AR068601A1 - Triazolopiridinas como inhibidores de 11- beta hidroxiesteroide tipo i - Google Patents

Triazolopiridinas como inhibidores de 11- beta hidroxiesteroide tipo i

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Publication number
AR068601A1
AR068601A1 ARP080104279A ARP080104279A AR068601A1 AR 068601 A1 AR068601 A1 AR 068601A1 AR P080104279 A ARP080104279 A AR P080104279A AR P080104279 A ARP080104279 A AR P080104279A AR 068601 A1 AR068601 A1 AR 068601A1
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alkyl
alkoxy
cycloalkyl
aryl
heteroaryl
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ARP080104279A
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Jeffrey A Robi
Lawrence J Kennedy
Jie Jack Li
Reginald O Cann
Chenkou Wei
An-Rong Li
James J Li
Michael A Galella
Laxma R Kolla
Haixia Wang
Xinhua Qian
Rajendra V Deshpande
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR068601A1 publication Critical patent/AR068601A1/es

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Abstract

Composicion farmacéutica, proceso para preparar los compuestos y uso para tratar, prevenir o ralentizar enfermedades como diabetes, hiperglucemia, obesidad, dislipidemia, hipertension, deterioro cognitivo, artritis reumatoidea, osteoartritis, glaucoma, Cushing y síndrome metabolico. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) sus enantiomeros, diastereoisomeros o sales, en la que: Q es L, Laa o Lee; X es C e Y es N; o X es N e Y es C; G es R4, R4aa o R4ee; L es -alquenil-(W1)n, -cicloalquil-(W1)n o -alquil-(W2)n; Laa es -alquenil-(W1)n o -alquil-(W2aa)n; Lee es -aIquenil-(W1ee)n, -cicloalquil-(W1)n o -alquil-(W2ee)n; n es 1 a 3; W1, cada vez que aparece, es independientemente halogeno, -OH, -CN, -CO2R6, -CONR8R8a, -OCONR8R8a, -SO2NR8R8a, -SOR6, -SO2R6, -NR9SO2R9a, -NR9CO2R9a, -NR9COR9a, alquilo, cicloalquilo, haloalquilo, alcoxi, ariloxi, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, amino, aminoalquilo, arilamino o heteroarilamino; W1ee es independientemente halogeno, -OH, -CN, -CO2R6, CONR8R8a, -OCONR8R8a, SO2NR8R8a, -SOR6, -SO2R6, NR9SO2R9a, NR9CO2R9a, -NR9COR9a, cicloalquilo, alquilo, haloalquilo, alcoxi, ariloxi, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, amino, aminoalquilo, arilamino o heteroarilamino; W2 es independientemente halogeno, -OH, -CO2H, -CN, -CO2R6, -CONR8R8a, -OCOR6, -OCONR8R8a, -SO2NR8R8a, -SO-alquilo, -SO2-alquilo, -NR9SO2R9a, -NR9CO2R9a, -NR9COR9a, cicloalquilo, alquilo, haloalquilo, alcoxi, alquenilo, haloalcoxi, alquiltio, alquilamino, amino o aminoalquilo; W2aa es independientemente halogeno, -OH, -CN, -CO2H, -CO2R6, CONR8R8a, -OCOR6, -OCONR8R8a, -SO2NR8R8a, -SO-alquilo, -SO2-alquilo, NR9SO2R9a, -NR9CO2R9a, -NR9COR9a, -OR9bOR9bSi(R9b)3, cicloalquilo, alquilo, haloalquilo, alcoxi. alquenilo, haloalcoxi, alquiltio, alquilamino, amino o aminoalquilo; W2ee es independientemente halogeno, -OH, -CN, -CO2H, -CO2R6, -CONR8R8a, -OCOR6, -OCONR8R8a, -SO2NR8R8a, -SO-alquilo, -SO2-alquilo, NR9SO2R9a, NR9CO2R9a, -NR9COR9a, cicloalquilo, alquilo, haloalquilo, alquenilo, haloalcoxi, alquiltio, amino, aminoalquilo, arilo, heteroarilo o heterociclilo, donde el arilo, heteroarilo o heterociclilo está opcionalmente sustituido con R7, R7a, R7b y R7c; con la condicion de que W2aa o W2ee no son unicamente halogeno o alquilo; R3, R3a y R3b son independientemente hidrogeno, halogeno, -OH, -CN, -NO2, CO2R8a, CONR8R8a, -SO2NR8R8a, -SOR8a, -SO2R8a, -NR8SO2R6, -NR8CO2R6, alquilo, haloalquilo, cicloalquilo, alcoxi, ariloxi, alquenilo, haloalcoxi, alquiltio, ariltio, arilsulfonilo, alquilamino, aminoalquilo, arilamino, heteroarilamino, arilo, heteroarilo o heterociclilo, pudiendo estar el arilo, heteroarilo o heterociclilo opcionalmente sustituido con R7, R7a, R7b, y R7c; R4 es alquilo, cicloalquilo o heterociclilo, los cuales pueden estar todos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6. -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR8R8a, -CONR8R8a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, pudiendo estar el alquilo, alcoxi, arilo, heteroarilo o heterociclilo opcionalmente sustituido con R7, R7a, R7b, y R7c; R4aa es cicloalquilo, que puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, CO2H, -OCONR8R8a, -CONR8R8a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, pudiendo estar el alquilo, alcoxi, arilo, heteroarilo o heterociclilo opcionalmente sustituido con R7, R7a, R7b, y R7c; R4ee es alquilo, que puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados de halogeno, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR8R8a, -CONR8R8a, -NR5CO2R6, -SO2R6, alquilo, alcoxi, arilo, amino, heterociclilo o heteroarilo, pudiendo estar el alquilo, alcoxi, arilo, heteroarilo o heterociclilo opcionalmente sustituido con R7, R7a, R7b y R7c; R5, cada vez que aparece, es independientemente hidrogeno, alquilo, cicloalquilo, arilo, haloalquilo, COR8a, CO2R8a, SO2NR8R8a o SO2R8a; R6, cada vez que aparece, es independientemente alquilo, cicloalquilo, arilo o heteroarilo, los cuales pueden estar todos opcionalmente sustituidos con R7, R7a, R7b, y R7c; R7, R7a, R7b, y R7c, cada vez que aparecen, son independientemente halo, alquilo, haloalquilo, cianoalquilo, alcoxi, haloalcoxi, arilo, ariloxi, arilarilo, arilalquilo, arilalquiloxi, alquenilo, cicloalquilo, cicloalquilalquilo, cicloalquilalquiloxi, amino, -OH, -CO2R8, -CONR8R8a, hidroxialquilo, acilo, heteroarilo, heteroariloxi, heteroarilalquilo, heteroarilalcoxi, ariloxialquilo, alquiltio, arilalquiltio, ariloxiarilo, alquilamido, alcanoilamino, arilcarbonilamino, alquilsilicealquiloxi, -SO2R9b -NO2, -CN o tiol, donde el arilo o heteroarilo puede estar opcionalmente sustituido con R10, R10a, R10b y R10c; R8 y R8a, cada vez que aparecen, son independientemente hidrogeno, alquilo, cicloalquilo, arilo, heteroarilo o heterociclilo, los cuales pueden estar todos opcionalmente sustituidos con R10, R10a, R10b, y R10c; o, como alternativa, R8 y R8a se pueden tomar junto con el nitrogeno al que están unidos formando un anillo heterociclilo que contiene 1, 2, 3 o 4 heteroátomos seleccionados independientemente entre el grupo constituido por N, NH, O y S, que puede estar opcionalmente sustituido con R10, R10a, R10b, y R10c; R9 y R9a, cada vez que aparecen, son independientemente hidrogeno, alquilo, cicloalquilo, arilo, arilalquilo, heteroarilo o heterociclilo, los cuales pueden estar todos opcionalmente sustituidos con R10, R10a, R10b, y R10c; R9b, cada vez que aparece, es independientemente alquilo, cicloalquilo, arilo o heteroarilo, los cuales pueden estar todos opcionalmente sustituidos con R10, R10a, R10b, y R10c; y R10, R10a, R10b, y R10c, cada vez que aparecen, son independientemente halo, alquilo, haloalquilo, cianoalquilo, 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; con la condicion de que: (a) W1, W1ee, W2 o W2aa no es cicloalquilo cuando n es 1 y R4, R4aa o R4ee son cicloalquilo; (b) W2ee no es cicloalquilo, arilo, heteroarilo o heterociclilo cuando n es 1 y R4ee es cicloalquilo; (c) R7, R7a, R7b, y R7c deben estar sustituidos con al menos un R10, R10a, R10b o R10c cuando (i) Lee es cicloalquilo, (ii) R4ee es cicloalquilo sustituido con arilo, heterociclilo o heteroarilo, (iii) el arilo, heteroarilo o heterociclilo está sustituido con R7, R7a, R7b o R7c y (iv) R7, R7a, R7b, y R7c es arilo, heteroarilo o heterociclilo; (d) Laa y Lee no son alquilo C1-3 o haloalquilo C1-3 cuando R4aa o R4ee están sustituidos con un resto arilo opcionalmente sustituido; y (e) W2ee no es halogeno, alquilo, haloalquilo o arilo cuando R4ee es alquilo.
ARP080104279A 2007-10-01 2008-09-30 Triazolopiridinas como inhibidores de 11- beta hidroxiesteroide tipo i AR068601A1 (es)

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US97650607P 2007-10-01 2007-10-01
US12/206,801 US8119658B2 (en) 2007-10-01 2008-09-09 Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors

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