AU780988B2 - Alpha V integrin receptor antagonists - Google Patents

Alpha V integrin receptor antagonists Download PDF

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Publication number
AU780988B2
AU780988B2 AU36488/01A AU3648801A AU780988B2 AU 780988 B2 AU780988 B2 AU 780988B2 AU 36488/01 A AU36488/01 A AU 36488/01A AU 3648801 A AU3648801 A AU 3648801A AU 780988 B2 AU780988 B2 AU 780988B2
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AU
Australia
Prior art keywords
acid
nonanoic acid
amino
alkyl
pyrimidin
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.)
Ceased
Application number
AU36488/01A
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English (en)
Other versions
AU3648801A (en
Inventor
Ben C. Askew
Michael J Breslin
Mark E. Duggan
John H. Hutchinson
Robert S. Meissner
Michael A. Patane
James J. Perkins
Thomas G. Steele
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.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU3648801A publication Critical patent/AU3648801A/en
Application granted granted Critical
Publication of AU780988B2 publication Critical patent/AU780988B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU36488/01A 2000-01-24 2001-01-19 Alpha V integrin receptor antagonists Ceased AU780988B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US17779200P 2000-01-24 2000-01-24
US60/177792 2000-01-24
US23046900P 2000-09-06 2000-09-06
US60/230469 2000-09-06
PCT/US2001/001953 WO2001053262A1 (en) 2000-01-24 2001-01-19 Alpha v integrin receptor antagonists

Publications (2)

Publication Number Publication Date
AU3648801A AU3648801A (en) 2001-07-31
AU780988B2 true AU780988B2 (en) 2005-04-28

Family

ID=26873652

Family Applications (1)

Application Number Title Priority Date Filing Date
AU36488/01A Ceased AU780988B2 (en) 2000-01-24 2001-01-19 Alpha V integrin receptor antagonists

Country Status (6)

Country Link
US (2) US6693101B2 (https=)
EP (1) EP1254116A4 (https=)
JP (1) JP2003520271A (https=)
AU (1) AU780988B2 (https=)
CA (1) CA2397665A1 (https=)
WO (1) WO2001053262A1 (https=)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
JP2004510766A (ja) * 2000-10-05 2004-04-08 メルク　エンド　カムパニー　インコーポレーテッド インテグリン受容体アンタゴニスト中間体を調製するための方法
US20040030134A1 (en) * 2001-10-01 2004-02-12 Mcwilliams James Christopher Process for preparation of integrin receptor antagonist intermediates
EP1457205A4 (en) 2001-11-30 2006-07-05 Santen Pharmaceutical Co Ltd INHIBITOR OF ANGIOGENESIS
CA2478317A1 (en) * 2002-03-04 2003-09-18 Medimmune, Inc. Methods of preventing or treating disorders by administering an integrin .alpha.v.beta.3 antagonist in combination with an hmg-coa reductase inhibitor or a bisphosphonate
WO2003075957A1 (en) * 2002-03-04 2003-09-18 Medimmune, Inc. The prevention or treatment of cancer using integrin alphavbeta3 antagonists in combination with other agents
US7285268B2 (en) 2002-11-26 2007-10-23 Pdl Biopharma, Inc. Chimeric and humanized antibodies to α5β1 integrin that modulate angiogenesis
US7276589B2 (en) 2002-11-26 2007-10-02 Pdl Biopharma, Inc. Chimeric and humanized antibodies to α5β1 integrin that modulate angiogenesis
WO2004066956A2 (en) * 2003-01-30 2004-08-12 Medimmune, Inc. Uses of integrin alphavbeta3 antagonists
DK1755659T3 (da) 2004-03-24 2012-02-27 Abbott Biotherapeutics Corp Anvendelse af anti-alfa5beta1-antistoffer til inhibering af kræftcelleproliferation
AU2005229015C1 (en) * 2004-04-02 2013-01-17 The Regents Of The University Of California Methods and compositions for treating and preventing disease associated with alphaVbeta5 integrin
EP2222636B1 (en) 2007-12-21 2013-04-10 Ligand Pharmaceuticals Inc. Selective androgen receptor modulators (sarms) and uses thereof
US20110172217A1 (en) 2008-09-05 2011-07-14 Shionogi & Co., Ltd. Ring-fused morpholine derivative having pi3k-inhibiting activity
EP2456460A4 (en) 2009-07-24 2013-02-20 Univ California METHOD AND COMPOSITIONS FOR TREATING AND PREVENTING DISEASES ASSOCIATED WITH AVB5 INTEGRIN
CN105164107B (zh) * 2012-12-20 2017-12-05 卢庆彬 用于与放射结合使用的放射增敏剂化合物
US8901144B2 (en) * 2013-02-07 2014-12-02 Scifluor Life Sciences, Llc Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
PT2953948T (pt) 2013-02-07 2017-12-12 Scifluor Life Sciences Inc Antagonistas de integrina fluorada
SI3050878T1 (sl) 2013-09-24 2022-01-31 Fujifilm Corporation Nova dušik-vsebujoča spojina ali njena sol ali kovinski kompleks le-te
US10898924B2 (en) * 2014-07-16 2021-01-26 Koninklijke Philips N.V. Tiled CMUT dies with pitch uniformity
US10913736B2 (en) 2014-08-22 2021-02-09 University Of Washington Specific inhibitors of methionyl-tRNA synthetase
US9790222B2 (en) 2015-02-19 2017-10-17 Scifluor Life Sciences, Inc. Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
BR112017020484B1 (pt) 2015-03-25 2023-03-28 Fujifilm Corporation Métodos para fabricar um composto contendo nitrogênio ou sal do mesmo e um complexo metálico, compostos contendo nitrogênio, complexos dos ditos compostos e composições farmacêuticas compreendendo os ditos complexos
US10287259B2 (en) 2016-03-14 2019-05-14 The Penn State Research Foundation Selenazolidine and thiazolidine compounds for treating cancer and other diseases
US10118929B2 (en) * 2016-04-27 2018-11-06 Scifluor Life Sciences, Inc. Nonanoic and decanoic acid derivatives and uses thereof
MX2019001918A (es) 2016-08-15 2019-09-06 Bayer Cropscience Ag Derivados del heterociclo biciclico condensado como agentes de control de plagas.
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
MX394210B (es) 2017-02-28 2025-03-04 Morphic Therapeutic Inc INHIBIDORES DE INTEGRINA AVß6.
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
WO2020047239A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
SI3844162T1 (sl) 2018-08-29 2025-06-30 Morphic Therapeutic, Inc. Zaviralci integrina alfa v beta6
WO2020214834A1 (en) 2019-04-19 2020-10-22 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
WO2024137442A1 (en) 2022-12-21 2024-06-27 Gilead Sciences, Inc. Combination therapy for treating cancer

Family Cites Families (7)

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Publication number Priority date Publication date Assignee Title
US5652363A (en) * 1995-10-05 1997-07-29 C.D. Searle & Co. Pyrido-1,4-oxazinylalkyl-benzamide derivatives
US5952341A (en) 1996-10-30 1999-09-14 Merck & Co., Inc. Integrin antagonists
US5872122A (en) * 1997-10-16 1999-02-16 Monsanto Company Pyrimidinylamidino β-amino acid derivatives useful as inhibitors of platelet aggregation
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
KR20010033248A (ko) * 1997-12-17 2001-04-25 폴락 돈나 엘. 인테그린 수용체 길항제
CN1589145A (zh) 1999-06-02 2005-03-02 麦克公司 αv整联蛋白受体拮抗剂
US7015216B2 (en) * 2000-07-21 2006-03-21 Elan Pharmaceuticals, Inc. Heteroaryl-β-alanine derivatives as alpha 4 integrin inhibitors

Also Published As

Publication number Publication date
US6693101B2 (en) 2004-02-17
US7153862B2 (en) 2006-12-26
CA2397665A1 (en) 2001-07-26
US20040019037A1 (en) 2004-01-29
AU3648801A (en) 2001-07-31
US20010053853A1 (en) 2001-12-20
EP1254116A1 (en) 2002-11-06
JP2003520271A (ja) 2003-07-02
EP1254116A4 (en) 2003-04-23
WO2001053262A1 (en) 2001-07-26

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