amgen Inc
Biovitrum Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from SE0401324A external-priority patent/SE0401324D0/xx
Priority claimed from SE0402509A external-priority patent/SE0402509D0/xx
Application filed by Amgen Inc, Biovitrum Ab filed Critical Amgen Inc
Publication of AR049344A1 publication Critical patent/AR049344A1/es

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Abstract

La presente se refiere a composiciones farmacéuticas que comprenden los compuestos, como también a métodos de uso de los compuestos para el tratamiento de trastornos asociados con la enzima deshidrogenasa 11-beta-hidroxiesteroide tipo 1 y para la preparacion de un medicamento que actua sobre la enzima deshidrogenasa 11-beta-hidroxiesteroide tipo 1 humana. Reivindicacion 1: Un compuesto de formula general (1), en el cual ya sea: a) Z es azufre, R1 es hidrogeno, R2 se selecciona de hidrogeno, cicloalquilo C3-10 sustituido en forma independiente y opcional por uno o más de alquilo C1-8 y arilo, cicloalquilC3-10-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclilo, heterociclil-alquiloC1-8, en el cual cualquier residuo arilo o heterociclilo está sustituido en forma independiente y opcional por uno o más alquilo C1-8 y halogeno, o R1 y R2 forman junto con el átomo de nitrogeno unido a éstos un heterociclilo monocíclico sustituido en forma independiente y opcional por uno o más de aril- alquiloC1-8, alquilo C1-8 y halogeno, R3 y R4 se seleccionan, cada uno en forma independiente, de hidrogeno, alquilo C1-8, cicloalquilC3-10-alquiloC1-8, ciano-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclil-alquiloC1-8, heteroaril-alquiloC1-8, o R3 y R4 forman junto con el átomo de carbono unido a éstos cicloalquilo C3-10, en el cual cualquier residuo arilo está sustituido en forma independiente y opcional por uno o más de hidroxi, o; b) Z es oxígeno, R1 es hidrogeno, R2 se selecciona de hidrogeno, cicloalquilo C5-10 sustituido en forma independiente y opcional por uno o más de alquilo C1-8 y arilo, cicloalquilC3-10-alquiloC1-8, arilo, pero no un grupo fenilo no sustituido, aril-alquiloC1-8, heterociclilo, heterociclil-alquiloC3-8, en el cual cualquier residuo arilo o heterociclilo está sustituido en forma independiente y opcional por uno o más alquilo C1-8 y halogeno, R3 y R4 se seleccionan, cada uno en forma independiente, de hidrogeno, alquilo C1-8, cicloalquilC3-10- alquiloC1-8, ciano-alquiloC1-8, arilo, pero no un grupo fenilo no sustituido, aril-alquiloC1-8, heterociclil-alquiloC1-8, heteroaril-alquiloC1-8, o R3 y R4 forman junto con el átomo de carbono unido a éstos cicloalquilo C3-10, en el cual cualquier residuo arilo está sustituido en forma independiente y opcional por uno o más de hidroxi, y; sus sales, solvatos, hidratos, isomeros geométricos, tautomeros, isomeros opticos, N-oxidos y formas de profármacos aceptables desde el punto de vista farmacéutico, con la salvedad de que: cuando R1 es hidrogeno y Z es azufre y R3 = R4 metilo, entonces R2 no es fenilo; Z es azufre y R3 = R4 metilo, entonces R2 no es 4-yodofenilo; Z es azufre y R3 = R4 fenilo, entonces R2 no es fenilo; Z es azufre, y R3 = etilo y R4 = H, entonces R2 no es 3-metilfenilo; Z es oxígeno y R3 = H, entonces R4 no es metilo. Reivindicacion 2: Un compuesto de formula general (2), en el cual: X es S u O; R5 se selecciona de hidrogeno, alquilo C1-8, cicloalquilo C3-10, cicloalquilC3-10-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclilo, heterociclil-alquiloC1-8 y haloalquilo; en el cual cualquier residuo arilo, cicloalquilo o heterociclilo está sustituido en forma independiente y opcional por uno o más alquilo C1- 8, arilo, halogeno, halo-alquiloC1-8, HO-alquiloC1-8, R8R9N-alquiloC1-8, -OR10-alquiloC1-8, -OR10, cicloalquilo C3-10 o alquilsulfonilo C1-8; R6 se selecciona de alquilo C1-8, alcoxi C1-8, cicloalquilo C3-10, heterociclilo, cicloalquilC3-10- alquiloC1-8, CN-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclil-alquiloC1-8 y haloalquilo; R7 se selecciona de -NR8R9, halo, alquilo C1-8, -(CR8R9)n-OR8, -S-alquiloC1-8, cicloalquilo C3-10, heterociclilo, cicloalquilC3-10-alquiloC1-8, ciano- alquiloC1-8, arilo, aril-alquiloC1-8, heterociclil-alquiloC1-8, heterociclil-C(O)-alquiloC1-8, heterociclil-SO2-alquiloC1-8, haloalquilo C1-8, R8R9N-alquiloC1-8, HO-alquiloC1-8, -C(O)-cicloalquiloC3-10, -C(O)-haloalquiloC1-8, -(CR8R9)n-Y-(CR8R9)n- heterociclilo y -(CR8R9)n-Y-(CR8R9)n-C(O)-R8 (en el cual n es 0-5, Y es NR10, O o S); en el cual cualquier residuo arilo, alquilo, heterociclilo o cicloalquilo está sustituido en forma opcional por uno o más de: -alquiloC1-8; -halo; -OH; -OR10; alquil-C1-8-SO2-; -SO2-arilo; -C(O)-(CR8R9)n-carbamato; C(O)-O-alquiloC1-8; -C(O)-alquiloC1-8; -C(O)-(CR8R9)n-C(O)-NR8R9; -C(O)-(CR8R9)n-NR8-C(O)-alquiloC1-8; -C(O)-(CR8R9)n-NR8R9; -C(O)-cicloalquiloC3-10; -C(O)-arilo; -C(O)-(CR8R9)n-heterociclilo; - alquilC1-8-OR8; -C(O)-halo-alquiloC1-8; o -C(O)-(CR8R9)n-arilo; en el cual cualquier residuo arilo, alquilo, cicloalquilo, o heterociclilo está sustituido en forma independiente y opcional por uno o más alquilo C1-8, arilo, halogeno, -NR10R10, haloalquiloC1-8, HO-alquiloC1-8, R8R9N-alquiloC1-8, -OR10-alquiloC1-8, -OR10, cicloalquilo C3-10 o alquilsulfonilo C1-8, -O-(CR8R9)n-heterociclilo, -O-(CR8R9)n-C(O)-NR8R9, -O-(CR8R9)n-NR8R9, -Y-(CR8R9)n-NR8-C(O)-alquiloC1-8, -Y-(CR8R9)n- heterociclilo, -O-(CR8R9)n-NR8R9, alquilC1-8-SO2, o -O-(CR8R9)n-N-C(O)-heterociclilo; en el cual R8 y R9 se seleccionan, cada uno en forma independiente, de hidrogeno, alquilo C1-8, alcoxi C1-8, -NR10R10, -S-alquiloC1-8, arilo y heterociclilo; cualquier alquilo, alcoxi, heterociclilo o arilo puede estar sustituido con uno a tres sustituyentes seleccionados de -halo, alquilo C1-8 no sustituido, alcoxi C1-8 no sustituido, tioalcoxi C1-8 no sustituido y arilalquilo C1-4 no sustituido; en el cual R10 se selecciona en forma independiente de hidrogeno, alquilo C1-8, arilalquilo C1-8, alcoxi C1-8, -S-alquiloC1-8, heterociclilo y arilo; cualquier alquilo, heterociclilo o arilo puede estar sustituido con uno a tres sustituyentes seleccionados de -halo, alquilo C1-8 no sustituido, alcoxi C1-8 no sustituido, tialcoxi C1-8 no sustituido y arilalquilo C1-4 no sustituido; o R6 y R7 forman, junto con el átomo de carbono unido a éstos, un cicloalquilo C3-10 saturado, parcialmente insaturado o insaturado o un heterociclilo C4-14 saturado, parcialmente insaturado o insaturado; en el cual el cicloalquilo o el heterociclilo pueden estar sustituidos en forma opcional por uno o más de alquilo C1-8, arilo, haloalquilo C1-8, aril- alquiloC1-8, cicloalquilo C3-10, -OR8, =O, =NR8, =N-OR8, -NR8R9, -SR8, -halo, -OC(O)R8, -C(O)R8, -CO2R8, -CONR8R9, -OC(O)NR8R9, -NR9C(O)R8, -NR8C(O)NR8R9, -NR8SO2NR8R9, -NR8CO2R9, -NHC(NH2)=NH, -NR8C(NH2)=NH, -NHC(NH2)=NR8, -S(O)R8, -SO2R8, - SO2NR8R9, -NR8SO2R9, -CN y -NO2; y sus sales, solvatos, hidratos, isomeros geométricos, tautomeros, isomeros opticos, N-oxidos y formas de profármacos aceptables desde el punto de vista farmacéutico, con la salvedad de que: cuando X es S, R6 = R7, entonces R5 no es fenilo o 4-yodofenilo; X es S, R6 = R7 = fenilo, entonces R5 no es fenilo; y X es S, R6 y R7 se combinan para formar un anillo ciclopropilo, entonces R5 no es n-butilo, ciclohexilo, bencilo, fenilo o naftilo. Reivindicacion 3: Un compuesto de formula general (3), en el cual: R5 se selecciona de hidrogeno, alquilo C1-8, cicloalquilo C3-10, cicloalquilC3-10-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclilo, heterociclil-alquiloC1-8 y haloalquilo; en el cual cualquier residuo arilo, cicloalquilo o heterociclilo está sustituido en forma independiente y opcional por uno o más alquilo C1-8, arilo, halogeno, halo-alquiloC1-8, HO-alquiloC1-8, R8R9N-alquiloC1-8, -OR10-alquiloC1-8, -OR10, cicloalquilo C3-10 o alquilsulfonilo C1- 8; R6 se selecciona de alquilo C1-8, alcoxi C1-8, cicloalquilo C3-10, heterociclilo, cicloalquilC3-10-alquiloC1-8, CN-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclil-alquiloC1-8 y haloalquilo; R7 se selecciona de -NR8R9, halo, alquilo C1-8, - (CR8R9)n-OR8, -S-alquiloC1-8, cicloalquilo C3-10, heterociclilo, cicloalquilC3-10-alquiloC1-8, ciano-alquiloC1-8, arilo, aril-alquiloC1-8, heterociclil-alquiloC1-8, heterociclil-C(O)-alquiloC1-8, heterociclil-SO2-alquiloC1-8, haloalquilo C1-8, R8R9N- alquiloC1-8, HO-alquiloC1-8, -C(O)-cicloalquiloC3-10, -C(O)-haloalquiloC1-8, -(CR8R9)n-Y-(CR8R9)n-heterociclilo y -(CR8R9)n-Y-(CR8R9)n-C(O)-R8 (en el cual n es 0-5, Y es NR10, O o S); en el cual cualquier residuo arilo, alquilo, heterociclilo o cicloalquilo está sustituido en forma opcional por uno o más de: -alquiloC1-8; -halo; -OH; -OR10; alquilC1-8-SO2-; -SO2-arilo; -C(O)-(CR8R9)n-carbamato; C(O)-O-alquiloC1-8; -C(O)-alquiloC1-8; -C(O)-(CR8R9)n-C(O)-NR8R9; -C(O)-(CR8R9)n-NR8-C(O)- alquiloC1-8; -C(O)-(CR8R9)n-NR8R9; -C(O)-cicloalquiloC3-10; -C(O)-arilo; -C(O)-(CR8R9)n-heterociclilo; -alquiloC1-8-OR8; -C(O)-halo-alquiloC1-8; o -C(O)-(CR8R9)n-arilo; en el cual cualquier residuo arilo, alquilo, cicloalquilo, o heterociclilo está sustituido en forma independiente y opcional por uno o más alquilo C1-8, arilo, halogeno, -NR10R10, haloalquilo C1-8, HO-alquiloC1-8, R8R9N-alquiloC1-8, -OR10-alquiloC1-8, -OR10, cicloalquilo C3-10 o alquilsulfonilo C1-8, -O-(CR8R9)n-heterociclilo, - O-(CR8R9)n-C(O)-NR8R9, -O-(CR8R9)n-NR8R9, -Y-(CR8R9)n-NR8-C(O)-alquiloC1-8, -Y-(CR8R9)n-heterociclilo, -O-(CR8R9)n-NR8R9, alquilC1-8-SO2, o -O-(CR8R9)n-N-C(O)-heterociclilo; en el cual R8 y R9 se seleccionan, cada uno en forma independiente, de hidrogeno, alquilo C1-8, alcoxi C1-8, -NR10R10, -S-alquiloC1-8, arilo y heterociclilo; cualquier alquilo, alcoxi, heterociclilo o arilo puede estar sustituido con uno a tres sustituyentes seleccionados de -halo, alquilo C1-8 no sustituido, alcoxi C1- 8 no sustituido, tioalcoxi C1-8 no sustituido y arilalquilo C1-4 no sustituido; en el cual R10 se selecciona en forma independiente de hidrogeno, alquilo C1-8, arilalquilo C1-8, alcoxi C1-8, -S-alquiloC1-8, heterociclilo y arilo; cualquier alquilo, heterociclilo o arilo puede estar sustituido con uno a tres sustituyentes seleccionados de -halo, alquilo C1-8 no sustituido, alcoxi C1-8 no sustituido, tialcoxi C1-8 no sustituido y arilalquilo C1-4 no sustituido; o R6 y R7 forman, junto con el átomo de carbono unido a éstos, un cicloalquilo C3-10 saturado, parcialmente insaturado o insaturado o un heterociclil
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