NO317179B1 - 2,4-Diaminopyrimidinderivater som dopamin D<N>4</N>-reseptorantagonister - Google Patents
2,4-Diaminopyrimidinderivater som dopamin D<N>4</N>-reseptorantagonister Download PDFInfo
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- NO317179B1 NO317179B1 NO19985228A NO985228A NO317179B1 NO 317179 B1 NO317179 B1 NO 317179B1 NO 19985228 A NO19985228 A NO 19985228A NO 985228 A NO985228 A NO 985228A NO 317179 B1 NO317179 B1 NO 317179B1
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- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 title claims description 12
- 229960003638 dopamine Drugs 0.000 title claims description 6
- YAAWASYJIRZXSZ-UHFFFAOYSA-N pyrimidine-2,4-diamine Chemical class NC1=CC=NC(N)=N1 YAAWASYJIRZXSZ-UHFFFAOYSA-N 0.000 title description 3
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 130
- -1 2,3-dihydro-1,4-benzodioxinyl Chemical group 0.000 claims abstract description 71
- 239000000203 mixture Substances 0.000 claims abstract description 40
- 102000003962 Dopamine D4 receptors Human genes 0.000 claims abstract description 37
- 108090000357 Dopamine D4 receptors Proteins 0.000 claims abstract description 37
- 238000000034 method Methods 0.000 claims abstract description 26
- 150000003839 salts Chemical class 0.000 claims abstract description 22
- 239000002253 acid Substances 0.000 claims abstract description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 20
- 239000001257 hydrogen Substances 0.000 claims abstract description 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 16
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims abstract description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 14
- 230000002285 radioactive effect Effects 0.000 claims abstract description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 8
- 125000003118 aryl group Chemical group 0.000 claims abstract description 8
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract description 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims abstract description 6
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims abstract description 6
- 238000003384 imaging method Methods 0.000 claims abstract description 6
- 125000001624 naphthyl group Chemical group 0.000 claims abstract description 6
- 210000000056 organ Anatomy 0.000 claims abstract description 6
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims abstract description 4
- 125000004104 aryloxy group Chemical group 0.000 claims abstract description 3
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- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims abstract description 3
- 125000004076 pyridyl group Chemical group 0.000 claims abstract description 3
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
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- DJLSKZGRIWATLN-UHFFFAOYSA-N 2-methyl-1H-pyrimidine-2,4-diamine Chemical compound CC1(N)NC=CC(N)=N1 DJLSKZGRIWATLN-UHFFFAOYSA-N 0.000 claims description 2
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—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
- A61P25/22—Anxiolytics
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- 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
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- 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
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Anesthesiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP96201283 | 1996-05-10 | ||
| PCT/EP1997/002506 WO1997043279A1 (en) | 1996-05-10 | 1997-05-02 | 2,4-diaminopyrimidine derivates as dopamine d4 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO985228D0 NO985228D0 (no) | 1998-11-09 |
| NO985228L NO985228L (no) | 1999-01-11 |
| NO317179B1 true NO317179B1 (no) | 2004-09-06 |
Family
ID=8223971
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO19985228A NO317179B1 (no) | 1996-05-10 | 1998-11-09 | 2,4-Diaminopyrimidinderivater som dopamin D<N>4</N>-reseptorantagonister |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US6159982A (cs) |
| EP (1) | EP0912552B1 (cs) |
| JP (1) | JP4264135B2 (cs) |
| KR (1) | KR100462524B1 (cs) |
| CN (1) | CN1134431C (cs) |
| AT (1) | ATE264853T1 (cs) |
| CA (1) | CA2253429C (cs) |
| CZ (1) | CZ289250B6 (cs) |
| DE (1) | DE69728768T2 (cs) |
| ES (1) | ES2221052T3 (cs) |
| HU (1) | HUP9903445A3 (cs) |
| IL (1) | IL126969A (cs) |
| MY (1) | MY116114A (cs) |
| NO (1) | NO317179B1 (cs) |
| NZ (1) | NZ332308A (cs) |
| PL (1) | PL187769B1 (cs) |
| TW (1) | TW504510B (cs) |
| WO (1) | WO1997043279A1 (cs) |
| ZA (1) | ZA974050B (cs) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ID23803A (id) * | 1997-08-15 | 2000-05-11 | Pfizer Prod Inc | Turunan-turunan 2-(4-aril atau heteroaril-piperazin-1-ilmetil)-1h-indola |
| WO2000018763A2 (en) * | 1998-09-29 | 2000-04-06 | Neurogen Corporation | 2-(2,3-dihydrobenzofuran-5-yl)-4-aminomethylimidazoles: dopamine receptor subtype specific ligands |
| US6288230B1 (en) | 1998-09-29 | 2001-09-11 | Neurogen Corporation | 2-(2, 3-dihydrobenzofuran-5-yl)-4-aminomethylimidazoles: dopamine receptor subtype specific ligands |
| US6284759B1 (en) | 1998-09-30 | 2001-09-04 | Neurogen Corporation | 2-piperazinoalkylaminobenzo-azole derivatives: dopamine receptor subtype specific ligands |
| US6107313A (en) * | 1998-10-02 | 2000-08-22 | Combichem, Inc. | Dopamine receptor antagonists |
| GB9915616D0 (en) * | 1999-07-05 | 1999-09-01 | Knoll Ag | Therapeutic agents |
| KR100394083B1 (ko) * | 2000-12-04 | 2003-08-06 | 학교법인 성신학원 | 도파민 ｄ3 및 ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 |
| CA2438318A1 (en) * | 2001-02-16 | 2002-08-29 | Aventis Pharmaceuticals Inc. | Novel heterocyclic amide derivatives and their use as dopamine d3 receptor ligands |
| ES2275853T3 (es) * | 2001-02-16 | 2007-06-16 | Aventis Pharmaceuticals Inc. | Derivados heterociclicos de urea y su uso como ligandos de receptores de dopamina d3. |
| DE60210944T3 (de) * | 2001-02-23 | 2015-07-23 | Merck Sharp & Dohme Corp. | N-substituierte nichtaryl-heterocyclische nmda/nr2b antagonisten |
| CA2489458A1 (en) * | 2002-06-14 | 2003-12-24 | Altana Pharma Ag | Substituted diaminopyrimidines |
| WO2004087707A1 (en) * | 2003-03-31 | 2004-10-14 | Vernalis (Cambridge) Limited | Pyrazolopyrimidine compounds and their use in medicine |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| US7196928B2 (en) * | 2005-04-05 | 2007-03-27 | Sandisk Corporation | Compensating for coupling during read operations of non-volatile memory |
| JO2769B1 (en) * | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor |
| US7855194B2 (en) * | 2006-03-27 | 2010-12-21 | Hoffmann-La Roche Inc. | Pyrimidine, quinazoline, pteridine and triazine derivatives |
| EP2384768B1 (en) | 2006-11-01 | 2013-08-21 | Purdue Pharma LP | Phenylpropionamide compounds and the use thereof |
| JO2642B1 (en) * | 2006-12-08 | 2012-06-17 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
| JO2849B1 (en) | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
| RS52518B (sr) | 2007-04-23 | 2013-04-30 | Janssen Pharmaceutica N.V. | Derivati 4-alkoksipiridazina kao brzo disocirajući dopamin 2 receptorski antagonisti |
| RU2489431C2 (ru) * | 2007-04-23 | 2013-08-10 | Янссен Фармацевтика Н.В. | Тиа(диа)золы как быстро диссоциирующие антагонисты рецептора допамина 2 |
| US20100137368A1 (en) * | 2007-04-23 | 2010-06-03 | Janssen Pharmaceutica N.V. | Pyridine derivatives as fast dissociating dopamine 2 receptor antagonists |
| WO2010012758A1 (en) | 2008-07-31 | 2010-02-04 | Janssen Pharmaceutica Nv | Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists |
| AU2011205485B2 (en) * | 2010-01-13 | 2014-09-25 | Glaxosmithkline Llc | Compounds and methods |
| SG11201701315VA (en) | 2014-08-28 | 2017-03-30 | Asceneuron Sa | Glycosidase inhibitors |
| CN106243088B (zh) | 2015-06-03 | 2019-01-04 | 广东东阳光药业有限公司 | 取代的哌嗪化合物及其使用方法和用途 |
| CA3014572C (en) | 2016-02-25 | 2023-10-03 | Asceneuron S.A. | Acid addition salts of piperazine derivatives |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| CA3012624A1 (en) | 2016-02-25 | 2017-08-31 | Asceneuron S.A. | Glycosidase inhibitors |
| CA3012560A1 (en) | 2016-02-25 | 2017-08-31 | Asceneuron S.A. | Glycosidase inhibitors |
| WO2018226976A1 (en) * | 2017-06-08 | 2018-12-13 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with mll proteins |
| WO2019037860A1 (en) * | 2017-08-24 | 2019-02-28 | Asceneuron S.A. | LINEAR INHIBITORS OF GLYCOSIDASE |
| EP3684361A4 (en) | 2017-09-20 | 2021-09-08 | Kura Oncology, Inc. | MENINE-MLL SUBSTITUTE INHIBITORS AND METHODS OF USE |
| WO2020039029A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Spiro compounds as glycosidase inhibitors |
| US12016852B2 (en) | 2018-08-22 | 2024-06-25 | Asceneuron Sa | Pyrrolidine glycosidase inhibitors |
| WO2020039028A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine glycosidase inhibitors |
| IL280841B2 (en) | 2018-08-22 | 2024-12-01 | Asceneuron S A | Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors |
| TWI716107B (zh) * | 2018-09-26 | 2021-01-11 | 美商美國禮來大藥廠 | 6-氟-2-甲基苯并[d]噻唑-5-基化合物 |
| CA3170252A1 (en) * | 2020-03-06 | 2021-09-10 | Chun-Ping Chang | Pyrimidine compounds and their pharmaceutical uses |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU206337B (en) * | 1988-12-29 | 1992-10-28 | Mitsui Petrochemical Ind | Process for producing pyrimidine derivatives and pharmaceutical compositions |
| US5681956A (en) * | 1990-12-28 | 1997-10-28 | Neurogen Corporation | 4-aryl substituted piperazinylmethyl phenylimidazole derivatives; a new class of dopamine receptor subtype specific ligands |
| GB9216298D0 (en) * | 1991-08-15 | 1992-09-16 | Ici Plc | Piperidine derivatives |
| SI9300097B (en) * | 1992-02-27 | 2001-12-31 | Janssen Pharmaceutica Nv | (benzodioxan, benzofuran or benzopyran) alkylamino) alkyl substituted guanidines |
-
1997
- 1997-05-01 TW TW086105766A patent/TW504510B/zh active
- 1997-05-02 HU HU9903445A patent/HUP9903445A3/hu unknown
- 1997-05-02 IL IL12696997A patent/IL126969A/xx not_active IP Right Cessation
- 1997-05-02 PL PL97329850A patent/PL187769B1/pl not_active IP Right Cessation
- 1997-05-02 JP JP54053697A patent/JP4264135B2/ja not_active Expired - Lifetime
- 1997-05-02 CN CNB971945160A patent/CN1134431C/zh not_active Expired - Lifetime
- 1997-05-02 CA CA002253429A patent/CA2253429C/en not_active Expired - Fee Related
- 1997-05-02 CZ CZ19983627A patent/CZ289250B6/cs not_active IP Right Cessation
- 1997-05-02 NZ NZ332308A patent/NZ332308A/xx unknown
- 1997-05-02 ES ES97923914T patent/ES2221052T3/es not_active Expired - Lifetime
- 1997-05-02 KR KR10-1998-0707915A patent/KR100462524B1/ko not_active Expired - Fee Related
- 1997-05-02 WO PCT/EP1997/002506 patent/WO1997043279A1/en not_active Ceased
- 1997-05-02 AT AT97923914T patent/ATE264853T1/de not_active IP Right Cessation
- 1997-05-02 US US09/180,364 patent/US6159982A/en not_active Expired - Lifetime
- 1997-05-02 DE DE69728768T patent/DE69728768T2/de not_active Expired - Lifetime
- 1997-05-02 EP EP97923914A patent/EP0912552B1/en not_active Expired - Lifetime
- 1997-05-07 MY MYPI97002019A patent/MY116114A/en unknown
- 1997-05-09 ZA ZA974050A patent/ZA974050B/xx unknown
-
1998
- 1998-11-09 NO NO19985228A patent/NO317179B1/no unknown
-
2000
- 2000-09-22 US US09/667,458 patent/US6395742B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| HUP9903445A3 (en) | 2002-01-28 |
| PL187769B1 (pl) | 2004-10-29 |
| CA2253429C (en) | 2006-08-08 |
| ES2221052T3 (es) | 2004-12-16 |
| MY116114A (en) | 2003-11-28 |
| TW504510B (en) | 2002-10-01 |
| CN1134431C (zh) | 2004-01-14 |
| ATE264853T1 (de) | 2004-05-15 |
| ZA974050B (en) | 1998-11-09 |
| IL126969A0 (en) | 1999-09-22 |
| EP0912552A1 (en) | 1999-05-06 |
| HUP9903445A2 (hu) | 2000-05-28 |
| JP4264135B2 (ja) | 2009-05-13 |
| NO985228D0 (no) | 1998-11-09 |
| US6395742B1 (en) | 2002-05-28 |
| DE69728768D1 (de) | 2004-05-27 |
| EP0912552B1 (en) | 2004-04-21 |
| WO1997043279A1 (en) | 1997-11-20 |
| US6159982A (en) | 2000-12-12 |
| NZ332308A (en) | 1999-08-30 |
| CZ289250B6 (cs) | 2001-12-12 |
| PL329850A1 (en) | 1999-04-12 |
| NO985228L (no) | 1999-01-11 |
| JP2000512623A (ja) | 2000-09-26 |
| IL126969A (en) | 2003-01-12 |
| AU708344B2 (en) | 1999-08-05 |
| AU2956197A (en) | 1997-12-05 |
| KR100462524B1 (ko) | 2005-06-13 |
| CN1218466A (zh) | 1999-06-02 |
| KR20000005228A (ko) | 2000-01-25 |
| CZ362798A3 (cs) | 1999-02-17 |
| CA2253429A1 (en) | 1997-11-20 |
| DE69728768T2 (de) | 2005-04-28 |
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