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AR105102A1 - Derivados bicíclicos, un proceso para su preparación y composiciones farmacéuticas que los contienen - Google Patents

Derivados bicíclicos, un proceso para su preparación y composiciones farmacéuticas que los contienen

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Publication number
AR105102A1
AR105102A1 ARP160101880A ARP160101880A AR105102A1 AR 105102 A1 AR105102 A1 AR 105102A1 AR P160101880 A ARP160101880 A AR P160101880A AR P160101880 A ARP160101880 A AR P160101880A AR 105102 A1 AR105102 A1 AR 105102A1
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Argentina
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group
alkyl
branched
linear
ring
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ARP160101880A
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English (en)
Inventor
Proszenyk Gnes
Ondi Levente
Sipos Szabolcs
Brooke Murray James
Edward Paul Davidson James
chen I
Jen - Geneste Olivier
Chanrion Maa
Kotschy Andrs
Szlvik Zoltn
Cskei Mrton
Blint Balzs
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Les Laboratoires Servier (Société Anonyme)
Vernalis R&D Ltd
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Publication of AR105102A1 publication Critical patent/AR105102A1/es

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    • 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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    • A61K31/4353—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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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

Medicamentos. Reivindicación 1: Compuesto de fórmula (1), en la que: A representa el grupo de fórmula (2), en la que 1 está unido al grupo W y 2 está unido al anillo fenilo, en la que: E representa un anillo furilo, tienilo o pirrolilo; X¹, X³, X⁴ y X⁵ independientemente uno de otro representan un átomo de carbono o un átomo de nitrógeno; X² representa un grupo C-R²¹ o un átomo de nitrógeno; y el anillo de línea punteada (del grupo de fórmula (2)) significa que el anillo es aromático; R¹ representa un átomo de halógeno, un grupo alquilo C₁₋₆ lineal o ramificado, un grupo alquenilo C₂₋₆ lineal o ramificado, un grupo alquinilo C₂₋₆ lineal o ramificado, un grupo polihaloalquilo C₁₋₆ lineal o ramificado, un grupo hidroxi, un grupo hidroxialquilo C₁₋₆, un grupo alcoxi C₁₋₆ lineal o ramificado, -S-alquilo C₁₋₆, un grupo ciano, un grupo nitro, -alquilo C₀₋₆-NR¹¹R¹¹, -O-alquilo C₁₋₆-NR¹¹R¹¹, -O-alquilo C₁₋₆-R¹², -C(O)-OR¹¹, -O-C(O)-R¹¹, -C(O)-NR¹¹R¹¹, -NR¹¹-C(O)-R¹¹, -NR¹¹-C(O)-OR¹¹, -alquilo C₁₋₆-NR¹¹-C(O)-R¹¹, -SO₂-NR¹¹R¹¹, -SO₂-alquilo C₁₋₆; R², R³, R⁴ y R⁵ independientemente uno de otro representan un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo C₁₋₆ lineal o ramificado, un grupo alquenilo C₂₋₆ lineal o ramificado, un grupo alquinilo C₂₋₆ lineal o ramificado, un polihaloalquilo C₁₋₆ lineal o ramificado, un grupo hidroxi, un grupo hidroxialquilo C₁₋₆, un grupo alcoxi C₁₋₆ lineal o ramificado, un grupo -S-alquilo C₁₋₆, un grupo ciano, un grupo nitro, -alquilo C₀₋₆-NR¹¹R¹¹, -O-alquilo C₁₋₆-NR¹¹R¹¹, -O-alquilo C₁₋₆-R¹², -C(O)-OR¹¹, -O-C(O)-R¹¹, -C(O)-NR¹¹R¹¹, -NR¹¹-C(O)-R¹¹, -NR¹¹-C(O)-OR¹¹, -alquilo C₁₋₆-NR¹¹-C(O)-R¹¹, SO₂-NR¹¹R¹¹, o -SO₂-alquilo C₁₋₆, o los sustituyentes de la pareja (R¹, R²) forman conjuntamente con los átomos de carbono a los que están unidos un anillo aromático o no aromático compuesto por de 5 a 7 miembros en el anillo, que puede contener de 1 a 3 heteroátomos seleccionados de oxigeno, azufre y nitrógeno, entendiéndose que el anillo resultante puede estar sustituido con de 1 a 2 grupos seleccionados de halógeno, alquilo C₁₋₆ lineal o ramificado, -alquilo C₀₋₆-NR¹¹R¹¹, -NR¹³R¹³, -alquilo C₀₋₆-Cy¹ u oxo; R⁶ y R⁷ independientemente uno de otro representan un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo C₁₋₆ lineal o ramificado, un grupo alquenilo C₂₋₆ lineal o ramificado, un grupo alquinilo C₂₋₆ lineal o ramificado, un polihaloalquilo C₁₋₆ lineal o ramificado, un grupo hidroxi, un grupo alcoxi C₁₋₆ lineal o ramificado, un grupo -S-alquilo C₁₋₆, un grupo ciano, un grupo nitro, -alquilo C₀₋₆-NR¹¹R¹¹, -O-Cy¹, -alquilo C₀₋₆-Cy¹, -alquenilo C₂₋₆-Cy¹, -alquinilo C₂₋₆-Cy¹, -O-alquilo C₁₋₆-R¹², -C(O)-OR¹¹, -O-C(O)-R¹¹, -C(O)-NR¹¹R¹¹, -NR¹¹-C(O)-R¹¹, -NR¹¹-C(O)-OR¹¹, -alquilo C₁₋₆-NR¹¹-C(O)-R¹¹, -SO₂-NR¹¹R¹¹, -SO₂-alquilo C₁₋₆, o los sustituyentes de la pareja (R⁶, R⁷), cuando se injertan en dos átomos de carbono adyacentes, forman conjuntamente con los átomos de carbono a los que están unidos un anillo aromático o no aromático compuesto por de 5 a 7 miembros en el anillo, que puede contener de 1 a 3 heteroátomos seleccionados de oxígeno, azufre y nitrógeno, entendiéndose que el anillo resultante puede estar sustituido con un grupo seleccionado de un grupo alquilo C₁₋₆ lineal o ramificado, -NR¹³R¹³ -alquilo C₀₋₆-Cy¹, o un oxo; W representa un grupo -CH₂-, un grupo -NH- o un átomo de oxígeno; R⁸ representa un átomo de hidrógeno, un grupo alquilo C₁₋₈ lineal o ramificado, un grupo -CHRᵃRᵇ, un grupo arilo, un grupo heteroarilo, un grupo arilalquilo C₁₋₆, o un grupo heteroarilalquilo C₁₋₆; R⁹ representa un átomo de hidrógeno, un grupo alquilo C₁₋₆ lineal o ramificado, un grupo alquenilo C₂₋₆ lineal o ramificado, un grupo alquinilo C₂₋₆ lineal o ramificado, -Cy², -alquilo C₁₋₆-Cy², -alquenilo C₂₋₆-Cy², -alquinilo C₂₋₆-Cy², -Cy²-Cy³, -alquinilo C₂₋₆-O-Cy², -Cy²-alquilo C₀₋₆-O-alquilo C₀₋₆-Cy³, un átomo de halógeno, un grupo ciano, -C(O)-R¹⁵, o -C(O)-NR¹⁵R¹⁵; R¹⁰ representa un átomo de hidrógeno, un grupo alquilo C₁₋₆ lineal o ramificado, un grupo alquenilo C₂₋₆ lineal o ramificado, un grupo alquinilo C₂₋₆ lineal o ramificado, un grupo arilalquilo C₁₋₆, un grupo cicloalquilalquilo C₁₋₆, un polihaloalquilo C₁₋₆ lineal o ramificado, -alquilo C₁₋₆-O-Cy⁴, o los sustituyentes de la pareja (R⁹, R¹⁰), cuando se injertan en dos átomos de carbono adyacentes, forman conjuntamente con los átomos de carbono a los que están unidos un anillo aromático o no aromático compuesto por de 5 a 7 miembros en el anillo, que puede contener de 1 a 3 heteroátomos seleccionados de oxígeno, azufre y nitrógeno; R¹¹ y R¹¹ independientemente uno de otro representan un átomo de hidrógeno, un grupo alquilo C₁₋₆ lineal o ramificado, o los sustituyentes de la pareja (R¹¹, R¹¹) forman conjuntamente con el átomo de nitrógeno al que están unidos un anillo aromático o no aromático compuesto por de 5 a 7 miembros en el anillo, que puede contener además del átomo de nitrógeno de 1 a 3 heteroátomos seleccionados de oxígeno, azufre y nitrógeno, entendiéndose que el nitrógeno en cuestión puede estar sustituido con un grupo que representa un átomo de hidrógeno, o un grupo alquilo C₁₋₆ lineal o ramificado; R¹² representa -Cy⁵, -Cy⁵-alquilo C₀₋₆-O-alquilo C₀₋₆-Cy⁶, -Cy⁵-alquilo C₀₋₆-Cy⁶, -Cy⁵-alquilo C₀₋₆-NR¹¹-alquilo C₀₋₆-Cy⁶, -Cy⁵-Cy⁶-O-alquilo C₀₋₆-Cy⁷, -C(O)-NR¹¹R¹¹, -NR¹¹R¹¹, -OR¹¹, -NR¹¹-C(O)-R¹¹, -O-alquilo C₁₋₆-OR¹¹, -SO₂-R¹¹, -C(O)-OR¹¹, o -NH-C(O)-NH-R¹¹; R¹³, R¹³, R¹⁵ y R¹⁵ independientemente uno de otro representan un átomo de hidrógeno, o un grupo alquilo C₁₋₆ lineal o ramificado sustituido opcionalmente; R¹⁴ representa un átomo de hidrógeno, un grupo hidroxi, o un grupo hidroxialquilo C₁₋₆; R²¹ representa un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo C₁₋₆ lineal o ramificado, o un grupo ciano; Rᵃ representa un átomo de hidrógeno o un grupo alquilo C₁₋₆ lineal o ramificado; Rᵇ representa un grupo -O-C(O)-O-Rᶜ, un grupo -O-C(O)-NRᶜRᶜ, o un grupo -O-P(O)(ORᶜ)₂; Rᶜ y Rᶜ independientemente uno de otro representan un átomo de hidrógeno, un grupo alquilo C₁₋₈ lineal o ramificado, un grupo cicloalquilo, un grupo alcoxi C₁₋₆alquilo C₁₋₆, un grupo alcoxi C₁₋₆carbonilalquilo C₁₋₆, o los sustituyentes de la pareja (Rᶜ, Rᶜ) forman conjuntamente con el átomo de nitrógeno al que están unidos un anillo no aromático compuesto por de 5 a 7 miembros en el anillo, que puede contener además del átomo de nitrógeno de 1 a 3 heteroátomos seleccionados de oxígeno y nitrógeno, entendiéndose que el nitrógeno en cuestión puede estar sustituido con un grupo que representa un grupo alquilo C₁₋₆ lineal o ramificado; Cy¹, Cy², Cy³, Cy⁴, Cy⁵, Cy⁶ y Cy⁷ independientemente uno de otro, representan un grupo cicloalquilo, un grupo heterocicloalquilo, un grupo arilo, o un grupo heteroarilo; n es un número entero igual a 0 ó 1; entendiéndose que: arilo significa un grupo fenilo, naftilo, bifenilo, indanilo o indenilo; heteroarilo significa cualquier grupo mono- o bi-cíclico compuesto por de 5 a 10 miembros en el anillo, que tiene al menos un resto aromático y que contiene de 1 a 3 heteroátomos seleccionados de oxígeno, azufre y nitrógeno; cicloalquilo significa cualquier grupo carbocíclico no aromático mono- o bi-cíclico que contiene de 3 a 10 miembros en el anillo; heterocicloalquilo significa cualquier grupo carbocíclico no aromático mono- o bi-cíclico que contiene de 3 a 10 miembros en el anillo, y que contiene de 1 a 3 heteroátomos seleccionados de oxígeno, azufre y nitrógeno, que puede incluir sistemas de anillos fusionados, con puente o espiro, siendo posible para los grupos arilo, heteroarilo, cicloalquilo y heterocicloalquilo así definidos y los grupos alquilo, alquenilo, alquinilo, alcoxi, estar sustituidos con de 1 a 4 grupos seleccionados de alquilo C₁₋₆ lineal o ramificado sustituido opcionalmente, alquenilo C₂₋₆ lineal o ramificado sustituido opcionalmente, alquinilo C₂₋₆ lineal o ramificado sustituido opcionalmente, alcoxi C₁₋₆ lineal o ramificado sustituido opcionalmente, alquilo C₁₋₆-S- sustituido opcionalmente, hidroxi, oxo (o N-óxido cuando sea apropiado), nitro, ciano, -C(O)-OR, -O-C(O)-R, -C(O)-NRR, -O-C(O)-NRR, -NRR, -(C=NR)-OR, -O-P(O)(OR)₂, -O-P(O)(O⁻M⁺)₂, polihaloalquilo C₁₋₆ lineal o ramificado, trifluorometoxi, halógeno, o una aldohexosa de fórmula (3) ó (4) en la que cada R es independiente; entendiéndose que R y R independientemente uno de otro representan un átomo de hidrógeno o un grupo alquilo C₁₋₆ lineal o ramificado sustituido opcionalmente; y M⁺ representa un catión monovalente farmacéuticamente aceptable; con la condición de que el compuesto de fórmula (5) no puede representar un compuesto de fórmula (6); sus enantiómeros, diastereoisómeros y atropisómeros, y sales de adición de estos con un ácido o base farmacéuticamente aceptable.
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