JP2004522694A5 - - Google Patents
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- JP2004522694A5 JP2004522694A5 JP2002508451A JP2002508451A JP2004522694A5 JP 2004522694 A5 JP2004522694 A5 JP 2004522694A5 JP 2002508451 A JP2002508451 A JP 2002508451A JP 2002508451 A JP2002508451 A JP 2002508451A JP 2004522694 A5 JP2004522694 A5 JP 2004522694A5
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- JP
- Japan
- Prior art keywords
- pharmaceutical composition
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- prodrug
- cancer cells
- group
- 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.)
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- 210000004027 cell Anatomy 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 239000000651 prodrug Substances 0.000 claims 7
- 229940002612 prodrug Drugs 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 claims 4
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 239000002777 nucleoside Substances 0.000 claims 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 229910019142 PO4 Inorganic materials 0.000 claims 2
- -1 R 5 is OH Chemical class 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229940127073 nucleoside analogue Drugs 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 2
- 239000010452 phosphate Substances 0.000 claims 2
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 210000004881 tumor cell Anatomy 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000017143 RNA Polymerase I Human genes 0.000 claims 1
- 108010013845 RNA Polymerase I Proteins 0.000 claims 1
- 102000009572 RNA Polymerase II Human genes 0.000 claims 1
- 108010009460 RNA Polymerase II Proteins 0.000 claims 1
- 102000014450 RNA Polymerase III Human genes 0.000 claims 1
- 108010078067 RNA Polymerase III Proteins 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000000873 masking effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000035407 negative regulation of cell proliferation Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000026731 phosphorylation Effects 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21641800P | 2000-07-06 | 2000-07-06 | |
| PCT/US2001/041242 WO2002003997A1 (en) | 2000-07-06 | 2001-07-03 | Pyrido[2,3-d]pyrimidine and pyrimido[4,5-d]pyrimidine nucleosides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004522694A JP2004522694A (ja) | 2004-07-29 |
| JP2004522694A5 true JP2004522694A5 (enExample) | 2005-03-17 |
Family
ID=22806989
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002508451A Withdrawn JP2004522694A (ja) | 2000-07-06 | 2001-07-03 | ピリド［２，３−ｄ］ピリミジンおよびピリミド［４，５−ｄ］ピリミジンヌクレオシド |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7081449B2 (enExample) |
| EP (1) | EP1303282A4 (enExample) |
| JP (1) | JP2004522694A (enExample) |
| KR (1) | KR20030032944A (enExample) |
| CN (1) | CN1440292A (enExample) |
| AU (2) | AU7367001A (enExample) |
| BR (1) | BR0111531A (enExample) |
| CA (1) | CA2405798A1 (enExample) |
| CZ (1) | CZ20024052A3 (enExample) |
| HU (1) | HUP0301614A3 (enExample) |
| IL (1) | IL151849A0 (enExample) |
| MX (1) | MXPA02012156A (enExample) |
| NO (1) | NO20030033L (enExample) |
| NZ (1) | NZ521457A (enExample) |
| PL (1) | PL359559A1 (enExample) |
| SK (1) | SK112003A3 (enExample) |
| UA (1) | UA72612C2 (enExample) |
| WO (1) | WO2002003997A1 (enExample) |
| ZA (1) | ZA200208010B (enExample) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003532643A (ja) | 2000-04-13 | 2003-11-05 | フアーマセツト・リミテツド | 肝炎ウイルス感染症を治療するための３’−または２’−ヒドロキシメチル置換ヌクレオシド誘導体 |
| MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| CZ301182B6 (cs) | 2000-05-26 | 2009-12-02 | Idenix (Cayman) Limited | Použití nukleosidových derivátu pro výrobu farmaceutických prostredku pro lécení infekcí vyvolaných flaviviry a pestiviry |
| JP4942915B2 (ja) | 2002-04-26 | 2012-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積 |
| MXPA04012802A (es) | 2002-06-28 | 2005-04-19 | Idenix Cayman Ltd | Ester 2'-c-metil-3'-o-l-valina de ribofuranosil-citidina para el tratamiento de infecciones por flaviviridae. |
| NZ537662A (en) | 2002-06-28 | 2007-10-26 | Idenix Cayman Ltd | 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections |
| CA2494340C (en) | 2002-08-01 | 2012-01-24 | Pharmasset Inc. | Compounds with the bicyclo[4.2.1]nonane system for the treatment of flaviviridae infections |
| WO2004046331A2 (en) | 2002-11-15 | 2004-06-03 | Idenix (Cayman) Limited | 2’-branched nucleosides and flaviviridae mutation |
| US7598373B2 (en) | 2002-12-12 | 2009-10-06 | Idenix Pharmaceuticals, Inc. | Process for the production of 2-C-methyl-D-ribonolactone |
| US7300924B2 (en) | 2003-04-25 | 2007-11-27 | Gilead Sciences, Inc. | Anti-infective phosphonate analogs |
| MXPA05011296A (es) | 2003-04-25 | 2006-01-24 | Gilead Sciences Inc | Conjugados de fosfonato inhibidores de la cinasa. |
| US7470724B2 (en) | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
| US7432261B2 (en) | 2003-04-25 | 2008-10-07 | Gilead Sciences, Inc. | Anti-inflammatory phosphonate compounds |
| US7427636B2 (en) | 2003-04-25 | 2008-09-23 | Gilead Sciences, Inc. | Inosine monophosphate dehydrogenase inhibitory phosphonate compounds |
| EP1628685B1 (en) | 2003-04-25 | 2010-12-08 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| US7452901B2 (en) | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
| WO2005002626A2 (en) | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
| US7407965B2 (en) | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
| WO2004113357A2 (en) * | 2003-05-20 | 2004-12-29 | The Board Of Trustees Of The University Of Illinois | Nucleoside analog inhibitors of reverse transcriptase |
| EP2345659A1 (en) | 2003-05-30 | 2011-07-20 | Pharmasset, Inc. | Modified fluorinated nucleoside analogues |
| DE602004028841D1 (de) | 2003-07-25 | 2010-10-07 | Centre Nat Rech Scient | Purin nucleoside für die behandlung von durch flavividrae verursachten krankheiten, einschliesslich hepatitis c |
| US7432273B2 (en) | 2003-10-24 | 2008-10-07 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
| EP1678321A1 (en) | 2003-10-24 | 2006-07-12 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
| WO2005044279A1 (en) | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Purine nucleoside phosphonate conjugates |
| JP2007515495A (ja) | 2003-12-22 | 2007-06-14 | ギリアード サイエンシーズ， インコーポレイテッド | ４’−置換カルボビル誘導体およびアバカビル誘導体ならびにｈｉｖおよびｈｃｖ抗ウイルス活性を有する関連化合物 |
| US20050182252A1 (en) | 2004-02-13 | 2005-08-18 | Reddy K. R. | Novel 2'-C-methyl nucleoside derivatives |
| US7378423B2 (en) | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| RU2364596C2 (ru) * | 2004-06-11 | 2009-08-20 | Джапан Тобакко Инк. | ПРОИЗВОДНЫЕ 5-АМИНО-2,4,7-ТРИОКСО-3,4,7,8-ТЕТРАГИДРО-2Н-ПИРИДО[2,3-d] ПИРИМИДИНА, ОБЛАДАЮЩИЕ ПРОТИВООПУХОЛЕВОЙ АКТИВНОСТЬЮ |
| CN101023094B (zh) * | 2004-07-21 | 2011-05-18 | 法莫赛特股份有限公司 | 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备 |
| WO2006110157A2 (en) | 2004-07-27 | 2006-10-19 | Gilead Sciences, Inc. | Nucleoside phosphonate conjugates as anti hiv agents |
| ES2769377T3 (es) * | 2004-09-14 | 2020-06-25 | Gilead Pharmasset Llc | Intermedios de D-ribonolactona con sustitución de 2-fluoro-2-alquilo |
| AU2006222563A1 (en) * | 2005-03-08 | 2006-09-14 | Biota Scientific Management Pty Ltd. | Bicyclic nucleosides and nucleotides as therapeutic agents |
| US7951789B2 (en) * | 2006-12-28 | 2011-05-31 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| BRPI0815563A2 (pt) * | 2007-07-12 | 2015-02-18 | Univ South Florida | Inibidores de akt/pkb com atividade antitumoral |
| US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
| HRP20120700T1 (hr) | 2008-07-08 | 2012-09-30 | Gilead Sciences | SOLI SPOJEVA INHIBITORA HIV-a |
| AU2009329917B2 (en) | 2008-12-23 | 2016-03-31 | Gilead Pharmasset Llc | Nucleoside analogs |
| CN102695513A (zh) | 2008-12-23 | 2012-09-26 | 吉利德制药有限责任公司 | 核苷氨基磷酸酯 |
| BRPI0923815A2 (pt) | 2008-12-23 | 2015-07-14 | Pharmasset Inc | Síntese de nucleosídeos de purina |
| US20100249068A1 (en) | 2009-03-20 | 2010-09-30 | Alios Biopharma, Inc. | Substituted nucleoside and nucleotide analogs |
| US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
| TWI583692B (zh) | 2009-05-20 | 2017-05-21 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
| SMT201700412T1 (it) | 2010-03-31 | 2017-11-15 | Gilead Pharmasset Llc | Procedimento per la cristallizzazione di (s)-isopropil 2-(((s)-(perfluorofenossi)(fenossi)fosforil)ammino)propanoato |
| US8563530B2 (en) | 2010-03-31 | 2013-10-22 | Gilead Pharmassel LLC | Purine nucleoside phosphoramidate |
| EA025341B1 (ru) | 2010-09-22 | 2016-12-30 | Алиос Биофарма, Инк. | Замещенные аналоги нуклеотидов |
| WO2012158197A2 (en) * | 2010-11-11 | 2012-11-22 | Lyndor Biosciences L.L.C. | Compounds useful as akt/pkb modulators and uses thereof |
| PT3042910T (pt) | 2010-11-30 | 2019-04-16 | Gilead Pharmasset Llc | 2'-espiro-nucleósidos para utilização na terapia da hepatite c |
| EP2709613B2 (en) | 2011-09-16 | 2020-08-12 | Gilead Pharmasset LLC | Methods for treating hcv |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| EP2794627B1 (en) | 2011-12-22 | 2018-09-26 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2013096680A1 (en) | 2011-12-22 | 2013-06-27 | Alios Biopharma, Inc. | Substituted phosphorothioate nucleotide analogs |
| KR20140138911A (ko) * | 2012-03-14 | 2014-12-04 | 루핀 리미티드 | Ｍｅｋ 억제제로서 헤테로사이클릴 화합물 |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| US8916538B2 (en) | 2012-03-21 | 2014-12-23 | Vertex Pharmaceuticals Incorporated | Solid forms of a thiophosphoramidate nucleotide prodrug |
| NZ630805A (en) | 2012-03-22 | 2016-01-29 | Alios Biopharma Inc | Pharmaceutical combinations comprising a thionucleotide analog |
| HUE029038T2 (en) | 2012-05-25 | 2017-01-30 | Janssen Sciences Ireland Uc | Uracil spirooxetan nucleosides |
| CN102816197B (zh) * | 2012-08-24 | 2015-04-29 | 四川大学华西医院 | 一种新的嘧啶并嘧啶类核苷类似物、制备方法及其形成的超分子结构和应用 |
| EP2935303B1 (en) | 2012-12-21 | 2021-02-17 | Janssen BioPharma, Inc. | 4'-fluoro-nucleosides, 4'-fluoro-nucleotides and analogs thereof for the treatment of hcv |
| PL2950786T3 (pl) | 2013-01-31 | 2020-05-18 | Gilead Pharmasset Llc | Formulacja skojarzona dwóch związków przeciwwirusowych |
| PL3038601T3 (pl) | 2013-08-27 | 2020-08-24 | Gilead Pharmasset Llc | Formulacja złożona dwóch związków przeciwwirusowych |
| AU2014331863C1 (en) | 2013-10-11 | 2019-05-16 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2015123352A1 (en) | 2014-02-13 | 2015-08-20 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and their uses |
| CN106687118A (zh) | 2014-07-02 | 2017-05-17 | 配体药物公司 | 前药化合物及其用途 |
| US10358458B2 (en) | 2014-09-26 | 2019-07-23 | Riboscience Llc | 4′-vinyl substituted nucleoside derivatives as inhibitors of respiratory syncytial virus RNA replication |
| ES2892402T3 (es) | 2017-08-01 | 2022-02-04 | Gilead Sciences Inc | Formas cristalinas de ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il)oxi)metil)(fenoxi)fosforil)-L-alaninato de etilo para tratar infecciones virales |
| CN111788196A (zh) | 2018-01-09 | 2020-10-16 | 配体药物公司 | 缩醛化合物及其治疗用途 |
| DK3794012T3 (da) * | 2018-05-15 | 2024-01-08 | Illumina Inc | Sammensætninger og fremgangsmåder til kemisk spaltning og afbeskyttelse af overfladebundne oligonukleotider |
| MX2021011606A (es) | 2019-04-02 | 2021-12-10 | Aligos Therapeutics Inc | Compuestos dirigidos a prmt5. |
| CN111995649A (zh) * | 2020-04-09 | 2020-11-27 | 瀚海新拓(杭州)生物医药有限公司 | 一种蝶啶酮核苷酸类似物及其药物组合物、制备方法和医药用途 |
| CN117120090A (zh) * | 2021-02-12 | 2023-11-24 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
| JP2024509192A (ja) | 2021-03-05 | 2024-02-29 | ニンバス サターン， インコーポレイテッド | Ｈｐｋ１アンタゴニスト及びその使用 |
| JP2024513011A (ja) | 2021-03-29 | 2024-03-21 | ニンバス サターン， インコーポレイテッド | Ｈｐｋ１アンタゴニスト及びその使用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3423398A (en) * | 1965-05-10 | 1969-01-21 | Pfizer & Co C | Sangivamycin and derivatives thereof |
| JPH0725788B2 (ja) * | 1985-09-09 | 1995-03-22 | 帝人株式会社 | オリゴまたはポリヌクレオチド |
| US5034393A (en) * | 1989-07-27 | 1991-07-23 | Dowelanco | Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives |
-
2001
- 2001-03-07 UA UA2002119182A patent/UA72612C2/uk unknown
- 2001-07-03 CZ CZ20024052A patent/CZ20024052A3/cs unknown
- 2001-07-03 NZ NZ521457A patent/NZ521457A/en unknown
- 2001-07-03 KR KR1020027014601A patent/KR20030032944A/ko not_active Abandoned
- 2001-07-03 WO PCT/US2001/041242 patent/WO2002003997A1/en not_active Ceased
- 2001-07-03 IL IL15184901A patent/IL151849A0/xx unknown
- 2001-07-03 MX MXPA02012156A patent/MXPA02012156A/es unknown
- 2001-07-03 AU AU7367001A patent/AU7367001A/xx active Pending
- 2001-07-03 CN CN01812327A patent/CN1440292A/zh active Pending
- 2001-07-03 HU HU0301614A patent/HUP0301614A3/hu unknown
- 2001-07-03 JP JP2002508451A patent/JP2004522694A/ja not_active Withdrawn
- 2001-07-03 US US10/221,397 patent/US7081449B2/en not_active Expired - Fee Related
- 2001-07-03 SK SK11-2003A patent/SK112003A3/sk unknown
- 2001-07-03 BR BR0111531-6A patent/BR0111531A/pt not_active IP Right Cessation
- 2001-07-03 EP EP01952967A patent/EP1303282A4/en not_active Withdrawn
- 2001-07-03 CA CA002405798A patent/CA2405798A1/en not_active Abandoned
- 2001-07-03 PL PL01359559A patent/PL359559A1/xx not_active Application Discontinuation
- 2001-07-03 AU AU2001273670A patent/AU2001273670B2/en not_active Expired - Fee Related
-
2002
- 2002-10-04 ZA ZA200208010A patent/ZA200208010B/en unknown
-
2003
- 2003-01-03 NO NO20030033A patent/NO20030033L/no not_active Application Discontinuation
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