AR077513A2 - Derivados de benceno sustituidos por glucopiranosilo, medicamentos que contienen esos compuestos, su aplicacion y procedimiento para su preparacion - Google Patents

Derivados de benceno sustituidos por glucopiranosilo, medicamentos que contienen esos compuestos, su aplicacion y procedimiento para su preparacion

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AR077513A2
AR077513A2 ARP100102779A ARP100102779A AR077513A2 AR 077513 A2 AR077513 A2 AR 077513A2 AR P100102779 A ARP100102779 A AR P100102779A AR P100102779 A ARP100102779 A AR P100102779A AR 077513 A2 AR077513 A2 AR 077513A2
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Argentina
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alkyl
carbonyl
group
substituted
cycloalkyl
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ARP100102779A
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English (en)
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Leo Thomas
Peter Eickelmann
Edward Leon Barsoumian
Matthias Eckhardt
Frank Himmelsbach
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Boehringer Ingelheim Int
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Priority claimed from DE102004012676A external-priority patent/DE102004012676A1/de
Priority claimed from DE102004040168A external-priority patent/DE102004040168A1/de
Priority claimed from DE102004061145A external-priority patent/DE102004061145A1/de
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR077513A2 publication Critical patent/AR077513A2/es

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    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings

Abstract

Derivados de benceno sustituidos por glucopiranosilo de la formula general (1) en la que R1 esta seleccionado de entre los significados del grupo A y si R3 está seleccionado de entre los significados del grupo B, R1 puede adicionalmente estar seleccionado de entre los significados hidrogeno, fluor, cloro, bromo, yodo, alquilo-C1-4, alquenilo-C2-4alquilo-C1-4, alquinilo-C2-4-alquilo-C1-4, alquenilo-C2-4-alcoxi-C1-4, alquinilo-C2-4alcoxi-C1-4, cicloalquilo-C3-7-alquilo-C1-4, cicloalquenilo-C5-7-alquilo-C1-4, un grupo metilo sustituido por 1 a 3 átomos de fluor, un grupo etilo sustituido por 1 a 5 átomos de fluor, alcoxi-C1-4, un grupo metoxi sustituido por 1 a 3 átomos de fluor, un grupo etoxi sustituido por 1 a 5 átomos de fluor, un grupo alquilo-C1-4, sustituido por un grupo hidroxi- o alcoxi-C1-3 , un grupo alcoxi-C2-4 sustituido por un grupo hidroxi o alcoxi-C1-3, cicloalquil-C3-6-alcoxi-C1-3 o hidroxi, pudiendo en los anillos de cicloalquilo y cicloalquenilo mencionados en lo que antecede, estar sustituidos uno o dos grupos metilo, independientemente el uno del otro, por O o CO, y R2 puede ser hidrogeno, fluor, cloro, bromo, hidroxi, alquilo-C1-4, alcoxi-C1-4, ciano o nitro, pudiendo el grupo alquilo o alcoxi estar sustituido una o varias veces por fluor, y R3 está seleccionado de entre los significados del Grupo B y si R1 está seleccionado de entre los significados del Grupo A, R3 puede estar seleccionado adicionalmente de entre los significados hidrogeno, fluor, cloro, bromo, yodo, alquilo-C1-6, alquenilo-C2-4-alquilo-C1-4, alquinilo-C2-4 -alquilo-C1-4, alquenilo-C2-4-alcoxi-C1-4, alquinilo-C2-4-alcoxi-C1-4, cicloalquilo-C3-7, cicloalquenilo-C5-7, cicloalquilo-C3-7alquilo-C1-4, cicloalquenilo-C5-7-alquilo-C1-4, cicloalquiliden-C3-6-metilo, hidroxi, alcoxi-C1-6, cicloalquilo-C3-6-alcoxi-C1-3, arilo, arilalquilo-C1-3, heteroarilo, heteroarilalquilo-C1-3, ariloxi, arilalquil-C1-3-oxi, un grupo metilo o metoxi sustituido por 1 a 3 átomos de fluor, un grupo alquilo-C2-4 o alcoxi-C2-4 sustituido por 1 a 5 átomos de fluor, un grupo alquilo-C1-4 sustituido por un grupo ciano, un grupo alquilo-C1-4 sustituido por un grupo hidroxi o alquil-C1-3-oxi, ciano, carboxi, alcoxi-C1-3-carbonilo, aminocarbonilo, (alquil-C1-3-amino)carbonilo, diamino(alquil-C1-3)carbonilo, pirrolidin-1-il-carbonilo, piperidin-1-ilcarbonilo, morfolin-4-il-carbonilo, piperazin-1-il-carbonilo, 4-(alquil-C1-3)-piperazin-1-il-carbonilo, (alquil-C1-4)-carbonilamino, alquil-C1-4-sulfonilamino, alquil-C1-4-sulfanilo, alquil-C1-4-sulfinilo, alquil-C1-4-sulfonilo, arilsulfonilamino, arilalquil-C1-3-sulfonilamino o arilsulfonilo, R4, R5 independientemente el uno del otro, hidrogeno, fluor, cloro, bromo, yodo, ciano, nitro, alquilo-C1-3, alcoxi-C1-3, metilo o metoxi sustituido por 1 a 3 átomos de fluor, A significa alquin-C2-6-1-ilo, alquen-C2-6-1-ilo, cicloalquilo-C3-7, cicloalquenilo-C5-7, arilo, heteroarilo, alquil-C1-4-carbonilo, arilcarbonilo, heteroarilcarbonilo, aminocarbonilo, alquil-C1-4-aminocarbonilo, di-amino(alquil-C1-3)carbonilo, pirrolidin-1-ilcarbonilo, piperidin-1-il-carbonilo, morfolin-4-il-carbonilo, piperazin-1-il-carbonilo, 4-(alquil-C1-4)piperazin-1-il-carbonilo, arilamino-carbonilo, heteroarilaminocarbonilo, alcoxi-C1-4-carbonilo, arilalcoxi-C1-3-alcoxicarbonilo, heteroarilalcoxi-C1-3-carbonilo, amino, alquil-C1-4-amino, di-(alquil-C1-3)amino, pirrolidin-1-ilo, pirrolidin-2-on-1-ilo, piperidin-1-ilo, piperidin-2-on-1-ilo, morfolin-4-ilo, morfolin-3-on-4-ilo, piperazin-1-ilo, 4-(alquil-C1-3)-piperazin-1-ilo, alquil-C1-4-carbonilamino, arilcarbonilamino, heteroarilcarbonilamino, cicloalquil-C3-7-oxi, cicloalquenil-C5-7-oxi, ariloxi, heteroariloxi, alquil-C1-4-sulfinilo, alquil-C1-4-sulfonilo, cicloalquil-C3-7-sulfanilo, cicloalquil-C3-7-sulfinilo, cicloalquil-C3-7-sulfonilo, cicloalquenil-C5-7-sulfanilo, cicloalquenil-C5-7-sulfinilo, cicloalquenil-C5-7-sulfonilo, arilsulfanilo, arilsulfinilo, arilsulfonilo, heteroarilsulfanilo, heteroarilsulfinilo, heteroarilsulfonilo, ciano o nitro, pudiendo los grupos alquinilo y alquenilo mencionados en lo que antecede, estar sustituidos una o varias veces por fluor o cloro, y pudiendo los grupos alquinilo y alquenilo mencionados en lo que antecede, estar sustituidos una o dos veces por restos L1 iguales o diversos, y pudiendo los anillos de cicloalquilo y cicloalquenilo mencionados en lo que antecede, estar sustituidos una o dos veces, independientemente el uno del otro, por sustituyentes seleccionados de entre fluor y alquilo-C1-3, y pudiendo en los anillos de cicloalquilo y alquenilo mencionados en lo que antecede, estar sustituidos uno o dos grupos metileno una o dos veces, independientemente el uno del otro, por O, S, CO, SO, SO2 o NRN, B significa tri-(alquil-C1-4)silil-alquil-C1-6, alquin-C2-6-1-ilo, alquenC2-6-1-ilo, amino, alquil-C1-3-amino, di-(alquil-C1-3)amino, pirrolidin-1-ilo, pirrolidin-2-on-1-ilo, piperidin-1-ilo, piperidin-2-on-1-ilo, morfolin-4-ilo, morfolin-3-on-4-ilo, piperazin-1-ilo, 4- (alquil-C1-3)piperazin-1-ilo, arilcarbonilamino, heteroarilcarbonilamino, nitro, cicloalquil-C3-10-oxi, cicloalquenil-C5-10-oxi, cicloalquil-C3-10-sulfanilo, cicloalquil-C3-10-sulfinilo, cicloalquil-C3-10-sulfonilo, cicloalquenil-C5-10-sulfanilo, cicloalquenil-C5-10-sulfinilo, cicloalquenil-C5-10-sulfonilo, arilsulfanilo, arilsulfinilo, heteroarilsulfanilo o heteroarilsulfinilo, pudiendo los grupos alquinilo y alquenilo mencionados en lo que antecede estar sustituidos una o varias veces por fluor o cloro, y pudiendo los grupos alquinilo y alquenilo mencionados en lo que antecede estar sustituidos una o dos veces por restos L1 iguales o diversos; pudiendo los anillos de cicloalquilo y cicloalquenilo mencionados en lo que antecede estar sustituidos por fluor o cloro, independientemente el uno del otro, una o dos veces por sustituyentes seleccionados de entre fluor y alquilo-C1-3, y pudiendo en los anillos de cicloalquilo y cicloalquenilo mencionados en lo que antecede, uno o dos grupos de metileno estar sustituidos, independientemente el uno del otro, por O, S, CO, SO, SO2 o NRN, RN H, alquilo-C1-4, alquil-C1-4-carbonilo o alquil-C1-4-sulfonilo, L1 independientemente el uno del otro, seleccionado de entre el grupo consistente en hidroxi, ciano, nitro, cicloalquilo-C3-7, arilo, heteroarilo, alquil-C1-4-carbonilo, arilcarbonilo, heteroarilocarbonilo, aminocarbonilo, alquil-C1-4-aminocarbonilo-, di-amino(alquil-C1-3)carbonilo, pirrolidin-1-il-carbonilo, piperidin-1-il-carbonilo, morfolin-4-il-carbonilo, arilaminocarbonilo, heteroarilaminocarbonilo, alcoxi-C1-4-carbonilo, arilalcoxi-C1-3-carbonilo, heteroarilalcoxi-C1-3-carbonilo, alquil-C1-4-oxi, ariloxi, heteroariloxi, alquil-C1-4-sulfanilo, arilsulfanilo, heteroarilsulfanilo, alquil-C1-4-sulfinilo, arilsulfinilo, heteroarilsulfinilo, alquil-C1-4-sulfonilo, arilsulfonilo y heteroarilsulfonilo; y L2 independientemente el uno del otro, seleccionado de entre el grupo consistente en fluor, cloro, bromo, yodo, alquilo-C1-3, difluorometilo, trifluorometilo, alcoxi-C1-3, difluorometoxi, trifluorometoxi y ciano; y R6, R7a, R7b, R7c poseen, independientemente el uno del otro, un significado seleccionado de entre el grupo hidrogeno, (alquil-C1-18)carbonilo, (alquil-C1-18)oxicarbonilo, arilcarbonilo y aril-(alquil-C1-3)-carbonilo, debiendo entenderse por los grupos arilo mencionados en la definicion de los restos nombrados en lo que antecede, grupos fenilo o naftilo, los cuales, independientemente el uno del otro, pueden estar sustituidos una o dos veces por restos L2 iguales o diversos; y debiendo entenderse por los grupos heteroarilo mencionados en la definicion de los restos nombrados en lo que antecede, un grupo pirrolilo, furanilo, tienilo, piridilo, indolilo, benzofuranilo, benzotiofenilo, quinolinilo, isoquinolinilo o tetrazolilo, o bien un grupo pirrolilo, furanilo, tienilo o piridilo, en el que uno o dos grupos metino están reemplazados por átomos de nitrogeno, o bien un grupo indolilo, benzofuranilo, benzotiofenilo, quilnolinilo o isoquinolinilo, en el que uno a tres grupos metino están reemplazados por átomos de nitrogeno, pudiendo los grupos heteroarilo mencionados en lo que antecede, estar sustituidos, independientemente el uno del otro, una o dos veces por restos L2 iguales o diversos; pudiendo, en cuanto no se indicare algo distinto, los grupos alquilo mencionados en lo que antecede, ser de cadena recta o ramificados, sus tautomeros, sus estereoisomeros, sus mezclas y sus sales. Los compuestos conformes a la invencion son apropiados para el tratamiento de enfermedades metabolicas. Reivindicacion 1: Derivados de benceno sustituidos por glucopiranosilo de la formula general (1) caracterizados porque R1 es etinilo, prop-1-in-1-ilo, but-1-in-1-ilo, ciano, ciclopropiloxi, ciclobutiloxi, ciclopentiloxi o ciclohexiloxi; y R2 es hidrogeno; y R3 está seleccionado de entre hidrogeno, fluor, cloro, metilo, etilo, isopropilo, ter-butilo, etinilo, 1-propinilo, trimetilsililetilo, difluorometilo, trifluorometilo, ciclopropilo, ciclobutilo, ciclopentilo, metoxi, etoxi, isopropoxi, ciclopentiloxi, difluorometoxi, trifluorometoxi, pentafluoretoxi, tetrahidrofuran-3-iloxi, tetrahidrofuran-2-on-3-iloxi, metilsulfanilo, etilsulfanilo, isopropilsulfanilo y ciclopropildenemetilo; y R4 y R5 significa hidrogeno; y R6, R7a, R7b, R7c significan hidrogeno.
ARP100102779A 2004-03-16 2010-07-30 Derivados de benceno sustituidos por glucopiranosilo, medicamentos que contienen esos compuestos, su aplicacion y procedimiento para su preparacion AR077513A2 (es)

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