DE60002554T2 - Pyrazino(aza)indolderivate - Google Patents
Pyrazino(aza)indolderivate Download PDFInfo
- Publication number
- DE60002554T2 DE60002554T2 DE60002554T DE60002554T DE60002554T2 DE 60002554 T2 DE60002554 T2 DE 60002554T2 DE 60002554 T DE60002554 T DE 60002554T DE 60002554 T DE60002554 T DE 60002554T DE 60002554 T2 DE60002554 T2 DE 60002554T2
- Authority
- DE
- Germany
- Prior art keywords
- indole
- hydrogen
- chloro
- mmol
- compound
- 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 - Fee Related
Links
- 150000002475 indoles Chemical class 0.000 title description 5
- 229940054051 antipsychotic indole derivative Drugs 0.000 title description 2
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 18
- 150000003839 salts Chemical class 0.000 claims abstract description 13
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- 125000000217 alkyl group Chemical group 0.000 claims description 41
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- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 150000003222 pyridines Chemical class 0.000 description 1
- 125000004590 pyridopyridyl group Chemical group N1=C(C=CC2=C1C=CC=N2)* 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000001422 pyrrolinyl group Chemical group 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 235000018770 reduced food intake Nutrition 0.000 description 1
- 208000017443 reproductive system disease Diseases 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 229940076279 serotonin Drugs 0.000 description 1
- 231100000872 sexual dysfunction Toxicity 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 235000010288 sodium nitrite Nutrition 0.000 description 1
- 239000001476 sodium potassium tartrate Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 229940080313 sodium starch Drugs 0.000 description 1
- RSIJVJUOQBWMIM-UHFFFAOYSA-L sodium sulfate decahydrate Chemical compound O.O.O.O.O.O.O.O.O.O.[Na+].[Na+].[O-]S([O-])(=O)=O RSIJVJUOQBWMIM-UHFFFAOYSA-L 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
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- 125000005017 substituted alkenyl group Chemical group 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000004426 substituted alkynyl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 150000003457 sulfones Chemical group 0.000 description 1
- 150000003462 sulfoxides Chemical group 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- MJPLUXLNYQHWIU-UHFFFAOYSA-N tert-butyl n-(3-methylpyridin-2-yl)carbamate Chemical compound CC1=CC=CN=C1NC(=O)OC(C)(C)C MJPLUXLNYQHWIU-UHFFFAOYSA-N 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 150000003568 thioethers Chemical group 0.000 description 1
- 150000003573 thiols Chemical group 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
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Classifications
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Silver Salt Photography Or Processing Solution Therefor (AREA)
- Apparatus For Disinfection Or Sterilisation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9902047.1A GB9902047D0 (en) | 1999-01-29 | 1999-01-29 | Chemical compounds XI |
| GB9902047 | 1999-01-29 | ||
| PCT/GB2000/000244 WO2000044753A1 (en) | 1999-01-29 | 2000-01-28 | Pirazino(aza)indole derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60002554D1 DE60002554D1 (de) | 2003-06-12 |
| DE60002554T2 true DE60002554T2 (de) | 2004-03-25 |
Family
ID=10846774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60002554T Expired - Fee Related DE60002554T2 (de) | 1999-01-29 | 2000-01-28 | Pyrazino(aza)indolderivate |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US6800627B1 (enExample) |
| EP (1) | EP1147110B1 (enExample) |
| JP (1) | JP2002535408A (enExample) |
| KR (1) | KR100633375B1 (enExample) |
| CN (2) | CN100418968C (enExample) |
| AT (1) | ATE239731T1 (enExample) |
| AU (1) | AU758685B2 (enExample) |
| BR (1) | BR0008979A (enExample) |
| CA (1) | CA2359034A1 (enExample) |
| DE (1) | DE60002554T2 (enExample) |
| DK (1) | DK1147110T3 (enExample) |
| ES (1) | ES2199132T3 (enExample) |
| GB (1) | GB9902047D0 (enExample) |
| MX (1) | MXPA01007643A (enExample) |
| PT (1) | PT1147110E (enExample) |
| TR (1) | TR200102161T2 (enExample) |
| WO (1) | WO2000044753A1 (enExample) |
| ZA (1) | ZA200106202B (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
| FR2799757B1 (fr) * | 1999-10-15 | 2001-12-14 | Adir | Nouveaux derives polycycliques azaindoliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| WO2002010169A1 (en) * | 2000-07-31 | 2002-02-07 | F. Hoffmann-La Roche Ag | Piperazine derivatives |
| SE0004245D0 (sv) | 2000-11-20 | 2000-11-20 | Pharmacia Ab | Novel compounds and their use |
| JP4204315B2 (ja) | 2000-11-20 | 2009-01-07 | ビオヴィトルム・アクチボラゲット（プブリクト） | セロトニン５−ｈｔ２レセプターのアンタゴニストとしてのピペラジニルピラジン化合物 |
| HUP0303316A2 (hu) * | 2000-12-20 | 2004-01-28 | Bristol-Myers Squibb Pharma Company | Aril- és amino-aril-szubsztituált szerotoninreceptor agonista és antagonista ligandumok és ezeket tartalmazó gyógyszerkészítmények |
| GB0106177D0 (en) * | 2001-03-13 | 2001-05-02 | Hoffmann La Roche | Piperazine derivatives |
| ATE318821T1 (de) | 2001-06-01 | 2006-03-15 | Alcon Inc | Pyranoindazole und ihre verwendung in der glaukombehandlung |
| CA2447156A1 (en) | 2001-06-01 | 2002-12-12 | Alcon, Inc. | Novel fused indazoles and indoles and their use for the treatment of glaucoma |
| AU2002259312B2 (en) | 2001-06-01 | 2007-01-04 | Alcon, Inc. | Novel arylaminopropane analogues and their use for the treatment of glaucoma |
| US6825198B2 (en) | 2001-06-21 | 2004-11-30 | Pfizer Inc | 5-HT receptor ligands and uses thereof |
| TW593302B (en) | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
| GB0202015D0 (en) | 2002-01-29 | 2002-03-13 | Hoffmann La Roche | Piperazine Derivatives |
| BR0311970A (pt) | 2002-06-19 | 2005-03-29 | Biovitrum Ab | Novos compostos, seu uso e preparação |
| BR0316775A (pt) | 2002-12-13 | 2005-11-01 | Alcon Inc | Novos análogos de benzopirano e seu uso para o tratamento de glaucoma |
| EP1636224B1 (en) * | 2003-05-21 | 2010-07-14 | Prosidion Limited | Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phoshorylase |
| US7405210B2 (en) | 2003-05-21 | 2008-07-29 | Osi Pharmaceuticals, Inc. | Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase |
| GB0314967D0 (en) * | 2003-06-26 | 2003-07-30 | Hoffmann La Roche | Piperazine derivatives |
| US7476687B2 (en) | 2003-11-26 | 2009-01-13 | Alcon, Inc. | Substituted furo[2,3-g]indazoles for the treatment of glaucoma |
| AR046890A1 (es) | 2003-12-15 | 2005-12-28 | Alcon Inc | [1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma. |
| US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
| US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
| JP5173190B2 (ja) | 2004-08-25 | 2013-03-27 | 武田薬品工業株式会社 | 腹圧性尿失禁の予防・治療剤及びそのスクリーニング方法 |
| WO2006062839A1 (en) | 2004-12-08 | 2006-06-15 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
| CA2609634C (en) * | 2005-05-03 | 2011-02-01 | F. Hoffmann-La Roche Ag | Tetracyclic azapyrazinoindolines as 5-ht2 ligands |
| UA95788C2 (en) | 2005-12-15 | 2011-09-12 | Ф. Хоффманн-Ля Рош Аг | Fused pyrrole derivatives |
| BRPI0619985A2 (pt) | 2005-12-16 | 2011-10-25 | Hoffmann La Roche | compostos, processo para a sua manufatura, composições farmacêuticas, métodos para o tratamento e/ou prevenção de enfermidades que estão associadas com a modulação de receptores de h3, de obesidade e de diabetes do tipo ii em um ser humano ou animal e usos dos compostos |
| JP5528699B2 (ja) | 2006-05-16 | 2014-06-25 | 武田薬品工業株式会社 | 縮合複素環化合物およびその用途 |
| JP5520051B2 (ja) | 2007-11-15 | 2014-06-11 | 武田薬品工業株式会社 | 縮合ピリジン誘導体およびその用途 |
| EP2254886B1 (en) * | 2008-03-28 | 2016-05-25 | Nerviano Medical Sciences S.r.l. | 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| WO2011071136A1 (ja) | 2009-12-11 | 2011-06-16 | アステラス製薬株式会社 | 線維筋痛症治療剤 |
| US20130267500A1 (en) | 2010-09-01 | 2013-10-10 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
| MX363662B (es) * | 2012-10-08 | 2019-03-27 | Centro De Investig Y De Estudios Avanzados Del I P N Star | Métodos para incrementar la sensibilidad a insulina mediante agonistas de receptores serotonérgicos 5-ht2. |
| WO2015066344A1 (en) | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
| JP6217561B2 (ja) * | 2014-08-21 | 2017-10-25 | 信越化学工業株式会社 | 新規オニウム塩化合物及びレジスト組成物並びにパターン形成方法 |
| WO2019131902A1 (ja) | 2017-12-27 | 2019-07-04 | 武田薬品工業株式会社 | 腹圧性尿失禁および便失禁の治療薬 |
| IL292631A (en) * | 2019-10-31 | 2022-07-01 | Holosmedic | Novel compound and pharmaceutical composition for prevention or treatment of cancer comprising same |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE792724A (fr) * | 1971-12-16 | 1973-06-14 | Merck Patent Gmbh | Derives de pyrazinoindole et leur procede de preparation |
| EP0572863A1 (de) * | 1992-06-05 | 1993-12-08 | F. Hoffmann-La Roche Ag | ZNS Pyrazinoindole |
| TW334423B (en) | 1993-10-22 | 1998-06-21 | Hoffmann La Roche | Tricyclic 1-aminoethylpyrrole-derivatives |
| US5854245A (en) * | 1996-06-28 | 1998-12-29 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| GB9819032D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds IV |
| GB9819019D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds II |
| GB9819035D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Res Ltd | Chemical compounds VII |
| GB9819033D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds VI |
| GB9918962D0 (en) * | 1999-08-11 | 1999-10-13 | Cerebrus Ltd | Chemical compounds xxii |
-
1999
- 1999-01-29 GB GBGB9902047.1A patent/GB9902047D0/en not_active Ceased
-
2000
- 2000-01-28 DE DE60002554T patent/DE60002554T2/de not_active Expired - Fee Related
- 2000-01-28 AU AU21196/00A patent/AU758685B2/en not_active Ceased
- 2000-01-28 CA CA002359034A patent/CA2359034A1/en not_active Abandoned
- 2000-01-28 WO PCT/GB2000/000244 patent/WO2000044753A1/en not_active Ceased
- 2000-01-28 JP JP2000596009A patent/JP2002535408A/ja active Pending
- 2000-01-28 TR TR2001/02161T patent/TR200102161T2/xx unknown
- 2000-01-28 BR BR0008979-6A patent/BR0008979A/pt not_active Application Discontinuation
- 2000-01-28 KR KR1020017009583A patent/KR100633375B1/ko not_active Expired - Fee Related
- 2000-01-28 EP EP00901240A patent/EP1147110B1/en not_active Expired - Lifetime
- 2000-01-28 US US09/890,186 patent/US6800627B1/en not_active Expired - Fee Related
- 2000-01-28 DK DK00901240T patent/DK1147110T3/da active
- 2000-01-28 ES ES00901240T patent/ES2199132T3/es not_active Expired - Lifetime
- 2000-01-28 MX MXPA01007643A patent/MXPA01007643A/es not_active IP Right Cessation
- 2000-01-28 CN CNB2006100710947A patent/CN100418968C/zh not_active Expired - Fee Related
- 2000-01-28 AT AT00901240T patent/ATE239731T1/de not_active IP Right Cessation
- 2000-01-28 CN CNB008031398A patent/CN1289499C/zh not_active Expired - Fee Related
- 2000-01-28 PT PT00901240T patent/PT1147110E/pt unknown
-
2001
- 2001-07-27 ZA ZA200106202A patent/ZA200106202B/en unknown
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2003
- 2003-08-05 US US10/633,532 patent/US20040039200A1/en not_active Abandoned
- 2003-10-16 US US10/685,799 patent/US7145009B2/en not_active Expired - Fee Related
-
2006
- 2006-03-14 US US11/374,157 patent/US20060160816A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DE60002554D1 (de) | 2003-06-12 |
| CN100418968C (zh) | 2008-09-17 |
| KR20010101873A (ko) | 2001-11-15 |
| AU758685B2 (en) | 2003-03-27 |
| CN1289499C (zh) | 2006-12-13 |
| EP1147110A1 (en) | 2001-10-24 |
| WO2000044753A1 (en) | 2000-08-03 |
| AU2119600A (en) | 2000-08-18 |
| DK1147110T3 (da) | 2003-09-01 |
| JP2002535408A (ja) | 2002-10-22 |
| US20060160816A1 (en) | 2006-07-20 |
| CA2359034A1 (en) | 2000-08-03 |
| PT1147110E (pt) | 2003-09-30 |
| EP1147110B1 (en) | 2003-05-07 |
| US6800627B1 (en) | 2004-10-05 |
| CN1337963A (zh) | 2002-02-27 |
| ZA200106202B (en) | 2002-07-29 |
| ES2199132T3 (es) | 2004-02-16 |
| KR100633375B1 (ko) | 2006-10-16 |
| MXPA01007643A (es) | 2003-06-24 |
| US20040039200A1 (en) | 2004-02-26 |
| US20040092525A1 (en) | 2004-05-13 |
| BR0008979A (pt) | 2002-02-05 |
| TR200102161T2 (tr) | 2002-05-21 |
| US7145009B2 (en) | 2006-12-05 |
| CN1837207A (zh) | 2006-09-27 |
| ATE239731T1 (de) | 2003-05-15 |
| GB9902047D0 (en) | 1999-03-17 |
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