HUP0003760A2 - Metalloproteináz és TNF-felszabadulás inhibitor hatású tio-szubsztituált peptidek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Metalloproteináz és TNF-felszabadulás inhibitor hatású tio-szubsztituált peptidek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0003760A2
HUP0003760A2 HU0003760A HUP0003760A HUP0003760A2 HU P0003760 A2 HUP0003760 A2 HU P0003760A2 HU 0003760 A HU0003760 A HU 0003760A HU P0003760 A HUP0003760 A HU P0003760A HU P0003760 A2 HUP0003760 A2 HU P0003760A2
Authority
HU
Hungary
Prior art keywords
alkyl
group
heteroaryl
aryl
alkenyl
Prior art date
Application number
HU0003760A
Other languages
English (en)
Inventor
Andrew Douglas Baxter
John Gary Montana
David Alan Owen
Original Assignee
Darwin Discovery Ltd.
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 GBGB9520354.3A external-priority patent/GB9520354D0/en
Priority claimed from GBGB9607126.1A external-priority patent/GB9607126D0/en
Application filed by Darwin Discovery Ltd. filed Critical Darwin Discovery Ltd.
Publication of HUP0003760A2 publication Critical patent/HUP0003760A2/hu
Publication of HUP0003760A3 publication Critical patent/HUP0003760A3/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological 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
    • 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
    • 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
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Heart & Thoracic Surgery (AREA)
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Abstract

A találmány tárgya (I) általános képletű peptidszármazékok, ahol aképletben R1 jelentése 1-7 szénatomos alkil-, 2-6 szénatomos alkenil-, (1-6szénatomos alkil)-aril-, aril-, (1-6 szénatomos alkil)-heteroaril-,heteroaril- vagy (1-6 szénatomos alkil)-AR9 általános képletű csoport; R2 jelentése hidrogénatom vagy 1-6 szénatomos alkilcsoport; R3 jelentése[Alk]nR6 általános képletű csoport, ahol Alk jelentése 1-6 szénatomos alkil- vagy 2-6 szénatomos alkenilcsoport, és n jelentéseegész szám, melynek értéke 0 vagy 1; X jelentése heteroarilcsoport vagy CONR4R5 általános képletű csoport; R7 jelentése hidrogénatom vagy R10CO általános képletű csoport, aholR10 jelentése 1-4 szénatomos alkil-, (1-4 szénatomos alkil)-aril-, (1-4 szénatomos alkil)-heteroaril-, ciklo(3-6 szénatomos alkil)-, ciklo-(3-6 szénatomos alkil)-(1-4 szénatomos alkil-, 2-6 szénatomosalkenil-, 2-6 szénatomos alkenil-aril-, aril- vagy heteroaril-csoport; R8 és R16 jelentése azonosan vagy eltérően 1-4 szénatomos alkil R11,R16 jelentése hidrogénatom is lehet; A találmány szerinti vegyületekmátrix metalloproteináz inhibitorok, valamint a TNFa-felszabadulást isgátolják. Ó
HU0003760A 1995-10-05 1996-10-04 Thio-substituted peptides as inhibitors for metalloproteinases and tnf liberation, process for production thereof and their use HUP0003760A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9520354.3A GB9520354D0 (en) 1995-10-05 1995-10-05 Compounds
GBGB9607126.1A GB9607126D0 (en) 1996-04-04 1996-04-04 Compounds
PCT/GB1996/002438 WO1997012902A1 (en) 1995-10-05 1996-10-04 Thio-substituted peptides as inhibitors for metalloproteinases and tnf liberation

Publications (2)

Publication Number Publication Date
HUP0003760A2 true HUP0003760A2 (hu) 2001-04-28
HUP0003760A3 HUP0003760A3 (en) 2001-05-28

Family

ID=26307887

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0003760A HUP0003760A3 (en) 1995-10-05 1996-10-04 Thio-substituted peptides as inhibitors for metalloproteinases and tnf liberation, process for production thereof and their use

Country Status (20)

Country Link
US (1) US5981490A (hu)
EP (1) EP0859784B1 (hu)
JP (1) JPH11512733A (hu)
KR (1) KR100472752B1 (hu)
CN (1) CN1145637C (hu)
AT (1) ATE229972T1 (hu)
AU (1) AU710072B2 (hu)
BR (1) BR9610922A (hu)
CA (1) CA2229434A1 (hu)
CZ (1) CZ289711B6 (hu)
DE (1) DE69625506T2 (hu)
DK (1) DK0859784T3 (hu)
ES (1) ES2186803T3 (hu)
HU (1) HUP0003760A3 (hu)
IL (1) IL123430A (hu)
MX (1) MX9802680A (hu)
NO (1) NO981520D0 (hu)
NZ (1) NZ319222A (hu)
PL (1) PL185312B1 (hu)
WO (1) WO1997012902A1 (hu)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9607120D0 (en) * 1996-04-04 1996-06-12 Chiroscience Ltd Compounds
US6953788B1 (en) 1996-09-19 2005-10-11 Aventis Pharmaceuticals Inc. 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
WO1998039024A1 (en) * 1997-03-03 1998-09-11 Darwin Discovery Limited Selective mmp inhibitors having reduced side-effects
EP1123308A1 (en) 1998-10-23 2001-08-16 Darwin Discovery Limited Single morphic forms of known peptide metalloproteinase inhibitors
NL1013404C2 (nl) * 1999-10-27 2001-05-01 Dsm Nv Werkwijze voor de bereiding van een dipeptide en tussenproduct in een dergelijke werkwijze.
US6808902B1 (en) 1999-11-12 2004-10-26 Amgen Inc. Process for correction of a disulfide misfold in IL-1Ra Fc fusion molecules
ES2208595T3 (es) 2000-05-15 2004-06-16 Darwin Discovery Limited Derivados del acido hidroxamico.
HUP0304058A2 (hu) * 2001-01-30 2004-04-28 Bristol-Myers Squibb Company Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
CZ20032902A3 (cs) * 2001-04-26 2004-01-14 Bristol-Myers Squibb Company Farmaceutická tableta s vysokým obsahem účinné látky
KR20040023630A (ko) 2001-06-26 2004-03-18 아브게닉스, 인크. Ｏｐｇｌ에 결합하는 항체
US6960567B2 (en) * 2001-11-30 2005-11-01 Bristol Myers Squibb Company Method of producing n-[(2S)-sulfanyl-4-(1,5,5-trimethylhydantoinyl)butanoyl]-L-leucyl-L-tert-leucine N-methylamide and intermediate thereof
US20060167334A1 (en) * 2003-06-26 2006-07-27 Anstadt Mark P Method and apparatus for direct mechanical ventricular actuation with favorable conditioning and minimal heart stress
US7723376B2 (en) * 2003-07-15 2010-05-25 Korea Research Institute Of Bioscience And Biotechnology 2-oxo-heterocyclic compounds and pharmaceutical compositions
TW200630337A (en) * 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
WO2007110449A1 (en) 2006-03-29 2007-10-04 Euro-Celtique S.A. Benzenesulfonamide compounds and their use
TW200812963A (en) 2006-04-13 2008-03-16 Euro Celtique Sa Benzenesulfonamide compounds and the use thereof
WO2007118853A1 (en) 2006-04-13 2007-10-25 Euro-Celtique S.A. Benzenesulfonamide compounds and their use as blockers of calcium channels
WO2008124118A1 (en) * 2007-04-09 2008-10-16 Purdue Pharma L.P. Benzenesulfonyl compounds and the use therof
WO2009040659A2 (en) 2007-09-28 2009-04-02 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
CN103254291B (zh) * 2013-05-30 2014-06-25 常州亚当生物技术有限公司 肿瘤坏死因子-α多肽抑制剂及其应用
CN103285373A (zh) * 2013-05-30 2013-09-11 苏州普罗达生物科技有限公司 肿瘤坏死因子-α多肽抑制剂制备及其应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8311286D0 (en) * 1983-04-26 1983-06-02 Searle & Co Carboxyalkyl peptide derivatives
WO1988006890A1 (en) * 1987-03-17 1988-09-22 Research Corporation Technologies, Inc. Synthetic inhibitors of mammalian collagenase
DE4311021A1 (de) * 1993-03-31 1994-10-27 Diagnostikforschung Inst Bifunktionelle Chelatbildner, deren Technetium- und Rhenium-Komplexe, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende radiopharmazeutische Mittel
NZ271893A (en) * 1993-08-23 1997-11-24 Immunex Corp Inhibitors of tnf-alpha secretion
GB9323165D0 (en) * 1993-11-10 1994-01-05 Chiros Ltd Compounds
WO1996011209A1 (en) * 1994-10-05 1996-04-18 Chiroscience Limited Peptidyl compounds and their therapeutic use as inhibitors of metalloproteases
CA2217859A1 (en) * 1995-05-10 1996-11-14 David Alan Owen Peptidyl compounds which inhibit metalloproteinase and tnf liberation and their therapeutic use
CA2217850A1 (en) * 1995-05-10 1996-11-14 Chirotech Technology Limited Peptide compounds which inhibit metalloproteinase and tnf liberation, and their therapeutic use

Also Published As

Publication number Publication date
CZ101798A3 (cs) 1998-08-12
IL123430A0 (en) 1998-09-24
ES2186803T3 (es) 2003-05-16
BR9610922A (pt) 1999-12-21
CN1145637C (zh) 2004-04-14
IL123430A (en) 2001-04-30
US5981490A (en) 1999-11-09
NO981520L (no) 1998-04-03
DE69625506T2 (de) 2003-07-24
DE69625506D1 (de) 2003-01-30
DK0859784T3 (da) 2003-04-22
KR100472752B1 (ko) 2006-01-27
CA2229434A1 (en) 1997-04-10
EP0859784A1 (en) 1998-08-26
JPH11512733A (ja) 1999-11-02
KR19990063996A (ko) 1999-07-26
PL185312B1 (pl) 2003-04-30
HUP0003760A3 (en) 2001-05-28
WO1997012902A1 (en) 1997-04-10
AU7139896A (en) 1997-04-28
CN1198747A (zh) 1998-11-11
CZ289711B6 (cs) 2002-03-13
ATE229972T1 (de) 2003-01-15
NZ319222A (en) 1999-09-29
EP0859784B1 (en) 2002-12-18
MX9802680A (es) 1998-11-30
NO981520D0 (no) 1998-04-03
PL325824A1 (en) 1998-08-03
AU710072B2 (en) 1999-09-16

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