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AR056217A1 - Compuestos heterociclicos utiles para el tratamiento de la enfermedad de alzheimer, neurodegeneracion y demencia - Google Patents

Compuestos heterociclicos utiles para el tratamiento de la enfermedad de alzheimer, neurodegeneracion y demencia

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Publication number
AR056217A1
AR056217A1 ARP060104956A ARP060104956A AR056217A1 AR 056217 A1 AR056217 A1 AR 056217A1 AR P060104956 A ARP060104956 A AR P060104956A AR P060104956 A ARP060104956 A AR P060104956A AR 056217 A1 AR056217 A1 AR 056217A1
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AR
Argentina
Prior art keywords
heterocycloalkyl
alkyl
cycloalkyl
heteroaryl
aryl
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ARP060104956A
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Astrazeneca Ab
Astex Therapeutics Ltd
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38049090&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056217(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab, Astex Therapeutics Ltd filed Critical Astrazeneca Ab
Publication of AR056217A1 publication Critical patent/AR056217A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/20—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 4
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) o una sal farmacéuticamente aceptable, tautomero o precursor hidrolizable in vivo de los mismos, en los cuales, G es O, NR7 o CR8R9; R1 es H, alquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con 1, 2, 3, 4 o 5 R14; R2 es Q o -L-Q; o R1 y R2, junto con el átomo de carbono al cual están unidos, forman un grupo cicloalquilo de 3-14 miembros o un grupo heterocicloalquilo de 3-14 miembros, cada uno de los cuales está sustituido con Cy2 y está optativamente sustituido con 1, 2, 3, 4 o 5 A4; R3, R4, R5 y R6 son, independientemente, H, CN, NO2, ORa, SRa, OC(O)Ra, OC(O)ORb, OC(O)NRcRd, C(O)Ra, C(O)ORb, C(O)NRcRd, NRcRd, NRcC(O)Ra, NRcC(O)ORb, NRcS(O)2Rb, S(O)Ra, S(O)NRcRd, S(O)2Ra, S(O)2NRcRd, alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con 1, 2 o 3 R14; R7 es H, C(O)Ra, C(O)ORb, C(O)NRcRd, S(O)Ra, S(O)2Ra, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde cada uno del alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido 1, 2, 3, 4 o 5 R14; R8 y R9 son, independientemente, H, CN, NO2, ORa, SRa, OC(O)Ra, OC(O)ORb, C(O)ORb, OC(O)NRcRd, NRcRd, NRcC(O)Ra, NRcC(O)ORb, NRcS(O)2Rb, S(O)Ra, S(O)NRcRd, S(O)2Ra, S(O)2NRcRd, alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2- 10, arilo, . cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con 1, 2 o 3 R14; o R8 y R9, junto con el átomo de carbono al cual están unidos, forman un grupo cicloalquilo de 3-14 miembros o un grupo heterocicloalquilo de 3-14 miembros, cada uno de los cuales está sustituido con 1, 2 o 3 R14; cada uno de R12 y R13 es, independientemente, H, halo, alquilo C1-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(O)Rb', C(O)NRc'Rd', C(O)ORa', OC(O)Rb', OC(O)NRc'Rd', NRc'Rd', NRc'C(O)Rd', NRc'C(O)ORa', NRc'S(O)2Rb', S(O)Rb', S(O)NRc'Rd', S(O)2Rb', o S(O)2NRc'Rd'; R14 es halo, alquilo C1-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(O)Rb', C(O)NRc'Rd', C(O)ORa', OC(O)Rb', OC(O)NRc'Rd', NRc'Rd', NRc'C(O)Rd', NRc'C(O)ORa', NRc'S(O)2Rb', S(O)Rb', S(O)NRc'Rd', S(O)2Rb', o S(O)2NRc'Rd'; Q es arilo, cicloalquilo, heteroarilo o heterocicloalquilo, cada uno de los cuales está optativamente sustituido con 1, 2, 3, 4 o 5 Cy1 o A1; L es alquenilenilo C2-10, alquinilenilo C2-10, (CR12R13)q, (CR12R13)q1O(CR12R13)q2, (CR12R13)q1S(CR12R13)q2, (CR12R13)q1SO2(CR12R13)q2, (CR12R13)q1SO(CR12R13)q2, (CR12R13)q1CO(CR12R13)q2, (CR12R13)q1NRe(CR12R13)q2, o (CR12R13)q1CONRe(CR12R13)q2; Cy1 es arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, cada uno de los cuales está optativamente sustituido con 1, 2, 3, 4 o 5 A2; Cy2 es arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, cada uno de los cuales está optativamente sustituido con 1, 2, 3, 4 o 5 A3; A1 es halo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, NRcS(O)2Rb, S(O)Rb, S(O)NRcRd, S(O)2Rb, o S(O)2NRcRd, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, dialquilamino C2-8, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo o heterocicloalquilalquilo, donde cada uno de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo o heterocicloalquilalquilo está optativamente sustituido con 1, 2, 3, 4 o 5 halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, NRcS(O)2Rb', S(O)Rb, S(O)NRcRd, S(O)2Rb, o S(O)2NRcRd; cada uno de A2, A3, y A4 es, independientemente, halo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, NRcS(O)2Rb, S(O)Rb, S(O)NRcRd, S(O)2Rb, o S(O)2NRcRd, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, dialquilamino C2-8, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, donde cada uno de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, arilo, cicloalquilo, heteroarilo o heterocicloalquilo está optativamente sustituido con 1, 2, 3, 4 o 5 halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, NRcS(O)2Rb, S(O)Rb, S(O)NRcRd, S(O)2Rb, o S(O)2NRcRd; cada uno de Ra y Ra' es, independientemente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquillquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo, cada uno de Rb y Rb' es, independientemente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo, cada uno de Rc y Rd es, independientemente, H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo, o Rc y Rd junto con el átomo de N al cual están unidos, forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; cada uno de Rc' y Rd' es, independientemente, H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está optativamente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo, o bien Rc' y Rd' junto con el átomo de N al cual están unidos, forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; Re es H, alquilo C1-4, haloalquilo C1-4, alquenilo C2-4, alquinilo C2-4, o CO-(alquilo C1-4); q es 1, 2, 3, 4, 5 o 6; q1 es 0, 1, 2 o 3; y q2 es 0, 1, 2 o 3; con las siguientes salvedades: a) cuando G es NH o CH2; R2 es -L-Q; L es -CH2, -CH=CH-, o -CsC-; y R1 es H o metilo, luego Q no ha de ser fenilo no sustituido y b) cuando G es NR7 o CR8R9; R7 es H, metilo, o fenilo optativamente sustituido con halo; cada uno de R8 y R9 es independientemente, H o metilo, R2 es Q; y R1 es H o metilo, luego Q es arilo, cicloalquilo, heteroarilo, o heterocicloalquilo, cada uno de los cuales está optativamente sustituido con por lo menos un Cy3 y está optativamente sustituido con 1, 2 o 3 A4.
ARP060104956A 2005-11-15 2006-11-13 Compuestos heterociclicos utiles para el tratamiento de la enfermedad de alzheimer, neurodegeneracion y demencia AR056217A1 (es)

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US (1) US20080293709A1 (es)
EP (1) EP1957462A4 (es)
JP (1) JP2009520685A (es)
KR (1) KR20080070744A (es)
CN (1) CN101360714A (es)
AR (1) AR056217A1 (es)
AU (1) AU2006316256A1 (es)
BR (1) BRPI0618607A2 (es)
CA (1) CA2629831A1 (es)
IL (1) IL191057A0 (es)
NO (1) NO20082481L (es)
TW (1) TW200804290A (es)
UY (1) UY29919A1 (es)
WO (1) WO2007058583A2 (es)
ZA (1) ZA200803859B (es)

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