DE60224707T2 - Inhibitoren von cytosolischen phospholipase a2 - Google Patents

Inhibitoren von cytosolischen phospholipase a2 Download PDF

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Publication number
DE60224707T2
DE60224707T2 DE60224707T DE60224707T DE60224707T2 DE 60224707 T2 DE60224707 T2 DE 60224707T2 DE 60224707 T DE60224707 T DE 60224707T DE 60224707 T DE60224707 T DE 60224707T DE 60224707 T2 DE60224707 T2 DE 60224707T2
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DE
Germany
Prior art keywords
ethyl
chloro
benzhydryl
indol
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE60224707T
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German (de)
English (en)
Other versions
DE60224707D1 (de
Inventor
John Caedmon Arlington MCKEW
Steve Yik-Kai Wellesly TAM
James Donald Acton CLARK
Katherine Lin West Newton LEE
Lihren Bedford CHEN
Paresh Boston THAKKER
Fuk-Wah Pomona SUM
Mark Leo Somerville BEHNKE
Baihua Audubon HU
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Wyeth LLC
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Wyeth LLC
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Publication of DE60224707D1 publication Critical patent/DE60224707D1/de
Publication of DE60224707T2 publication Critical patent/DE60224707T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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]
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/12—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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems

Landscapes

  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
DE60224707T 2001-12-03 2002-12-02 Inhibitoren von cytosolischen phospholipase a2 Expired - Lifetime DE60224707T2 (de)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US33458801P 2001-12-03 2001-12-03
US33459101P 2001-12-03 2001-12-03
US33460501P 2001-12-03 2001-12-03
US334605P 2001-12-03
US334591P 2001-12-03
US334588P 2001-12-03
US41966402P 2002-10-18 2002-10-18
US419664P 2002-10-18
PCT/US2002/038311 WO2003048122A2 (en) 2001-12-03 2002-12-02 Inhibitors of cytosolic phospholipase a2

Publications (2)

Publication Number Publication Date
DE60224707D1 DE60224707D1 (de) 2008-03-06
DE60224707T2 true DE60224707T2 (de) 2009-02-26

Family

ID=27502498

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60224707T Expired - Lifetime DE60224707T2 (de) 2001-12-03 2002-12-02 Inhibitoren von cytosolischen phospholipase a2

Country Status (24)

Country Link
EP (1) EP1451154B1 (enExample)
JP (1) JP4657605B2 (enExample)
KR (1) KR100973665B1 (enExample)
CN (1) CN100503566C (enExample)
AR (1) AR037684A1 (enExample)
AT (1) ATE384045T1 (enExample)
AU (1) AU2002351182B2 (enExample)
BR (1) BR0214672A (enExample)
CA (1) CA2469138C (enExample)
CO (1) CO5580763A2 (enExample)
CY (1) CY1107383T1 (enExample)
DE (1) DE60224707T2 (enExample)
DK (2) DK1892239T3 (enExample)
EC (1) ECSP045131A (enExample)
ES (2) ES2300490T3 (enExample)
HU (1) HUP0402577A3 (enExample)
IL (2) IL162052A0 (enExample)
IN (1) IN2005KO00312A (enExample)
NO (1) NO327256B1 (enExample)
NZ (1) NZ533269A (enExample)
PL (1) PL370445A1 (enExample)
PT (1) PT1451154E (enExample)
TW (1) TWI334778B (enExample)
WO (1) WO2003048122A2 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7605156B2 (en) 2001-12-03 2009-10-20 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2
US7713964B2 (en) 2001-12-03 2010-05-11 Wyeth Llc Methods for treating asthmatic conditions
TW200510305A (en) * 2003-07-25 2005-03-16 Wyeth Corp Process for the preparation of CPLA2 inhibitors
WO2005049566A1 (en) 2003-11-17 2005-06-02 Wyeth Processes for the preparation of n-substituted phthalimides
HN2004000536A (es) * 2003-12-16 2009-02-18 Wyeth Corp Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles
AR048239A1 (es) 2004-02-25 2006-04-12 Wyeth Corp Procesos para la preparacion de haluros de aril- y heteroaril-alquilsulfonilo e intermediarios de sintesis de los mismos
US20050244367A1 (en) * 2004-05-03 2005-11-03 Ilypsa, Inc. Phospholipase inhibitors localized in the gastrointestinal lumen
AR053410A1 (es) 2004-08-19 2007-05-09 Wyeth Corp Proceso para la sintesis de indoles n-alquilados c-2, c-3 sustituidos. compuestos intermediarios
MY147864A (en) 2005-04-13 2013-01-31 Astion Dev As Beta-2 adrenoceptor agonists for treating connective tissue diseases of the skin
TW200718687A (en) 2005-05-27 2007-05-16 Wyeth Corp Inhibitors of cytosolic phospholipase A2
AU2006272886B2 (en) * 2005-07-21 2012-03-01 Novartis Ag Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts
WO2007056281A2 (en) 2005-11-03 2007-05-18 Ilypsa, Inc. Multivalent indole compounds and use thereof as phospholipase-a2 inhibitors
FR2899471A1 (fr) * 2006-04-06 2007-10-12 Pasteur Institut Utilisation d'au moins un inhibiteur de la phospholipase a2 cytosolique comme medicament pour le traitement des maladies respiratoires
US20080009485A1 (en) * 2006-05-26 2008-01-10 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
CL2007003145A1 (es) * 2006-10-31 2008-01-25 Wyeth Corp Composicion farmaceutica que comprende un compuestos derivado de indol y un sistema portador que comprende 10-50% de un primer solubilizante, 10-50% de un segundo solubilizante y 10-30% de un diluyente; proceso de preparacion; y forma farmaceutica.
BRPI0718066A2 (pt) * 2006-10-31 2013-11-05 Wyeth Corp Composição farmacêutica; forma de dosagem farmacêutica; processo para preparar uma composição farmacêutica;e produto.
US8293781B2 (en) 2007-03-29 2012-10-23 Daiichi Sankyo Company, Limited Indole derivatives having cPLA2 inhibiting activity and applications and production methods of the same
AU2009241038B2 (en) 2008-04-28 2011-12-22 Asahi Kasei Pharma Corporation Phenylpropionic acid derivative and use thereof
EP2488025A4 (en) * 2009-10-15 2013-04-03 Childrens Medical Center SEPIAPTERIC INTREDUCTASE INHIBITION FOR PAIN TREATMENT
EP2614144B1 (en) 2010-09-08 2015-07-22 Twincore Zentrum für Experimentelle und Klinische Infektionsforschung GmbH Use of inhibitors of phospholipase a2 for the treatment or prevention of flavivirus infection

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2079374C (en) * 1991-09-30 2003-08-05 Merck Frosst Canada Incorporated (bicyclic-azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5994398A (en) * 1996-12-11 1999-11-30 Elan Pharmaceuticals, Inc. Arylsulfonamides as phospholipase A2 inhibitors
EA200000868A1 (ru) * 1998-02-25 2001-04-23 Дженетикс Инститьют, Инк. Ингибиторы фосфолипаз
CA2322162A1 (en) * 1998-02-25 1999-09-02 Genetics Institute, Llc Inhibitors of phospholipase enzymes

Also Published As

Publication number Publication date
PT1451154E (pt) 2008-04-21
IL162052A (en) 2013-04-30
PL370445A1 (en) 2005-05-30
EP1451154B1 (en) 2008-01-16
DK1451154T3 (da) 2008-05-19
JP2005515997A (ja) 2005-06-02
HK1065799A1 (en) 2005-03-04
KR20050044661A (ko) 2005-05-12
KR100973665B1 (ko) 2010-08-04
DK1892239T3 (da) 2013-03-25
TWI334778B (en) 2010-12-21
ATE384045T1 (de) 2008-02-15
EP1451154A2 (en) 2004-09-01
IL162052A0 (en) 2005-11-20
TW200301695A (en) 2003-07-16
IN2005KO00312A (enExample) 2015-08-14
DE60224707D1 (de) 2008-03-06
ES2401454T3 (es) 2013-04-19
JP4657605B2 (ja) 2011-03-23
WO2003048122A2 (en) 2003-06-12
NZ533269A (en) 2006-03-31
NO20042679L (no) 2004-06-25
BR0214672A (pt) 2004-10-19
CY1107383T1 (el) 2012-12-19
HUP0402577A2 (hu) 2005-03-29
CA2469138A1 (en) 2003-06-12
ES2300490T3 (es) 2008-06-16
WO2003048122A3 (en) 2003-09-18
CO5580763A2 (es) 2005-11-30
HK1113798A1 (en) 2008-10-17
NO327256B1 (no) 2009-05-25
CN1617855A (zh) 2005-05-18
AR037684A1 (es) 2004-12-01
CA2469138C (en) 2012-04-17
ECSP045131A (es) 2004-07-23
AU2002351182B2 (en) 2009-01-15
HUP0402577A3 (en) 2011-05-30
CN100503566C (zh) 2009-06-24
AU2002351182A1 (en) 2003-06-17

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