EP0934305A4 - Integrin antagonists - Google Patents

Integrin antagonists

Info

Publication number
EP0934305A4
EP0934305A4 EP97938568A EP97938568A EP0934305A4 EP 0934305 A4 EP0934305 A4 EP 0934305A4 EP 97938568 A EP97938568 A EP 97938568A EP 97938568 A EP97938568 A EP 97938568A EP 0934305 A4 EP0934305 A4 EP 0934305A4
Authority
EP
European Patent Office
Prior art keywords
integrin antagonists
integrin
antagonists
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.)
Withdrawn
Application number
EP97938568A
Other languages
German (de)
French (fr)
Other versions
EP0934305A1 (en
Inventor
Mark E Duggan
George D Hartman
William F Hoffman
Robert S Meissner
James J Perkins
Ben C Askew
Paul J Coleman
John H Hutchinson
Adel M Naylor-Olsen
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
Priority claimed from GBGB9703015.9A external-priority patent/GB9703015D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0934305A1 publication Critical patent/EP0934305A1/en
Publication of EP0934305A4 publication Critical patent/EP0934305A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Biophysics (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP97938568A 1996-08-29 1997-08-25 Integrin antagonists Withdrawn EP0934305A4 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US2512396P 1996-08-29 1996-08-29
US25123P 1996-08-29
US3357996P 1996-12-19 1996-12-19
US33579P 1996-12-19
GBGB9703015.9A GB9703015D0 (en) 1997-02-13 1997-02-13 Alpha v B3 antagonists
GB9703015 1997-02-13
US4717797P 1997-05-20 1997-05-20
US47177P 1997-05-20
PCT/US1997/014912 WO1998008840A1 (en) 1996-08-29 1997-08-25 Integrin antagonists

Publications (2)

Publication Number Publication Date
EP0934305A1 EP0934305A1 (en) 1999-08-11
EP0934305A4 true EP0934305A4 (en) 2001-04-11

Family

ID=27451604

Family Applications (1)

Application Number Title Priority Date Filing Date
EP97938568A Withdrawn EP0934305A4 (en) 1996-08-29 1997-08-25 Integrin antagonists

Country Status (5)

Country Link
EP (1) EP0934305A4 (en)
JP (1) JP2002511052A (en)
AU (1) AU724191B2 (en)
CA (1) CA2263999A1 (en)
WO (1) WO1998008840A1 (en)

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US6211191B1 (en) 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists
US6017926A (en) * 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
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EP1065208A1 (en) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Substituted purine derivatives as inhibitors of cell adhesion
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ATE344249T1 (en) 1999-07-19 2006-11-15 Merck Frosst Canada Ltd PYRAZINONES, COMPOSITIONS CONTAINING THESE COMPOUNDS
AU6316900A (en) 1999-08-05 2001-03-05 Meiji Seika Kaisha Ltd. Omega-amino-alpha-hydroxycarboxylic acid derivatives having integrin alphavbeta3antagonism
CA2386030A1 (en) 1999-10-04 2001-04-12 Merck & Co., Inc. Integrin receptor antagonists
IL148841A0 (en) * 1999-10-06 2002-09-12 Basf Ag INHIBITORS OF THE ENDOTHELIN SIGNALLING PATHWAY AND αvβ3 INTEGRIN RECEPTOR ANTAGONISTS FOR COMBINATION THERAPY
US7182953B2 (en) * 1999-12-15 2007-02-27 Celgene Corporation Methods and compositions for the prevention and treatment of atherosclerosis restenosis and related disorders
AU780364B2 (en) 2000-01-20 2005-03-17 Merck Sharp & Dohme Corp. Alpha V integrin receptor antagonists
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
EP1268463B1 (en) 2000-04-05 2005-02-16 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
CA2405306A1 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
JP2004501077A (en) 2000-04-17 2004-01-15 ファルマシア・コーポレーション Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
US6511973B2 (en) 2000-08-02 2003-01-28 Bristol-Myers Squibb Co. Lactam inhibitors of FXa and method
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
EP1351686A2 (en) 2000-11-20 2003-10-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
JP2004518688A (en) 2001-01-30 2004-06-24 ブリストル−マイヤーズ スクイブ カンパニー Factor Xa inhibitor sulfonamide lactam and method thereof
CA2444821C (en) 2001-04-24 2012-07-10 Merck Patent Gesellschaft Mit Beschraenkter Haftung Combination therapy using anti-angiogenic agents and tnfa
WO2003024933A1 (en) * 2001-09-12 2003-03-27 Kaken Pharmaceutical Co., Ltd. 2-phenyl-3-heteroarylpropionic acid derivative or salt thereof and medicine containing the same
US7105559B2 (en) 2001-10-03 2006-09-12 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
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US20030171368A1 (en) * 2002-02-06 2003-09-11 Werner Seitz Pyrimidinonesulfamoylureas`
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WO2007084670A2 (en) 2006-01-18 2007-07-26 Merck Patent Gmbh Specific therapy using integrin ligands for treating cancer
AU2008207095B2 (en) 2007-01-18 2013-08-29 Merck Patent Gmbh Specific therapy and medicament using integrin ligands for treating cancer
US20120130146A1 (en) 2009-05-25 2012-05-24 Merck Patent Gmbh Continuous administration of cilengitide in cancer treatments
HUE063437T2 (en) 2013-09-24 2024-01-28 Fujifilm Corp Pharmaceutical composition of a nitrogen-containing compound or salt thereof, or metal complex thereof
KR20160147007A (en) 2014-05-30 2016-12-21 화이자 인코포레이티드 Carbonitrile derivatives as selective androgen receptor modulators
TW201835078A (en) 2017-02-28 2018-10-01 美商萊築理公司 Inhibitors of [alpha]v[beta]6 integrin
EP3589285A4 (en) 2017-02-28 2020-08-12 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
SG11202101913PA (en) 2018-08-29 2021-03-30 Morphic Therapeutic Inc INHIBITING aV ß6 INTEGRIN
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

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WO1994008577A1 (en) * 1992-10-14 1994-04-28 Merck & Co., Inc. Fibrinogen receptor antagonists
WO1995014683A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Novel isoxazoline and isoxazole fibrinogen receptor antagonists
WO1995014682A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Isoxazoline compounds useful as fibrinogen receptor antagonists
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WO1994008577A1 (en) * 1992-10-14 1994-04-28 Merck & Co., Inc. Fibrinogen receptor antagonists
WO1995014683A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Novel isoxazoline and isoxazole fibrinogen receptor antagonists
WO1995014682A1 (en) * 1993-11-24 1995-06-01 The Du Pont Merck Pharmaceutical Company Isoxazoline compounds useful as fibrinogen receptor antagonists
WO1995017397A1 (en) * 1993-12-20 1995-06-29 Merck & Co., Inc. Fibrinogen receptor antagonists
WO1995018111A1 (en) * 1993-12-28 1995-07-06 The Du Pont Merck Pharmaceutical Company Compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
WO1995032710A1 (en) * 1994-05-27 1995-12-07 Merck & Co., Inc. Compounds for inhibiting osteoclast-mediated bone resorption

Non-Patent Citations (3)

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Title
See also references of WO9808840A1 *
WITYAK,J. ET AL.: "Discovery of Potent Isoxazoline Glycoprotein IIb/IIIa Receptor Antagonists", J.MED.CHEM., vol. 40, no. 1, 3 January 1997 (1997-01-03), WASHINGTON, pages 50 - 60, XP002158237 *
XUE,C.B. ET AL.: "Discovery of an Orally Active Series of Isoxazoline Glycoprotein IIb/IIIa Antagonists", J.MED.CHEM., vol. 40, no. 13, 20 June 1997 (1997-06-20), WASHINGTON, pages 2064.2084, XP002158238 *

Also Published As

Publication number Publication date
CA2263999A1 (en) 1998-03-05
AU4086597A (en) 1998-03-19
AU724191B2 (en) 2000-09-14
JP2002511052A (en) 2002-04-09
WO1998008840A1 (en) 1998-03-05
EP0934305A1 (en) 1999-08-11

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