DE60117835T2 - Amino- substituierte tetracyclische Verbindungen,die als entzündungshemmende Mittel nützlich sind, und diese enthaltende Arzneimittel - Google Patents
Amino- substituierte tetracyclische Verbindungen,die als entzündungshemmende Mittel nützlich sind, und diese enthaltende Arzneimittel Download PDFInfo
- Publication number
- DE60117835T2 DE60117835T2 DE60117835T DE60117835T DE60117835T2 DE 60117835 T2 DE60117835 T2 DE 60117835T2 DE 60117835 T DE60117835 T DE 60117835T DE 60117835 T DE60117835 T DE 60117835T DE 60117835 T2 DE60117835 T2 DE 60117835T2
- Authority
- DE
- Germany
- Prior art keywords
- alkyl
- substituted
- methyl
- pharmaceutically acceptable
- benzo
- 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.)
- Expired - Lifetime
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- 239000003814 drug Substances 0.000 title claims description 14
- 229940121363 anti-inflammatory agent Drugs 0.000 title description 2
- 239000002260 anti-inflammatory agent Substances 0.000 title description 2
- 125000003277 amino group Chemical group 0.000 title 1
- 229940124599 anti-inflammatory drug Drugs 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract description 32
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- 230000002757 inflammatory effect Effects 0.000 claims abstract description 7
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- 125000000217 alkyl group Chemical group 0.000 claims description 79
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 36
- 238000011282 treatment Methods 0.000 claims description 29
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 25
- 229910052757 nitrogen Inorganic materials 0.000 claims description 23
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- 125000003118 aryl group Chemical group 0.000 claims description 18
- 150000003254 radicals Chemical class 0.000 claims description 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 13
- 150000002367 halogens Chemical class 0.000 claims description 13
- 125000003545 alkoxy group Chemical group 0.000 claims description 11
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- 125000004414 alkyl thio group Chemical group 0.000 claims description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
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- 125000005605 benzo group Chemical group 0.000 claims description 6
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 3
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- WTPHYSIDMNOBOL-UHFFFAOYSA-N 12-thia-14,17-diazatetracyclo[8.7.0.03,8.011,15]heptadeca-1,3,5,7,9,11(15),13,16-octaene Chemical compound C1=CC=CC2=CC3=C(SC=N4)C4=CN=C3C=C21 WTPHYSIDMNOBOL-UHFFFAOYSA-N 0.000 claims description 2
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- UMGOIQFASVFXBU-UHFFFAOYSA-N chembl230184 Chemical compound C1=CC=C2C=C(N3C(C)=CN=C3C(NCCO)=N3)C3=CC2=C1 UMGOIQFASVFXBU-UHFFFAOYSA-N 0.000 claims description 2
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- XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical compound N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 claims 4
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- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- KFIFSKNSIUVOCG-UHFFFAOYSA-N chembl230185 Chemical compound N=1C2=CC3=CC=CC=C3C=C2N2C(C)=CN=C2C=1NCCN1CCCCC1 KFIFSKNSIUVOCG-UHFFFAOYSA-N 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 1
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- 238000005160 1H NMR spectroscopy Methods 0.000 description 25
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
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- 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
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- 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
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- 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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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
-
- 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
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Virology (AREA)
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- Pulmonology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Rheumatology (AREA)
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- Pain & Pain Management (AREA)
- Immunology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22330400P | 2000-10-03 | 2000-10-03 | |
| US223304P | 2000-10-03 | ||
| PCT/US2001/042387 WO2002028860A2 (en) | 2000-10-03 | 2001-09-27 | Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60117835D1 DE60117835D1 (de) | 2006-05-04 |
| DE60117835T2 true DE60117835T2 (de) | 2006-10-19 |
Family
ID=22835931
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60117835T Expired - Lifetime DE60117835T2 (de) | 2000-10-03 | 2001-09-27 | Amino- substituierte tetracyclische Verbindungen,die als entzündungshemmende Mittel nützlich sind, und diese enthaltende Arzneimittel |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6960585B2 (enExample) |
| EP (1) | EP1325009B1 (enExample) |
| JP (1) | JP5021148B2 (enExample) |
| AT (1) | ATE319713T1 (enExample) |
| AU (2) | AU1182702A (enExample) |
| CA (1) | CA2424303A1 (enExample) |
| DE (1) | DE60117835T2 (enExample) |
| ES (1) | ES2260300T3 (enExample) |
| HU (1) | HUP0302925A3 (enExample) |
| WO (1) | WO2002028860A2 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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| EP1363993A4 (en) * | 2001-02-01 | 2008-11-12 | Bristol Myers Squibb Co | METHOD FOR THE TREATMENT OF INFLAMMATORY AND IMMUNE DISEASES USING I KAPPA B KINASE (IKK) |
| AU2002365611A1 (en) | 2001-12-05 | 2003-06-17 | F. Hoffmann - La Roche Ag | Inflammation modulators |
| US7199119B2 (en) | 2002-10-31 | 2007-04-03 | Amgen Inc. | Antiinflammation agents |
| PE20060373A1 (es) | 2004-06-24 | 2006-04-29 | Smithkline Beecham Corp | Derivados 3-piperidinil-7-carboxamida-indazol como inhibidores de la actividad cinasa de ikk2 |
| TW200626142A (en) | 2004-09-21 | 2006-08-01 | Glaxo Group Ltd | Chemical compounds |
| US8063071B2 (en) | 2007-10-31 | 2011-11-22 | GlaxoSmithKline, LLC | Chemical compounds |
| MX2007016541A (es) | 2005-06-30 | 2008-03-07 | Smithkline Beecham Corp | Compuestos quimicos. |
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| KR101563103B1 (ko) * | 2006-12-13 | 2015-10-23 | 아스카 세이야쿠 가부시키가이샤 | 퀴녹살린 유도체 |
| PE20081889A1 (es) | 2007-03-23 | 2009-03-05 | Smithkline Beecham Corp | Indol carboxamidas como inhibidores de ikk2 |
| CN102171204B (zh) | 2008-10-02 | 2014-08-20 | 旭化成制药株式会社 | 8位取代异喹啉衍生物及其用途 |
| WO2010102968A1 (en) | 2009-03-10 | 2010-09-16 | Glaxo Group Limited | Indole derivatives as ikk2 inhibitors |
| CN102288753A (zh) * | 2011-05-10 | 2011-12-21 | 重庆市科学技术研究院 | 快速检测四环素、金霉素、土霉素与多西环素残留的四联胶体金免疫层析试纸条及其制备方法 |
| PE20170131A1 (es) * | 2014-05-09 | 2017-03-19 | Pimera Inc | Composiciones novedosas usos y metodos para hacerlas |
| US9758518B2 (en) | 2015-03-04 | 2017-09-12 | Pimera, Inc. | Compositions, uses and methods for making them |
| JP2020512975A (ja) * | 2017-03-28 | 2020-04-30 | ピメラ，インク． | Ｐｏｌ１阻害剤の新規な結晶形態 |
| JOP20180094A1 (ar) | 2017-10-18 | 2019-04-18 | Hk Inno N Corp | مركب حلقي غير متجانس كمثبط بروتين كيناز |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
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| US4160097A (en) | 1977-01-07 | 1979-07-03 | Westwind Pharmaceuticals, Inc. | 1-(2-Phenylureylene)imidazoles |
| US4225724A (en) | 1977-01-07 | 1980-09-30 | Westwood Pharmaceuticals, Inc. | 1-(2-Phenylureylene)imidazoles |
| US4236015A (en) | 1977-01-07 | 1980-11-25 | Westwood Pharmaceuticals, Inc. | 1-(2-Acylaminophenyl)imidazoles |
| US5153196A (en) * | 1991-06-05 | 1992-10-06 | Eli Lilly And Company | Excitatory amino acid receptor antagonists and methods for the use thereof |
| US5196421A (en) | 1991-06-05 | 1993-03-23 | Eli Lilly And Company | Excitatory amino acid receptor antagonists in methods for the use thereof |
| US5182386A (en) | 1991-08-27 | 1993-01-26 | Neurogen Corporation | Certain imidazoquinoxalinones; a new class of gaba brain receptor ligands |
| US5266575A (en) * | 1991-11-06 | 1993-11-30 | Minnesota Mining And Manufacturing Company | 2-ethyl 1H-imidazo[4,5-ciquinolin-4-amines |
| FR2696466B1 (fr) | 1992-10-02 | 1994-11-25 | Rhone Poulenc Rorer Sa | Dérivés de 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, leur préparation et les médicaments les contenant. |
| IT1276167B1 (it) | 1995-11-24 | 1997-10-27 | Foscama Biomed Chim Farma | Imidazo(1,2-alfa)chinossalin-4-ammine attivi come antagonisti adenosinici,procedimento per la loro preparazione e loro composizioni |
| US6235740B1 (en) | 1997-08-25 | 2001-05-22 | Bristol-Myers Squibb Co. | Imidazoquinoxaline protein tyrosine kinase inhibitors |
| CA2322311C (en) | 1998-03-04 | 2009-10-13 | Bristol-Myers Squibb Company | Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors |
| US6869956B2 (en) * | 2000-10-03 | 2005-03-22 | Bristol-Myers Squibb Company | Methods of treating inflammatory and immune diseases using inhibitors of IκB kinase (IKK) |
| EP1363993A4 (en) * | 2001-02-01 | 2008-11-12 | Bristol Myers Squibb Co | METHOD FOR THE TREATMENT OF INFLAMMATORY AND IMMUNE DISEASES USING I KAPPA B KINASE (IKK) |
-
2001
- 2001-09-27 ES ES01979911T patent/ES2260300T3/es not_active Expired - Lifetime
- 2001-09-27 AU AU1182702A patent/AU1182702A/xx active Pending
- 2001-09-27 HU HU0302925A patent/HUP0302925A3/hu unknown
- 2001-09-27 CA CA002424303A patent/CA2424303A1/en not_active Abandoned
- 2001-09-27 WO PCT/US2001/042387 patent/WO2002028860A2/en not_active Ceased
- 2001-09-27 JP JP2002532443A patent/JP5021148B2/ja not_active Expired - Fee Related
- 2001-09-27 AU AU2002211827A patent/AU2002211827B2/en not_active Ceased
- 2001-09-27 EP EP01979911A patent/EP1325009B1/en not_active Expired - Lifetime
- 2001-09-27 AT AT01979911T patent/ATE319713T1/de not_active IP Right Cessation
- 2001-09-27 US US09/965,977 patent/US6960585B2/en not_active Expired - Lifetime
- 2001-09-27 DE DE60117835T patent/DE60117835T2/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0302925A2 (hu) | 2003-12-29 |
| CA2424303A1 (en) | 2002-04-11 |
| EP1325009B1 (en) | 2006-03-08 |
| EP1325009A2 (en) | 2003-07-09 |
| ES2260300T3 (es) | 2006-11-01 |
| US6960585B2 (en) | 2005-11-01 |
| ATE319713T1 (de) | 2006-03-15 |
| JP5021148B2 (ja) | 2012-09-05 |
| AU2002211827B2 (en) | 2006-12-14 |
| AU1182702A (en) | 2002-04-15 |
| US20020072523A1 (en) | 2002-06-13 |
| WO2002028860A3 (en) | 2002-09-06 |
| JP2004512281A (ja) | 2004-04-22 |
| HUP0302925A3 (en) | 2004-10-28 |
| WO2002028860A2 (en) | 2002-04-11 |
| DE60117835D1 (de) | 2006-05-04 |
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