CA2703688C - Use of bile acid or bile salt fatty acid conjugates - Google Patents

Use of bile acid or bile salt fatty acid conjugates Download PDF

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Publication number
CA2703688C
CA2703688C CA2703688A CA2703688A CA2703688C CA 2703688 C CA2703688 C CA 2703688C CA 2703688 A CA2703688 A CA 2703688A CA 2703688 A CA2703688 A CA 2703688A CA 2703688 C CA2703688 C CA 2703688C
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CA
Canada
Prior art keywords
acid
bile
fatty acid
animals
diet
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
CA2703688A
Other languages
English (en)
French (fr)
Other versions
CA2703688A1 (en
Inventor
Tuvia Gilat
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Galmed Research and Development Ltd
Original Assignee
Galmed International 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
Application filed by Galmed International Ltd filed Critical Galmed International Ltd
Publication of CA2703688A1 publication Critical patent/CA2703688A1/en
Application granted granted Critical
Publication of CA2703688C publication Critical patent/CA2703688C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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

Landscapes

  • 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)
CA2703688A 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates Expired - Lifetime CA2703688C (en)

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
CA2444266A CA2444266C (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CA2444266A Division CA2444266C (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates

Publications (2)

Publication Number Publication Date
CA2703688A1 CA2703688A1 (en) 2002-10-24
CA2703688C true CA2703688C (en) 2012-07-31

Family

ID=11075322

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2703688A Expired - Lifetime CA2703688C (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates
CA2444266A Expired - Lifetime CA2444266C (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2444266A Expired - Lifetime CA2444266C (en) 2001-04-17 2002-04-15 Use of bile acid or bile salt fatty acid conjugates

Country Status (24)

Country Link
US (2) US7501403B2 (https=)
EP (2) EP1379254B1 (https=)
JP (1) JP4324706B2 (https=)
KR (1) KR100883080B1 (https=)
CN (1) CN1259918C (https=)
AT (2) ATE432705T1 (https=)
AU (2) AU2002307771B2 (https=)
BR (1) BR0208924A (https=)
CA (2) CA2703688C (https=)
CY (1) CY1106853T1 (https=)
CZ (2) CZ309042B6 (https=)
DE (2) DE60232559D1 (https=)
DK (2) DK1790346T3 (https=)
EA (1) EA007565B1 (https=)
ES (2) ES2289137T3 (https=)
HU (1) HU230548B1 (https=)
IL (1) IL142650A (https=)
MX (1) MXPA03009553A (https=)
NO (2) NO333910B1 (https=)
NZ (1) NZ528868A (https=)
PL (2) PL211438B1 (https=)
PT (2) PT1379254E (https=)
UA (1) UA78699C2 (https=)
WO (1) WO2002083147A1 (https=)

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
SI2182954T1 (sl) * 2007-07-25 2019-04-30 Medizinische Universitat Graz Uporaba nor-žolčnih kislin pri zdravljenju arterioskleroze
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
US9314444B2 (en) 2009-01-12 2016-04-19 Biokier, Inc. Composition and method for treatment of NASH
US20120157419A1 (en) 2009-02-02 2012-06-21 Tuvia Gilat Methods and compositions for treating alzheimer's disease
US20120202890A1 (en) 2011-02-08 2012-08-09 Nian Wu Polymer-carbohydrate-lipid conjugates
BR112014027204A2 (pt) 2012-05-01 2017-06-27 Catabasis Pharmaceuticals Inc conjugados d ácido graxo de estatina e agonistas fxr; composições e método de usos
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
WO2014084421A1 (en) * 2012-11-29 2014-06-05 Mediplex Corp. 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
SI3077047T1 (sl) * 2013-12-04 2019-09-30 Galmed Research & Development Ltd. Soli aramchola
JP2017519726A (ja) * 2014-06-01 2017-07-20 ガルメッド リサーチ アンド ディベロップメント リミテッド． リポジストロフィー治療用脂肪酸胆汁酸複合体
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

Family Cites Families (14)

* 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
US3856953A (en) * 1973-05-15 1974-12-24 Intellectual Property Dev Corp Method of treating fatty liver
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
US6576660B1 (en) * 1997-10-31 2003-06-10 Arch Development Corporation Methods and compositions for regulation of 5-α-reductase activity
IL123998A (en) * 1998-04-08 2004-09-27 Galmed Int Ltd Conjugates of bile salts and pharmaceutical preparations containing them
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

Also Published As

Publication number Publication date
IL142650A (en) 2007-06-03
DE60220775D1 (de) 2007-08-02
EA007565B1 (ru) 2006-12-29
US20090149537A1 (en) 2009-06-11
CZ2008296A3 (https=) 2004-04-14
EA200301017A1 (ru) 2005-04-28
UA78699C2 (en) 2007-04-25
EP1790346B1 (en) 2009-06-03
ES2328966T3 (es) 2009-11-19
CN1259918C (zh) 2006-06-21
HUP0400801A3 (en) 2012-09-28
EP1790346A2 (en) 2007-05-30
PL205057B1 (pl) 2010-03-31
NO20034609D0 (no) 2003-10-15
HUP0400801A2 (hu) 2004-08-30
ATE432705T1 (de) 2009-06-15
NO335087B1 (no) 2014-09-08
BR0208924A (pt) 2004-04-20
NO20034609L (no) 2003-11-28
US8110564B2 (en) 2012-02-07
DK1379254T3 (da) 2007-10-15
US20040121993A1 (en) 2004-06-24
JP4324706B2 (ja) 2009-09-02
NO333910B1 (no) 2013-10-14
EP1379254A1 (en) 2004-01-14
EP1379254B1 (en) 2007-06-20
AU2007200191B2 (en) 2008-09-04
AU2007200191A1 (en) 2007-02-08
CZ20032710A3 (cs) 2004-04-14
CN1529603A (zh) 2004-09-15
EP1790346A3 (en) 2007-08-22
CA2703688A1 (en) 2002-10-24
CZ309042B6 (cs) 2021-12-22
NZ528868A (en) 2005-09-30
CZ300489B6 (cs) 2009-06-03
CA2444266C (en) 2010-07-27
CA2444266A1 (en) 2002-10-24
NO20131219L (no) 2003-11-28
DK1790346T3 (da) 2009-10-12
ATE365044T1 (de) 2007-07-15
DE60220775T2 (de) 2008-03-06
PT1790346E (pt) 2009-09-04
KR100883080B1 (ko) 2009-02-10
ES2289137T3 (es) 2008-02-01
CY1106853T1 (el) 2012-05-23
KR20030092063A (ko) 2003-12-03
DE60232559D1 (de) 2009-07-16
US7501403B2 (en) 2009-03-10
PT1379254E (pt) 2007-07-10
MXPA03009553A (es) 2004-05-24
HU230548B1 (hu) 2016-11-28
PL366585A1 (en) 2005-02-07
JP2004525962A (ja) 2004-08-26
IL142650A0 (en) 2002-03-10
AU2002307771B2 (en) 2006-10-19
PL211438B1 (pl) 2012-05-31
WO2002083147A1 (en) 2002-10-24

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