AR058095A1 - Derivados de triazolopiridina en calidad de inhibidores de lipasas y fosfolipasas. procesos de obtencion y composiciones farmaceuticas. - Google Patents

Derivados de triazolopiridina en calidad de inhibidores de lipasas y fosfolipasas. procesos de obtencion y composiciones farmaceuticas.

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AR058095A1
AR058095A1 ARP060104518A ARP060104518A AR058095A1 AR 058095 A1 AR058095 A1 AR 058095A1 AR P060104518 A ARP060104518 A AR P060104518A AR P060104518 A ARP060104518 A AR P060104518A AR 058095 A1 AR058095 A1 AR 058095A1
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alkyl
alkylene
cycloalkyl
aryl
amino
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ARP060104518A
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Sanofi Aventis
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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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    • 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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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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Abstract

Reivindicacion 1: Un compuesto de la formula (1) en la que los significados son X de manera idéntica o diferente, =C(-R)- o =N-, en que al menos uno y a lo sumo dos X es/son =N-; W -(C=O)-, -(S=O)-, -(SO2)-; R de manera idéntica o diferente, hidrogeno, halogeno, alquilo (C1-6), haloalquilo (C1-3), alquiloxi (C1-3)-alquileno C1-3), hidroxi, fenoxi, amino, alquil (C1-6)-amino, di-alquil (C2-12)-amino, ciano, nitro, COOR3, mono-alquil (C1-6)-aminocarbonilo, di-alquil (C2-8)-aminocarbonilo, alquil (C1-6)-mercapto, alquil (C1-6)-sulfinilo, alquil (C1-6)-sulfonilo, aminosulfonilo, pentafluorosulfanilo, arilo, heteroarilo, cicloalquilo (C3-12), alquil (C1-6)-carbonilo, O-CO-NR3R3a, O-CO-alquilen (C1-6)-CO-O-alquilo (C1-6), O-CO-alquilen (C1-6)-CO-OH, O-CO-alquilen (C1-6)-CO-NR3R3a o alquiloxi (C1-6) no sustituido o mono- o poli-F-sustituido; R1 alquilo (C5-16), cicloalquilo (C5-12), Y-arilo, Y-heteroarilo, Y-cicloalquilo (C5-12), biciclo, en que arilo, heteroarilo, cicloalquilo o biciclo puede estar sustituido, una o más veces, con halogeno, alquilo (C1-6), alquiloxi (C1-6), hidroxi, alquil (C1-6)-mercapto, amino, alquil (C1-6)-amino, di-alquil (C2-12)-amino, mono-alquil (C1-6)-aminocatbonilo, di-alquil (C2-8)- aminocarbonilo, alquiloxi (C1-6)-carbonilo, alquil (C1-6)-carbonilo, ciano, nitro, trifluorometilo, trifluorometoxi, alquil (C1-6)-sulfonilo, aminosulfonilo; Y alquileno (C1-3), que puede estar sustituido, una o más veces, con halogeno, alquilo (C1- 2) o hidroxi; R2 hidrogeno, alquilo (C4-12); o R1 y R2, junto con el átomo de nitrogeno que los porta, pueden formar un sistema de anillo de 4 a 7 miembros, monocíclico, saturado o parcialmente insaturado o un sistema de anillo de 8 a 14 miembros, bicíclico, saturado o parcialmente insaturado, cuyos miembros individuales de los sistemas de anillo pueden estar reemplazados por uno a tres átomos o grupos atomicos de la serie -CHR4-, -CR4R5-, =(C-R4)-, -NR5-, -C(=O)-, -O-, -S-, -SO-, -SO2-, con la condicion de que dos unidades de la serie -O-, -S-, -SO-, -SO2- no puedan estar adyacentes; R3, R3a, de manera idéntica o diferente, hidrogeno, alquilo (C1-6), bencilo; R4, R5, de manera idéntica o diferente, alquilo (C1-12), alquiloxi (C1-6), halogeno, haloalquilo (C1-3), haloalquiloxi (C1-3), COOR3, nitro, ciano, arilo, heterociclo, cicloalquilo (C3-12), alquilen (C1-3)-arilo, alquilen (C1-3)-heterociclo, alquilen (C1-3)-cicloalquilo, en que arilo, heterociclo o cicloalquilo puede estar sustituido, una o más veces, con halogeno, alquilo (C1-6), alquiloxi (C1-6), O-alquilen (C1-3)-arilo, trifluorometilo, trifluorometoxi, hidroxi, mono-alquil (C1-6)-aminocarbonilo, di-alquil (C2-8)-aminocarbonilo, CO-alquilo (C1-6), CO-O-alquilo (C1- 6), NR3R3a; las formas tautomeras de los compuestos y sus sales fisiologicamente toleradas; con la condicion de que debe excluirse el compuesto de la formula 1 con los significados X en las posiciones 4, 5 y 6 = =C(-R)-, en la posicion 7 = =N-, W = - (C=O)-, R = hidrogeno, R1 y R2 forman una morfolina; y con la condicion de que deben excluirse loc compuestos de la formula 1 con los significados X en las posiciones 4 y 6 = =C(-R)-, en las posiciones 5 y 7 = =N-, W = -(C=O)-, R = arilo, heteroarilo, fenoxi.
ARP060104518A 2005-10-19 2006-10-17 Derivados de triazolopiridina en calidad de inhibidores de lipasas y fosfolipasas. procesos de obtencion y composiciones farmaceuticas. AR058095A1 (es)

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DE102005049954A DE102005049954A1 (de) 2005-10-19 2005-10-19 Triazolopyridin-derivate als Inhibitoren von Lipasen und Phospholipasen

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US (2) US7718669B2 (es)
EP (1) EP1940838B1 (es)
JP (1) JP2009512649A (es)
KR (1) KR20080057299A (es)
CN (1) CN101291932A (es)
AR (1) AR058095A1 (es)
AU (1) AU2006303551A1 (es)
BR (1) BRPI0617712A2 (es)
CA (1) CA2625442A1 (es)
CR (1) CR9851A (es)
DE (1) DE102005049954A1 (es)
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NO (1) NO20082159L (es)
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DE102005049954A1 (de) * 2005-10-19 2007-05-31 Sanofi-Aventis Deutschland Gmbh Triazolopyridin-derivate als Inhibitoren von Lipasen und Phospholipasen
EP1976828B1 (en) 2005-12-29 2016-12-21 Celtaxsys, Inc. Diamine derivatives as inhibitors of leukotriene a4 hydrolase
FR2915198B1 (fr) * 2007-04-18 2009-12-18 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique.
FR2915199B1 (fr) 2007-04-18 2010-01-22 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique.
FR2915197B1 (fr) * 2007-04-18 2009-06-12 Sanofi Aventis Sa Derives de triazolopyridine-carboxamides, leur preparation et leur application therapeutique.
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
AR072707A1 (es) 2008-07-09 2010-09-15 Sanofi Aventis Compuestos heterociclicos, procesos para su preparacion, medicamentos que comprenden estos compuestos y el uso de los mismos
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AU2011261375B2 (en) 2010-06-04 2016-09-22 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
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