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ES2561105T3 - Derivado heterocíclico como inhibidor de prostaglandina E sintasa microsómica (mPGES) - Google Patents

Derivado heterocíclico como inhibidor de prostaglandina E sintasa microsómica (mPGES) Download PDF

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Publication number
ES2561105T3
ES2561105T3 ES12823510T ES12823510T ES2561105T3 ES 2561105 T3 ES2561105 T3 ES 2561105T3 ES 12823510 T ES12823510 T ES 12823510T ES 12823510 T ES12823510 T ES 12823510T ES 2561105 T3 ES2561105 T3 ES 2561105T3
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optionally substituted
alkyl
group
alkoxy
cycloalkyl
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Hironori Otsu
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Nippon Shinyaku Co Ltd
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Nippon Shinyaku Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/4164—1,3-Diazoles
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Abstract

Un derivado heterocíclico representado por la fórmula general [1]:**Fórmula** o su tautómero o una sal farmacéuticamente aceptable del mismo, en donde el anillo A es un grupo representado por las fórmulas generales [2], [3] o [4]:**Fórmula** en donde X1 es NH, N-alquilo u O; A1 es hidrógeno o alquilo; A2 es i) hidrógeno; ii) halógeno; iii) alquilo opcionalmente sustituido con de uno a tres grupos seleccionados del grupo que consiste en halógeno, amino, monolaquilamino, dialquilamino, carbamoilo, monoalquilaminocarbonilo, dialquilaminocarbonilo, un aminocarbonilo cíclico saturado, alcoxi, alcoxialcoxi y alquilcarboniloxi; iv) cicloalquilo opcionalmente sustituido con alquilo opcionalmente sustituido con de uno a tres halógenos; v) alcoxi; vi) un grupo heterociclo saturado opcionalmente sustituido con alquilo, alquiloxicarbonilo, alquilcarbonilo u oxo; vii) alquiltio; viii) alquilsulfonilo; ix) alquilsulfinilo; x) un grupo representado por la fórmula general [5]:**Fórmula** en donde R3 y R4 son el mismo grupo o diferente seleccionado de: a) hidrógeno; b) alquilo opcionalmente sustituido con un grupo seleccionado del grupo que consiste en monoalquilamino, dialquilamino, un amino cíclico saturado opcionalmente sustituido con alquilo, un grupo heterociclo saturado opcionalmente sustituido con alquilo, alcoxi, hidroxicarbonilo, hidroxilo, alquiloxicarbonilo, y alquiltio, o c) cicloalquilo; o xi) un amino cíclico saturado opcionalmente sustituido con alquilo, amino, monoalquilamino, dialquilamino, alcoxi o hidroxilo; R1 es fenilo, bencilo, naftilo, cicloalquilo, cicloalquilmetilo, heteroarilo, heteroarilmetilo, 1,2,3,4- tetrahidronaftalen-5-ilo, 1,2,3,4-tetrahidronaftalen-6-ilo, 2,3-dihidro-1H-inden-4-ilo, 2,3-dihidro-1H-inden-5-ilo, 1,2-dihidrociclobutabencen-3-ilo, 1,2-dihidrociclobutabencen-4-ilo o alquilo, en donde dicho fenilo, bencilo, cicloalquilo, cicloalquilmetilo, heteroarilo, y heteroarilmetilo está opcionalmente sustituido con de uno a tres grupos seleccionados del grupo que consiste en i) halógeno, ii) alquilo opcionalmente sustituido con de uno a tres grupos seleccionados del grupo que consiste en halógeno, hidroxi y fenilo, iii) alcoxi, iv) hidroxi, y v) ciano; R2 es fenilo o piridilo, en donde dicho fenilo y piridilo está opcionalmente sustituido con de uno a tres grupos seleccionados del grupo que consiste en i) halógeno, ii) alquilsulfonilo, iii) alcoxi opcionalmente sustituido con de uno a tres halógenos o alcoxi, iv) alquinilo opcionalmente sustituido con alcoxialquilo o cicloalquilo, y v) alquilo opcionalmente sustituido con de uno a tres grupos seleccionados del grupo que consiste en alcoxi, alcoxialcoxi, cicloalquilo, fenilo y halógeno.
ES12823510T 2011-08-18 2012-08-17 Derivado heterocíclico como inhibidor de prostaglandina E sintasa microsómica (mPGES) Active ES2561105T3 (es)

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