AR092270A1 - Sulfamoilarilamidas y su uso como medicamentos para el tratamiento de la hepatitis b - Google Patents
Sulfamoilarilamidas y su uso como medicamentos para el tratamiento de la hepatitis bInfo
- Publication number
- AR092270A1 AR092270A1 ARP130103057A ARP130103057A AR092270A1 AR 092270 A1 AR092270 A1 AR 092270A1 AR P130103057 A ARP130103057 A AR P130103057A AR P130103057 A ARP130103057 A AR P130103057A AR 092270 A1 AR092270 A1 AR 092270A1
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- AR
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- Prior art keywords
- alkyl
- independently selected
- group
- ring
- cfh2
- Prior art date
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
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- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
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- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
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- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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- 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
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- A61K31/341—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 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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- C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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Abstract
La presente también se relaciona con procesos para preparar dichos compuestos, composiciones farmacéuticas que los contienen y su uso, solos o en combinación con otros inhibidores del VHB, en una terapia contra el VHB. Reivindicación 1: Un compuesto de fórmula (1), o un estereoisómero o forma tautomérica del mismo, donde: B representa un anillo aromático monocíclico de 5 ó 6 miembros, que contiene opcionalmente uno o más heteroátomos seleccionados en forma independiente entre sí entre el grupo que consiste en O, S y N, donde dicho anillo aromático de 5 ó 6 miembros está opcionalmente sustituido con uno o más sustituyentes seleccionados en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, alquilo C₁₋₃, CN, CFH₂, CF₂H y CF₃; R¹ representa hidrógeno o C₁₋₃alquilo; R² representa alquilo C₁₋₆, alquenilo C₁₋₆, alquil C₁₋₆-R⁵, C(=O)-R⁵, CFH₂, CF₂H, CF₃, una unidad dihidroindenilo o tetrahidronaftalenilo opcionalmente sustituida con OH, o un anillo saturado de 3 - 7 miembros que contiene opcionalmente uno o más heteroátomos seleccionados en forma independiente entre sí entre el grupo que consiste en O, S y N, donde dicho anillo saturado de 3 - 7 miembros, alquil C₁₋₆-R⁵ o alquilo C₁₋₆ está opcionalmente sustituido con uno o más sustituyentes seleccionados en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, alquiloxi C₁₋₄, alquiloxi C₁₋₄carbonilo, oxo, C (=O)-alquilo C₁₋₃, alquilo C₁₋₄, OH, CN, CFH₂, CF₂H y CF₃; o R¹ y R² junto con el nitrógeno al cual están unidos forman un anillo bicíclico o en puente de 6 - 10 miembros o un anillo saturado de 5 - 7 miembros, donde dicha unidad bicíclica o en puente o anillo saturado contiene opcionalmente uno o más heteroátomos adicionales seleccionados en forma independiente entre sí entre el grupo que consiste en O, S y N, donde dicho anillo saturado de 5 - 7 miembros está opcionalmente sustituido con uno o más sustituyentes seleccionados en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, alquiloxi C₁₋₄, alquiloxi C₁₋₄carbonilo, oxo, C (=O)-alquilo C₁₋₃, alquilo C₁₋₄, OH, CN, CFH₂, CF₂H y CF₃; cada R⁴ se selecciona en forma independiente entre hidrógeno, halo, alquiloxi C₁₋₄, alquilo C₁₋₄, alquenilo C₁₋₄, OH, CN, CFH₂, CF₂H, CF₃, HCºC o un anillo saturado de 3 - 5 miembros que contiene opcionalmente uno o más heteroátomos seleccionados en forma independiente entre sí entre el grupo que consiste en O y N, donde dicho alquilo C₁₋₄ está opcionalmente sustituido con OH; R⁵ representa alquilo C₁₋₆, CFH₂, CF₂H, CF₃, fenilo, piridilo o un anillo saturado de 3 - 7 miembros que contiene opcionalmente uno o más heteroátomos seleccionados en forma independiente entre sí entre el grupo que consiste en O, S y N, donde dicho anillo saturado de 3 - 7 miembros está opcionalmente sustituido con uno o más sustituyentes seleccionados en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, alquiloxi C₁₋₄, alquiloxi C₁₋₄carbonilo, oxo, C(=O)-alquilo C₁₋₃, alquilo C₁₋₄, OH, CN, CFH₂, CF₂H y CF₃; o una sal farmacéuticamente aceptable o un solvato del mismo.
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