WO2003002114A3 - Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis - Google Patents

Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis Download PDF

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Publication number
WO2003002114A3
WO2003002114A3 PCT/IB2002/003303 IB0203303W WO03002114A3 WO 2003002114 A3 WO2003002114 A3 WO 2003002114A3 IB 0203303 W IB0203303 W IB 0203303W WO 03002114 A3 WO03002114 A3 WO 03002114A3
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WO
WIPO (PCT)
Prior art keywords
potent
selective
non toxic
inhibitor
mastocytosis
Prior art date
Application number
PCT/IB2002/003303
Other languages
French (fr)
Other versions
WO2003002114A2 (en
Inventor
Alain Moussy
Jean-Pierre Kinet
Original Assignee
Ab Science
Alain Moussy
Jean-Pierre Kinet
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 Ab Science, Alain Moussy, Jean-Pierre Kinet filed Critical Ab Science
Priority to EP02755513A priority Critical patent/EP1401429A2/en
Priority to US10/482,179 priority patent/US20050054617A1/en
Priority to CA002452171A priority patent/CA2452171A1/en
Priority to JP2003508353A priority patent/JP2005503361A/en
Publication of WO2003002114A2 publication Critical patent/WO2003002114A2/en
Publication of WO2003002114A3 publication Critical patent/WO2003002114A3/en

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    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/01—Hydrocarbons
    • A61K31/015—Hydrocarbons carbocyclic
    • 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
    • A61K31/095—Sulfur, selenium, or tellurium compounds, e.g. thiols
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/66—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70596—Molecules with a "CD"-designation not provided for elsewhere in G01N2333/705

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

The present invention relates to a method for treating mastocytosis comprising administering a tyrosine kinase inhibitor to a human in need of such treatment, more particularly a non toxic, potent and selective c-kit inhibitor, wherein said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3. The invention also contemplates a composition for topical application comprising said inhibitor for treating category I mastocytosis.
PCT/IB2002/003303 2001-06-29 2002-06-28 Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis WO2003002114A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP02755513A EP1401429A2 (en) 2001-06-29 2002-06-28 Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis
US10/482,179 US20050054617A1 (en) 2001-06-29 2002-06-28 Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis
CA002452171A CA2452171A1 (en) 2001-06-29 2002-06-28 Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis
JP2003508353A JP2005503361A (en) 2001-06-29 2002-06-28 Use of potent, selective and non-toxic c-kit inhibitors for the treatment of mastocytosis

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30140601P 2001-06-29 2001-06-29
US60/301,406 2001-06-29

Publications (2)

Publication Number Publication Date
WO2003002114A2 WO2003002114A2 (en) 2003-01-09
WO2003002114A3 true WO2003002114A3 (en) 2003-09-25

Family

ID=23163206

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2002/003303 WO2003002114A2 (en) 2001-06-29 2002-06-28 Use of potent, selective and non toxic c-kit inhibitors for treating mastocytosis

Country Status (5)

Country Link
US (1) US20050054617A1 (en)
EP (1) EP1401429A2 (en)
JP (1) JP2005503361A (en)
CA (1) CA2452171A1 (en)
WO (1) WO2003002114A2 (en)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE330608T1 (en) * 2001-06-29 2006-07-15 Ab Science THE USE OF N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES
ATE343415T1 (en) * 2001-06-29 2006-11-15 Ab Science THE USE OF C-KIT INHIBITORS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE
CA2452368A1 (en) * 2001-06-29 2003-01-09 Ab Science New potent, selective and non toxic c-kit inhibitors
EP1401413B1 (en) 2001-06-29 2006-11-22 AB Science Use of tyrosine kinase inhibitions for treating allergic diseases
EP1401412A2 (en) * 2001-06-29 2004-03-31 AB Science Use of potent, selective and non toxic c-kit inhibitors for treating tumor angiogenesis
EP1461032B1 (en) * 2001-09-20 2008-07-16 AB Science Use of c-kit inhibitors for promoting hair growth
DE60228278D1 (en) * 2001-09-20 2008-09-25 Ab Science THE USE OF POTENTIALS, SELECTIVE AND NONTOXIC C-THICKNESSES FOR THE TREATMENT OF INTERSTITIAL BUBBLE IGNITION
ATE334693T1 (en) * 2002-02-27 2006-08-15 Ab Science USE OF TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CNS DISEASES
US8450302B2 (en) 2002-08-02 2013-05-28 Ab Science 2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors
PT1525200E (en) 2002-08-02 2008-01-10 Ab Science 2-(3-aminoaryl)amino-4-aryl-thiazoles and their use as c-kit inhibitors
WO2004029204A2 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
CA2517308A1 (en) * 2003-02-27 2004-09-10 Ab Science Tailored treatment suitable for different forms of mastocytosis
EP1473039A1 (en) * 2003-05-02 2004-11-03 Centre National De La Recherche Scientifique (Cnrs) Use of inhibitors and antisense oligonucleotides of BTK for the treatment of proliferative mastocytosis
DK1684750T3 (en) 2003-10-23 2010-08-09 Ab Science 2-aminoaryloxazole compounds as tyrosine kinase inhibitors
KR101153647B1 (en) 2003-11-18 2012-06-18 노파르티스 아게 Inhibitors of the mutant form of kit
CN101217954B (en) 2005-04-04 2013-07-10 Ab科学公司 Substituted oxazole derivatives and their use as tyrosine kinase inhibitors
RU2445960C2 (en) * 2005-05-02 2012-03-27 Новартис Аг Use of pyrimidylaminobenzamide derivatives for treating systemic mastocytosis
AU2006257919A1 (en) * 2005-06-09 2006-12-21 Bristol-Myers Squibb Company Methods of identifying and treating individuals exhibiting mutant kit protein
AU2006271652B2 (en) * 2005-07-20 2010-04-29 Peter Valent Compositions for treatment of systemic mastocytosis
US20090281115A1 (en) * 2006-06-30 2009-11-12 Board of Regents, The University of Texas System, a Texas University Inhibitors of c-kit and uses thereof
MX2009008665A (en) 2007-02-13 2009-08-21 Ab Science Process for the synthesis of 2-aminothiazole compounds as kinase inhibitors.
US20140147415A1 (en) * 2010-11-05 2014-05-29 Ab Science Treatment of mastocytosis with masitinib
US10045978B2 (en) 2010-11-05 2018-08-14 Ab Science Treatment of mastocytosis with masitinib
BR112014001977A2 (en) 2011-07-27 2017-02-21 Ab Science selective protein kinase inhibitors
CA3089630A1 (en) * 2018-01-31 2019-08-08 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
SG11202007198WA (en) 2018-01-31 2020-08-28 Deciphera Pharmaceuticals Llc Combination therapy for the treatment of gastrointestinal stromal tumors
CN114364798A (en) 2019-03-21 2022-04-15 欧恩科斯欧公司 Combination of Dbait molecules with kinase inhibitors for the treatment of cancer
MX2022001863A (en) 2019-08-12 2022-05-30 Deciphera Pharmaceuticals Llc Ripretinib for treating gastrointestinal stromal tumors.
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
KR20220123058A (en) 2019-12-30 2022-09-05 데시페라 파마슈티칼스, 엘엘씨. 1-(4-Bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl ) -3-Phenylurea composition
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

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WO2001047517A1 (en) * 1999-12-29 2001-07-05 The Trustees Of Columbia University In The City Of New York Methods for inhibiting mastocytosis

Patent Citations (2)

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WO2001045689A2 (en) * 1999-12-22 2001-06-28 Sugen, Inc. Indolinone derivatives for modulation of c-kit tyrosine protein kinase
WO2001047517A1 (en) * 1999-12-29 2001-07-05 The Trustees Of Columbia University In The City Of New York Methods for inhibiting mastocytosis

Non-Patent Citations (2)

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Title
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MA YONGSHENG ET AL: "Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells.", JOURNAL OF INVESTIGATIVE DERMATOLOGY, vol. 114, no. 2, February 2000 (2000-02-01), pages 392 - 394, XP001127437, ISSN: 0022-202X *

Also Published As

Publication number Publication date
US20050054617A1 (en) 2005-03-10
CA2452171A1 (en) 2003-01-09
JP2005503361A (en) 2005-02-03
EP1401429A2 (en) 2004-03-31
WO2003002114A2 (en) 2003-01-09

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