CA2419033A1 - Traitement du syndrome de la resistance a l'insuline - Google Patents

Traitement du syndrome de la resistance a l'insuline Download PDF

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Publication number
CA2419033A1
CA2419033A1 CA002419033A CA2419033A CA2419033A1 CA 2419033 A1 CA2419033 A1 CA 2419033A1 CA 002419033 A CA002419033 A CA 002419033A CA 2419033 A CA2419033 A CA 2419033A CA 2419033 A1 CA2419033 A1 CA 2419033A1
Authority
CA
Canada
Prior art keywords
ethyl
dihydro
pyrazolo
pyrimidin
sildenafil
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.)
Abandoned
Application number
CA002419033A
Other languages
English (en)
Inventor
Earl Michael Gibbs
David Albert Fryburg
Nandan Parmanand Koppiker
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.)
Pfizer Ltd Great Britain
Original Assignee
Individual
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
Priority claimed from GB0030649A external-priority patent/GB0030649D0/en
Priority claimed from GB0106468A external-priority patent/GB0106468D0/en
Priority claimed from GB0106465A external-priority patent/GB0106465D0/en
Priority claimed from GB0117134A external-priority patent/GB0117134D0/en
Application filed by Individual filed Critical Individual
Publication of CA2419033A1 publication Critical patent/CA2419033A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/28—Insulins
    • 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
    • A61K31/33—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/519—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic 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
    • 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
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Zoology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

L'invention concerne l'utilisation d'un inhibiteur sélectif de cGMP PDE5 ou d'une composition pharmaceutique de celui-ci dans la préparation d'un médicament pour le traitement curatif, palliatif ou prophylactique du syndrome de la résistance à l'insuline, ledit syndrôme étant caractérisé par l'existence concomitante chez un sujet de deux ou plusieurs des éléments suivants: la dyslipidémie; l'hypertension; le diabète sucré de type 2, l'affaiblissement de la tolérance au glucose (IGT) ou des antécédents familiaux de diabète; l'hyperuricémie et/ou la goutte; un état pro-coagulant; l'athérosclérose; ou l'obésité tronculaire. L'inhibiteur ci-dessus peut être utilisé seul ou en combinaison avec d'autres agents pour le traitement du syndrome de la résistance à l'insuline ou des aspects individuels du syndrome de résistance à l'insuline.
CA002419033A 2000-08-11 2001-08-06 Traitement du syndrome de la resistance a l'insuline Abandoned CA2419033A1 (fr)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US22492800P 2000-08-11 2000-08-11
US60/224,928 2000-08-11
GB0030649A GB0030649D0 (en) 2000-12-15 2000-12-15 Treatment of the insulin resistance syndrome
GB0030649.8 2000-12-15
US26608301P 2001-02-02 2001-02-02
US60/266,083 2001-02-02
GB0106465.8 2001-03-15
GB0106468A GB0106468D0 (en) 2001-03-15 2001-03-15 Treatment of diabetes mellitus
GB0106468.2 2001-03-15
GB0106465A GB0106465D0 (en) 2001-03-15 2001-03-15 Treatment of the insulin resistance syndrome
GB0117134A GB0117134D0 (en) 2001-07-13 2001-07-13 Treatment of the insulin resistance syndrome
GB0117134.7 2001-07-13
PCT/IB2001/001428 WO2002013798A2 (fr) 2000-08-11 2001-08-06 Traitement du syndrome de la resistance a l'insuline

Publications (1)

Publication Number Publication Date
CA2419033A1 true CA2419033A1 (fr) 2002-02-21

Family

ID=27546614

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002419033A Abandoned CA2419033A1 (fr) 2000-08-11 2001-08-06 Traitement du syndrome de la resistance a l'insuline

Country Status (9)

Country Link
EP (1) EP1307183A2 (fr)
JP (1) JP2004506009A (fr)
KR (1) KR20030023747A (fr)
CN (1) CN1446084A (fr)
AU (1) AU2001276607A1 (fr)
CA (1) CA2419033A1 (fr)
HU (1) HUP0300725A3 (fr)
IL (1) IL154158A0 (fr)
WO (1) WO2002013798A2 (fr)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA03006936A (es) * 2001-02-02 2003-11-18 Pfizer Tratamiento de diabetes mellitus.
US6933127B2 (en) 2001-07-05 2005-08-23 Eucro European Contract Research Gmbh & Co. Kg Substrate for PP2C
DE10135815A1 (de) * 2001-07-23 2003-02-06 Bayer Ag Verwendung von 2-Alkoxyphenyl-substituierten Imidazotriazinonen
US20030114469A1 (en) * 2001-09-27 2003-06-19 Cohen David Saul Combinations
US7019010B2 (en) 2001-09-27 2006-03-28 Novertis Ag Combinations
EP1444009A1 (fr) * 2001-11-02 2004-08-11 Pfizer Products Inc. Traitement du syndrome de resistance a l'insuline ainsi que du diabete du type 2 au moyen d'inhibiteurs de la phosphodiesterase 9 (pde9)
US20030181461A1 (en) * 2002-01-25 2003-09-25 Lautt Wilfred Wayne Use of phosphodiesterase antagonists to treat insulin resistance
BR0307595A (pt) * 2002-02-07 2005-02-01 Pfizer Uso de inibidores de pde5 tal como sildenafil no tratamento de sìndrome de ovário policìstico
JP2004018524A (ja) * 2002-06-13 2004-01-22 Eucro European Contract Research Gmbh & Co Kg 動脈硬化症を処置するための方法
GB0214784D0 (en) * 2002-06-26 2002-08-07 Pfizer Ltd Novel combination
EP1605925A1 (fr) * 2003-03-17 2005-12-21 Pfizer Products Inc. Traitement du diabete insulino-dependant a l'aide d'inhibiteurs de pde5
CN100439371C (zh) * 2003-04-29 2008-12-03 辉瑞大药厂 可用于治疗高血压的5,7-二氨基吡唑并[4,3-d]嘧啶
EA008596B1 (ru) 2003-04-29 2007-06-29 Пфайзер Инк. 5,7-ДИАМИНОПИРАЗОЛО[4,3-d]ПИРИМИДИНЫ, ПОЛЕЗНЫЕ ПРИ ЛЕЧЕНИИ ГИПЕРТЕНЗИИ
WO2005023253A1 (fr) 2003-09-05 2005-03-17 Altana Pharma Ag Utilisation d'inhibiteurs de pde4 pour le traitement du diabete sucre
US7572799B2 (en) 2003-11-24 2009-08-11 Pfizer Inc Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
DE602005011784D1 (de) 2004-04-07 2009-01-29 Pfizer Pyrazoloä4,3-düpyrimidine
AU2006222060B2 (en) 2005-03-08 2011-09-01 Takeda Gmbh Roflumilast for the treatment of diabetes mellitus
WO2007010337A2 (fr) * 2005-07-15 2007-01-25 Proxomed Medizintechnik Gmbh Utilisation d'inhibiteurs de phosphodiesterase type 5 pour la prevention et le traitement de maladies ou de troubles, et systemes d'administration associes
JP2010502670A (ja) 2006-09-07 2010-01-28 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング 真性糖尿病のための組合せ治療
ES2465216T3 (es) 2007-06-04 2014-06-05 Ben Gurion University Of The Negev Research And Development Authority Compuestos de triarilo y composiciones que comprenden los mismos
AT512084A1 (de) 2011-10-20 2013-05-15 Univ Wien Tech Diazabicyclo- und diazaspiro-alkanderivate als phosphodiesterase-5 inhibitoren
US20130315891A1 (en) 2012-05-25 2013-11-28 Matthew Charles Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
EP2854841B1 (fr) 2012-06-04 2017-02-22 Diamedica Inc. Isoformes de glycosylation de la kallikréine-1 tissulaire d'origine humaine
MX2015006023A (es) * 2012-11-13 2016-03-31 Nusirt Sciences Inc Composiciones y metodos para incrementar el metabolismo energetico.
EP2803362B1 (fr) * 2013-05-14 2017-07-26 SciMar Ltd. Substance sensibilisant à l'insuline hépatique et repas de test pour une sensibilisation à l'insuline
CR20160207A (es) 2013-11-05 2016-08-10 Ben Gurion Univ Of The Negev Res And Dev Authority Compuestos para el tratamiento de la diabetes y las complicaciones que surgen de la misma enfermedad
CN110446501A (zh) 2017-03-09 2019-11-12 代阿麦迪卡股份有限公司 组织激肽释放酶1的剂型
MX2017016930A (es) * 2017-12-19 2019-06-20 Malesil Research & Tech Llc Uso del maleato de sildenafil en el tratamiento de ulceras de pie diabetico.
KR102068299B1 (ko) * 2018-12-21 2020-01-20 한국기초과학지원연구원 Cyp4a 저해 화합물을 유효성분으로 포함하는 대사질환의 예방 또는 치료용 조성물

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GB9511220D0 (en) * 1995-06-02 1995-07-26 Glaxo Group Ltd Solid dispersions
AU722514B2 (en) * 1995-12-28 2000-08-03 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
EP0977756A1 (fr) * 1997-04-25 2000-02-09 Pfizer Limited PYRAZOLOPYRIMIDINONES INHIBANT LA PHOSPHODIESTERASE D'ACIDE GUANOSINE-3'5'-MONOPHOSPHATE CYCLIQUE (cGMP PDE5) S'UTILISANT POUR TRAITER DES DYSFONCTIONS SEXUELLES
IL133575A0 (en) * 1997-06-27 2001-04-30 Fujisawa Pharmaceutical Co Sulfonamide compounds, a method for producing same and pharmaceutical compositions containing same
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CA2368023A1 (fr) * 1999-03-22 2000-09-28 Guixue Yu Composes fusionnes de pyridopyridazine inhibiteurs de la cgmp phosphodiesterase
DE19944161A1 (de) * 1999-09-15 2001-03-22 Bayer Ag Neue Kombination zur Behandlung von sexueller Dysfunktion
DE60007592T2 (de) * 1999-09-30 2004-09-16 Pfizer Products Inc., Groton Bicyclische Pyrrolylamide als Glycogenphosphorylase-Inhibitoren
US6503908B1 (en) * 1999-10-11 2003-01-07 Pfizer Inc Pharmaceutically active compounds
CA2406947A1 (fr) * 2000-04-19 2001-10-25 Johns Hopkins University Procedes de prevention et de traitement des troubles gastro-intestinaux

Also Published As

Publication number Publication date
AU2001276607A1 (en) 2002-02-25
EP1307183A2 (fr) 2003-05-07
HUP0300725A3 (en) 2005-11-28
HUP0300725A2 (hu) 2003-11-28
WO2002013798A3 (fr) 2003-01-23
IL154158A0 (en) 2003-07-31
CN1446084A (zh) 2003-10-01
JP2004506009A (ja) 2004-02-26
WO2002013798A2 (fr) 2002-02-21
KR20030023747A (ko) 2003-03-19

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