CO5570682A2 - Mezclas analogas de ciclosporina y su uso como agentes inmunomoduladores - Google Patents

Mezclas analogas de ciclosporina y su uso como agentes inmunomoduladores

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Publication number
CO5570682A2
CO5570682A2 CO04035672A CO04035672A CO5570682A2 CO 5570682 A2 CO5570682 A2 CO 5570682A2 CO 04035672 A CO04035672 A CO 04035672A CO 04035672 A CO04035672 A CO 04035672A CO 5570682 A2 CO5570682 A2 CO 5570682A2
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Colombia
Prior art keywords
isomer
isomeric mixture
compound
blends
immunomodulating agents
Prior art date
Application number
CO04035672A
Other languages
English (en)
Inventor
Naicker Selvaraj
Randall W Yatscoff
Robert T Foster
Original Assignee
Isotechnika Inc
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Publication date
Application filed by Isotechnika Inc filed Critical Isotechnika Inc
Publication of CO5570682A2 publication Critical patent/CO5570682A2/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • C07K7/645Cyclosporins; Related peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13Cyclosporins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dispersion Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)

Abstract

1.- Un compuesto que comprende una mezcla isómera de un análogo de ciclosporina modificado en el residuo 1-amino ácido con un dieno 1,3 sustituyente, en el que la gama de la mezcla isómera por el dieno sustituyente corresponde de entre alrededor del 10% hasta alrededor del 90% del isómero E y alrededor del 90% hasta alrededor del 10% del isómero Z.2.- El compuesto de la Reivindicación 1, en la que los isómeros no-deuterados constituyen los isómeros E y Z, según se especifica a continuación:3.- El compuesto de la Reivindicación 1 ó 2, en el que la mezcla isómera comprende alrededor del 15% hasta alrededor del 85% del isómero E y alrededor del 85% hasta alrededor del 15% del isómero Z.4.- El compuesto de la Reivindicación 1 ó 2, en el que la mezcla isómera comprende alrededor del 25% hasta alrededor del 75% del isómero E y alrededor del 75% hasta alrededor del 25% del isómero Z.5.- El compuesto de la Reivindicación 1 ó 2, en el que la mezcla isómera comprende alrededor del 35% hasta alrededor del 65% del isómero E y alrededor del 65% hasta alrededor del 35% del isómero Z.
CO04035672A 2001-10-19 2004-04-19 Mezclas analogas de ciclosporina y su uso como agentes inmunomoduladores CO5570682A2 (es)

Applications Claiming Priority (1)

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US34620101P 2001-10-19 2001-10-19

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CO5570682A2 true CO5570682A2 (es) 2005-10-31

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ID=23358378

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CO04035672A CO5570682A2 (es) 2001-10-19 2004-04-19 Mezclas analogas de ciclosporina y su uso como agentes inmunomoduladores

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US (2) US20110092669A1 (es)
EP (2) EP1436322B1 (es)
JP (4) JP2005511538A (es)
KR (1) KR100992850B1 (es)
CN (1) CN100344648C (es)
AR (1) AR036853A1 (es)
AT (1) ATE401339T1 (es)
AU (1) AU2002331510B2 (es)
BE (1) BE2022C547I2 (es)
BR (1) BR0213659A (es)
CA (2) CA2727642C (es)
CO (1) CO5570682A2 (es)
CY (1) CY1108410T1 (es)
DE (1) DE60227686D1 (es)
DK (1) DK1436322T3 (es)
EC (3) ECSP045059A (es)
ES (1) ES2310604T3 (es)
FI (1) FIC20220041I1 (es)
FR (1) FR22C1051I2 (es)
HK (1) HK1062567A1 (es)
HR (1) HRP20040353B1 (es)
IL (2) IL160762A0 (es)
LT (1) LTC1436322I2 (es)
MA (1) MA26337A1 (es)
ME (1) ME00487B (es)
MX (1) MXPA04003624A (es)
MY (1) MY187182A (es)
NO (2) NO331745B1 (es)
NZ (1) NZ531945A (es)
PL (1) PL210697B1 (es)
PT (1) PT1436322E (es)
RU (1) RU2337106C2 (es)
SI (1) SI1436322T1 (es)
TN (1) TNSN04069A1 (es)
UY (1) UY27502A1 (es)
WO (1) WO2003033527A2 (es)
ZA (1) ZA200402270B (es)

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KR100982466B1 (ko) 2001-10-19 2010-09-16 이소테크니카 인코포레이티드 시클로스포린 유사체의 합성
JP2005511538A (ja) * 2001-10-19 2005-04-28 アイソテクニカ インコーポレーテッド シクロスポリン類似体混合物及びそれらの免疫調節剤としての使用
TW200505946A (en) * 2003-04-08 2005-02-16 Hoffmann La Roche Process for preparation of cyclosporin a analog
EP1828229A4 (en) * 2004-12-17 2010-06-30 Isotechnika Inc METABOLITES OF CYCLOSPORINANALOGA
US7696166B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
US7696165B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
AU2008310956B2 (en) 2007-10-08 2014-08-07 Aurinia Pharmaceuticals Inc. Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors
US9017725B2 (en) 2009-06-09 2015-04-28 Aurinia Pharmaceuticals Inc. Topical drug delivery systems for ophthalmic use
GB0912584D0 (en) * 2009-07-20 2009-08-26 Ucl Business Plc Cyclosporin conjugates
PT2651965T (pt) 2010-12-15 2019-01-28 Contravir Pharmaceuticals Inc Moléculas analógas de ciclosporinas modificadas ao nivel dos aminoácidos 1 e 3
GB201222455D0 (en) 2012-12-13 2013-01-30 Perioc Ltd Novel pharmaceutical formulations and their use in the treatment of periodontaldisease
US20210104302A1 (en) * 2016-11-30 2021-04-08 Schrödinger, Inc. Graphical user interface for chemical transition state calculations
EP4252629A3 (en) 2016-12-07 2023-12-27 Biora Therapeutics, Inc. Gastrointestinal tract detection methods, devices and systems
WO2018106928A1 (en) 2016-12-08 2018-06-14 Contravir Pharmaceuticals, Inc. Treatment and prevention of hbv diseases by cyclosporine analogue molecules modified at amino acides 1 and 3
WO2018112255A1 (en) 2016-12-14 2018-06-21 Progenity Inc. Treatment of a disease of the gastrointestinal tract with an immunosuppressant
US10286036B2 (en) * 2017-05-12 2019-05-14 Aurinia Pharmaceuticals Inc. Protocol for treatment of lupus nephritis
US20190224275A1 (en) 2017-05-12 2019-07-25 Aurinia Pharmaceuticals Inc. Protocol for treatment of lupus nephritis
WO2019246312A1 (en) 2018-06-20 2019-12-26 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an immunomodulator
EP4201952A1 (en) 2021-12-21 2023-06-28 Curia Spain, S.A.U. Process for the controlled synthesis of voclosporin
WO2024052941A1 (en) * 2022-09-09 2024-03-14 Dr. Reddy's Laboratories Limited Improved process for the preparation of voclosporin

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DK0991660T3 (da) * 1997-10-08 2006-02-13 Isotechnika Inc Deuterede og udeuterede cyclosporinanaloger og deres anvendelse som immunmodulerende midler
KR100982466B1 (ko) * 2001-10-19 2010-09-16 이소테크니카 인코포레이티드 시클로스포린 유사체의 합성
JP2005511538A (ja) * 2001-10-19 2005-04-28 アイソテクニカ インコーポレーテッド シクロスポリン類似体混合物及びそれらの免疫調節剤としての使用

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CA2727642A1 (en) 2003-04-24
HRP20040353B1 (hr) 2012-10-31
ATE401339T1 (de) 2008-08-15
EP1816138A1 (en) 2007-08-08
TNSN04069A1 (en) 2006-06-01
IL160762A0 (en) 2004-08-31
IL160762A (en) 2010-11-30
ME00487B (me) 2011-10-10
PL370501A1 (en) 2005-05-30
JP2005511538A (ja) 2005-04-28
JP2013136597A (ja) 2013-07-11
LTC1436322I2 (es) 2023-06-26
SI1436322T1 (sl) 2008-12-31
CA2460685C (en) 2014-05-27
NO331745B1 (no) 2012-03-19
AU2002331510B2 (en) 2008-05-01
ECSP045060A (es) 2004-07-23
ECSP045059A (es) 2004-07-23
FIC20220041I1 (fi) 2022-10-14
DE60227686D1 (de) 2008-08-28
WO2003033527A2 (en) 2003-04-24
UY27502A1 (es) 2003-04-30
FR22C1051I1 (fr) 2022-12-16
CN1571794A (zh) 2005-01-26
HK1062567A1 (en) 2004-11-12
ES2310604T3 (es) 2009-01-16
RU2004110941A (ru) 2005-08-10
FR22C1051I2 (fr) 2023-11-17
PT1436322E (pt) 2008-10-23
US20110092669A1 (en) 2011-04-21
EP1436322A2 (en) 2004-07-14
ECSP045061A (es) 2004-08-27
KR100992850B1 (ko) 2010-11-09
NO20042029L (no) 2004-05-14
KR20050037421A (ko) 2005-04-21
CY1108410T1 (el) 2012-05-23
NZ531945A (en) 2006-01-27
JP2009197036A (ja) 2009-09-03
JP2011006417A (ja) 2011-01-13
WO2003033527A3 (en) 2003-10-16
MY187182A (en) 2021-09-08
JP5272140B2 (ja) 2013-08-28
NO2022042I1 (no) 2022-10-14
EP1436322B1 (en) 2008-07-16
CA2460685A1 (en) 2003-04-24
RU2337106C2 (ru) 2008-10-27
MXPA04003624A (es) 2004-12-06
MA26337A1 (fr) 2004-10-01
CN100344648C (zh) 2007-10-24
PL210697B1 (pl) 2012-02-29
DK1436322T3 (da) 2008-11-03
CA2727642C (en) 2014-02-04
US20140288266A1 (en) 2014-09-25
ZA200402270B (en) 2005-05-25
AR036853A1 (es) 2004-10-06
BR0213659A (pt) 2004-10-26
LTPA2022521I1 (es) 2022-11-10
BE2022C547I2 (es) 2022-10-19
HRP20040353A2 (en) 2005-04-30

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