AR057357A1 - Heterociclos nitrogenados como inhibidores de heteroaril 11-beta hidroxiesteroide deshidrogenasa tipo 1. composiciones farmaceuticas - Google Patents

Heterociclos nitrogenados como inhibidores de heteroaril 11-beta hidroxiesteroide deshidrogenasa tipo 1. composiciones farmaceuticas

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Publication number
AR057357A1
AR057357A1 ARP060102405A ARP060102405A AR057357A1 AR 057357 A1 AR057357 A1 AR 057357A1 AR P060102405 A ARP060102405 A AR P060102405A AR P060102405 A ARP060102405 A AR P060102405A AR 057357 A1 AR057357 A1 AR 057357A1
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heteroaryl
heterocyclyl
aryl
alkyl
optionally substituted
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ARP060102405A
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English (en)
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James J Li
Lawrence G Hamann
Haixia Wang
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Bristol Myers Squibb Co
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Publication of AR057357A1 publication Critical patent/AR057357A1/es

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract

Reivindicacion 1: Compuesto caracterizado porque la formula W-L-Z enantiomeros, diastereomeros, solvatos, sales o profármacos del mismo, en donde: W es arilo, cicloalquilo, heteroarilo o heterociclilo, todos los cuales pueden ser opcionalmente sustituidos con R1, R1a, R1b, R1c y R1d; R1, R1a, R1b, R1c y R1d son independientemente hidrogeno, halogeno, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, SOR2a, SO2R2a, -NR2SO2R6, -NR2CO2R6, alquilo, haloalquilo, cicloalquilo, alcoxi, ariloxi, alquenilo, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, aminoalquilo, arilamino, heteroarilamino, arilo, heteroarilo o heterociclilo, en donde el arilo, heteroarilo o heterociclilo pueden ser opcionalmente sustituidos con R7, R7a, R7b y R7c; o alternativamente algunos dos de R1, R1a, R1b, R1c y R1d se pueden tomar conjuntamente para formar un anillo de arilo, heteroarilo, heterociclilo fusionado o anillo heterociclilo espiro; L es un enlace, O, S, SO, SO2, alquenilo, cicloalquilo, NR5, CR2R2a, CR2CR2aCR2bR2c, SO2NR2, OCR2R2a, OCR2R2aCR2bR2c, CR2R2aO, CR2bR2cCR2R2aO, N(R5)CR2R2a, CR2R2aN(R5), SCR2R2a, CR2R2aS, CR2R2aSO, CR2R2aSO2, SOCR2R2a, SO2CR2R2a, CR2R2aOCR2bR2c, CR2R2aSCR2bR2c, CR2R2SO2CR2bR2c, SO2NR2CR2aR2b, COCR2R2a. CR2R2aCO, CONR5CR2aR2b, CR2R2aCR2bR2cS, CR2R2aCR2bR2cSO, siempre que L no sea un enlace cuendo W es fenilo; R2, R2a, R2b y R2c son independientemente hidrogeno, halogeno, alquilo o halo alquilo; o alternativamente algunos dos de R2, R2a, R2b y R2c se pueden tomar conjuntamente con el átomo al cual se unen para formar un anillo cicloalquilo, cicloalquilo sustituido con halogeno o heterociclilo; Z se selecciona de los siguientes grupos heteroarilo bicíclicos: (a) (b) (c) (d) (e) (f) (g) (h); R3, R3a y R3b son independientemente hidrogeno, halogeno, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, -NR2SO2R6, -NR2CO2R6, alquilo, haloalquilo, cicloalquilo, alcoxi, ariloxi, alquenilo, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, aminoalquilo, arilamino, heteroatilamino, arilo, heteroarilo o heterociclilo, en donde el arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b y R7c, R4 es bibiclo[2,2,2]octilo o biciclo[2,2,1]heptilo, ambos se pueden sustituir opcionalmente con uno o más sustituyentes seleccionados de halogeno, -OH, OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, CONR2R2a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b y R7c; o R4 cicloalquilo, diferente de biciclo[2,2,2]octilo o biciclo[2,2,1]heptilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b, y R7c; o R4 es heterociclilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, OCONR2R2a, -NR5CO2R6, SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b, y R7c; o R4 es alquilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, OR6, -SR6, -OCOR6, -CN, -NR5COR6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, en donde el alquilo, alcoxi, arilo, heteroarilo o heterociclilo se puede sustituir opcionalmente con R7, R7a, R7b, y R7c; o R4a es hidrogeno, CN, alquilo, haloalquilo, arilo, arilosustituido, heteroarilo o heteroarilo sustituido; R5 en cada caso, es independientemente hidrogeno, alquilo, cicloalquilo, arilo, haloalquilo, COR2a, CO2R2a, SO2NR2R2a, o SO2R2a; R6, en cada caso, es independientemente alquilo, cicloalquilo, arilo o heteroarilo, todos los cuales se pueden sustituir opcionalmente con R7, R7a, R7b, y R7c; y R7, R7a, R7b, y R7b, en cada caso, son independientemente halo, alquilo, haloalquilo, alcoxi, arilo, ariloxi, arilarilo, arilalquilo, arilalquiloxi, alquenilo, cicloalquilo , cicloalquilalquilo, cicloalquilalquiloxi, amino, -OH, hidroxialquilo, acilo, heteroarilo, heteroariloxi, heteroarilalquilo, heteroarilalcoxi, ariloxialquilo, alquiltio, arilalquiltio, ariloxiarilo, alquilamido, alcanoilamino, arilcarbonilamino, - NO2, -CN o tiol; excluyendo los compuestos que tienen la formula (1) en donde W es fenilo, el fenilo es opcionalmente sustituido con R1, R1a, R1b, R1c y R1d; R1, R1a, R1b, R1c y R1d son independientemente hidrogeno, halogeno, alquilo o haloalquilo; Les CH2, O, S o SO2; y R4 es C3-10cicloalquilo, diferente de biciclo[2,2,2]octilo o biciclo [2,2,1]heptilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, CN, -NHCOR6, -NHSO2R6, C1-6alquilo, perhaloC1-6alquilo, C1-6alcoxi, perhaloC1-6alcoxi, C1-10heterociclilo, C1-10heteroarilo o fenilo; o R4 es C1-10heterociclilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, CN, -NHCOR6, - NHSO2R6, C1-6alquilo, perhaloC1-6alquilo, C1-6alcoxi, perhaloC1-6alcoxi, C1-10heterociclilo, C1-10heteroarilo o fenilo; o R4 es C1-6alquilo, el cual puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, OH, CN, - NHCOR6, -NHSO2R6, C1-6alquilo, perhaloC1-6alquilo, C1-6alcoxi, perhaloC1-6alcoxi, C1-10heterociclilo, C1-10heteroarilo o fenilo. Composiciones farmacéuticas que los comprenden.
ARP060102405A 2005-06-09 2006-06-08 Heterociclos nitrogenados como inhibidores de heteroaril 11-beta hidroxiesteroide deshidrogenasa tipo 1. composiciones farmaceuticas AR057357A1 (es)

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US68899305P 2005-06-09 2005-06-09
US11/448,946 US7572807B2 (en) 2005-06-09 2006-06-07 Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors

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US (2) US7572807B2 (es)
EP (1) EP1912986B1 (es)
JP (1) JP5124450B2 (es)
KR (1) KR20080018942A (es)
AR (1) AR057357A1 (es)
AU (1) AU2006258077B2 (es)
ES (1) ES2392656T3 (es)
MX (1) MX2007015283A (es)
NO (1) NO20076054L (es)
PE (1) PE20070002A1 (es)
TW (1) TW200716116A (es)
WO (1) WO2006135667A1 (es)

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