KR100883080B1 - 담즙산 또는 담즙산염 지방산 컨쥬게이트의 용도 - Google Patents

담즙산 또는 담즙산염 지방산 컨쥬게이트의 용도 Download PDF

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Publication number
KR100883080B1
KR100883080B1 KR1020037013339A KR20037013339A KR100883080B1 KR 100883080 B1 KR100883080 B1 KR 100883080B1 KR 1020037013339 A KR1020037013339 A KR 1020037013339A KR 20037013339 A KR20037013339 A KR 20037013339A KR 100883080 B1 KR100883080 B1 KR 100883080B1
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South Korea
Prior art keywords
bile
acid
fatty acid
formula
acids
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Expired - Lifetime
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KR1020037013339A
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English (en)
Korean (ko)
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KR20030092063A (ko
Inventor
길라트투비아
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갈메드 인터내쇼날 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Botany (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020037013339A 2001-04-17 2002-04-15 담즙산 또는 담즙산염 지방산 컨쥬게이트의 용도 Expired - Lifetime KR100883080B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IL142650A IL142650A (en) 1998-04-08 2001-04-17 Use of bile acid conjugates or bile salts and fatty acids or fatty acids in the preparation of pharmaceuticals for lowering cholesterol, for the treatment of fatty liver and for the treatment of hyperglycemia and diabetes
IL142650 2001-04-17
PCT/IL2002/000303 WO2002083147A1 (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates

Publications (2)

Publication Number Publication Date
KR20030092063A KR20030092063A (ko) 2003-12-03
KR100883080B1 true KR100883080B1 (ko) 2009-02-10

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ID=11075322

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Application Number Title Priority Date Filing Date
KR1020037013339A Expired - Lifetime KR100883080B1 (ko) 2001-04-17 2002-04-15 담즙산 또는 담즙산염 지방산 컨쥬게이트의 용도

Country Status (24)

Country Link
US (2) US7501403B2 (enExample)
EP (2) EP1379254B1 (enExample)
JP (1) JP4324706B2 (enExample)
KR (1) KR100883080B1 (enExample)
CN (1) CN1259918C (enExample)
AT (2) ATE432705T1 (enExample)
AU (2) AU2002307771B2 (enExample)
BR (1) BR0208924A (enExample)
CA (2) CA2444266C (enExample)
CY (1) CY1106853T1 (enExample)
CZ (2) CZ300489B6 (enExample)
DE (2) DE60232559D1 (enExample)
DK (2) DK1790346T3 (enExample)
EA (1) EA007565B1 (enExample)
ES (2) ES2289137T3 (enExample)
HU (1) HU230548B1 (enExample)
IL (1) IL142650A (enExample)
MX (1) MXPA03009553A (enExample)
NO (2) NO333910B1 (enExample)
NZ (1) NZ528868A (enExample)
PL (2) PL205057B1 (enExample)
PT (2) PT1790346E (enExample)
UA (1) UA78699C2 (enExample)
WO (1) WO2002083147A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL142650A (en) 1998-04-08 2007-06-03 Galmed Int Ltd Use of bile acid conjugates or bile salts and fatty acids or fatty acids in the preparation of pharmaceuticals for lowering cholesterol, for the treatment of fatty liver and for the treatment of hyperglycemia and diabetes
US8975246B2 (en) 2001-04-17 2015-03-10 Galmed Research And Development Ltd. Bile acid or bile salt fatty acid conjugates
US20100311708A1 (en) * 2007-07-25 2010-12-09 Tarek Moustafa Use of nor-bile acids in the treatment of arteriosclerosis
US9314444B2 (en) 2009-01-12 2016-04-19 Biokier, Inc. Composition and method for treatment of NASH
RS56054B1 (sr) * 2009-01-12 2017-09-29 Biokier Inc Smeša i metod za lečenje dijabetesa
US9006288B2 (en) 2009-01-12 2015-04-14 Biokier, Inc. Composition and method for treatment of diabetes
EP2391370B1 (en) 2009-02-02 2015-06-03 Galmed Research and Development Ltd. Methods and compositions for treating alzheimer's disease
US20120202890A1 (en) 2011-02-08 2012-08-09 Nian Wu Polymer-carbohydrate-lipid conjugates
US9084826B2 (en) 2012-05-01 2015-07-21 Catabasis Pharmaceuticals, Inc. Fatty acid conjugates of statin and FXR agonists; compositions and method of uses
CN103571617A (zh) * 2012-07-26 2014-02-12 丰益(上海)生物技术研发中心有限公司 改进的动物油脂加工工艺
US10702546B2 (en) 2012-11-29 2020-07-07 St Pharm Co., Ltd. Bile acid oligomer conjugate for novel vesicular transport and use thereof
IL227890A0 (en) * 2013-08-08 2014-01-30 Galderm Therapeutics Ltd Antiaging compounds containing bile acid and fatty acid conjugates
US11571431B2 (en) 2013-12-04 2023-02-07 Galmed Research And Development Ltd Aramchol salts
TR201909447T4 (tr) * 2013-12-04 2019-07-22 Galmed Res & Development Ltd Aramkol tuzları.
US20170196891A1 (en) * 2014-06-01 2017-07-13 Galmed Research And Development Ltd. Fatty acid bile acid conjugates for treatment of lipodystrophy
US10849911B2 (en) 2015-06-10 2020-12-01 Galmed Research And Development Ltd. Low dose compositions of Aramachol salts
IL243707A0 (en) 2016-01-20 2016-05-01 Galmed Res And Dev Ltd Treatment to regulate the microbiota in the intestine
US11197870B2 (en) 2016-11-10 2021-12-14 Galmed Research And Development Ltd Treatment for hepatic fibrosis
CN116687850A (zh) 2022-02-24 2023-09-05 甘莱制药有限公司 包含环状膦酸酯化合物的药物组合物及其制备方法与用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3856953A (en) 1973-05-15 1974-12-24 Intellectual Property Dev Corp Method of treating fatty liver
WO1999052932A1 (en) * 1998-04-08 1999-10-21 Galmed International Ltd. Fatty acid derivatives of bile acids and bile acid derivatives

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3859437A (en) * 1972-06-02 1975-01-07 Intellectual Property Dev Corp Reducing cholesterol levels
IT1167479B (it) * 1981-07-24 1987-05-13 Carlo Scolastico Derivati dell'acido chenodesossicolico
IT1167478B (it) * 1981-07-24 1987-05-13 Carlo Scolastico Derivati dell'acido ursodesossicolico
JPS6164701A (ja) * 1984-09-06 1986-04-03 Meito Sangyo Kk カチオン化デキストラン誘導体とポリウロン酸の高分子電解質錯体及びその利用
DE3930696A1 (de) * 1989-09-14 1991-03-28 Hoechst Ag Gallensaeurederivate, verfahren zu ihrer herstellung, verwendung als arzneimittel
US5278320A (en) * 1992-09-11 1994-01-11 Merck & Co., Inc. Cholesterol lowering compounds produced by directed biosynthesis
DE4432708A1 (de) * 1994-09-14 1996-03-21 Hoechst Ag Modifizierte Gallensäuren, Verfahren zu ihrer Herstellung und ihre Verwendung
US20030153541A1 (en) * 1997-10-31 2003-08-14 Robert Dudley Novel anticholesterol compositions and method for using same
EP1027045A4 (en) * 1997-10-31 2004-12-08 Arch Dev Corp METHODS AND COMPILATIONS FOR REGULATING S-ALPHA REDUCTASE ACTIVITY
IL142650A (en) 1998-04-08 2007-06-03 Galmed Int Ltd Use of bile acid conjugates or bile salts and fatty acids or fatty acids in the preparation of pharmaceuticals for lowering cholesterol, for the treatment of fatty liver and for the treatment of hyperglycemia and diabetes
US6620821B2 (en) * 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
JP2006306800A (ja) * 2005-04-28 2006-11-09 Kirin Brewery Co Ltd ファルネソイドｘ受容体活性化剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3856953A (en) 1973-05-15 1974-12-24 Intellectual Property Dev Corp Method of treating fatty liver
WO1999052932A1 (en) * 1998-04-08 1999-10-21 Galmed International Ltd. Fatty acid derivatives of bile acids and bile acid derivatives

Also Published As

Publication number Publication date
EP1379254B1 (en) 2007-06-20
NO20131219L (no) 2003-11-28
NO333910B1 (no) 2013-10-14
NZ528868A (en) 2005-09-30
EA200301017A1 (ru) 2005-04-28
CZ2008296A3 (enExample) 2004-04-14
CZ20032710A3 (cs) 2004-04-14
JP2004525962A (ja) 2004-08-26
DE60220775D1 (de) 2007-08-02
CA2703688C (en) 2012-07-31
JP4324706B2 (ja) 2009-09-02
ATE432705T1 (de) 2009-06-15
AU2007200191A1 (en) 2007-02-08
PL205057B1 (pl) 2010-03-31
NO20034609L (no) 2003-11-28
CA2703688A1 (en) 2002-10-24
PT1379254E (pt) 2007-07-10
PL366585A1 (en) 2005-02-07
HU230548B1 (hu) 2016-11-28
EP1790346A3 (en) 2007-08-22
EP1790346B1 (en) 2009-06-03
EA007565B1 (ru) 2006-12-29
ES2289137T3 (es) 2008-02-01
CY1106853T1 (el) 2012-05-23
CZ300489B6 (cs) 2009-06-03
PT1790346E (pt) 2009-09-04
IL142650A0 (en) 2002-03-10
ATE365044T1 (de) 2007-07-15
CA2444266C (en) 2010-07-27
DE60232559D1 (de) 2009-07-16
DK1379254T3 (da) 2007-10-15
CN1259918C (zh) 2006-06-21
PL211438B1 (pl) 2012-05-31
US7501403B2 (en) 2009-03-10
IL142650A (en) 2007-06-03
HUP0400801A3 (en) 2012-09-28
NO20034609D0 (no) 2003-10-15
US20040121993A1 (en) 2004-06-24
DK1790346T3 (da) 2009-10-12
CZ309042B6 (cs) 2021-12-22
CN1529603A (zh) 2004-09-15
US8110564B2 (en) 2012-02-07
UA78699C2 (en) 2007-04-25
DE60220775T2 (de) 2008-03-06
US20090149537A1 (en) 2009-06-11
EP1379254A1 (en) 2004-01-14
WO2002083147A1 (en) 2002-10-24
MXPA03009553A (es) 2004-05-24
EP1790346A2 (en) 2007-05-30
HUP0400801A2 (hu) 2004-08-30
BR0208924A (pt) 2004-04-20
NO335087B1 (no) 2014-09-08
CA2444266A1 (en) 2002-10-24
AU2007200191B2 (en) 2008-09-04
KR20030092063A (ko) 2003-12-03
AU2002307771B2 (en) 2006-10-19
ES2328966T3 (es) 2009-11-19

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