ZA200404160B - Adenosine A2A receptor antagonists. - Google Patents
Adenosine A2A receptor antagonists. Download PDFInfo
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- ZA200404160B ZA200404160B ZA200404160A ZA200404160A ZA200404160B ZA 200404160 B ZA200404160 B ZA 200404160B ZA 200404160 A ZA200404160 A ZA 200404160A ZA 200404160 A ZA200404160 A ZA 200404160A ZA 200404160 B ZA200404160 B ZA 200404160B
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- South Africa
- Prior art keywords
- alkyl
- group
- alkoxy
- disease
- mmol
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- 239000002467 adenosine A2a receptor antagonist Substances 0.000 title 1
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- 239000012047 saturated solution Substances 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 238000012026 site acceptance test Methods 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- OUFRIWNNMFWZTM-UHFFFAOYSA-M sodium arsanilate Chemical compound [Na+].NC1=CC=C([As](O)([O-])=O)C=C1 OUFRIWNNMFWZTM-UHFFFAOYSA-M 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 150000003890 succinate salts Chemical class 0.000 description 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 150000003567 thiocyanates Chemical class 0.000 description 1
- LBLYYCQCTBFVLH-UHFFFAOYSA-M toluenesulfonate group Chemical group C=1(C(=CC=CC1)S(=O)(=O)[O-])C LBLYYCQCTBFVLH-UHFFFAOYSA-M 0.000 description 1
- 125000005490 tosylate group Chemical group 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- GYUURHMITDQTRU-UHFFFAOYSA-N tributyl(pyridin-2-yl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C1=CC=CC=N1 GYUURHMITDQTRU-UHFFFAOYSA-N 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
- NHDIQVFFNDKAQU-UHFFFAOYSA-N tripropan-2-yl borate Chemical compound CC(C)OB(OC(C)C)OC(C)C NHDIQVFFNDKAQU-UHFFFAOYSA-N 0.000 description 1
- BWHDROKFUHTORW-UHFFFAOYSA-N tritert-butylphosphane Chemical compound CC(C)(C)P(C(C)(C)C)C(C)(C)C BWHDROKFUHTORW-UHFFFAOYSA-N 0.000 description 1
- 230000028838 turning behavior Effects 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical class CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 230000024883 vasodilation Effects 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
Classifications
-
- 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
- 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
- A61P25/08—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
- 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
- A61P25/18—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
- A61P25/24—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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33429301P | 2001-11-30 | 2001-11-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200404160B true ZA200404160B (en) | 2005-04-08 |
Family
ID=23306533
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200404160A ZA200404160B (en) | 2001-11-30 | 2004-05-27 | Adenosine A2A receptor antagonists. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7041666B2 (https=) |
| EP (1) | EP1453835B1 (https=) |
| JP (2) | JP4284181B2 (https=) |
| KR (1) | KR20050044607A (https=) |
| CN (1) | CN1596258A (https=) |
| AR (1) | AR038366A1 (https=) |
| AT (1) | ATE317844T1 (https=) |
| AU (1) | AU2002346572A1 (https=) |
| CA (1) | CA2468681C (https=) |
| DE (1) | DE60209251T2 (https=) |
| ES (1) | ES2258164T3 (https=) |
| HU (1) | HUP0402270A3 (https=) |
| IL (1) | IL161572A0 (https=) |
| MX (1) | MXPA04005156A (https=) |
| PE (1) | PE20030739A1 (https=) |
| TW (1) | TW200300686A (https=) |
| WO (1) | WO2003048164A2 (https=) |
| ZA (1) | ZA200404160B (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004029056A1 (ja) * | 2002-09-24 | 2004-04-08 | Kyowa Hakko Kogyo Co., Ltd. | [１，２，４]トリアゾロ[１，５−ｃ]ピリミジン誘導体 |
| TWI331036B (en) | 2002-12-19 | 2010-10-01 | Schering Corp | Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| US20060106040A1 (en) | 2002-12-19 | 2006-05-18 | Michael Grzelak | Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| WO2004092172A2 (en) * | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosin e receptor antagonists |
| WO2005039506A2 (en) * | 2003-10-24 | 2005-05-06 | Exelixis, Inc. | P70s6 kinase modulators and method of use |
| AR050926A1 (es) | 2004-09-03 | 2006-12-06 | Astrazeneca Ab | Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac) |
| WO2006129626A1 (ja) * | 2005-05-30 | 2006-12-07 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]トリアゾロ[1,5-c]ピリミジン誘導体の製造法 |
| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
| CA2687942A1 (en) * | 2007-05-24 | 2008-12-04 | Mitsubishi Tanabe Pharma Corporation | Therapeutic agent for cerebral infarction |
| CA2690748A1 (en) * | 2007-06-25 | 2008-12-31 | Neurogen Corporation | Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues |
| US20100093764A1 (en) * | 2008-10-13 | 2010-04-15 | Devraj Chakravarty | AMINES AND SULFOXIDES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| US20100093756A1 (en) * | 2008-10-13 | 2010-04-15 | Berbay J Kent | HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| BRPI0921570A2 (pt) | 2008-11-25 | 2019-09-24 | Nissan Motor | membro condutor de eletricidade e célula de combustível de eletrólito de polímero utilizando o mesmo |
| WO2010126811A1 (en) * | 2009-04-27 | 2010-11-04 | Boehringer Ingelheim International Gmbh | Cxcr3 receptor antagonists |
| WO2011084985A1 (en) | 2010-01-07 | 2011-07-14 | Boehringer Ingelheim International Gmbh | Cxcr3 receptor antagonists |
| AU2011306358B2 (en) * | 2010-09-24 | 2014-08-14 | Impetis Biosciences Ltd. | Fused tricyclic compounds as adenosine receptor antagonist |
| WO2012127472A1 (en) * | 2011-03-22 | 2012-09-27 | Mapi Pharma Ltd. | Process and intermediates for the preparation of preladenant and related compounds |
| PL3611174T3 (pl) * | 2017-04-07 | 2022-08-08 | Medshine Discovery Inc. | Pochodne [1,2,4]triazolo[1,5-c]pirymidyny jako inhibitor receptora a2a |
| TWI877770B (zh) * | 2018-02-27 | 2025-03-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之咪唑并嘧啶及三唑并嘧啶 |
| PL3766884T3 (pl) * | 2018-04-28 | 2022-07-18 | Medshine Discovery Inc. | Postać krystaliczna i rodzaj soli związku triazolopirymidynowego oraz sposób jej wytwarzania |
| EP3810610A1 (en) * | 2018-05-18 | 2021-04-28 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| WO2020010197A1 (en) | 2018-07-05 | 2020-01-09 | Incyte Corporation | Fused pyrazine derivatives as a2a / a2b inhibitors |
| AR116315A1 (es) * | 2018-09-12 | 2021-04-21 | Dizal Jiangsu Pharmaceutical Co Ltd | Compuestos de triazolo-pirimidina y usos de los mismos |
| US12414952B2 (en) | 2018-11-20 | 2025-09-16 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| AU2019383948A1 (en) | 2018-11-20 | 2021-05-20 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2020112700A1 (en) | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| AU2019388872A1 (en) | 2018-11-30 | 2021-05-27 | Merck Sharp & Dohme Llc | 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| CA3124088A1 (en) | 2018-12-20 | 2020-06-25 | Incyte Corporation | Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2 |
| WO2020128036A1 (en) * | 2018-12-21 | 2020-06-25 | Ryvu Therapeutics S.A. | Modulators of the adenosine a2a receptor |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU622330B2 (en) | 1989-06-23 | 1992-04-02 | Takeda Chemical Industries Ltd. | Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides |
| IT1264901B1 (it) | 1993-06-29 | 1996-10-17 | Schering Plough S P A | Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina |
| WO1995003806A1 (en) | 1993-07-27 | 1995-02-09 | Kyowa Hakko Kogyo Co., Ltd. | Remedy for parkinson's disease |
| IT1277392B1 (it) | 1995-07-28 | 1997-11-10 | Schering Plough S P A | Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina |
| DE69820866T2 (de) * | 1997-03-24 | 2004-12-30 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-DERIVATE |
| IT1291372B1 (it) | 1997-05-21 | 1999-01-07 | Schering Plough S P A | Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie |
| WO2000017201A1 (en) * | 1998-09-22 | 2000-03-30 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES |
| DE60110219T2 (de) | 2000-05-26 | 2006-03-09 | Schering Corp. | Adenosin a2a rezeptor antagonisten |
| JPWO2002079204A1 (ja) * | 2001-03-28 | 2004-07-22 | 協和醗酵工業株式会社 | ８−チアゾリル［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体 |
| IL161573A0 (en) | 2001-11-30 | 2004-09-27 | Schering Corp | [1,2,4]-TRIAZOLE BICYCLIC ADENOSINE A2a RECEPTOR ANTAGONISTS |
-
2002
- 2002-11-25 AR ARP020104528A patent/AR038366A1/es unknown
- 2002-11-25 TW TW091134178A patent/TW200300686A/zh unknown
- 2002-11-25 PE PE2002001128A patent/PE20030739A1/es not_active Application Discontinuation
- 2002-11-26 AU AU2002346572A patent/AU2002346572A1/en not_active Abandoned
- 2002-11-26 CA CA2468681A patent/CA2468681C/en not_active Expired - Fee Related
- 2002-11-26 DE DE60209251T patent/DE60209251T2/de not_active Expired - Lifetime
- 2002-11-26 MX MXPA04005156A patent/MXPA04005156A/es active IP Right Grant
- 2002-11-26 AT AT02784641T patent/ATE317844T1/de not_active IP Right Cessation
- 2002-11-26 HU HU0402270A patent/HUP0402270A3/hu unknown
- 2002-11-26 ES ES02784641T patent/ES2258164T3/es not_active Expired - Lifetime
- 2002-11-26 JP JP2003549354A patent/JP4284181B2/ja not_active Expired - Fee Related
- 2002-11-26 IL IL16157202A patent/IL161572A0/xx unknown
- 2002-11-26 EP EP02784641A patent/EP1453835B1/en not_active Expired - Lifetime
- 2002-11-26 KR KR1020047008031A patent/KR20050044607A/ko not_active Withdrawn
- 2002-11-26 WO PCT/US2002/038134 patent/WO2003048164A2/en not_active Ceased
- 2002-11-26 US US10/304,504 patent/US7041666B2/en not_active Expired - Lifetime
- 2002-11-26 CN CNA028239229A patent/CN1596258A/zh active Pending
-
2004
- 2004-05-27 ZA ZA200404160A patent/ZA200404160B/en unknown
-
2008
- 2008-06-04 JP JP2008147394A patent/JP2008303217A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| DE60209251T2 (de) | 2006-11-09 |
| PE20030739A1 (es) | 2003-08-28 |
| AR038366A1 (es) | 2005-01-12 |
| KR20050044607A (ko) | 2005-05-12 |
| HUP0402270A2 (hu) | 2005-02-28 |
| TW200300686A (en) | 2003-06-16 |
| ES2258164T3 (es) | 2006-08-16 |
| HUP0402270A3 (en) | 2008-09-29 |
| MXPA04005156A (es) | 2004-08-11 |
| ATE317844T1 (de) | 2006-03-15 |
| EP1453835A2 (en) | 2004-09-08 |
| CN1596258A (zh) | 2005-03-16 |
| IL161572A0 (en) | 2004-09-27 |
| US7041666B2 (en) | 2006-05-09 |
| AU2002346572A1 (en) | 2003-06-17 |
| CA2468681C (en) | 2011-01-25 |
| CA2468681A1 (en) | 2003-06-12 |
| HK1064100A1 (en) | 2005-01-21 |
| JP4284181B2 (ja) | 2009-06-24 |
| EP1453835B1 (en) | 2006-02-15 |
| US20030212080A1 (en) | 2003-11-13 |
| JP2008303217A (ja) | 2008-12-18 |
| JP2005511698A (ja) | 2005-04-28 |
| WO2003048164A2 (en) | 2003-06-12 |
| DE60209251D1 (de) | 2006-04-20 |
| WO2003048164A3 (en) | 2003-10-16 |
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