DE60108759T2 - Tetrahydro-heterocycloazepinyl-pyrimidin-derivate - Google Patents

Tetrahydro-heterocycloazepinyl-pyrimidin-derivate Download PDF

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Publication number
DE60108759T2
DE60108759T2 DE60108759T DE60108759T DE60108759T2 DE 60108759 T2 DE60108759 T2 DE 60108759T2 DE 60108759 T DE60108759 T DE 60108759T DE 60108759 T DE60108759 T DE 60108759T DE 60108759 T2 DE60108759 T2 DE 60108759T2
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Prior art keywords
methyl
formula
nitro
pyrimidin
azepin
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Expired - Lifetime
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DE60108759T
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German (de)
English (en)
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DE60108759D1 (de
Inventor
Alfred Binggeli
Hans-Peter Maerki
Vincent Mutel
Wolfgang Wostl
Maurice Wilhelm
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Obesity (AREA)
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  • Hematology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
DE60108759T 2000-07-18 2001-07-16 Tetrahydro-heterocycloazepinyl-pyrimidin-derivate Expired - Lifetime DE60108759T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00115450 2000-07-18
EP00115450 2000-07-18
PCT/EP2001/008186 WO2002006288A1 (en) 2000-07-18 2001-07-16 Tetrahydro-heterocycloazepinyl pyrimidine derivatives

Publications (2)

Publication Number Publication Date
DE60108759D1 DE60108759D1 (de) 2005-03-10
DE60108759T2 true DE60108759T2 (de) 2006-05-11

Family

ID=8169290

Family Applications (1)

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DE60108759T Expired - Lifetime DE60108759T2 (de) 2000-07-18 2001-07-16 Tetrahydro-heterocycloazepinyl-pyrimidin-derivate

Country Status (17)

Country Link
US (1) US6369222B1 (enExample)
EP (1) EP1303521B1 (enExample)
JP (1) JP4060705B2 (enExample)
KR (1) KR100525214B1 (enExample)
CN (1) CN1187358C (enExample)
AR (1) AR031715A1 (enExample)
AT (1) ATE288437T1 (enExample)
AU (2) AU2002210418B2 (enExample)
BR (1) BR0112586A (enExample)
CA (1) CA2415966C (enExample)
DE (1) DE60108759T2 (enExample)
DK (1) DK1303521T3 (enExample)
ES (1) ES2236317T3 (enExample)
MX (1) MXPA03000428A (enExample)
PT (1) PT1303521E (enExample)
WO (1) WO2002006288A1 (enExample)
ZA (1) ZA200300163B (enExample)

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EP1074549B1 (en) * 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
DE10238722A1 (de) 2002-08-23 2004-03-11 Bayer Ag Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse
US20040215284A1 (en) * 2003-01-30 2004-10-28 Recordati S.A. Treatment of neuromuscular dysfunction of the lower urinary tract with selective mGlu5 antagonists
DE10320785A1 (de) 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Arylmethyl-substituierte Pyrazolopyrimidine
DE10328479A1 (de) 2003-06-25 2005-01-13 Bayer Ag 6-Arylamino-5-cyano-4-pyrimidinone
DE102004001873A1 (de) 2004-01-14 2005-09-29 Bayer Healthcare Ag Cyanopyrimidinone
DE102004019708A1 (de) * 2004-04-20 2005-11-17 Basf Ag Offenzellige Schaumstoffe und Verfahren zu ihrer Herstellung
KR101216984B1 (ko) * 2004-06-30 2013-01-02 아더시스 인코포레이티드 세로토닌 수용체 조절자로서의 치환된 아제핀 유도체
US7459448B2 (en) 2004-10-04 2008-12-02 Millennium Pharmaceuticals, Inc. Lactam compounds useful as protein kinase inhibitors
WO2007072095A1 (en) * 2005-12-20 2007-06-28 Richter Gedeon Nyrt. New compounds
PE20080145A1 (es) 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
CA2694359A1 (en) * 2007-08-02 2009-02-05 Recordati Ireland Limited Novel heterocyclic compounds as mglu5 antagonists
JP5498392B2 (ja) 2007-11-30 2014-05-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １，５−ジヒドロ−ピラゾロ［３，４−ｄ］ピリミジン−４−オン誘導体及びｃｎｓ障害の治療のためのｐｄｅ９ａモジュレーターとしてのそれらの使用
JP5562865B2 (ja) 2007-12-17 2014-07-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｔｒｐｖ１のイミダゾロ−、オキサゾロ−、及びチアゾロピリミジン・モジュレーター
UA105362C2 (en) 2008-04-02 2014-05-12 Бьорингер Ингельхайм Интернациональ Гмбх 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
EA201100446A1 (ru) 2008-09-08 2011-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Пиразолопиримидины и их применение для лечения нарушений цнс
JP5684719B2 (ja) 2008-12-05 2015-03-18 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｐｌｋ阻害剤としての５，７−ジヒドロ−６ｈ−ピリミド［５、−４ｄ］［１］ベンゾアゼピン−６−チオン
US20100317630A1 (en) * 2009-02-04 2010-12-16 Recordati Ireland Limited Novel heterocyclic compounds as mglu5 antagonists
WO2010112437A1 (en) 2009-03-31 2010-10-07 Boehringer Ingelheim International Gmbh 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
US20120028931A1 (en) 2009-09-14 2012-02-02 Recordati Ireland Limited Heterocyclic m-glu5 antagonists
ES2492694T3 (es) 2010-07-09 2014-09-10 Recordati Ireland Limited Nuevos compuestos espiroheterocíclicos como antagonistas de mGlu5
AU2011288503C1 (en) 2010-08-12 2015-08-06 Boehringer Ingelheim International Gmbh 6-Cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as PDE9A inhibitors
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
US8822464B2 (en) 2011-11-28 2014-09-02 Boehringer Ingelheim International Gmbh N-aryl-piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors
US8741892B2 (en) 2011-12-05 2014-06-03 Boehringer Ingelheim International Gmbh Compounds
US8846948B2 (en) 2011-12-13 2014-09-30 Boehringer Ingelheim International Gmbh Compounds
US8796467B2 (en) * 2011-12-13 2014-08-05 Boehringer Ingelheim International Gmbh Compounds
US8716277B2 (en) 2011-12-14 2014-05-06 Boehringer Ingelheim International Gmbh Substituted imidazole compounds useful as positive allosteric modulators of mGlu5 receptor activity
US8937176B2 (en) 2011-12-14 2015-01-20 Boehringer Ingelheim International Gmbh Compounds
US8883789B2 (en) 2011-12-14 2014-11-11 Boehringer Ingelheim International Gmbh Piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors
US8889677B2 (en) 2012-01-17 2014-11-18 Boehringer Ingellheim International GmbH Substituted triazoles useful as mGlu5 receptor modulators

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US3940395A (en) * 1969-08-29 1976-02-24 American Home Products Corporation 4-Amino-2-phenyl-6-thiopryimidines
BG17785A3 (bg) * 1970-08-14 1973-12-25 Dr. Karl Thomae Gmbh Метод за получаване на нови азетинови производни
BE790287A (fr) * 1971-10-28 1973-04-19 Delalande Sa Acides pyrimidin-6yl acethydroxamiques, leur procede de preparation et leur application en therapeutique
FR2608607B1 (fr) 1986-12-23 1989-04-28 Sanofi Sa Procede de preparation de thienylethylamines et dithienylethylamines ainsi obtenues
DE3820775A1 (de) 1988-06-20 1989-12-21 Thomae Gmbh Dr K Neue 4,5,7,8-tetrahydro-6h-thiazolo(5,4,-d)azepine, ihre herstellung und ihre verwendung als arzneimittel
BR9107070A (pt) * 1990-11-06 1994-05-31 Pfizer Processo para a preparação de derivados de quinazolina uteis para melhorar a atividade antitumoral.

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JP2004504324A (ja) 2004-02-12
AR031715A1 (es) 2003-10-01
EP1303521B1 (en) 2005-02-02
CA2415966C (en) 2009-10-27
CN1187358C (zh) 2005-02-02
PT1303521E (pt) 2005-05-31
US20020045635A1 (en) 2002-04-18
DE60108759D1 (de) 2005-03-10
CA2415966A1 (en) 2002-01-24
AU2002210418B2 (en) 2006-08-17
AU1041802A (en) 2002-01-30
JP4060705B2 (ja) 2008-03-12
WO2002006288A1 (en) 2002-01-24
CN1441804A (zh) 2003-09-10
KR20030015397A (ko) 2003-02-20
ATE288437T1 (de) 2005-02-15
MXPA03000428A (es) 2003-06-24
KR100525214B1 (ko) 2005-11-01
US6369222B1 (en) 2002-04-09
BR0112586A (pt) 2003-05-20
ES2236317T3 (es) 2005-07-16
EP1303521A1 (en) 2003-04-23
DK1303521T3 (da) 2005-06-13
ZA200300163B (en) 2004-04-07

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