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AR092279A1 - Pirrol carboxamidas fluorometilo sustituidas - Google Patents

Pirrol carboxamidas fluorometilo sustituidas

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Publication number
AR092279A1
AR092279A1 ARP130103069A ARP130103069A AR092279A1 AR 092279 A1 AR092279 A1 AR 092279A1 AR P130103069 A ARP130103069 A AR P130103069A AR P130103069 A ARP130103069 A AR P130103069A AR 092279 A1 AR092279 A1 AR 092279A1
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AR
Argentina
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alkyl
mono
poly
substituted
unsubstituted
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ARP130103069A
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Gruenenthal Gmbh
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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]
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    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/323—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Bloqueadores de canales de calcio activados por voltaje, a composiciones farmacéuticas que contienen estos compuestos y al uso de estos compuestos para el tratamiento y/o profilaxis del dolor y otras enfermedades y/o trastornos. Reivindicación 1: Un compuesto de la fórmula general (1), caracterizado porque n representa 0, 1 ó 2; m representa 0 ó 1 con la condición que n ³ m; X es seleccionado del grupo que consiste de O, S, NH y N-alquilo C₁₋₆; R¹, R² y R³, son cada uno seleccionados independientemente uno de otro del grupo que consiste de H; F; Cl; Br; I; NO₂; CN; alquilo C₁₋₆; CF₃ CF₂H; CFH₂ CF₂Cl; CFCl₂; C(=O)-H; C(=O)-alquilo C₁₋₆; C(=O)-OH; C(=O)-O-alquilo C₁₋₆; C(=O)-N(H)(OH); C(=O)-NH₂; C(=O)N(H)(alquilo C₁₋₆); C(=O)-N(alquilo C₁₋₆)₂; C(=N-OH)-H; C=(N-OH)-alquilo C₁₋₆; C(=N-O-alquilo C₁₋₆)-H; C(=N-O-alquilo C₁₋₆)-alquilo C₁₋₆; OH; OCF₃ OCF₂H; OCFH₂ OCF₂Cl; OCFCl₂; O-alquilo C₁₋₆; O-C(=O)-alquilo C₁₋₆; O-C(=O)-O-alquilo C₁₋₆; O-(C=O)-N(H)(alquilo C₁₋₆); O-C(=O)N(alquilo C₁₋₆)₂; O-S(=O)₂-alquilo C₁₋₆; O-S(=O)₂-OH; O-S(=O)₂-O-alquilo C₁₋₆; O-S(=O)₂-NH₂; O-S(=O)₂-N(H)(alquilo C₁₋₆); O-S(=O)₂-N(alquilo C₁₋₆)₂; NH₂; N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)₂; N(H)-C(=O)-alquilo C₁₋₆; N(H)-C(=O)-O-alquilo C₁₋₆; N(H)-C(=O)-NH₂; N(H)-C(O)-N(H)(alquilo C₁₋₆); N(H)-C(=O)-N(alquilo C₁₋₆)₂; N(alquilo C₁₋₆)-C(=O)-alquilo C₁₋₆; N(alquilo C₁₋₆)-C(=O)-O-alquilo C₁₋₆; N(alquilo C₁₋₆)-C(=O)-NH₂; N(alquilo C₁₋₆)-C(=O)-N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)-C(=O)-N(alquilo C₁₋₆)₂; N(H)-S(=O)₂OH; N(H)-S(=O)₂-alquilo C₁₋₆; N(H)-S(=O)₂-O-alquilo C₁₋₆; N(H)-S(=O)₂-NH₂; N(H)-S(=O)₂-N(H)(alquilo C₁₋₆); N(H)-S(=O)₂N(alquilo C₁₋₆)₂; N(alquilo C₁₋₆)-S(=O)₂-OH; N(alquilo C₁₋₆)-S(=O)₂-alquilo C₁₋₆; N(alquilo C₁₋₆)-S(=O)₂-O-alquilo C₁₋₆; N(alquilo C₁₋₆)-S(=O)₂-NH₂N(alquilo C₁₋₆)-S(=O)₂-N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)-S(=O)₂-N(alquilo C₁₋₆)₂; SH; SCF₃ SCF₂H; SCFH₂ SCF₂Cl; SCFCl₂; S-alquilo C₁₋₆; S(=O)-alquilo C₁₋₆; S(=O)₂-alquilo C₁₋₆; S(=O)₂-OH; S(=O)₂-O-alquilo C₁₋₆; S(=O)₂-NH₂; S(=O)₂-N(H)(alquilo C₁₋₆); o S(=O)₂-N(alquilo C₁₋₆)₂, por medio del cual en cada caso alquilo C₁₋₆ puede ser ramificado o no ramificado; no sustituido o mono o poli-sustituido; un residuo cicloalifático C₃₋₆ o un residuo heterocicloalifático de 3 a 7 miembros, en cada caso no sustituido o mono o poli-sustituido; R⁴ representa CH₂F; CHF₂, o CF₃; R⁵ representa H, alquilo C₁₋₆, ramificado o no ramificado, no sustituido o mono- o poli- sustituido a residuo cicloalifático C₃₋₆ o un residuo heterocicloalifático de 3 a 7 miembros, en cada caso no sustituido o mono o poli-sustituido OH; O-alquilo C₁₋₆; NH₂; N(H)-alquilo C₁₋₆; N(-alquilo C₁₋₆)₂ o SO₂(-alquilo C₁₋₆), por medio del cual en cada caso alquilo C₁₋₆ puede ser ramificado o no ramificado; no sustituido o mono o poli-sustituido; R⁶, R⁷ y R⁸, son cada uno independientemente uno de otro seleccionados del grupo que consiste de H; F; Cl; Br; I; NO₂ CN; alquilo C₁₋₆; CF₃ CF₂H; CFH₂ CF₂Cl; CFCl₂; C(=O)-H; C(=O)-alquilo C₁₋₆; C(=O)-OH; C(=O)-O-alquilo C₁₋₆; C(=O)-N(H)(OH); C(=O)-NH₂; C(=O)-N(H)(alquilo C₁₋₆); C(=O)-N(alquilo C₁₋₆)₂; C(=N-OH)-H; C(=N-OH)-alquilo C₁₋₆; C(=N-O-alquilo C₁₋₆)-H; C(=N-O-alquilo C₁₋₆)-alquilo C₁₋₆; OH; OCF₃; OCF₂H; OCFH₂; OCF₂Cl; OCFCl₂; O-alquilo C₁₋₆; O-C(=O)-alquilo C₁₋₆; O-C(=O)-O-alquilo C₁₋₆; O-(C=O)-N(H)(alquilo C₁₋₆); O-C(=O)N(alquilo C₁₋₆)₂; O-S(=O)₂-alquilo C₁₋₆; O-S(=O)₂-OH; O-S(=O)₂-O-alquilo C₁₋₆; O-S(=O)₂-NH₂; O-S(=O)₂-N(H)(alquilo C₁₋₆); O-S(=O)₂-N(alquilo C₁₋₆)₂; NH₂; N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)₂; N(H)-C(=O)-alquilo C₁₋₆; N(H)-C(=O)-O-alquilo C₁₋₆; N(H)-C(=O)-NH₂; N(H)-C(=O)-N(H)(alquilo C₁₋₆); N(H)-C(=O)-N(alquilo C₁₋₆)₂; N(alquilo C₁₋₆)-C(=O)-alquilo C₁₋₆; N(alquilo C₁₋₆)-C(=O)-O-alquilo C₁₋₆; N(alquilo C₁₋₆)-C(=O)-NH₂; N(alquilo C₁₋₆)-C(=O)-N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)-C(=O)-N(alquilo C₁₋₆)₂; N(H)-S(=O)₂OH; N(H)-S(=O)₂-alquilo C₁₋₆; N(H)S(=O)₂-O-alquilo C₁₋₆; N(H)-S(=O)₂-NH₂; N(H)-S(=O)₂-N(H)(alquilo C₁₋₆); N(H)-S(=O)₂N(alquilo C₁₋₆)₂; N(alquilo C₁₋₆)-S(=O)₂-OH; N(alquilo C₁₋₆)-S(=O)₂-alquilo C₁₋₆; N(alquilo C₁₋₆)-S(=O)₂-O-alquilo C₁₋₆; N(alquilo C₁₋₆)-S(=O)₂-NH₂ N(alquilo C₁₋₆)-S(=O)₂-N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)-S(=O)₂-N(alquilo C₁₋₆)₂; SH; SCF₃ SCF₂H; SCFH₂ SCF₂Cl; SCFCl₂; S-alquilo C₁₋₆; S(O)-alquilo C₁₋₆; S(=O)₂-alquilo C₁₋₆; S(=O)₂-OH; S(=O)₂-O-alquilo C₁₋₆; S(=O)₂-NH₂; S(=O)₂-N(H)(alquilo C₁₋₆); o S(=O)₂- N(alquilo C₁₋₆)₂, por medio del cual en cada caso alquilo C₁₋₆ puede ser ramificado o no ramificado; no sustituido o mono- o poli-sustituido; un residuo cicloalifático C₃₋₆ o un residuo heterocicloalifático de 3 a 7 miembros, en cada caso no sustituido o mono o poli-sustituido; R⁹ representa H, un residuo alifático C₁₋₁₀, ramificado o no ramificado, no sustituido o mono- o poli-sustituido; un residuo cicloaIifático C₃₋₁₀ o un residuo heterocicloalifático de 3 a 10 miembros, en cada caso no sustituido o mono- o poli-sustituido y en cada caso opcionalmente unidos a través de un grupo alquileno C₁₋₈, ramificado o no ramificado, el cual a su vez puede ser no sustituido o mono o poli-sustituido; R¹⁰ representa H, un residuo alifático C₁₋₁₀, ramificado o no ramificado, no sustituido o mono o poli-sustituido, un residuo cicloalifático C₃₋₁₀, un residuo heterocicloalifático de 3 a 10 miembros o un residuo heteroarilo, en cada caso no sustituido o mono- o poli-sustituido y en cada caso opcionalmente unido a través de un grupo alquileno C₁₋₈, ramificado o no ramificado, el cual a su vez puede ser no sustituido o mono o poli-sustituido; o R⁹ y R¹⁰ junto con el átomo de nitrógeno que los contacta forman un residuo heterocicloalifático de 3 a 10 miembros, el cual puede ser no sustituido o mono o poli-sustituido; opcionalmente en la forma de un esteroisómero simple o una mezcla de esteroisómeros, en forma de compuesto libre y/o una sal fisiológicamente aceptable y/o un solvato fisiológicamente aceptable de los mismos.
ARP130103069A 2012-08-29 2013-08-29 Pirrol carboxamidas fluorometilo sustituidas AR092279A1 (es)

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EP (1) EP2906534B1 (es)
JP (1) JP6114392B2 (es)
KR (1) KR20150046321A (es)
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JP2016540821A (ja) * 2013-12-19 2016-12-28 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング フルオロメチル置換ピロールカルボキサミドｉｉｉ
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TW201718557A (zh) * 2015-10-08 2017-06-01 歌林達有限公司 經吡唑基取代之四氫吡喃基碸
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PE20150403A1 (es) 2015-04-16
SI2906534T1 (sl) 2017-03-31
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