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AR075071A1 - COMPUESTOS DERIVADOS DE SULFONAMIDAS , USO DE LOS MISMOS PARA LA PREPARACIoN DE MEDICAMENTOS , COMPOSICIONES FARMACÉUTICAS Y PROCESO DE PREPARACIoN DE LOS MISMOS - Google Patents

COMPUESTOS DERIVADOS DE SULFONAMIDAS , USO DE LOS MISMOS PARA LA PREPARACIoN DE MEDICAMENTOS , COMPOSICIONES FARMACÉUTICAS Y PROCESO DE PREPARACIoN DE LOS MISMOS

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Publication number
AR075071A1
AR075071A1 ARP090102946A ARP090102946A AR075071A1 AR 075071 A1 AR075071 A1 AR 075071A1 AR P090102946 A ARP090102946 A AR P090102946A AR P090102946 A ARP090102946 A AR P090102946A AR 075071 A1 AR075071 A1 AR 075071A1
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Argentina
Prior art keywords
carbon atoms
optionally substituted
groups
alkyl
atoms
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ARP090102946A
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Novartis Ag
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/52—Sulfur atoms
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C311/48—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 having nitrogen atoms of sulfonamide groups further bound to another hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-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
    • C07D307/10—Heterocyclic compounds containing five-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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/14—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/40—Radicals substituted by oxygen atoms
    • C07D307/42—Singly bound oxygen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
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    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Furan Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula 1: o solvatos, hidratos o sales farmacéuticamente aceptables del mismo, en donde: R1 es H, un grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, un grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, (alquilo de 1 a 4 átomos de carbono)-grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, (alquilo de 1 a 4 átomos de carbono)-grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno, grupos CN u OH, alcoxilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno o grupos OH, o un grupo éter que contiene de 2 a 10 átomos de carbono y de 1 a 3 átomos de oxígeno, en donde el grupo éter está opcionalmente sustituido por uno o más sustituyentes, cada uno independientemente seleccionado a partir de OH, halogeno, un grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, y un grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z; R2 es un grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, un grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, (alquilo de 1 a 4 átomos de carbono)-grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, (alquilo de 1 a 4 átomos de carbono)-grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno, grupos CN u OH, alcoxilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno o grupos OH, o un grupo éter que contiene de 2 a 10 átomos de carbono y de 1 a 3 átomos de oxígeno, en donde el grupo éter está opcionalmente sustituido por uno o más sustituyentes, cada uno independientemente seleccionado a partir de OH, halogeno, un grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, y un grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z; o R1 y R2 junto con el átomo de carbono con el que están unidos, forman un grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, o un grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z; R3 es hidrogeno, halogeno o ciano; R4 es H, alquilo de 1 a 8 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono, cicloalquenilo de 5 a 8 átomos de carbono o (alquilo de 1 a 4 átomos de carbono)-R6, en donde los grupos alquilo están cada uno opcionalmente sustituidos por uno o más átomos de halogeno; R5 es alquilo de 1 a 8 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono, cicloalquenilo de 5 a 8 átomos de carbono, (alquilo de 1 a 4 átomos de carbono) cicloalquilo de 3 a 8 átomos de carbono o (alquilo de 1 a 4 átomos de carbono)-cicloalquenilo de 5 a 8 átomos de carbono, en donde los grupos alquilo están cada uno opcionalmente sustituidos por uno o más átomos de halogeno: o R4 y R5, junto con los átomos de nitrogeno y oxígeno con los que están unidos, forman un grupo heterocíclico de 5 a 10 miembros opcionalmente sustituido por uno o más grupos Z; R6 se selecciona a partir de un grupo carbocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, un grupo heterocíclico de 3 a 10 miembros opcionalmente sustituido por uno o más grupos Z, NR7R9, NR7(SO2)R9, (SO2)NR7R8, (SO2)R9, NR7C(O)R9, C(O)NR7R9, NR7C(O)NR8R9, NR7C(O)OR9, C(O)OR7, OC(O)R9, OC(O)NR7, C(O)R9, SR7, CN y NO2; R7 y R8 se seleccionan cada uno independientemente a partir de H, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 10 átomos de carbono, cicloalquenilo de 5 a 10 átomos de carbono y -(alquileno de 1 a 3 átomos de carbono)-cicloalquilo de 3 a 10 átomos de carbono; R9 se selecciona a partir de H, alquilo de 1 a 6 átomos de carbono, -(alquileno de 1 a 3 átomos de carbono)-cicloalquilo de 3 a 10 átomos de carbono, un grupo carbocíclico de 3 a 10 miembros, y un grupo heterocíclico de 3 a 10 miembros, en donde cada uno de los grupos alquilo y sistemas de anillos está opcionalmente sustituido por OH, halogeno, alquilo de 1 a 3 átomos de carbono, y alcoxilo de 1 a 3 átomos de carbono; X es CR14 o N; Z se selecciona independientemente a partir de OH; un grupo carbocíclico de 3 a 10 miembros: un grupo heterocíclico de 3 a 10 miembros; bencilo; alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno, grupos CN u OH; alcoxilo de 1 a 6 átomos de carbono opcionalmente sustituido por uno o más átomos de halogeno, grupos CN u OH; -Oarilo; -Obencilo; -O(CH2)aC(O)E; NR10(SO2)R12 (SO2)NR10R11; (SO2)R12; NR10C(O)R12; C(O)NR10R12; NR10C(O)NR11R12; NR10C(O)OR12; NR10R12; C(O)OR10; OC(O)R12; OC(O)NR10; C(O)R12; SR12; CN; NO2 y halogeno; o en donde hay dos o más sustituyentes Z, dos sustituyentes Z junto con los átomos con los que están unidos opcionalmente forman un sustituyente carbocíclico de 5 a 7 miembros o heterocíclico de 4 a 7 miembros fusionado con el sistema de anillos; a es 0, 1, 2, 3 o 4, en donde el grupo alquileno está opcionalmente sustituido por OH o NH, cuando a es 1, 2, 3 o 4; E es NR10R12 u OR12; cada R10 y R11 se selecciona independientemente a partir de H, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 10 átomos de carbono, cicloalquenilo de 5 a 10 átomos de carbono y -(alquileno de 1 a 3 átomos de carbono)-cicloalquilo de 3 a 10 átomos de carbono; cada R12 se selecciona a partir de H, alquilo de 1 a 6 átomos de carbono, -(alquileno de 1 a 3 átomos de carbono)-cicloalquilo de 3 a 10 átomos de carbono, un grupo carbocíclico de 3 a 10 miembros, y un grupo heterocíclico de 3 a 10 miembros, en donde cada uno de los sistemas de anillos está opcionalmente sustituido por OH, halogeno, alquilo de 1 a 3 átomos de carbono, y alcoxilo de 1 a 3 átomos de carbono; y R14 es H o alquilo de 1 a 6 átomos de carbono. Reivindicacion 10: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 8, en la fabricacion de un medicamento para el tratamiento de condiciones o enfermedades inflamatorias o alérgicas. Reivindicacion 12: Una composicion farmacéutica, la cual comprende un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 8, junto con un vehiculo o excipiente farmacéuticamente aceptable. Reivindicacion 14: Un proceso para la preparacion de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 8, cuyo proceso comprende hacer reaccionar un compuesto de la formula 2: en donde R3, R4 y R5 son como se definen en la reivindicacion 1, con un compuesto de la formula 3: en donde X, R1 y R2 son como se definen en la reivindicacion 1; aislar el producto.
ARP090102946A 2008-08-04 2009-07-31 COMPUESTOS DERIVADOS DE SULFONAMIDAS , USO DE LOS MISMOS PARA LA PREPARACIoN DE MEDICAMENTOS , COMPOSICIONES FARMACÉUTICAS Y PROCESO DE PREPARACIoN DE LOS MISMOS AR075071A1 (es)

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