AR034116A2 - Derivados de piperazinas y piperidinas con efecto analgesico, composiciones farmaceuticas que los contienen, uso de los mismos para la fabricacion de un medicamento y un proceso para la preparacion de dichos compuestos - Google Patents

Derivados de piperazinas y piperidinas con efecto analgesico, composiciones farmaceuticas que los contienen, uso de los mismos para la fabricacion de un medicamento y un proceso para la preparacion de dichos compuestos

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Publication number
AR034116A2
AR034116A2 ARP010100517A ARP010100517A AR034116A2 AR 034116 A2 AR034116 A2 AR 034116A2 AR P010100517 A ARP010100517 A AR P010100517A AR P010100517 A ARP010100517 A AR P010100517A AR 034116 A2 AR034116 A2 AR 034116A2
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
hydrogen
independently
cycloalkyl
Prior art date
Application number
ARP010100517A
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English (en)
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Astra Pharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astra Pharma Inc filed Critical Astra Pharma Inc
Publication of AR034116A2 publication Critical patent/AR034116A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • 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
    • A61P25/04—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • 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
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • 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
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Derivados de piperazinas y piperidinas, que comprenden la fórmula general (1), en donde: G es un átomo de carbono o un átomo de nitrógeno; A es seleccionado de: (i) fenilo substituido por cualquiera de -COOH, -CONH2, -COOCH3, -CN, -NH2 ó -COCH3; (ii) naftilo, benzofuranilo, y quinolinilo; y (iii) un compuesto de fórmulas (2), (3), (4), (5) y (6), en donde el anillo fenilo de cada substituyente de A puede ser opcional e independientemente substituido por 1 ó 2 substituyentes seleccionados de hidrógeno, CH3, (CH2)oCF3, halógeno, CONR7R8, CO2R7, COR7, (CH2)oNR7R8, (CH2)oCH3(CH2)oSOR7, (CH2)oSO2R7 y (CH2)oSO2NR7R8, en donde o es 0, 1 ó 2, y R7 y R8 son como se definen a continuación; R1 es seleccionado de hidrógeno, un alquilo C1-6 ramificado o recto, alquenilo C1-6, -CO-(alquilo C1-6), (alquilo C1-6)-B, en donde B es como se define a continuación, cicloalquilo C3-8, (alquilo-cicloalquilo) C4-8 en donde alquilo es alquilo C1-2, y cicloalquilo es cicloalquilo C3-6, arilo C6-10, y heteroarilo que tiene de 5-10 átomos seleccionados de cualquiera de C, S, N, u O; y por lo cual el arilo C6-10, y el heteroarilo pueden ser opcionalmente substituidos por 1 ó 2 substituyentes seleccionados de hidrógeno, CH3, (CH2)oCF3, halógeno, CONR7R8, CO2R7, COR7, (CH2)oNR7R8, (CH2)oCH3(CH2)oSOR7, (CH2)oSO2R7 y (CH2)oSO2NR7R8, en donde o es 0, 1 ó 2, y R7 y R8 son como se definen a continuación; R7 y R8 son cada uno independientemente como se define para R1 anterior; R2 es seleccionado de hidrógeno, CH3, OR1, CO2R1, y CH2CO2R1, en donde R1 es como se define anteriormente; R9, R10, R11, R12, R13, R14, R15, R16, R17 y R18, es cada uno independientemente como se define para R1 anterior; B es una porción aromática substituida o no substituida, una hidroaromática C5-10 opcionalmente substituida, una heteroaromática o una heterohidroaromática, teniendo cada una desde 5 a 10 átomos seleccionados de cualquiera de C, S, N, y O, y cada una siendo opcional e independientemente substituida por 1 ó 2 substituyentes independientemente seleccionados de hidrógeno, CH3, CF3, halógeno, (CH2)pCONR7R8, (CH2)pNR7R8, (CH2)pCOR7, (CH2)pCO2R7, OR7, (CH2)pSOR7, (CH2)pSO2R7 y (CH2)pSO2NR7R8; en donde p es 0, 1, 2 ó 3 y en donde R7 y R8 son como se definen con anterioridad; R3, R4, R5 y R6 es, cada uno e independientemente seleccionado de R7, (CH2)pCONR7R(, (CH2)pNR7R(, (CH2)pCO2R7, (CH2)pPh, (CH2)p(p-OH Ph), (CH2)p-3-indolil, (CH2)pSR7, y (CH2)pOR7; en donde p es 0, 1, 2, 3 ó 4 y R7 y R8 son como se definen con anterioridad; así como también sales farmacéuticamente aceptables de los compuestos de la fórmula (1), isómeros, hidratos, isoformas y profármacos de los mismos; con la condición de que cuando A es un anillo fenilo substituido por un grupo -CN o por un grupo -NH2, B no puede ser un resto de fórmula (7) en donde Z1 es hidroxi y ésteres del mismo, hidroximetilo y ésteres del mismo, o amino, y carboxamidas y sulfonamidas. Composiciones farmacéuticas que los contienen, uso de los mismos para la fabricación de un medicamento para el tratamiento de danos espinales y un proceso para la preparación de dichos compuestos.
ARP010100517A 1995-12-22 2001-02-05 Derivados de piperazinas y piperidinas con efecto analgesico, composiciones farmaceuticas que los contienen, uso de los mismos para la fabricacion de un medicamento y un proceso para la preparacion de dichos compuestos AR034116A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE9504661A SE9504661D0 (sv) 1995-12-22 1995-12-22 New compounds

Publications (1)

Publication Number Publication Date
AR034116A2 true AR034116A2 (es) 2004-02-04

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ID=20400739

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP960105834A AR005420A1 (es) 1995-12-22 1996-12-20 Compuestos derivados de piperazinas y piperidinas con efecto analgésico, composiciones farmacéuticas que los contienen, uso de los mismos para la fabricación de un medicamento y un proceso para la preparación de dichos compuestos.
ARP010100517A AR034116A2 (es) 1995-12-22 2001-02-05 Derivados de piperazinas y piperidinas con efecto analgesico, composiciones farmaceuticas que los contienen, uso de los mismos para la fabricacion de un medicamento y un proceso para la preparacion de dichos compuestos

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ARP960105834A AR005420A1 (es) 1995-12-22 1996-12-20 Compuestos derivados de piperazinas y piperidinas con efecto analgésico, composiciones farmacéuticas que los contienen, uso de los mismos para la fabricación de un medicamento y un proceso para la preparación de dichos compuestos.

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US (3) US6130222A (es)
EP (2) EP1408037A1 (es)
JP (1) JP2000502679A (es)
KR (2) KR20050047534A (es)
CN (1) CN1119336C (es)
AR (2) AR005420A1 (es)
AU (1) AU715547B2 (es)
BR (1) BR9612204A (es)
CA (1) CA2239174C (es)
CZ (1) CZ296159B6 (es)
EE (1) EE04640B1 (es)
EG (1) EG25688A (es)
HU (1) HUP9901304A3 (es)
IL (1) IL124996A (es)
IS (1) IS1839B (es)
MY (1) MY115662A (es)
NO (1) NO310869B1 (es)
NZ (1) NZ324887A (es)
PL (1) PL193061B1 (es)
RU (2) RU2307833C2 (es)
SE (1) SE9504661D0 (es)
SK (1) SK282743B6 (es)
TR (1) TR199801180T2 (es)
TW (1) TW458971B (es)
UA (1) UA71538C2 (es)
WO (1) WO1997023466A1 (es)
ZA (1) ZA9610352B (es)

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