ATE120753T1 - Bisphosphonsäurederivate als antiarthritische mittel. - Google Patents

Bisphosphonsäurederivate als antiarthritische mittel.

Info

Publication number
ATE120753T1
ATE120753T1 AT91916549T AT91916549T ATE120753T1 AT E120753 T1 ATE120753 T1 AT E120753T1 AT 91916549 T AT91916549 T AT 91916549T AT 91916549 T AT91916549 T AT 91916549T AT E120753 T1 ATE120753 T1 AT E120753T1
Authority
AT
Austria
Prior art keywords
acid derivatives
bisphosphonic acid
antiarthritic agents
bisphosphonates
agents
Prior art date
Application number
AT91916549T
Other languages
English (en)
Inventor
Richard Allen Nugent
Original Assignee
Upjohn Co
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 Upjohn Co filed Critical Upjohn Co
Application granted granted Critical
Publication of ATE120753T1 publication Critical patent/ATE120753T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4025—Esters of poly(thio)phosphonic acids
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/6533—Six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings
    • C07F9/6541—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/6552—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a six-membered ring
    • C07F9/65522—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a six-membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655363—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a six-membered ring
    • C07F9/655372—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a six-membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Detergent Compositions (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AT91916549T 1990-08-21 1991-08-09 Bisphosphonsäurederivate als antiarthritische mittel. ATE120753T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57027490A 1990-08-21 1990-08-21

Publications (1)

Publication Number Publication Date
ATE120753T1 true ATE120753T1 (de) 1995-04-15

Family

ID=24278957

Family Applications (1)

Application Number Title Priority Date Filing Date
AT91916549T ATE120753T1 (de) 1990-08-21 1991-08-09 Bisphosphonsäurederivate als antiarthritische mittel.

Country Status (9)

Country Link
US (2) US5412141A (de)
EP (1) EP0544812B1 (de)
JP (1) JPH06500112A (de)
AT (1) ATE120753T1 (de)
AU (1) AU8495091A (de)
DE (1) DE69108733T2 (de)
DK (1) DK0544812T3 (de)
ES (1) ES2072015T3 (de)
WO (1) WO1992003451A1 (de)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07509241A (ja) * 1992-07-16 1995-10-12 ジ・アップジョン・カンパニー 抗炎症および抗関節炎薬としてのホスホノ誘導体
AU4859493A (en) * 1992-10-09 1994-05-09 Upjohn Company, The Pyrimidine bisphosphonate esters and (alkoxymethylphosphinyl)alkyl phosphonic acids as anti-inflammatories
JPH06135976A (ja) * 1992-10-30 1994-05-17 Toray Ind Inc メタンジホスホン酸誘導体、その製造方法およびその医薬用途
AU6556894A (en) * 1993-05-18 1994-12-12 Upjohn Company, The Bisphosphonate esters for treating gastric disorders
EP0625522B1 (de) * 1993-05-18 1998-08-19 Takeda Chemical Industries, Ltd. Benzopyran-Derivate und ihre Verwendung
US5795985A (en) * 1996-03-05 1998-08-18 Ciba Specialty Chemicals Corporation Phenyl alkyl ketone substituted by cyclic amine and a process for the preparation thereof
GB9607945D0 (en) * 1996-04-17 1996-06-19 Univ Nottingham Bisphosponates as Anti-inflammatory agents
US5994563A (en) * 1997-04-01 1999-11-30 Ortho Pharmaceutical Corporation Arylmethylphosphonic acid derivatives useful in treating bone wasting diseases
US5990307A (en) * 1997-08-01 1999-11-23 American Home Products Corporation Process for the preparation of [2-((8.9)-Dioxo-2,6-Diazabicyclo [5.2.0]-Non-1(7)-en-2yl) Ethyl]Phosphonic acid
HUP0102782A3 (en) 1998-06-19 2002-12-28 Smithkline Beecham Corp Salycilanilide as inhibitors of transcription factor nf-kb
CA2353867C (en) * 1998-12-09 2013-10-08 The Arizona Disease Control Research Commission Anticancer agents based on prevention of protein prenylation
BR0010708A (pt) 1999-05-04 2002-02-19 Strakan Ltd Glicosìdeos androgênicos e atividade androgênica dos mesmos
US6410520B2 (en) 2000-02-01 2002-06-25 The Procter & Gamble Company Selective crystallization of 3-pyridyl-1-hydroxyethylidene-1, 1-bisphosphonic acid sodium as the hemipentahydrate or monohydrate
US6562974B2 (en) 2000-02-01 2003-05-13 The Procter & Gamble Company Process for making geminal bisphosphonates
US20060269602A1 (en) * 2001-04-13 2006-11-30 Dasch James R Method of modifying the release profile of sustained release compositions
US6558702B2 (en) * 2001-04-13 2003-05-06 Alkermes Controlled Therapeutics, Inc. Method of modifying the release profile of sustained release compositions
WO2004026245A2 (en) * 2002-09-19 2004-04-01 Ilex Oncology Research, Sarl Substituted phosphonate compounds having bone anabolic activity
JP4463274B2 (ja) * 2003-06-27 2010-05-19 明 小谷 ビスホスホネート錯体
TW200514775A (en) * 2003-10-22 2005-05-01 Wyeth Corp Methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl} phosphonic acid and esters thereof
CN1964715A (zh) 2004-05-06 2007-05-16 默克公司 治疗狗的关节炎状况的方法
DE102005009457A1 (de) * 2005-03-02 2006-09-07 Bayer Cropscience Ag Verfahren zum Herstellen von Alkylaniliden
WO2008016632A1 (en) * 2006-08-01 2008-02-07 University Of Massachusetts Deoxybenzoin-based anti-flammable polyphosphonate and poly(arylate-phosphonate) copolymer compounds, compositions and related methods of use
ES2537216T3 (es) 2009-09-01 2015-06-03 Duke University Composiciones de bisfosfonato y métodos para tratar la insuficiencia cardíaca
US9949992B2 (en) 2011-11-16 2018-04-24 Duke University Bisphosphonate compositions and methods for treating and\or reducing cardiac dysfunction
CN103787910B (zh) * 2014-03-05 2015-06-24 南通大学 一种有机中间体苯甲酰乙酰苯胺的制备方法
EP3867227A4 (de) * 2018-10-19 2022-08-03 Auckland Uniservices Limited Verbindungen zur behandlung von diabetes und/oder assoziierten erkrankungen

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US3683080A (en) * 1970-08-28 1972-08-08 Procter & Gamble Compositions for inhibiting anomalous deposition and mobilization of calcium phosphate in animal tissue
DE2637477A1 (de) * 1976-08-20 1978-02-23 Hoechst Ag Dihydro-oxo-nicotinsaeuren und verfahren zu ihrer herstellung
US4297360A (en) * 1980-03-28 1981-10-27 Sterling Drug Inc. 5-(Pyridinyl)pyridine-2,3-diamines, preparation thereof and their cardiotonic use
NZ195564A (en) * 1979-11-26 1983-09-30 Sterling Drug Inc 5-pyridinyl-2(1h)-pyridinones pharmaceutical compositions intermediate pyridine compounds
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FR2531088B1 (fr) * 1982-07-29 1987-08-28 Sanofi Sa Produits anti-inflammatoires derives de l'acide methylenediphosphonique et leur procede de preparation
IT8367883A0 (it) * 1982-08-23 1983-08-22 Rorer Int Overseas Composti cardiotonici del 2 piridone 5 biciclico eteroaril sostituito e relative composizioni farmaceutiche
PH27078A (en) * 1984-12-21 1993-02-01 Procter & Gamble Pharmaceutical compositions containing geminal diphosphonates
DE3540150A1 (de) * 1985-11-13 1987-05-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
JPS63295595A (ja) * 1986-10-27 1988-12-01 Yamanouchi Pharmaceut Co Ltd ３−置換−３−オキソープロピリデン−１，１−ジホスホン酸
JPS63185993A (ja) * 1987-01-27 1988-08-01 Yamanouchi Pharmaceut Co Ltd ２−置換−２−オキソ−エチレン−１，１−ジホスホン酸
FR2611203B1 (fr) * 1987-02-20 1989-06-09 Sturtz Georges Analogues gem-diphosphoniques d'amethopterine (methotrexate) et de derives deaza-n-10 amethopterine. leur preparation et les compositions pharmaceutiques qui les contiennent
DE3719513A1 (de) * 1987-06-11 1988-12-22 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
GB8809481D0 (en) * 1988-04-21 1988-05-25 Smith Kline French Lab Chemical compounds
ATE91689T1 (de) * 1989-04-03 1993-08-15 Upjohn Co Geminale bisphosphonsaeuren und deren derivate als antiarthritische mittel.

Also Published As

Publication number Publication date
US5412141A (en) 1995-05-02
WO1992003451A1 (en) 1992-03-05
AU8495091A (en) 1992-03-17
EP0544812B1 (de) 1995-04-05
JPH06500112A (ja) 1994-01-06
DE69108733T2 (de) 1995-09-14
ES2072015T3 (es) 1995-07-01
EP0544812A1 (de) 1993-06-09
DE69108733D1 (de) 1995-05-11
US5602115A (en) 1997-02-11
DK0544812T3 (da) 1995-08-21

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