ATE458483T1 - Selektive pyrimidin-a2b-antagonistenverbindungen, ihre synthese und verwendung - Google Patents
Selektive pyrimidin-a2b-antagonistenverbindungen, ihre synthese und verwendungInfo
- Publication number
- ATE458483T1 ATE458483T1 AT02805676T AT02805676T ATE458483T1 AT E458483 T1 ATE458483 T1 AT E458483T1 AT 02805676 T AT02805676 T AT 02805676T AT 02805676 T AT02805676 T AT 02805676T AT E458483 T1 ATE458483 T1 AT E458483T1
- Authority
- AT
- Austria
- Prior art keywords
- alkyl
- substituted
- heterocyclic
- monocyclic
- heteroaryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000002950 monocyclic group Chemical group 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 101150078577 Adora2b gene Proteins 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D401/12—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 chain containing hetero atoms as chain links
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- 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
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
- 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
-
- 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
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- 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
- A61P9/10—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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34259501P | 2001-12-20 | 2001-12-20 | |
| PCT/US2002/041273 WO2003053366A2 (en) | 2001-12-20 | 2002-12-20 | Pyrimidine a2b selective antagonist compounds, their synthesis and use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE458483T1 true ATE458483T1 (de) | 2010-03-15 |
Family
ID=23342484
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT02805676T ATE458483T1 (de) | 2001-12-20 | 2002-12-20 | Selektive pyrimidin-a2b-antagonistenverbindungen, ihre synthese und verwendung |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US6916804B2 (de) |
| EP (1) | EP1465631B1 (de) |
| JP (1) | JP4440642B2 (de) |
| KR (1) | KR20040068317A (de) |
| CN (1) | CN1620294A (de) |
| AT (1) | ATE458483T1 (de) |
| AU (1) | AU2002366811B2 (de) |
| BR (1) | BR0215202A (de) |
| CA (1) | CA2471059C (de) |
| DE (1) | DE60235500D1 (de) |
| EA (2) | EA007468B1 (de) |
| MX (1) | MXPA04005862A (de) |
| WO (1) | WO2003053366A2 (de) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0103836A3 (en) | 1998-06-02 | 2003-05-28 | Osi Pharmaceuticals Inc Uniond | Pyrrolo[2,3d]pyrimidine compositions and their use |
| US6403567B1 (en) * | 1999-06-22 | 2002-06-11 | Cv Therapeutics, Inc. | N-pyrazole A2A adenosine receptor agonists |
| USRE47351E1 (en) | 1999-06-22 | 2019-04-16 | Gilead Sciences, Inc. | 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists |
| CA2671940A1 (en) | 2000-02-23 | 2001-08-30 | Cv Therapeutics, Inc. | Identification of partial agonists of the a2a adenosine receptor |
| US6680324B2 (en) | 2000-12-01 | 2004-01-20 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A1 receptors and uses thereof |
| JP2005529062A (ja) * | 2001-11-30 | 2005-09-29 | オーエスアイ・ファーマスーティカルズ・インコーポレーテッド | アデノシンa1及びa3受容体に特異的な化合物とその使用 |
| DE60236458D1 (de) * | 2001-12-20 | 2010-07-01 | Osi Pharm Inc | Pyrrolopyrimidin a2b selektive antagonistische verbindungen, deren synthese und verwendung |
| KR20040068317A (ko) | 2001-12-20 | 2004-07-30 | 오에스아이 파마슈티컬스, 인코포레이티드 | 피리미딘 a₂b 선택성 길항 화합물, 그의 합성 방법 및용도 |
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| US20050020915A1 (en) * | 2002-07-29 | 2005-01-27 | Cv Therapeutics, Inc. | Myocardial perfusion imaging methods and compositions |
| US8470801B2 (en) | 2002-07-29 | 2013-06-25 | Gilead Sciences, Inc. | Myocardial perfusion imaging methods and compositions |
| WO2004011010A1 (en) * | 2002-07-29 | 2004-02-05 | Cv Therapeutics, Inc. | Myocardial perfusion imaging using a2a receptor agonists |
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| NZ544820A (en) * | 2003-08-11 | 2009-02-28 | Hoffmann La Roche | Piperazine with or-substituted phenyl group and their use as GlyT1 inhibitors |
| US7816353B2 (en) * | 2003-10-24 | 2010-10-19 | Exelixis, Inc. | P70S6 kinase modulators and method of use |
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| EP2311462A1 (de) * | 2004-10-15 | 2011-04-20 | Cv Therapeutics, Inc. | Verfahren zur Verhinderung und Behandlung von Atemwegsneumodellierung und pulmonaler Entzündung über A2B-Adenosinrezeptorantagonisten |
| EP1802317A2 (de) | 2004-10-20 | 2007-07-04 | Cv Therapeutics, Inc. | Verwendung von a2a-adenosin-rezeptoragonisten |
| PL1828154T3 (pl) * | 2004-12-09 | 2009-10-30 | Hoffmann La Roche | Pochodne fenylopiperazynometanonu |
| CA2595994A1 (en) | 2005-01-27 | 2006-08-03 | Alma Mater Studiorum - Universita' Di Bologna | Organic compounds useful for the treatment of alzheimer's disease, their use and method of preparation |
| CN101193862B (zh) | 2005-04-13 | 2013-08-21 | 阿斯特克斯治疗有限公司 | 羟基苯甲酰胺衍生物和其作为hsp90抑制剂的用途 |
| WO2006124897A2 (en) * | 2005-05-13 | 2006-11-23 | Lexicon Genetics Incorporated | Methods and compositions for improving cognition |
| CN101193635A (zh) * | 2005-05-13 | 2008-06-04 | 莱西肯医药有限公司 | 多环化合物及其使用方法 |
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| EP2520567A3 (de) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Mit cyclischen Gruppen substituierte, stickstoffhaltige heterocyclische Derivate |
| US7754725B2 (en) | 2006-03-01 | 2010-07-13 | Astex Therapeutics Ltd. | Dihydroxyphenyl isoindolymethanones |
| US20090081120A1 (en) * | 2006-09-01 | 2009-03-26 | Cv Therapeutics, Inc. | Methods and Compositions for Increasing Patient Tolerability During Myocardial Imaging Methods |
| MX2009002299A (es) * | 2006-09-01 | 2009-03-20 | Cv Therapeutics Inc | Metodos y composiciones para incrementar la tolerancia del paciente durante metodos de formacion de imagenes del miocardio. |
| WO2008042796A2 (en) * | 2006-09-29 | 2008-04-10 | Cv Therapeutics, Inc. | Methods for myocardial imaging in patients having a history of pulmonary disease |
| US8883790B2 (en) | 2006-10-12 | 2014-11-11 | Astex Therapeutics Limited | Pharmaceutical combinations |
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| JP5518478B2 (ja) | 2006-10-12 | 2014-06-11 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| JP5721949B2 (ja) | 2006-10-12 | 2015-05-20 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | 複合薬剤 |
| US8916552B2 (en) | 2006-10-12 | 2014-12-23 | Astex Therapeutics Limited | Pharmaceutical combinations |
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| GB0806527D0 (en) | 2008-04-11 | 2008-05-14 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| US10517839B2 (en) | 2008-06-09 | 2019-12-31 | Cornell University | Mast cell inhibition in diseases of the retina and vitreous |
| TWI433838B (zh) * | 2008-06-25 | 2014-04-11 | 必治妥美雅史谷比公司 | 作為趨化因子受體活性調節劑之六氫吡啶衍生物 |
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| KR20110063556A (ko) * | 2008-09-29 | 2011-06-10 | 길리애드 사이언시즈, 인코포레이티드 | 다검출 전산화 단층 촬영법에 사용하기 위한 a-2-알파 수용체 길항제와 속도 조절제의 조합물 |
| US8642622B2 (en) | 2010-06-16 | 2014-02-04 | Bristol-Myers Squibb Company | Piperidinyl compound as a modulator of chemokine receptor activity |
| CN101967209B (zh) * | 2010-10-20 | 2012-11-07 | 南京大学 | 一种n-乙酰基乙二胺螯合树脂及其制备方法 |
| CA2888899C (en) | 2012-10-24 | 2023-02-21 | Japan Innovative Therapeutics, Inc. | Use of tryptase inhibitors in the treatment retinopathy of prematurity |
| MX364895B (es) | 2013-03-13 | 2019-05-10 | Forma Therapeutics Inc | Nuevos compuestos y composiciones para la inhibicion de fasn. |
| US9920073B2 (en) | 2013-10-04 | 2018-03-20 | Drexel University | Compositions useful for inhibiting HIV-1 infection and methods using same |
| US20200352931A1 (en) * | 2017-12-12 | 2020-11-12 | Phenex Discovery Verwaltungs-GmbH | Oxalamides as modulators of indoleamine 2,3-dioxygenase |
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| CN113382633A (zh) | 2018-10-29 | 2021-09-10 | 福马治疗股份有限公司 | (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式 |
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-
2002
- 2002-12-20 KR KR10-2004-7009798A patent/KR20040068317A/ko not_active Abandoned
- 2002-12-20 WO PCT/US2002/041273 patent/WO2003053366A2/en not_active Ceased
- 2002-12-20 JP JP2003554126A patent/JP4440642B2/ja not_active Expired - Fee Related
- 2002-12-20 CA CA2471059A patent/CA2471059C/en not_active Expired - Fee Related
- 2002-12-20 BR BR0215202-9A patent/BR0215202A/pt not_active Application Discontinuation
- 2002-12-20 AU AU2002366811A patent/AU2002366811B2/en not_active Ceased
- 2002-12-20 AT AT02805676T patent/ATE458483T1/de not_active IP Right Cessation
- 2002-12-20 EA EA200400830A patent/EA007468B1/ru not_active IP Right Cessation
- 2002-12-20 EP EP02805676A patent/EP1465631B1/de not_active Expired - Lifetime
- 2002-12-20 DE DE60235500T patent/DE60235500D1/de not_active Expired - Lifetime
- 2002-12-20 US US10/326,204 patent/US6916804B2/en not_active Expired - Fee Related
- 2002-12-20 CN CNA028282701A patent/CN1620294A/zh active Pending
- 2002-12-20 EA EA200600315A patent/EA011809B1/ru not_active IP Right Cessation
-
2004
- 2004-06-16 MX MXPA04005862A patent/MXPA04005862A/es active IP Right Grant
- 2004-11-18 US US10/992,239 patent/US7501407B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EA011809B1 (ru) | 2009-06-30 |
| EP1465631B1 (de) | 2010-02-24 |
| KR20040068317A (ko) | 2004-07-30 |
| WO2003053366A3 (en) | 2004-01-29 |
| EA007468B1 (ru) | 2006-10-27 |
| JP2005517659A (ja) | 2005-06-16 |
| AU2002366811A1 (en) | 2003-07-09 |
| US7501407B2 (en) | 2009-03-10 |
| EA200400830A1 (ru) | 2004-12-30 |
| EA200600315A1 (ru) | 2006-06-30 |
| BR0215202A (pt) | 2004-10-13 |
| WO2003053366A2 (en) | 2003-07-03 |
| CA2471059C (en) | 2011-04-26 |
| EP1465631A2 (de) | 2004-10-13 |
| MXPA04005862A (es) | 2004-11-01 |
| US20050119271A1 (en) | 2005-06-02 |
| US20030162764A1 (en) | 2003-08-28 |
| JP4440642B2 (ja) | 2010-03-24 |
| CA2471059A1 (en) | 2003-07-03 |
| AU2002366811B2 (en) | 2009-01-15 |
| US6916804B2 (en) | 2005-07-12 |
| CN1620294A (zh) | 2005-05-25 |
| DE60235500D1 (de) | 2010-04-08 |
| EP1465631A4 (de) | 2005-03-30 |
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