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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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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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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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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