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AR071236A1 - Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 - Google Patents

Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1

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Publication number
AR071236A1
AR071236A1 ARP090101584A ARP090101584A AR071236A1 AR 071236 A1 AR071236 A1 AR 071236A1 AR P090101584 A ARP090101584 A AR P090101584A AR P090101584 A ARP090101584 A AR P090101584A AR 071236 A1 AR071236 A1 AR 071236A1
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AR
Argentina
Prior art keywords
alkyl
alkoxy
nhs
2nhc
alkylamino
Prior art date
Application number
ARP090101584A
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English (en)
Original Assignee
Vitae Pharmaceuticals Inc
Boehringer Ingelheim Int
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 PCT/US2008/009017 external-priority patent/WO2009017664A1/en
Application filed by Vitae Pharmaceuticals Inc, Boehringer Ingelheim Int filed Critical Vitae Pharmaceuticals Inc
Publication of AR071236A1 publication Critical patent/AR071236A1/es

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Abstract

xi C1-6, halocicloalcoxi C3-6, halocicloalquilalcoLa presente solicitud se refiere a sales farmacéutxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquilalquiltio C4-7, haloalquiltio C1-6, halocicicamente aceptables de los mismos y a composiciones farmacéuticas de los mismos, que son utiles paraloalquiltio C3-6, halocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, ci el tratamiento terapéutico de enfermedades asociacloalquilalcanosulfinilo C4-7, haloalcanosulfinilodas con la modulacion o inhibicion de 11beta-HSD1 en mamíferos, también se refiere a composiciones f C1-6, halocicloalcanosulfinilo C3-6, halocicloalqarmacéuticas de los compuestos y a métodos para suuilalcanosulfinilo C4-7, alcanosulfonilo C1-6, cic uso en la reduccion o control de la produccion deloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo cortisol en una célula o la inhibicion de la conv C4-7, haloalcanosulfonilo C1-6, halocicloalcanosulfonilo C3-6, halocicloalquilalcanosulfonilo C4-7,ersion de cortisona en cortisol en una célula. Reivindicacion 1: Un compuesto de formula (1) en la q alquilamino C1-6, dialquilamino C1-6, alcoxi C1-6-alcoxi C1-6, haloalcoxi C1-6-alcoxi C1-6, alcoxicue: R1 está (a) ausente o (b) se selecciona entre arbonilo C1-6, H2NCO, H2NSO2, alquilaminocarboniloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-3-alcoxi C1-3 o alcoxi C1-3-alquilo C1-3 y e C1-6, dialquilaminocarbonilo C1-6, alcoxi C1-3-alstá opcionalmente sustituido hasta con cuatro grupquilaminocarbonilo C1-3, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquilaminosulfonilo C1os seleccionados independientemente entre fluor, c-6, heterociclilsulfonilo, alquilcarbonilamino C1-iano, oxo, R4, R4O-, (R4)2N-, R4O2C-, R4S, R4S(=O)6, alquilcarbonilamino C1-6-alquilo C1-6, alquilsu-, R4S(=O)2-, R4C(=O)NR4-, (R4)2NC(=O)-, (R4)2NC(=O)O-, (R4)2NC(=O)NR4-, R4OC(=O)NR4-, (R4)2NC(=NCN)lfonilamino C1-6, alquilsulfonilamino C1-6-alquilo C1-6, alcoxicarbonil C1-6-alcoxi C1-6, alcoxi C1-NR4-, (R4O)2P(=O)O-, (R4O)2P(=O)NR4-, R4OS(=O)2NR4-, (R4)2NS(=O)2O-, (R4)2NS(=O)2NR4-, R4S(=O)2NR4-,6-alquilo C1-6, haloalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1- R4S(=O)2NHC(=O)-, R4S(=O)2NHC(=O)O-, R4S(=O)2NHC(=O)NR4-, R4OS(=O)2NHC(=O)-, R4OS(=O)2NHC(=O)O-, R46, alquilamino C1-6-alquilo C1-6, dialquilamino C1OS(=O)2NHC(=O)NR4-, (R4)2NS(=O)2NHC(=O)-, (R4)2NS(-6-alquilamino C1-6-alcoxi C2-6, alquilamino C1-6-alcoxi C2-6, dialquilamino C1-6-alcoxi C2-6, alqui=O)2NHC(=O)O-, (R4)2NS(=O)2NHC(=O)NR4-, R4C(=O)NHS(=O)2-, R4C(=O)NHS(=O)2O-, R4C(=O)NHS(=O)2NR4-, R4lcarbonilo C1-6, cicloalquilcarbonilo C3-6, cicloaOC(=O)NHS(=O)2-, R4OC(=O)NHS(=O)2O-, R4OC(=O)NHS(=lquilaminocarbonilo C3-6, cicloalquil C3-6-alquil O)2NR4-, (R4)2NC(=O)NHS(=O)2-, (R4)2NC(=O)NHS(=O)2C1-6aminocarbonilo, dicicloalquilaminocarbonilo C3O-, (R4)2NC(=O)NHS(=O)2NR4, heterociclilo, heteroa-6, cicloalquilaminosulfonilo C3-6, cicloalquil C3-6-alquil C1-6aminosulfonilo, dicicloalquilaminosurilo, arilamino y heteroarilamino; A1 es (a) un enlace o (b) alquileno C1-3, CH2CH2O, donde el oxígelfonilo C3-6, cianoalquilo C1-6, aminocarbonilalquilo C1-6, alquilaminocarbonil C1-6-alquilo C1-6, dno está unido a Cy1 o CH2C(=O), donde el carbono dialquilaminocarbonil C1-6-alquilo C1-6, cicloalquiel carbonilo está unido a Cy1; Cy1 es arilo, heteroarilo, cicloalquilo monocíclico o heterociclilo mlaminocarbonil C3-6-alquilo C1-6, cicloalquil C3-6-alquil C1-6-aminocarbonilalquilo C1-6 y dicicloalonocíclico y está opcionalmente sustituido con 1 aquilaminocarbonil C3-6-alquilo C1-6; R3 se selecci 4 grupos seleccionados independientemente entre fona entre alquilo C1-6, alquenilo C2-6, alquinilo luor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, C2-6, cicloalquil C3-5-alquilo C1-4, alcoxi C1-3-acicloalquilo C3-6, hidroxicicloalquilo C3-6, ciclolcoxi C1-3 o alcoxi C1-3-alquilo C1-3 y está opcionalmente sustituido hasta con cuatro grupos seleccalquilalquilo C4-7, alquenilo C2-6, haloalquenilo ionados independientemente entre fluor, ciano, oxoC2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, haloalquilo C1-6, halo, R4, R4O-, (R4)2N-, R4O2C-, R4C(=O)O-, R4S, R4S(=cicloalquilo C3-6, halocicloalquilalquilo C4-7, alO)-, R4S(=O)2-, R4C(=O)NR4-, (R4)2NC(=O)-, (R4)2NCcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-(=O)O-, (R4)2NC(=O)NR4-, R4OC(=O)NR4-, (R4)2NC(=NC7, haloalcoxi C1-6, halocicloalcoxi C3-6, halociclN)NR4-, (R4O)2P(=O)O-, (R4O)2P(=O)NR4-, R4OS(=O)2Noalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltioR4-, (R4)2NS(=O)2O-, (R4)2NS(=O)2NR4-, R4S(=O)2NR4 C3-6, cicloalquilalquiltio C4-7, haloalquiltio C1-, R4S(=O)2NHC(=O)-, R4S(=O)2NHC(=O)O-, R4S(=O)2NH-6, halocicloalquiltio C3-6, halocicloalquilalquilC(=O)NR4-, R4OS(=O)2NHC(=O)-, R4OS(=O)2NHC(=O)O-, tio C4-7, alcanosulfinilo C1-6, cicloalcanosulfiniR4OS(=O)2NHC(=O)NR4-, (R4)2NS(=O)2NHC(=O)-, (R4)2Nlo C3-6, cicloalquilalcanosulfinilo C4-7, haloalcaS(=O)2NHC(=O)O-, (R4)2NS(=O)2NHC(=O)NR4-, R4C(=O)NHS(=O)2-, R4C(=O)NHS(=O)2O-, R4C(=O)NHS(=O)2NR4-, nosulfinilo C1-6, halocicloalcanosulfinilo C3-6, halocicloalquilalcanosulfinilo C4-7, alcanosulfonilR4OC(=O)NHS(=O)2-, R4OC(=O)NHS(=O)2O-, R4OC(=O)NHS(=O)2NR4-, (R4)2NC(=O)NHS(=O)2-, (R4)2NC(=O)NHS(=Oo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalca)2O-, (R4)2NC(=O)NHS(=O)2NR4, espirocicloalquilo; nosulfonilo C4-7, haloalcanosulfonilo C1-6, halocicloalcanosulfonilo (3-6, halocicloalquilalcanosulfheterociclilo (opcionalmente sustituido con alquilo, haloalquilo, halogeno o oxo), heteroarilo (opcionilo C4-7, alquilamino C1-6, dialquilamino C1-6, alcoxi C1-6-alcoxi C1-6, haloalcoxi C1-6-alcoxi C1onalmente sustituido con alquilo, haloalquilo, alc-6, alcoxicarbonilo C1-6, H2NCO, H2NSO2, alquilamioxi, alquiltio, alquilsulfonilo, halogeno, trifluonocarbonilo C1-6, dialquilaminocarbonilo C1-6, alcrometilo, dialquilamino, nitro, ciano, CO2H, CONH2, amido N-monoalquil sustituido, amido N,N-dialquioxi C1-3-alquilaminocarbonilo C1-3, heterociclilcal-sustituido u oxo), aril-amino (opcionalmente susrbonilo, alquilaminosulfonilo C1-6, dialquilaminostituido con alquilo, alcoxi, alquiltio, alquilsulfulfonilo C1-6, heterociclilsulfonilo, alquilcarbononilo, halogeno, trifluorometilo, dialquilamino, nilamino C1-6, alquil C1-6- carbonilaminoalquilo C1-6, alquilsulfonilamino C1-6, alquil C1-6-sulfonilitro, ciano, CO2H, CONH2, amido N-monoalquil-sustiaminoalquilo C1-6, alcoxicarbonil C1-6-alcoxi C1-6tuido y amido N,N-dialquil-sustituido) y heteroari, alcoxi C1-6-alquilo C1-6, haloalcoxi C1-6-alquillamino (opcionalmente sustituido con alquilo, haloo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminalquilo, alcoxi, alquiltio, alquilsulfonilo, halogeno, trifluorometilo, dialquilamino, nitro, ciano,oalquilo C1-6, alquilamino C1-6-alquilo C1-6, dial CO2H, CONH2, amido N-monoalquil-sustituido, amidoquilamino C1-6-alquilamino C1-6-alcoxi C2-6, alquilamino C1-6-alcoxi C2-6, dialquilamino C1-6-alcoxi N,N-dialquil-sustituido u oxo); y R4 se seleccion C2-6, alquilcarbonilo C1-6, cicloalquilcarbonilo a independientemente entre H, alquilo C1-6, haloalquilo C1-6, aminoalquilo C1-6, alquilamino C1-6-alC3-6, cicloalquilaminocarbonilo C3-6, cicloalquil quilo C1-6, dialquilamino C1-6-alquilo C1-6, hidroC3-6-alquil C1-6aminocarbonilo, dicicloalquilaminoxialquilo C1-6 y alcoxi C1-6-alquilo C1-6; o una scarbonilo C3-6, cicloalquilaminosulfonilo C3-6, cial farmacéuticamente aceptable, enantiomero o diascloalquil C3-6-alquil C1-6aminosulfonilo, dicicloalquilaminosulfonilo C3-6, cianoalquilo C1-6, aminotereomero del mismo, con la condicion de que el cocarbonilalquilo C1-6, alquilaminocarbonil C1-6-alqmpuesto no sea un compuesto representado por la fouilo C1-6, dialquilaminocarbonil C1-6-alquilo C1-6rmulas estructurales PR-258 o PR-291, o una sal farmacéuticamente aceptable, enantiomero o diastereo, cicloalquilaminocarbonil C3-6- alquilo C1-6, cicloalquil C3-6-alquil C1-6aminocarbonilalquilo C1-6mero del mismo. y dicicloalquilaminocarbonil C3-6-alquilo C1-6; el anillo de piridina en la formula (1) está opcionalmente sustituido con 1 a 4 grupos seleccionados independientemente entre fluor, cloro, bromo, yodo, ciano, nitro, amino, hidroxi, carboxi, alquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-6, hidroxicicloalquilo C3-6, cicloalquilalquilo C4-7, alquenilo C2-6, haloalquenilo C2-6, hidroxialquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquinilo C2-4, haloalquilo C1-6, halocicloalquilo C3-6, halocicloalquilalquilo C4-7, alcoxi C1-6, cicloalcoxi C3-6, cicloalquilalcoxi C4-7, haloalcoxi C1-6, halocicloalcoxi C3-6, halocicloalquilalcoxi C4-7, alquiltio C1-6, cicloalquiltio C3-6, cicloalquilalquiltio C4-7, haloalquiltio C1-6, halocicloalquiltio C3-6, halocicloalquilalquiltio C4-7, alcanosulfinilo C1-6, cicloalcanosulfinilo C3-6, cicloalquilalcanosulfinilo C4-7, haloalcanosulfinilo C1-6, halocicloalcanosulfinilo C3-6, halocicloalquilalcanosulfinilo C4-7, alcanosulfonilo C1-6, cicloalcanosulfonilo C3-6, cicloalquilalcanosulfonilo C4-7, haloalcanosulfonilo C1-6, halocicloalcanosulfonilo C3-6, halocicloalquilalcanosulfonilo C4-7, alquilamino C1-6, dialquilamino C1-6, alcoxi C1-6-alcoxi C1-6, haloalcoxi C1-6-alcoxi C1-6, alcoxicarbonilo C1-6, H2NCO, H2NSO2, alquilaminocarbonilo C1-6, dialquilaminocarbonilo C1-6, alcoxi C1-3-alquilaminocarbonilo C1-3, heterociclilcarbonilo, alquilaminosulfonilo C1-6, dialquilaminosulfonilo C1-6, heterociclilsulfonilo, alquilcarbonilamino C1-6, alquilcarbonilamino C1-6-alquilo C1-6, alquilsulfonilamino C1-6, alquilsulfonilamino C1-6-alquilo C1-6, alcoxicarbonil C1-6-alcoxi C1-6, alcoxi C1-6-alquilo C1-6, haloalcoxi C1-6-alquilo C1-6, hidroxialcoxi C1-6, heteroarilo, oxo, aminoalquilo C1-6, alquilamino C1-6-alquilo C1-6, dialquilamino C1-6-alquilamino C1-6-alcoxi C2-6, alquilamino C1-6-alcoxi C2-6, dialquilamino C1-6-alcoxi C2-6, alquilcarbonilo C1-6, cicloalquilcarbonilo C3-6, cicloalquilaminocar
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