CN1263757C - 特异于腺苷a1,a2a和a3受体的化合物及其应用 - Google Patents

特异于腺苷a1,a2a和a3受体的化合物及其应用 Download PDF

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Publication number
CN1263757C
CN1263757C CNB018224601A CN01822460A CN1263757C CN 1263757 C CN1263757 C CN 1263757C CN B018224601 A CNB018224601 A CN B018224601A CN 01822460 A CN01822460 A CN 01822460A CN 1263757 C CN1263757 C CN 1263757C
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compound
disease
treatment
amino
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CN1489590A (zh
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阿林多·L·卡斯特利亚诺
布里安·麦吉本
戴维·J·威特
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OSI Pharmaceuticals LLC
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OSI Pharmaceuticals LLC
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Priority claimed from US09/728,616 external-priority patent/US7160890B2/en
Priority claimed from US09/728,316 external-priority patent/US6680322B2/en
Priority claimed from US09/728,607 external-priority patent/US6664252B2/en
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Publication of CN1489590A publication Critical patent/CN1489590A/zh
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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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/08—Bronchodilators
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/14—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
    • A—HUMAN NECESSITIES
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    • 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]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
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    • 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
    • A61P9/06—Antiarrhythmics
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CNB018224601A 2000-12-01 2001-11-30 特异于腺苷a1,a2a和a3受体的化合物及其应用 Expired - Fee Related CN1263757C (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US09/728,316 2000-12-01
US09/728,607 2000-12-01
US09/728,616 US7160890B2 (en) 1999-12-02 2000-12-01 Compounds specific to adenosine A3 receptor and uses thereof
US09/728,316 US6680322B2 (en) 1999-12-02 2000-12-01 Compounds specific to adenosine A1 receptors and uses thereof
US09/728,616 2000-12-01
US09/728,607 US6664252B2 (en) 1999-12-02 2000-12-01 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof

Publications (2)

Publication Number Publication Date
CN1489590A CN1489590A (zh) 2004-04-14
CN1263757C true CN1263757C (zh) 2006-07-12

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CNB018224601A Expired - Fee Related CN1263757C (zh) 2000-12-01 2001-11-30 特异于腺苷a1,a2a和a3受体的化合物及其应用

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Country Link
EP (1) EP1347980A4 (de)
JP (1) JP4579497B2 (de)
CN (1) CN1263757C (de)
AP (1) AP1893A (de)
AU (1) AU2002248151B2 (de)
BR (1) BR0115847A (de)
CA (1) CA2430577A1 (de)
CZ (1) CZ20031831A3 (de)
EA (1) EA007254B1 (de)
HU (1) HUP0400692A3 (de)
IL (1) IL155962A0 (de)
ME (1) MEP35308A (de)
MX (1) MXPA03004717A (de)
NO (1) NO327207B1 (de)
NZ (1) NZ525885A (de)
OA (1) OA13295A (de)
PL (1) PL363245A1 (de)
WO (1) WO2002057267A1 (de)
YU (1) YU42703A (de)
ZA (1) ZA200303729B (de)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104350056A (zh) * 2012-06-07 2015-02-11 霍夫曼-拉罗奇有限公司 端锚聚合酶的吡咯并嘧啶酮和吡咯并吡啶酮抑制剂
CN105473581A (zh) * 2013-06-21 2016-04-06 齐尼思表观遗传学公司 作为溴结构域抑制剂的新取代的双环化合物
US10010556B2 (en) 2013-06-21 2018-07-03 Zenith Epigenetics Ltd. Bicyclic bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CN110128316A (zh) * 2019-05-22 2019-08-16 北京大学深圳研究生院 5位取代的β-脯氨酸及其衍生物的制备方法
US10500209B2 (en) 2013-07-31 2019-12-10 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors

Families Citing this family (30)

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US5090531A (en) * 1990-01-10 1992-02-25 Lord Corporation Electrophoretic fluid differential
CZ302486B6 (cs) 1998-06-02 2011-06-15 Osi Pharmaceuticals, Inc. N-6-Substituovaný 7-deazapurin, zpusob jeho prípravy a farmaceutická kompozice s jeho obsahem
US6680324B2 (en) 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
DE10148883A1 (de) * 2001-10-04 2003-04-10 Merck Patent Gmbh Pyrimidinderivate
EP1450811B1 (de) * 2001-11-30 2009-10-21 OSI Pharmaceuticals, Inc. Verbindungen, die für Adenosin A1 und A3 Rezeptoren spezifisch sind, und deren Anwendungen
CA2469316A1 (en) * 2001-12-07 2003-06-19 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as gsk-3 inhibitors
EA011809B1 (ru) 2001-12-20 2009-06-30 Оси Фармасьютикалз, Инк. Пиримидиновые соединения, их применение в качестве a-селективных антагонистов и способ их получения
CN1816551A (zh) 2001-12-20 2006-08-09 Osi药物公司 吡咯并嘧啶A2b选择性拮抗剂化合物,它们的合成及用途
CA2502429A1 (en) * 2002-10-31 2004-05-21 Amgen Inc. Antiinflammation agents
HUP0203976A3 (en) * 2002-11-15 2004-08-30 Sanofi Aventis Adenozine a3 receptors, process for their preparation and pharmaceutical compositions containing them
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
EP3421471B1 (de) 2006-04-25 2021-05-26 Astex Therapeutics Limited Purin- und deazapurinderivate als pharmazeutische verbindungen
US20070260203A1 (en) * 2006-05-04 2007-11-08 Allergan, Inc. Vasoactive agent intraocular implant
TW200808819A (en) * 2006-06-19 2008-02-16 Solvay Pharm Gmbh Use of adenosine A1 antagonists in radiocontrast media induced nephrophaty
WO2009047563A1 (en) 2007-10-11 2009-04-16 Astrazeneca Ab Pyrrolo [2, 3 -d] pyrimidin derivatives as protein kinase b inhibitors
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
EP2247596A2 (de) 2008-01-11 2010-11-10 Natco Pharma Limited Neuartige pyrazol-[3,4-d-]pyrimidin-derivate als wirkstoffe gegen krebs
SI2694056T1 (sl) 2011-04-01 2019-12-31 Astrazeneca Ab Terapevtsko zdravljenje
DK2785349T4 (da) 2011-11-30 2023-01-09 Astrazeneca Ab Kombinationsbehandling af cancer
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
CN108349977B (zh) * 2015-01-20 2021-05-25 无锡福祈制药有限公司 Jak抑制剂
KR102006684B1 (ko) 2015-04-29 2019-08-02 우시 포춘 파마슈티컬 컴퍼니 리미티드 Jak 억제제
CA2983481C (en) 2015-05-29 2020-04-14 Wuxi Fortune Pharmaceutical Co., Ltd Janus kinase inhibitor
CN105771672B (zh) * 2016-04-18 2018-03-02 天津工业大学 一种抗污染抗菌芳香聚酰胺反渗透复合膜及制备方法
CN108570054B (zh) * 2017-03-07 2021-07-16 广州再极医药科技有限公司 氨基嘧啶并五元杂环化合物、其中间体、制备方法、药物组合物及应用
CN108017584B (zh) * 2017-06-20 2021-03-23 南开大学 A3腺苷受体的小分子拮抗剂
KR20210033444A (ko) * 2018-06-04 2021-03-26 엑스사이언티아 엘티디 아데노신 수용체 길항제로서 피라졸로피리미딘 화합물
CN110272373B (zh) * 2019-07-02 2022-07-29 天津国际生物医药联合研究院 一种具有选择性的腺苷a1受体拮抗剂及其应用
CN114085178A (zh) * 2021-12-29 2022-02-25 苏州楚凯药业有限公司 一种4-甲基-1-丙基-2-氨基-1h-吡咯-3-腈的制备方法

Family Cites Families (5)

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JP2895961B2 (ja) * 1992-12-17 1999-05-31 フアイザー・インコーポレイテツド Ｃｒｆアンタゴニストとしてのピロロピリミジン
US5780450A (en) * 1995-11-21 1998-07-14 Alcon Laboratories, Inc. Use of adenosine uptake inhibitors for treating retinal or optic nerve head damage
CZ302486B6 (cs) * 1998-06-02 2011-06-15 Osi Pharmaceuticals, Inc. N-6-Substituovaný 7-deazapurin, zpusob jeho prípravy a farmaceutická kompozice s jeho obsahem
KR100840727B1 (ko) * 1999-12-02 2008-06-23 오에스아이 파마슈티컬스, 인코포레이티드 아데노신 ａ1, ａ2ａ 및 ａ3 수용체 특이 화합물 및 그의 사용방법
EP1450811B1 (de) * 2001-11-30 2009-10-21 OSI Pharmaceuticals, Inc. Verbindungen, die für Adenosin A1 und A3 Rezeptoren spezifisch sind, und deren Anwendungen

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104350056A (zh) * 2012-06-07 2015-02-11 霍夫曼-拉罗奇有限公司 端锚聚合酶的吡咯并嘧啶酮和吡咯并吡啶酮抑制剂
CN105473581B (zh) * 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
US10010556B2 (en) 2013-06-21 2018-07-03 Zenith Epigenetics Ltd. Bicyclic bromodomain inhibitors
US10363257B2 (en) 2013-06-21 2019-07-30 Zenith Epigenetics Ltd. Bicyclic bromodomain inhibitors
US11026926B2 (en) 2013-06-21 2021-06-08 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
US10772892B2 (en) 2013-06-21 2020-09-15 Zenith Epigenetics Ltd. Bicyclic bromodomain inhibitors
US10226451B2 (en) 2013-06-21 2019-03-12 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CN105492439B (zh) * 2013-06-21 2019-11-22 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的取代的双环化合物
CN105473581A (zh) * 2013-06-21 2016-04-06 齐尼思表观遗传学公司 作为溴结构域抑制剂的新取代的双环化合物
US11446306B2 (en) 2013-06-21 2022-09-20 Zenith Epigenetics Ltd. Bicyclic bromodomain inhibitors
CN105492439A (zh) * 2013-06-21 2016-04-13 齐尼思表观遗传学公司 作为溴结构域抑制剂的新取代的双环化合物
US10166215B2 (en) 2013-06-21 2019-01-01 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
US10500209B2 (en) 2013-07-31 2019-12-10 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
CN110128316A (zh) * 2019-05-22 2019-08-16 北京大学深圳研究生院 5位取代的β-脯氨酸及其衍生物的制备方法
CN110128316B (zh) * 2019-05-22 2021-08-31 北京大学深圳研究生院 5位取代的β-脯氨酸及其衍生物的制备方法

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JP4579497B2 (ja) 2010-11-10
EP1347980A4 (de) 2005-02-09
ZA200303729B (en) 2004-05-14
MEP35308A (en) 2011-02-10
NO327207B1 (no) 2009-05-11
YU42703A (sh) 2006-03-03
OA13295A (en) 2007-04-13
CN1489590A (zh) 2004-04-14
CZ20031831A3 (cs) 2004-05-12
NO20032482D0 (no) 2003-06-02
MXPA03004717A (es) 2004-06-30
AU2002248151B2 (en) 2008-02-21
CA2430577A1 (en) 2002-07-25
BR0115847A (pt) 2004-02-25
NZ525885A (en) 2005-01-28
NO20032482L (no) 2003-07-28
HUP0400692A3 (en) 2007-09-28
IL155962A0 (en) 2003-12-23
EA007254B1 (ru) 2006-08-25
EA200300628A1 (ru) 2003-12-25
AP2003002807A0 (en) 2003-06-30
EP1347980A1 (de) 2003-10-01
WO2002057267A1 (en) 2002-07-25
AP1893A (en) 2008-09-23
PL363245A1 (en) 2004-11-15
JP2004517896A (ja) 2004-06-17
HUP0400692A2 (hu) 2004-07-28

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