ZA200110177B - Inhibitors of aspartyl protease. - Google Patents

Inhibitors of aspartyl protease. Download PDF

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Publication number
ZA200110177B
ZA200110177B ZA200110177A ZA200110177A ZA200110177B ZA 200110177 B ZA200110177 B ZA 200110177B ZA 200110177 A ZA200110177 A ZA 200110177A ZA 200110177 A ZA200110177 A ZA 200110177A ZA 200110177 B ZA200110177 B ZA 200110177B
Authority
ZA
South Africa
Prior art keywords
alkyl
optionally substituted
membered saturated
aryl
unsaturated
Prior art date
Application number
ZA200110177A
Other languages
English (en)
Inventor
Michael Robin Hale
Roger Tung
Stephen Price
Robin David Wilkes
Wayne Carl Schairer
Ashley Nicholas Jarvis
Andrew Spaltenstein
Eric Steven Furfine
Vicente Samano
Istvan Kaldor
John Franklin Miller
Michael Stephen Brieger
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of ZA200110177B publication Critical patent/ZA200110177B/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
ZA200110177A 1999-06-11 2001-12-11 Inhibitors of aspartyl protease. ZA200110177B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13907099P 1999-06-11 1999-06-11
US19021100P 2000-03-17 2000-03-17

Publications (1)

Publication Number Publication Date
ZA200110177B true ZA200110177B (en) 2003-01-13

Family

ID=26836833

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200110177A ZA200110177B (en) 1999-06-11 2001-12-11 Inhibitors of aspartyl protease.

Country Status (31)

Country Link
EP (2) EP1194404B1 (de)
JP (2) JP4503896B2 (de)
KR (1) KR100762188B1 (de)
CN (2) CN100516034C (de)
AR (1) AR031520A1 (de)
AT (2) ATE534622T1 (de)
AU (1) AU779994B2 (de)
BR (1) BR0011745A (de)
CA (1) CA2380858C (de)
CO (1) CO5160337A1 (de)
CY (1) CY1112632T1 (de)
CZ (1) CZ303052B6 (de)
DE (1) DE60027722T2 (de)
DK (2) DK1686113T3 (de)
ES (2) ES2375823T3 (de)
HK (1) HK1046899B (de)
HU (1) HUP0300385A3 (de)
IL (3) IL146918A0 (de)
MX (1) MXPA01012808A (de)
MY (1) MY137777A (de)
NO (1) NO323951B1 (de)
NZ (1) NZ516003A (de)
PE (1) PE20010230A1 (de)
PL (1) PL210227B1 (de)
PT (2) PT1194404E (de)
SI (1) SI1194404T1 (de)
TN (1) TNSN00129A1 (de)
TR (3) TR200202528T2 (de)
TW (3) TW593248B (de)
WO (1) WO2000076961A1 (de)
ZA (1) ZA200110177B (de)

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NZ508855A (en) * 1998-06-19 2003-10-31 Vertex Pharma Sulfonamide inhibitors of HIV aspartyl protease
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
BR0207862A (pt) 2001-02-14 2004-06-22 Tibotec Pharm Ltd Inibidores de protease de hiv 2-(amino-substituìda)-benzotiazol-sulfonamida de amplo espectro
US7285566B2 (en) * 2002-01-07 2007-10-23 Erickson John W Resistance-repellent retroviral protease inhibitors
MY142238A (en) * 2002-03-12 2010-11-15 Tibotec Pharm Ltd Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors
AU2003231765B9 (en) * 2002-04-26 2010-01-28 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such
US6632816B1 (en) * 2002-12-23 2003-10-14 Pharmacor Inc. Aromatic derivatives as HIV aspartyl protease inhibitors
EP1638960A4 (de) * 2003-06-27 2009-04-01 Smithkline Beecham Corp Herstellung chemischer verbindungen
PL1658277T3 (pl) * 2003-08-18 2012-10-31 H Lundbeck As Sól bursztynianowa i malonianowa trans-4-((1R,3S)-6-chloro-3-fenyloindan-1-ylo)-1,2,2-tri-metylopiperazyny i zastosowanie jako lek
EP2335701B1 (de) * 2003-12-15 2012-07-11 Schering Corporation Heterocyclische Aspartyl-Protease Inhibitoren
CA2559328A1 (en) 2004-03-11 2005-09-22 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
TWI383975B (zh) 2004-03-31 2013-02-01 悌柏泰克醫藥有限公司 製備（３Ｒ，３ａＳ，６ａＲ）六氫-呋喃并〔２，３-ｂ〕呋喃-３-醇之方法
US7388008B2 (en) 2004-08-02 2008-06-17 Ambrilia Biopharma Inc. Lysine based compounds
TWI376373B (en) 2005-02-16 2012-11-11 Lundbeck & Co As H Crystalline base of a pharmaceutical compound
TWI453198B (zh) 2005-02-16 2014-09-21 Lundbeck & Co As H 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s）-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法
JP2008533017A (ja) * 2005-03-11 2008-08-21 スミスクライン ビーチャム コーポレーション Ｈｉｖプロテアーゼ阻害薬
US8227450B2 (en) 2005-11-30 2012-07-24 Ambrilia Biopharma Inc. Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation
EP2069356A1 (de) * 2006-07-24 2009-06-17 Gilead Sciences, Inc. Bisfuranylproteasehemmer
ES2359949T3 (es) 2006-11-09 2011-05-30 Tibotec Pharmaceuticals Métodos para preparar hexhidrofuro(2,3-b)furan-3-ol.
EP2120562A4 (de) * 2006-11-21 2010-01-13 Purdue Research Foundation Verfahren und zusammensetzungen zur behandlung von hiv-infektionen
BRPI0810609A2 (pt) 2007-04-27 2014-10-21 Tibotec Pharm Ltd Métodos para a preparação de derivados de n-isobutil-n-(2-hidróxi-a-amino-4-fenilbutil)-p-nitrobe nzenossulfonilamida
GB2452952A (en) * 2007-09-20 2009-03-25 Npil Pharmaceuticals N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
CN102573815B (zh) 2009-09-22 2015-09-30 泰博特克药品公司 Hiv感染的治疗和预防
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
WO2016039403A1 (ja) * 2014-09-11 2016-03-17 塩野義製薬株式会社 持続性ｈｉｖプロテアーゼ阻害剤
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors

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CA2032259A1 (en) * 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids
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US5475013A (en) * 1990-11-19 1995-12-12 Monsanto Company Retroviral protease inhibitors
JP3657002B2 (ja) * 1992-08-25 2005-06-08 ジー．ディー．サール アンド カンパニー レトロウイルスプロテアーゼ阻害剤として有用なα−およびβ−アミノ酸ヒドロキシエチルアミノスルホンアミド
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
DK0666843T3 (da) * 1992-10-30 2000-03-20 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfaminsyrer, der kan anvendes som inhibitorer af retrovirale proteaser
AU7669794A (en) * 1993-08-24 1995-03-21 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1996022287A1 (en) * 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
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US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
JP2000515488A (ja) * 1995-11-15 2000-11-21 ジー．ディー．サール アンド カンパニー 置換スルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド レトロウイルスプロテアーゼ阻害剤
GB9712504D0 (en) * 1997-06-17 1997-08-20 Dundee Teaching Hospitals Nhs Thermal imaging method and apparatus
WO1999010374A1 (en) * 1997-08-26 1999-03-04 Wisconsin Alumni Research Foundation Cyclosporin a conjugates and uses therefor
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion

Also Published As

Publication number Publication date
HK1046899B (en) 2007-03-02
AU5600600A (en) 2001-01-02
IL146918A0 (en) 2002-08-14
TR200202528T2 (tr) 2003-02-21
JP4503896B2 (ja) 2010-07-14
AR031520A1 (es) 2003-09-24
CO5160337A1 (es) 2002-05-30
CZ20014431A3 (cs) 2002-06-12
TWI299000B (en) 2008-07-21
NO20016034D0 (no) 2001-12-10
DK1686113T3 (da) 2012-02-20
NO323951B1 (no) 2007-07-23
MXPA01012808A (es) 2002-07-22
ES2263478T3 (es) 2006-12-16
PT1194404E (pt) 2006-08-31
HUP0300385A2 (hu) 2003-07-28
KR100762188B1 (ko) 2007-10-04
CN101245058A (zh) 2008-08-20
TW200804252A (en) 2008-01-16
BR0011745A (pt) 2002-03-19
EP1194404B1 (de) 2006-05-03
HUP0300385A3 (en) 2007-05-29
EP1686113A1 (de) 2006-08-02
ATE325091T1 (de) 2006-06-15
DE60027722D1 (en) 2006-06-08
WO2000076961A1 (en) 2000-12-21
DK1194404T3 (da) 2006-09-04
EP1194404A1 (de) 2002-04-10
EP1686113B1 (de) 2011-11-23
CY1112632T1 (el) 2016-02-10
TWI318116B (en) 2009-12-11
PT1686113E (pt) 2012-02-20
AU779994B2 (en) 2005-02-24
NO20016034L (no) 2002-01-18
CN100516034C (zh) 2009-07-22
KR20020033642A (ko) 2002-05-07
NZ516003A (en) 2004-02-27
TW200425891A (en) 2004-12-01
CA2380858A1 (en) 2000-12-21
TR200200407T2 (tr) 2002-08-21
IL202633A0 (en) 2010-06-30
CZ303052B6 (cs) 2012-03-14
ES2375823T3 (es) 2012-03-06
TNSN00129A1 (fr) 2005-11-10
PE20010230A1 (es) 2001-03-15
ATE534622T1 (de) 2011-12-15
JP2009046493A (ja) 2009-03-05
MY137777A (en) 2009-03-31
TW593248B (en) 2004-06-21
CA2380858C (en) 2011-12-06
PL352830A1 (pl) 2003-09-08
PL210227B1 (pl) 2011-12-30
CN1361765A (zh) 2002-07-31
DE60027722T2 (de) 2007-04-26
SI1194404T1 (sl) 2006-10-31
TR200603871T2 (tr) 2007-01-22
HK1046899A1 (en) 2003-01-30
IL202633A (en) 2013-02-28
JP2003502309A (ja) 2003-01-21
IL146918A (en) 2010-06-16

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