AR037032A1 - Benzoimidazoles - Google Patents

Benzoimidazoles

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Publication number
AR037032A1
AR037032A1 ARP020104061A ARP020104061A AR037032A1 AR 037032 A1 AR037032 A1 AR 037032A1 AR P020104061 A ARP020104061 A AR P020104061A AR P020104061 A ARP020104061 A AR P020104061A AR 037032 A1 AR037032 A1 AR 037032A1
Authority
AR
Argentina
Prior art keywords
ny1y2
alkyl
heteroaryl
aryl
radicals
Prior art date
Application number
ARP020104061A
Other languages
English (en)
Original Assignee
Aventis 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
Priority claimed from FR0113868A external-priority patent/FR2831537B1/fr
Priority claimed from GB0206895A external-priority patent/GB0206895D0/en
Priority claimed from GB0206893A external-priority patent/GB0206893D0/en
Application filed by Aventis Pharma Inc filed Critical Aventis Pharma Inc
Publication of AR037032A1 publication Critical patent/AR037032A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)

Abstract

Reivindicación 1: Una composición farmacéutica que comprende un compuesto de fórmula general (1) en la cual: X representa C-R2 y W, Y y Z, que pueden ser idénticos o diferentes, representa CH ó CR3; ó W representa CH, X representa N, Y representa CH ó CR3, y Z representa CH ó CR3; ó W representa N, X representa CH ó CR2, Y representa CH y CR3, y Z representa CH ó CR3; ó W representa N, X representa CH ó CR2, Y representa N y Z es CH ó CR3; ó W representa N, X representa CH ó CR2, Y representa CH ó CR3, y Z representa N; ó W representa N, X representa N, Y representa CH ó CR3, y Z representa CH ó CR3; A5 representa H ó alquilo; R1 representa arilo o heteroarilo, cada uno sustituido en forma opcional por uno o más grupos seleccionados de carboxi, ciano, halo, haloalquilo, hidroxi, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -OS(O)nR4, -S(O)nR4, -S(O)nNY1Y2 y -S(O)nOR4; R2 y R3 son tales que: R2 y R3, que pueden ser idénticos o diferentes, representa H, carboxi, ciano, halo, haloalquilo, hidroxi, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(O)nR4, -S(O)nNY1Y2 ó -S(O)nOR4; ó R2 representa H, carboxi, ciano, halo, haloalquilo, hidroxi, nitro, R4, -C(=O)R4, -C(=O)NY1Y2, -C(=O)OR4, -NY1Y2, -N(R6)C(=O)R4, -N(R6)C(=O)NY1Y2, -N(R6)C(=O)OR4, -N(R6)SO2R4, -N(R6)SO2NY1Y2, -OR4, -OCF2H, -OCF3, -OC(=O)R4, -OC(=O)NY1Y2, -S(=O)nR4, -S(O)nNY1Y2 ó -S(O)nOR4 y R3 representa alquilo, haloalquilo, halógeno y OR6; ó los grupos R2 y R3 en los átomos de carbono adyacentes pueden forman un anillo con base de carbono de 5 a 6 elementos que contiene uno o más heteroátomos, que pueden ser idénticos o diferentes, elegidos de O, N y S, y que pueden estar sustituidos en forma opcional por alquilo; R4 es alquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo ó heteroarilo, cada uno sustituido en forma opcional con uno o más sustituyentes seleccionados de alquilo, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, halo, hidroxi, hidroxialquilo, -C(=O)NY3Y4, -C(=O)OR6, -N(R6)C(=O)NY1Y2, -NY1Y2, -OR5 ó alquilo sustituido por -NY3Y4; R5 es alquilo, alquenilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo o heterocicloalquilalquilo; R6 es alquilo, alquenilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo o heterocicloalquilalquilo; n es 0 o un entero 1 ó 2; Y1 e Y2 son, en forma independiente, hidrógeno, alquenilo, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, heterocicloalquilalquilo o alquilo sustituido en forma opcional por uno o más grupos seleccionados de ciano, arilo, heteroarilo, hidroxi, -C(=O)OR6, -C(=O)NY3Y4, -NY3Y4 y -OR5, ó el grupo -NY1Y2 pueden formar una amina cíclica; Y3 y Y4 son, en forma independiente, hidrógeno, alquenilo, alquilo, arilo, arilalquilo, cicloalquilo, heteroarilo o heteroarilalquilo; o el grupo -NY3Y4 pueden formar una amina cíclica; donde: todos los radicales alquilo, alq, alquenilo, cicloalquilo, heterocicloalquilo, arilo, arilalquilo, heteroarilo y heteroarilalquilo presentes en los radicales anteriores se sustituyen en forma opcional con uno o más radicales elegidos de átomos de halógeno y radicales hidroxilo, ciano, alquilo, alcoxi, acilamino (NH-COalq), -C(=O)OR6, -C(=O)R6, hidroxialquilo, carboxialquilo, S(O)n-alq, S(O)n-NH2, S(O)n-NH(alq), S(O)n-N(alq)2, CF3, OCF3, NO2, arilalcoxi, arilo, heteroarilo, ariloxi, ariloxialquilo, -C(=O)-NY3Y4 y NY3Y4, los últimos radicales contienen alquilo, arilo y heteroarilo que a su vez están sustituidos en forma opcional con uno o más radicales elegidos de átomos de halógeno y radicales alquilo, radicales carboxilo libres, salificados o esterificados y radicales de acilamino NH-C(O)R5; ó un N-óxido, profármaco, bioisóstero ácido, sal o solvato aceptable para uso farmacéutico de dicho compuesto; o un N-óxido, profármaco, o bioisóstero ácido de dicha sal o dicho solvato, junto con uno o más vehículos o excipientes aceptables para uso farmacéutico.Y composiciones que contienen dichos compuestos, y sus profármacos y las sales y los solvatos aceptables para uso farmacéutico de dichos compuestos y sus profármacos, como también a nuevos compuestos dentro del alcance de la fórmula (1), y a procesos para su preparación. Dichos compuestos y composiciones tienen valiosas propiedades farmacéuticas, en particular la capacidad de inhibir las quinasas.
ARP020104061A 2001-10-26 2002-10-25 Benzoimidazoles AR037032A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0113868A FR2831537B1 (fr) 2001-10-26 2001-10-26 Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation
GB0206895A GB0206895D0 (en) 2002-03-22 2002-03-22 Chemical compounds
GB0206893A GB0206893D0 (en) 2002-03-22 2002-03-22 Chemical compounds

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AR037032A1 true AR037032A1 (es) 2004-10-20

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US (2) US6897208B2 (es)
AR (1) AR037032A1 (es)
JO (1) JO2339B1 (es)
PA (1) PA8557101A1 (es)
PE (1) PE20030612A1 (es)
SV (1) SV2008001369A (es)

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