JP2006505627A - 新規エフェクター接合体、それらの生成方法及びそれらの医薬使用 - Google Patents

新規エフェクター接合体、それらの生成方法及びそれらの医薬使用 Download PDF

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Publication number
JP2006505627A
JP2006505627A JP2005506073A JP2005506073A JP2006505627A JP 2006505627 A JP2006505627 A JP 2006505627A JP 2005506073 A JP2005506073 A JP 2005506073A JP 2005506073 A JP2005506073 A JP 2005506073A JP 2006505627 A JP2006505627 A JP 2006505627A
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JP
Japan
Prior art keywords
dione
dihydroxy
tetramethyl
methyl
dioxa
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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.)
Pending
Application number
JP2005506073A
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English (en)
Japanese (ja)
Inventor
ベルガー，マルクス
シーマイシュテル，ゲルハルト
クラー，ウルリッヒ
ビルダ，ヨルグ
メンラド，アンドレアス
ボスレット，クラウス
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シエーリング アクチエンゲゼルシャフト
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Priority claimed from DE10234975A external-priority patent/DE10234975A1/de
Priority claimed from DE10305098A external-priority patent/DE10305098A1/de
Application filed by シエーリング アクチエンゲゼルシャフト filed Critical シエーリング アクチエンゲゼルシャフト
Publication of JP2006505627A publication Critical patent/JP2006505627A/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
    • A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00—Antineoplastic 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Cell Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
JP2005506073A 2002-07-31 2003-07-31 新規エフェクター接合体、それらの生成方法及びそれらの医薬使用 Pending JP2006505627A (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10234975A DE10234975A1 (de) 2002-07-31 2002-07-31 Neue Effektor-Konjugate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
DE10305098A DE10305098A1 (de) 2003-02-07 2003-02-07 Neue Effektor-Konjugate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
US45167303P 2003-03-05 2003-03-05
PCT/EP2003/008483 WO2004012735A2 (fr) 2002-07-31 2003-07-31 Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci

Publications (1)

Publication Number Publication Date
JP2006505627A true JP2006505627A (ja) 2006-02-16

Family

ID=31498923

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2005506073A Pending JP2006505627A (ja) 2002-07-31 2003-07-31 新規エフェクター接合体、それらの生成方法及びそれらの医薬使用

Country Status (16)

Country Link
EP (1) EP1524979A2 (fr)
JP (1) JP2006505627A (fr)
KR (1) KR20050026033A (fr)
AU (1) AU2003253365A1 (fr)
BR (1) BR0313043A (fr)
CA (1) CA2492437A1 (fr)
CO (1) CO5700741A2 (fr)
EC (1) ECSP055626A (fr)
HR (1) HRP20050186A2 (fr)
IL (1) IL166039A0 (fr)
IS (1) IS7708A (fr)
MX (1) MXPA05001282A (fr)
NO (1) NO20051038L (fr)
NZ (1) NZ537870A (fr)
PL (1) PL374528A1 (fr)
WO (1) WO2004012735A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006511469A (ja) * 2002-09-13 2006-04-06 ノバルティス アクチエンゲゼルシャフト エポチロン誘導体の新規製造方法、新規エポチロン誘導体ならびに当該製造方法のための中間体およびそれらの製造方法

Families Citing this family (21)

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Publication number Priority date Publication date Assignee Title
EP1161430A2 (fr) * 1999-02-11 2001-12-12 Schering Aktiengesellschaft Derives d'epothilone, leur procede de production et leur utilisation pharmaceutique
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
CN1759115A (zh) 2002-08-23 2006-04-12 索隆-基特林癌症研究协会 埃坡霉素(epothilone),合成埃坡霉素的中间体,其类似物及其用途
DE10256982A1 (de) 2002-12-05 2004-06-24 Schering Ag Neue Effektor-Konjugate, Verfahren zu Ihrer Herstellung und Ihre Pharmazeutische Verwendung
JP2006510626A (ja) * 2002-12-05 2006-03-30 シエーリング アクチエンゲゼルシャフト 増殖疾患の処理における部位特異的供給のためのエポチロン類似体
DE602005003453T2 (de) * 2004-01-30 2008-09-25 Bayer Schering Pharma Aktiengesellschaft Neue effektor-konjugate, verfahren zu ihrer herstellung und ihre pharmazeutische verwendung
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
WO2006012527A1 (fr) 2004-07-23 2006-02-02 Endocyte, Inc. Groupes de liaison bivalents et conjugués de ceux-ci
AR061181A1 (es) 2006-05-25 2008-08-13 Bristol Myers Squibb Co Compuestos de aziridinil-epotilona
PE20080102A1 (es) * 2006-05-25 2008-02-11 Bristol Myers Squibb Co Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos
CN101678124A (zh) 2007-03-14 2010-03-24 恩多塞特公司 结合配体连接的微管溶素递药缀合物
EP2152717A1 (fr) 2007-05-25 2010-02-17 Bristol-Myers Squibb Company Procedes de fabrication de composes et d'analogues d'epothilone
EP3569251A1 (fr) 2007-06-25 2019-11-20 Endocyte, Inc. Conjugués contenant des lieurs espaceurs hydrophiles
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
CA2703491C (fr) 2007-10-25 2017-06-13 Endocyte, Inc. Tubulysines et leurs procedes de preparation
IT1401451B1 (it) * 2010-06-10 2013-07-26 Chemi Spa Nuovo processo di preparazione di 2-idrossi-4-fenil-3,4-diidro-2h-cromen-6-il-metanolo e (r)-2-[3-(diisopropilammino)-1-fenilpropil]-4-(idrossimetil)fenolo.
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
AU2013331440A1 (en) 2012-10-16 2015-04-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
MX2019004434A (es) * 2016-10-17 2019-09-26 Pfizer Anticuerpos anti-edb y conjugados anticuerpo-fármaco.
KR102377416B1 (ko) * 2017-06-30 2022-03-21 엘지디스플레이 주식회사 표시장치

Family Cites Families (10)

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Publication number Priority date Publication date Assignee Title
DK130984A (da) * 1983-03-07 1984-09-08 Smithkline Beckman Corp Leukotrien-antagonister
IL107400A0 (en) * 1992-11-10 1994-01-25 Cortech Inc Bradykinin antagonists
US5942555A (en) * 1996-03-21 1999-08-24 Surmodics, Inc. Photoactivatable chain transfer agents and semi-telechelic photoactivatable polymers prepared therefrom
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
AU2001243372A1 (en) * 2000-03-01 2001-09-12 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
NZ546497A (en) * 2000-04-28 2008-04-30 Kosan Biosciences Inc Production of polyketides
US6441213B1 (en) * 2000-05-18 2002-08-27 National Starch And Chemical Investment Holding Corporation Adhesion promoters containing silane, carbamate or urea, and donor or acceptor functionality
AU2001266583A1 (en) * 2000-05-26 2001-12-11 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same
DE10041221A1 (de) * 2000-08-22 2002-03-14 Deutsches Krebsforsch Verfahren zur Herstellung von wasserlöslichen Saccharidkonjugaten und Saccharidmimetika durch Diels-Alder-Reaktion und ihre Verwendung als Therapeutika oder Diagnostika
GB0116143D0 (en) * 2001-07-02 2001-08-22 Amersham Pharm Biotech Uk Ltd Chemical capture reagent

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006511469A (ja) * 2002-09-13 2006-04-06 ノバルティス アクチエンゲゼルシャフト エポチロン誘導体の新規製造方法、新規エポチロン誘導体ならびに当該製造方法のための中間体およびそれらの製造方法

Also Published As

Publication number Publication date
MXPA05001282A (es) 2005-04-28
BR0313043A (pt) 2005-06-14
ECSP055626A (es) 2005-04-18
WO2004012735A3 (fr) 2004-05-27
EP1524979A2 (fr) 2005-04-27
NZ537870A (en) 2007-03-30
IS7708A (is) 2005-02-23
KR20050026033A (ko) 2005-03-14
CO5700741A2 (es) 2006-11-30
PL374528A1 (en) 2005-10-31
NO20051038L (no) 2005-04-06
IL166039A0 (en) 2006-01-15
HRP20050186A2 (en) 2005-10-31
WO2004012735A2 (fr) 2004-02-12
CA2492437A1 (fr) 2004-02-12
AU2003253365A1 (en) 2004-02-23

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