ATE190489T1 - Uracil-reductase-inaktivator - Google Patents

Uracil-reductase-inaktivator

Info

Publication number
ATE190489T1
ATE190489T1 AT91917260T AT91917260T ATE190489T1 AT E190489 T1 ATE190489 T1 AT E190489T1 AT 91917260 T AT91917260 T AT 91917260T AT 91917260 T AT91917260 T AT 91917260T AT E190489 T1 ATE190489 T1 AT E190489T1
Authority
AT
Austria
Prior art keywords
halo
inactivator
uracil reductase
uracil
reductase inactivator
Prior art date
Application number
AT91917260T
Other languages
English (en)
Inventor
Thomas Spector
David John Timothy Porter
Saad George Rahim
Original Assignee
Wellcome Found
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10682770&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE190489(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wellcome Found filed Critical Wellcome Found
Application granted granted Critical
Publication of ATE190489T1 publication Critical patent/ATE190489T1/de

Links

Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • Laminated Bodies (AREA)
  • Transformer Cooling (AREA)
  • Springs (AREA)
  • Vibration Dampers (AREA)
  • Semiconductor Lasers (AREA)
  • Medicinal Preparation (AREA)
AT91917260T 1990-09-26 1991-09-25 Uracil-reductase-inaktivator ATE190489T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB909020930A GB9020930D0 (en) 1990-09-26 1990-09-26 Pharmaceutical combinations
PCT/GB1991/001650 WO1992004901A1 (en) 1990-09-26 1991-09-25 Uracil reductase inactivators

Publications (1)

Publication Number Publication Date
ATE190489T1 true ATE190489T1 (de) 2000-04-15

Family

ID=10682770

Family Applications (1)

Application Number Title Priority Date Filing Date
AT91917260T ATE190489T1 (de) 1990-09-26 1991-09-25 Uracil-reductase-inaktivator

Country Status (29)

Country Link
US (5) US6268374B1 (de)
EP (2) EP0550580B1 (de)
JP (2) JP2682739B2 (de)
KR (1) KR100222329B1 (de)
AT (1) ATE190489T1 (de)
BR (1) BR1100356A (de)
CA (2) CA2390654A1 (de)
CZ (4) CZ288515B6 (de)
DE (1) DE69132052T2 (de)
DK (1) DK0550580T3 (de)
ES (1) ES2143465T3 (de)
FI (1) FI112601B (de)
GB (1) GB9020930D0 (de)
GR (1) GR3033388T3 (de)
HU (1) HU219589B (de)
IE (1) IE20010101A1 (de)
IL (2) IL99562A (de)
MC (1) MC2307A1 (de)
MY (1) MY128980A (de)
NO (2) NO313175B1 (de)
NZ (2) NZ250799A (de)
PT (1) PT99041B (de)
RU (1) RU2194511C2 (de)
SG (1) SG47912A1 (de)
SK (1) SK281894B6 (de)
TW (1) TW271397B (de)
UA (1) UA42679C2 (de)
WO (1) WO1992004901A1 (de)
ZA (1) ZA917667B (de)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6337209B1 (en) 1992-02-26 2002-01-08 Glaxo Wellcome Inc. Molecular constructs containing a carcinoembryonic antigen regulatory sequence
GB9020930D0 (en) * 1990-09-26 1990-11-07 Wellcome Found Pharmaceutical combinations
KR100245252B1 (ko) * 1991-05-15 2000-03-02 도로시 케이. 로빈슨 간에 의해 대사될 수 있는 프로드럭의 결정 및 그의 치료학적 용도
GB9322795D0 (en) * 1993-11-05 1993-12-22 Wellcome Found Novel compounds
US6849602B1 (en) * 1996-03-05 2005-02-01 The Regents Of The University Of California Compositions for alleviating neuropathic pain with prosaposin receptor agonists
NZ330360A (en) * 1997-06-02 1999-03-29 Hoffmann La Roche 5'-deoxy-cytidine derivatives, their manufacture and use as antitumoral agents
US6005098A (en) * 1998-02-06 1999-12-21 Hoffmann-La Roche Inc. 5'deoxycytidine derivatives
US7026301B2 (en) * 2002-10-17 2006-04-11 New York University Method of orally treating inflammatory skin conditions with prodrugs of 5-fluorouracil
AU2012200856B2 (en) * 2004-12-03 2013-10-10 Adherex Technologies Inc. Methods for administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs
JP2008521930A (ja) * 2004-12-03 2008-06-26 アドヘレックス テクノロジーズ， インコーポレイテッド ５−ｆｕおよび５−ｆｕプロドラッグと併用してｄｐｄ阻害物質を投与するための方法
US20080255168A1 (en) * 2004-12-03 2008-10-16 Adherex Technologies, Inc. Methods for administering dpd inhibitors in combination with 5-fu and 5-fu prodrugs
US20090196833A1 (en) * 2008-02-06 2009-08-06 Adherex Technologies Inc. Compositions comprising topical dpd inhibitors and methods of using same in the treatment of hand-foot syndrome
JP2013508293A (ja) * 2009-10-14 2013-03-07 アドヘレックス テクノロジーズ， インコーポレイテッド ５−ｆｕ又はそのプロドラッグと、ｄｐｄ阻害剤との組合せに付随した神経毒性の処置
WO2018170509A1 (en) * 2017-03-17 2018-09-20 Hampton University Fatty acid synthase inhibitors and methods of use

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3324126A (en) * 1963-08-07 1967-06-06 Univ Kansas State Production of 5-trifluoromethyluracil
US4124765A (en) 1975-05-13 1978-11-07 Ono Pharmaceutical Co., Ltd. 5-Fluorouracil derivatives
DE2522369A1 (de) 1975-05-21 1976-12-02 Ono Pharmaceutical Co 5-fluoruracilderivate und verfahren zu ihrer herstellung
DD122381A1 (de) * 1975-10-03 1976-10-05
JPS55111420A (en) * 1979-02-20 1980-08-28 Ono Pharmaceut Co Ltd Antitumorigenic agent
US4381344A (en) 1980-04-25 1983-04-26 Burroughs Wellcome Co. Process for producing deoxyribosides using bacterial phosphorylase
JPS6094971A (ja) * 1983-10-31 1985-05-28 Sagami Chem Res Center ５−ペルフルオロアルキルウラシル類の製造方法
US4719214A (en) 1985-07-25 1988-01-12 Southern Research Institute Carbocyclic analogues of thymine nucleosides
GB8629892D0 (en) 1986-12-15 1987-01-28 Wellcome Found Antiviral compounds
US4863927A (en) * 1987-05-11 1989-09-05 Merck & Co., Inc. 1-(2-hydroxymethyl)cycloalkylmethyl)-5-substituted uracils
US4874602A (en) 1988-02-22 1989-10-17 Paul Calabresi Reduction of the severity 3'-azido-3'-deoxythymidine-induced anemia using benzylacyclouridine
US5112835A (en) * 1988-03-31 1992-05-12 Mitsubishi Kasei Corporation 6-substituted acyclopyrimidine nucleoside derivatives and antiviral agents containing the same as active ingredient thereof
US5077280A (en) 1988-04-12 1991-12-31 Brown University Research Foundation Treatment of viral infections
US5198539A (en) * 1988-08-19 1993-03-30 Burroughs Wellcome Co. 5'-esters of 2',3'-dideoxy-3'-fluoro-5-ethynyluridine
US5157114A (en) * 1988-08-19 1992-10-20 Burroughs Wellcome Co. 2',3'-dideoxy-3'-fluoro-5-ethyngluridine
ATE109154T1 (de) * 1988-08-25 1994-08-15 Yoshitomi Pharmaceutical 2'-methylidenpyrimidin-nukleoside, ihre verwendung und verfahren zu ihrer herstellung.
IE902574A1 (en) 1989-07-17 1991-02-27 Univ Birmingham Antiviral pyrimidine nucleosides
WO1992001452A1 (en) * 1990-07-19 1992-02-06 The Wellcome Foundation Limited Enzyme inactivators
US5643913A (en) * 1990-07-19 1997-07-01 Glaxo Wellcome Inc. Pharmaceutical compositions of 5-substituted uracil compounds
GB9020930D0 (en) * 1990-09-26 1990-11-07 Wellcome Found Pharmaceutical combinations

Also Published As

Publication number Publication date
CZ170995A3 (en) 1995-12-13
HUT63765A (en) 1993-10-28
IL121947A0 (en) 1998-03-10
PT99041B (pt) 1999-02-26
NZ239927A (en) 1995-11-27
RU2194511C2 (ru) 2002-12-20
ES2143465T3 (es) 2000-05-16
DK0550580T3 (da) 2000-12-04
HK1004188A1 (en) 1998-11-20
IL99562A (en) 1999-11-30
EP0550580B1 (de) 2000-03-15
JPH06504263A (ja) 1994-05-19
SK23393A3 (en) 1993-07-07
MY128980A (en) 2007-03-30
CZ288520B6 (cs) 2001-07-11
ZA917667B (en) 1993-03-25
US20070078106A1 (en) 2007-04-05
CZ16296A3 (en) 1996-05-15
CZ50693A3 (en) 1994-02-16
KR100222329B1 (en) 1999-10-01
US7119096B2 (en) 2006-10-10
AU8540591A (en) 1992-04-15
NO313175B1 (no) 2002-08-26
HU219589B (hu) 2001-05-28
CA2390654A1 (en) 1992-04-02
BR1100356A (pt) 2003-02-25
US6268374B1 (en) 2001-07-31
PT99041A (pt) 1992-08-31
CZ288515B6 (cs) 2001-07-11
CA2092435A1 (en) 1992-03-27
SG47912A1 (en) 1998-04-17
IL99562A0 (en) 1992-08-18
HU9300863D0 (en) 1993-06-28
GB9020930D0 (en) 1990-11-07
UA42679C2 (uk) 2001-11-15
SK281894B6 (sk) 2001-09-11
MC2307A1 (fr) 1993-09-27
AU654505B2 (en) 1994-11-10
TW271397B (de) 1996-03-01
JP3003993B2 (ja) 2000-01-31
NO980717D0 (no) 1998-02-20
FI931337A0 (fi) 1993-03-25
CZ16196A3 (en) 1996-05-15
FI931337L (fi) 1993-03-25
IE20010101A1 (en) 2002-03-20
JP2682739B2 (ja) 1997-11-26
FI112601B (fi) 2003-12-31
DE69132052T2 (de) 2000-08-03
US5817664A (en) 1998-10-06
DE69132052D1 (de) 2000-04-20
US7704971B2 (en) 2010-04-27
JPH1045623A (ja) 1998-02-17
US6297223B1 (en) 2001-10-02
US20020042392A1 (en) 2002-04-11
EP0985415A1 (de) 2000-03-15
WO1992004901A1 (en) 1992-04-02
NO931118D0 (no) 1993-03-25
CA2092435C (en) 2002-11-12
GR3033388T3 (en) 2000-09-29
NO931118L (no) 1993-03-25
NZ250799A (en) 1995-11-27
EP0550580A1 (de) 1993-07-14
NO980717L (no) 1993-03-25

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Legal Events

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EELA Cancelled due to lapse of time