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AR071386A1 - Compuestos heterociclicos nitrogenados, inhibidores carbamato y urea de la 11-beta-hidroxiesteroide deshidrogenasa tipo 1(11 beta-hsd1),composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la obesidad,hipertension,trastornos cognitivos y otras enfermedades. - Google Patents

Compuestos heterociclicos nitrogenados, inhibidores carbamato y urea de la 11-beta-hidroxiesteroide deshidrogenasa tipo 1(11 beta-hsd1),composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la obesidad,hipertension,trastornos cognitivos y otras enfermedades.

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AR071386A1
AR071386A1 ARP090101394A ARP090101394A AR071386A1 AR 071386 A1 AR071386 A1 AR 071386A1 AR P090101394 A ARP090101394 A AR P090101394A AR P090101394 A ARP090101394 A AR P090101394A AR 071386 A1 AR071386 A1 AR 071386A1
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Argentina
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optionally substituted
alkyl
represented
cycloalkyl
heteroaryl
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Vitae Pharmaceuticals Inc
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Abstract

Composiciones farmacéuticas que los contienen y su uso en la reduccion o control de la produccion de cortisol en una célula o la inhibicion de la conversion de cortisona en cortisol en una célula. Reivindicacion 1: Un compuesto de formula (1), en la que Cy bicicloalquilo C7-12 o tricicloalquilo C9-12, donde 1-2 átomos de carbono se reemplazan opcionalmente por heteroátomos seleccionados independientemente entre N y O, y que está opcionalmente sustituido con 1-3 grupos seleccionados independientemente entre halogeno, nitro, (CH2)xCN, alquilo C1-3, haloalquilo C1-3, hidroxialquilo C1-3, (CH2)xOR4, haloalcoxi C1-3, (CH2)xN(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, arilo opcionalmente sustituido representado por Ar1, heteroarilo opcionalmente sustituido representado por HetAr1, heterociclilo opcionalmente sustituido representado por HetCy1 y cicloalquilo opcionalmente sustituido representado por Cy1, donde Ar1, HetAr1, HetCy1 y Cy1 están opcionalmente sustituidos con uno a tres grupos representados por R7; B es (a) -C(O)OR1 o (b) arilo o heteroarilo, cada uno opcionalmente sustituido con 1-4 grupos representados por R6; R1 es alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, heterociclilo, cicloalquil C3-8-alquilo C1-3, heterociclilalquilo C1-3, arilo, arilalquilo C1-3 o heteroarilalquilo C1-3, cada uno opcionalmente sustituido con 1-4 grupos seleccionados independientemente entre halogeno, nitro, (CH2)xCN, alquilo C1-3, haloalquilo C1-3, hidroxialquilo C1-3, (CH2)xOR4, haloalcoxi C1-3, (CH2)xN(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, arilo opcionalmente sustituido representado por Ar1, heteroarilo opcionalmente sustituido representado por HetAr1, heterociclilo opcionalmente sustituido representado por HetCy1 y cicloalquilo opcionalmente sustituido representado por Cy1, donde Ar1, HetAr1, HetCy1 y Cy1 están opcionalmente sustituidos con uno a tres grupos representados por R7; donde el alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, heterociclilo, cicloalquil C3-8-alquilo C1-3, heterociclilalquilo C1-3, la porcion alquilo de arilalquilo C1-3, heteroarilo y heteroarilalquilo C1-3 están opcionalmente sustituidos además con oxo; R2 y R3 son independientemente (a) hidrogeno; o (b) alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, heterociclilo, arilo, heteroarilo, cicloalquil C3-8-alquilo C1-3, heterociclilalquilo C1-3, arilalquilo C1-3, heteroarilalquilo C1-3 o (CH2)xCO2R4, cada uno opcionalmente sustituido con 1-4 grupos seleccionados independientemente entre halogeno, nitro, (CH2)xCN, alquilo C1-3, haloalquilo C1-3, haloalcoxi C1-3, hidroxialquilo C1-3, (CH2)xOR4, (CH2)xN(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, arilo opcionalmente sustituido representado por Ar1, heteroarilo opcionalmente sustituido representado por HetAr1, heterociclilo opcionalmente sustituido representado por HetCy1 y cicloalquilo opcionalmente sustituido representado por Cy1, donde Ar1, HetAr1, HetCy1 y Cy1 están opcionalmente sustituidos con uno a tres grupos representados por R7; donde el alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, heterociclilo, heteroarilo, cicloalquil C3-8-alquilo C1-3, heterociclilalquilo C1-3, la porcion alquilo de arilalquilo C1-3, heteroarilo y heteroarilalquilo C1-3 están opcionalmente sustituidos además con oxo; o R2 y R3 tomados juntos forman alquileno C1-4 opcionalmente sustituido hasta con 2 grupos alquilo C1-3; cada R4 es independientemente (a) hidrogeno; o (b) alquilo C1-10, cicloalquilo C3-8, arilo o arilalquilo C1-3, cada uno opcionalmente sustituido con halogeno, alcoxi C1-3, alquilo C1-3, haloalquilo C1-3, haloalcoxi C1-3, ciano o nitro; R5 es hidrogeno o alquilo C1-6; cada R6 se selecciona independientemente entre halogeno, nitro, (CH2)xCN, alquilo C1-3, haloalquilo C1-3, hidroxialquilo C1-3, (CH2)xOR4, haloalcoxi C1-3, (CH2)xN(R4)2, (CH2)xC(=NOH)NH2, (CH2)xNR4CON(R4)2, (CH2)xCON(R4)2, (CH2)xCO2R4, (CH2)xSO2N(R4)2, (CH2)xSO2R4, (CH2)xNR4COR4, (CH2)xNR4CO2R4, (CH2)xNR4SO2R4, (CH2)xOC(=O)N(R4)2, arilo opcionalmente sustituido representado por Ar1, heteroarilo opcionalmente sustituido representado por HetAr1, heterociclilo opcionalmente sustituido representado por HetCy1 y cicloalquilo opcionalmente sustituido representado por Cy1, donde Ar1, HetAr1, HetCy1 y Cy1 están opcionalmente sustituidos con uno a tres grupos representados por R7, donde, cuando B es heteroarilo, R6 también puede ser oxo; cada R7 se selecciona independientemente entre halogeno, nitro, ciano, alquilo C1-3, haloalquilo C1-3, alcoxi C1-3, haloalcoxi C1-3, y CON(R4)2, con la condicion de que R7 también incluya oxo cuando HetAr1, HetCy1 y Cy1 están sustituidos con R7; x es 0, 1, 2 o 3; A es un enlace o CH2; m es 0,1, 2, 3 o 4; n es 1, 2, 3 o 4; y Q es O o NR5; o una sal farmacéuticamente aceptable del mismo.
ARP090101394A 2008-04-22 2009-04-21 Compuestos heterociclicos nitrogenados, inhibidores carbamato y urea de la 11-beta-hidroxiesteroide deshidrogenasa tipo 1(11 beta-hsd1),composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la obesidad,hipertension,trastornos cognitivos y otras enfermedades. AR071386A1 (es)

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AR067673A1 (es) 2007-07-26 2009-10-21 Vitae Pharmaceuticals Inc Derivados de 1,3 oxazinan - 2 - ona como inhibidores ciclicos de la 11 beta -hidroxiesteroide deshidrogenasa 1. composiciones farmaceuticas.
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