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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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Publication number
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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AR
Argentina
Prior art keywords
alkyl
alkylene
cycloalkyl
aryl
amino
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ARP060104518A
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English (en)
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Sanofi Aventis
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Publication of AR058095A1 publication Critical patent/AR058095A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/04—Ortho-condensed systems
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005049954A DE102005049954A1 (de) 2005-10-19 2005-10-19 Triazolopyridin-derivate als Inhibitoren von Lipasen und Phospholipasen

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AR058095A1 true AR058095A1 (es) 2008-01-23

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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)
DO (1) DOP2006000227A (es)
EC (1) ECSP088376A (es)
HN (1) HN2006035237A (es)
IL (1) IL190715A0 (es)
MA (1) MA29857B1 (es)
MY (1) MY140514A (es)
NO (1) NO20082159L (es)
NZ (1) NZ567574A (es)
PE (1) PE20070820A1 (es)
RU (1) RU2008119435A (es)
TN (1) TNSN08178A1 (es)
TW (1) TW200800987A (es)
UY (1) UY29878A1 (es)
WO (1) WO2007045392A1 (es)
ZA (1) ZA200802369B (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
DK1976828T3 (en) 2005-12-29 2017-03-06 Celtaxsys Inc DIAMINE DERIVATIVES AS INhibitors of Leukotriene A4 HYDROLASE
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.
FR2915198B1 (fr) 2007-04-18 2009-12-18 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique.
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
UY31968A (es) 2008-07-09 2010-01-29 Sanofi Aventis Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos
EP2351744B1 (en) * 2008-10-17 2015-01-07 Shionogi & Co., Ltd. Acetic acid amide derivative having inhibitory activity on vascular endothelial lipase
AR075111A1 (es) * 2008-12-24 2011-03-09 Bial Portela & Ca Sa Derivados heterociclicos de diazoles y triazoles, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de trastornos del metabolismo y del sistema nervioso, entre otros.
KR20120123325A (ko) 2009-12-15 2012-11-08 시오노기세야쿠 가부시키가이샤 혈관 내피 리파아제 저해 활성을 갖는 옥사디아졸 유도체
NZ604035A (en) 2010-06-04 2015-02-27 Albany Molecular Res Inc Glycine transporter-1 inhibitors, methods of making them, and uses thereof
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
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JP6527851B2 (ja) 2013-03-12 2019-06-05 セルタクシス，インコーポレイテッド ロイコトリエンａ４加水分解酵素を阻害する方法
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