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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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Argentina
Prior art keywords
alkyl
alkoxy
cycloalkyl
aryl
heteroaryl
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Application number
ARP080104279A
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English (en)
Inventor
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
Original Assignee
Bristol Myers Squibb Co
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40523804&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR068601(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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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    • 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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  • Nitrogen Condensed Heterocyclic Rings (AREA)

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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AR068601A1 true AR068601A1 (es) 2009-11-18

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EP (1) EP2205598A1 (es)
JP (1) JP5611044B2 (es)
KR (1) KR20100085081A (es)
CN (1) CN101883772B (es)
AR (1) AR068601A1 (es)
AU (1) AU2008309101B2 (es)
BR (1) BRPI0817656A2 (es)
CA (1) CA2701355A1 (es)
CL (1) CL2008002916A1 (es)
CO (1) CO6280485A2 (es)
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NZ584386A (en) 2012-03-30
CL2008002916A1 (es) 2010-02-12
CN101883772A (zh) 2010-11-10
IL204799A0 (en) 2010-11-30
BRPI0817656A2 (pt) 2015-03-31
JP5611044B2 (ja) 2014-10-22
EA201391705A1 (ru) 2014-07-30

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