CN1318422C - 取代吡唑并嘧啶和噻唑并嘧啶 - Google Patents

取代吡唑并嘧啶和噻唑并嘧啶 Download PDF

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Publication number
CN1318422C
CN1318422C CNB028096886A CN02809688A CN1318422C CN 1318422 C CN1318422 C CN 1318422C CN B028096886 A CNB028096886 A CN B028096886A CN 02809688 A CN02809688 A CN 02809688A CN 1318422 C CN1318422 C CN 1318422C
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CN
China
Prior art keywords
pyrimidine
tetrahydro
pyrazole
methyl
phenyl
Prior art date
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Expired - Fee Related
Application number
CNB028096886A
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English (en)
Chinese (zh)
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CN1507447A (zh
Inventor
M·格尔拉赫
C·毛尔
U·-P·亚古施
B·松德曼
M·福尔
A·P·伊泽尔曼
M·迪森－德格罗特
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Grünenthal GmbH
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Grünenthal GmbH
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Filing date
Publication date
Priority claimed from DE2001112197 external-priority patent/DE10112197A1/de
Priority claimed from DE2001153344 external-priority patent/DE10153344A1/de
Application filed by Grünenthal GmbH filed Critical Grünenthal GmbH
Publication of CN1507447A publication Critical patent/CN1507447A/zh
Application granted granted Critical
Publication of CN1318422C publication Critical patent/CN1318422C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB028096886A 2001-03-14 2002-03-13 取代吡唑并嘧啶和噻唑并嘧啶 Expired - Fee Related CN1318422C (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE10112197.0 2001-03-14
DE2001112197 DE10112197A1 (de) 2001-03-14 2001-03-14 Substituierte Pyrazolo- und Thiazolopyrimidine
DE10153344.6 2001-10-29
DE2001153344 DE10153344A1 (de) 2001-10-29 2001-10-29 Verwendung von substituierten Pyrazolopyrimidinen als Liganden von Nucleosid-Transport-Proteinen und/oder von Purinorezeptoren
PCT/EP2002/002722 WO2002072585A2 (de) 2001-03-14 2002-03-13 Substituierte pyrazolo- und thiazolopyrimidine als analgetika

Publications (2)

Publication Number Publication Date
CN1507447A CN1507447A (zh) 2004-06-23
CN1318422C true CN1318422C (zh) 2007-05-30

Family

ID=26008763

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB028096886A Expired - Fee Related CN1318422C (zh) 2001-03-14 2002-03-13 取代吡唑并嘧啶和噻唑并嘧啶

Country Status (24)

Country Link
US (1) US7135568B2 (enExample)
EP (2) EP1368355B1 (enExample)
JP (1) JP2004527508A (enExample)
KR (1) KR20030082982A (enExample)
CN (1) CN1318422C (enExample)
AT (2) ATE404568T1 (enExample)
AU (1) AU2002302419B2 (enExample)
BR (1) BR0208244A (enExample)
CA (1) CA2440760C (enExample)
CY (1) CY1105507T1 (enExample)
CZ (1) CZ20032474A3 (enExample)
DE (2) DE50212652D1 (enExample)
DK (1) DK1368355T3 (enExample)
ES (2) ES2311920T3 (enExample)
HU (1) HUP0401211A3 (enExample)
IL (2) IL157895A0 (enExample)
MX (1) MXPA03008291A (enExample)
NO (1) NO20034031L (enExample)
NZ (2) NZ528639A (enExample)
PL (1) PL364388A1 (enExample)
PT (1) PT1368355E (enExample)
RU (1) RU2003129060A (enExample)
SK (1) SK11542003A3 (enExample)
WO (1) WO2002072585A2 (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
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PL382706A1 (pl) * 2002-08-26 2007-11-26 Takeda Pharmaceutical Company Limited Związek modulujący receptor wapnia i jego zastosowanie
UA81453C2 (en) * 2003-02-27 2008-01-10 Pyrazolopyridine derivates
GB0404434D0 (en) 2004-02-27 2004-03-31 Novartis Ag Organic compounds
WO2005112936A1 (en) * 2004-05-14 2005-12-01 The Regents Of The University Of Michigan Compositions and methods relating to protein kinase inhibitors
AR050188A1 (es) * 2004-08-03 2006-10-04 Uriach Y Compania S A J Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen
EP1736475A1 (en) * 2005-06-21 2006-12-27 Ferrer Internacional, S.A. Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates
KR100838692B1 (ko) 2007-07-11 2008-06-16 한국화학연구원 7-(3′,4′-디알콕시페닐)-4,5,6,7-테트라히드로피라졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는천식 및 만성폐쇄성 폐질환을 포함한 염증관련 질환,관절염, 아토피 피부염, 암 및 뇌질환의 치료 및 예방을위한 약제학적 조성물
RU2376291C1 (ru) * 2008-05-07 2009-12-20 Андрей Александрович Иващенко ЗАМЕЩЕННЫЕ 3,5-ДИАМИНО-4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 2-АМИНО-3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
RU2374249C1 (ru) * 2008-09-17 2009-11-27 Андрей Александрович Иващенко ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[е ИЛИ d]ПИРАЗОЛО[1,5-а]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТ6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
EA017805B1 (ru) * 2008-01-24 2013-03-29 Андрей Александрович ИВАЩЕНКО 2-АЛКИЛАМИНО-3-АРИЛСУЛЬФОНИЛЦИКЛОАЛКАНО[e ИЛИ d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
RU2369600C1 (ru) * 2008-01-24 2009-10-10 Андрей Александрович Иващенко ЗАМЕЩЕННЫЕ 4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ5-HT6 РЕЦЕПТОРОВ, АКТИВНЫЙ КОМПОНЕНТ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЛЕКАРСТВЕННОЕ СРЕДСТВО И СПОСОБЫ ИХ ПОЛУЧЕНИЯ
JP5584627B2 (ja) * 2008-01-24 2014-09-03 アンドレイ・アレクサンドロビッチ・イワシェンコ 置換されたシクロアルキル［ｅ又はｄ］ピラゾロ［１，５−ａ］ピリミジン−セロトニン５−ＨＴ６受容体のアンタゴニスト、その調製の方法及び使用
JP2012504663A (ja) * 2008-10-06 2012-02-23 アンドレイ・アレクサンドロビッチ・イワシェンコ 置換された３−アリールスルホニル−ピラゾロ［１，５−ａ］ピリミジン、セロトニン５−ＨＴ６受容体アンタゴニスト、その調製のための方法及び使用
EP2379566A2 (en) * 2008-12-22 2011-10-26 Schering Corporation Gamma secretase modulators
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
CN102775412B (zh) * 2012-08-21 2013-05-01 四川大学 一种镇静催眠的化合物及其制备方法和用途
CN102977106B (zh) * 2012-12-12 2014-12-10 中国药科大学 一类具有外周镇痛作用的κ阿片受体激动剂
US10179781B2 (en) * 2013-03-15 2019-01-15 Chromocell Corporation Sodium channel modulators for the treatment of pain
CN105611923B (zh) * 2013-09-10 2019-08-23 卓莫赛尔公司 用于治疗疼痛和糖尿病的钠通道调节剂
WO2016123629A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
CA3002144C (en) 2015-10-16 2024-01-23 Eisai R&D Management Co., Ltd. Ep4 antagonists
WO2018133835A1 (en) * 2017-01-20 2018-07-26 National Institute Of Biological Sciences, Beijing Nucleoside analogue regulating mammalian circadian rhythm
AU2018257332B2 (en) 2017-04-27 2021-11-04 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2018199235A1 (ja) * 2017-04-27 2018-11-01 武田薬品工業株式会社 複素環化合物
CN113354644B (zh) * 2020-03-04 2023-07-04 烟台药物研究所 一类用作dpp-iv抑制剂的吡唑并嘧啶结构的化合物及应用
IL297963A (en) 2020-05-07 2023-01-01 Adorx Therapeutics Ltd Antagonists of the adenosine a2a receptor
CN116023382B (zh) * 2023-02-22 2025-09-23 北京师范大学 一种合成手性四氢吡唑并[1,5-a]嘧啶的方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0398283A1 (en) * 1989-05-16 1990-11-22 Merrell Dow Pharmaceuticals Inc. Excitatory amino acid antagonists
US5426106A (en) * 1992-03-23 1995-06-20 Merck Sharp & Dohme Limited Pyrrolo-pyridazinone derivatives
FR2722786A1 (fr) * 1994-07-20 1996-01-26 Rhone Poulenc Rorer Sa Derives de 4-hydroxy-3-phenyl-indeno(1,2-b)pyridine-2(1h)- one, leur preparation et les medicaments les contenant
US5602144A (en) * 1994-12-15 1997-02-11 Merck Patent Gesellschaft Mit Beschrankter Haftung Thienopyridones
US5789406A (en) * 1994-03-28 1998-08-04 Rhone-Poulenc Rorer S.A. Indeno 1,2-E!pyrazine-4-ones, their preparation and the medicaments containing them

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
US4847256A (en) * 1986-10-16 1989-07-11 American Cyanamid Company 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines
EP0264773A1 (en) 1986-10-16 1988-04-27 American Cyanamid Company 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidines
JP2003288537A (ja) 2000-09-25 2003-10-10 Everyd.Com:Kk 商品宅配システムおよび方法
DE10112197A1 (de) 2001-03-14 2002-09-19 Gruenenthal Gmbh Substituierte Pyrazolo- und Thiazolopyrimidine

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0398283A1 (en) * 1989-05-16 1990-11-22 Merrell Dow Pharmaceuticals Inc. Excitatory amino acid antagonists
US5426106A (en) * 1992-03-23 1995-06-20 Merck Sharp & Dohme Limited Pyrrolo-pyridazinone derivatives
US5789406A (en) * 1994-03-28 1998-08-04 Rhone-Poulenc Rorer S.A. Indeno 1,2-E!pyrazine-4-ones, their preparation and the medicaments containing them
FR2722786A1 (fr) * 1994-07-20 1996-01-26 Rhone Poulenc Rorer Sa Derives de 4-hydroxy-3-phenyl-indeno(1,2-b)pyridine-2(1h)- one, leur preparation et les medicaments les contenant
US5602144A (en) * 1994-12-15 1997-02-11 Merck Patent Gesellschaft Mit Beschrankter Haftung Thienopyridones

Also Published As

Publication number Publication date
CY1105507T1 (el) 2010-04-28
CA2440760C (en) 2010-02-09
NZ528639A (en) 2005-07-29
EP1368355A2 (de) 2003-12-10
JP2004527508A (ja) 2004-09-09
EP1637533A1 (de) 2006-03-22
DK1368355T3 (da) 2006-10-09
RU2003129060A (ru) 2005-04-10
ES2311920T3 (es) 2009-02-16
DE50212652D1 (de) 2008-09-25
US7135568B2 (en) 2006-11-14
PT1368355E (pt) 2006-09-29
NO20034031L (no) 2003-10-21
EP1368355B1 (de) 2006-06-07
ATE328886T1 (de) 2006-06-15
AU2002302419B2 (en) 2007-01-18
ES2263779T3 (es) 2006-12-16
KR20030082982A (ko) 2003-10-23
CA2440760A1 (en) 2002-09-19
HUP0401211A3 (en) 2008-03-28
NO20034031D0 (no) 2003-09-11
CN1507447A (zh) 2004-06-23
EP1637533B1 (de) 2008-08-13
IL157895A (en) 2009-12-24
US20040127508A1 (en) 2004-07-01
ATE404568T1 (de) 2008-08-15
WO2002072585A2 (de) 2002-09-19
DE50207103D1 (en) 2006-07-20
CZ20032474A3 (cs) 2003-12-17
IL157895A0 (en) 2004-03-28
MXPA03008291A (es) 2003-12-11
HK1061034A1 (en) 2004-09-03
BR0208244A (pt) 2004-03-02
NZ540574A (en) 2006-11-30
SK11542003A3 (sk) 2004-07-07
PL364388A1 (en) 2004-12-13
WO2002072585A3 (de) 2003-02-20
HUP0401211A2 (hu) 2004-10-28

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