RU2278117C2 - Антибактериальные гетеробициклические замещенные фенилоксазолидиноны - Google Patents
Антибактериальные гетеробициклические замещенные фенилоксазолидиноны Download PDFInfo
- Publication number
- RU2278117C2 RU2278117C2 RU2002103379/04A RU2002103379A RU2278117C2 RU 2278117 C2 RU2278117 C2 RU 2278117C2 RU 2002103379/04 A RU2002103379/04 A RU 2002103379/04A RU 2002103379 A RU2002103379 A RU 2002103379A RU 2278117 C2 RU2278117 C2 RU 2278117C2
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- Prior art keywords
- formula
- compound according
- group
- mmol
- compound
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Links
- 0 CC*(B=C)*=C(C(*)(*)N(C)C1(*)*)C1=*C Chemical compound CC*(B=C)*=C(C(*)(*)N(C)C1(*)*)C1=*C 0.000 description 2
- KRMSGDZIIUIOLC-INIZCTEOSA-N CC(NC[C@@H](CN1c(cc2F)ccc2-[n]2cc(cncc3)c3c2)OC1=O)=O Chemical compound CC(NC[C@@H](CN1c(cc2F)ccc2-[n]2cc(cncc3)c3c2)OC1=O)=O KRMSGDZIIUIOLC-INIZCTEOSA-N 0.000 description 1
- AKRSGQPSZWNVSP-INIZCTEOSA-N CC(NC[C@@H](CN1c(cc2F)ccc2N(C2)Cc3c2ccnc3)OC1=O)=O Chemical compound CC(NC[C@@H](CN1c(cc2F)ccc2N(C2)Cc3c2ccnc3)OC1=O)=O AKRSGQPSZWNVSP-INIZCTEOSA-N 0.000 description 1
- LUJNHYPDRJJTCQ-KRWDZBQOSA-N CC(NC[C@@H](CN1c(cc2F)ccc2N(C2)Cc3c2cnc(-c2ncccc2)n3)OC1=O)=O Chemical compound CC(NC[C@@H](CN1c(cc2F)ccc2N(C2)Cc3c2cnc(-c2ncccc2)n3)OC1=O)=O LUJNHYPDRJJTCQ-KRWDZBQOSA-N 0.000 description 1
- IFWFSZKABQCYCQ-HNNXBMFYSA-N CC(NC[C@@H](CN1c(cc2F)ccc2N(C2)Cc3c2cnc(C)n3)OC1=O)=O Chemical compound CC(NC[C@@H](CN1c(cc2F)ccc2N(C2)Cc3c2cnc(C)n3)OC1=O)=O IFWFSZKABQCYCQ-HNNXBMFYSA-N 0.000 description 1
- AEAXDUVTXJYBPV-CVMIBEPCSA-N CC1O[C@@H](CC(C(c2ccccc22)=O)C2=O)CN1c(cc1F)ccc1N1Cc2ncccc2C1 Chemical compound CC1O[C@@H](CC(C(c2ccccc22)=O)C2=O)CN1c(cc1F)ccc1N1Cc2ncccc2C1 AEAXDUVTXJYBPV-CVMIBEPCSA-N 0.000 description 1
- SOYZYGIUZGIPKP-HNNXBMFYSA-N CCOC(NC[C@@H](CN1c(cc2F)ccc2N2Cc3ncccc3C2)OC1=O)=O Chemical compound CCOC(NC[C@@H](CN1c(cc2F)ccc2N2Cc3ncccc3C2)OC1=O)=O SOYZYGIUZGIPKP-HNNXBMFYSA-N 0.000 description 1
- XQAJEOMKVSIEPL-INIZCTEOSA-N CCS/C(/NC[C@@H](CN1c(cc2F)ccc2-[n]2cc3ncccc3c2)OC1=O)=N\C#N Chemical compound CCS/C(/NC[C@@H](CN1c(cc2F)ccc2-[n]2cc3ncccc3c2)OC1=O)=N\C#N XQAJEOMKVSIEPL-INIZCTEOSA-N 0.000 description 1
- DDYHWAGZGNBPGX-UHFFFAOYSA-N CN1Cc2cnccc2C1 Chemical compound CN1Cc2cnccc2C1 DDYHWAGZGNBPGX-UHFFFAOYSA-N 0.000 description 1
- UHOSSLQGONSMQB-OAHLLOKOSA-N O=C1O[C@@H](COc2n[s]nc2)CN1c(cc1F)ccc1N1Cc2cnccc2C1 Chemical compound O=C1O[C@@H](COc2n[s]nc2)CN1c(cc1F)ccc1N1Cc2cnccc2C1 UHOSSLQGONSMQB-OAHLLOKOSA-N 0.000 description 1
- JDXHDLULUWEYIU-UHFFFAOYSA-N [O-][N+](c(cc1F)ccc1N1Cc2ncccc2C1)=O Chemical compound [O-][N+](c(cc1F)ccc1N1Cc2ncccc2C1)=O JDXHDLULUWEYIU-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- Oncology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14862199P | 1999-08-12 | 1999-08-12 | |
| US60/148,621 | 1999-08-12 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2002103379A RU2002103379A (ru) | 2003-09-20 |
| RU2278117C2 true RU2278117C2 (ru) | 2006-06-20 |
Family
ID=22526580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2002103379/04A RU2278117C2 (ru) | 1999-08-12 | 2000-08-02 | Антибактериальные гетеробициклические замещенные фенилоксазолидиноны |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US6413981B1 (https=) |
| EP (1) | EP1206469B1 (https=) |
| JP (1) | JP2003516404A (https=) |
| KR (1) | KR100463634B1 (https=) |
| CN (1) | CN1330647C (https=) |
| AR (1) | AR025225A1 (https=) |
| AT (1) | ATE260276T1 (https=) |
| AU (1) | AU783088B2 (https=) |
| BR (1) | BR0013237A (https=) |
| CA (1) | CA2378183C (https=) |
| CZ (1) | CZ2002882A3 (https=) |
| DE (1) | DE60008545T2 (https=) |
| DK (1) | DK1206469T3 (https=) |
| ES (1) | ES2215713T3 (https=) |
| HU (1) | HUP0202447A3 (https=) |
| IL (1) | IL147868A0 (https=) |
| MX (1) | MXPA02001559A (https=) |
| MY (1) | MY125359A (https=) |
| PL (1) | PL198558B1 (https=) |
| PT (1) | PT1206469E (https=) |
| RU (1) | RU2278117C2 (https=) |
| TW (1) | TW593313B (https=) |
| WO (1) | WO2001042242A1 (https=) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2556234C2 (ru) * | 2008-10-10 | 2015-07-10 | Траюс Терапьютикс | Способы получения оксазолидинонов и содержащих их композиций |
| US9624250B2 (en) | 2009-02-03 | 2017-04-18 | Merck Sharp & Dohme Corp. | Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| US10913752B2 (en) | 2015-11-25 | 2021-02-09 | Dana-Farber Cancer Institute, Inc. | Bivalent bromodomain inhibitors and uses thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6608081B2 (en) * | 1999-08-12 | 2003-08-19 | Ortho-Mcneil Pharmaceutical, Inc. | Bicyclic heterocyclic substituted phenyl oxazolidinone antibacterials, and related compositions and methods |
| GB9928568D0 (en) | 1999-12-03 | 2000-02-02 | Zeneca Ltd | Chemical compounds |
| DE19962924A1 (de) * | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| GB0009803D0 (en) | 2000-04-25 | 2000-06-07 | Astrazeneca Ab | Chemical compounds |
| DE60118241T2 (de) * | 2000-10-17 | 2006-12-28 | Pharmacia & Upjohn Co. Llc, Kalamazoo | Verfahren zur herstellung von oxazolidinonverbindungen |
| DE10129725A1 (de) | 2001-06-20 | 2003-01-02 | Bayer Ag | Kombinationstherapie substituierter Oxazolidinone |
| WO2003093247A2 (en) * | 2002-04-30 | 2003-11-13 | Orchid Chemicals & Pharmaceuticals Ltd | Antibacterial agents |
| WO2003106454A1 (en) * | 2002-06-12 | 2003-12-24 | Orchid Chemicals & Pharmaceuticals Ltd | 1h-isoquinoline-oxazolidinone derivaties and their use as antibacterial agents |
| AU2002339721A1 (en) | 2002-09-20 | 2004-04-08 | Lupin Limited | Oxazolidinone derivatives, process for their preperation and their use as antimycobacterial agents |
| AR043050A1 (es) | 2002-09-26 | 2005-07-13 | Rib X Pharmaceuticals Inc | Compuestos heterociclicos bifuncionales y metodos para preparar y usar los mismos |
| DE10355461A1 (de) | 2003-11-27 | 2005-06-23 | Bayer Healthcare Ag | Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung |
| KR100854211B1 (ko) | 2003-12-18 | 2008-08-26 | 동아제약주식회사 | 신규한 옥사졸리디논 유도체, 그의 제조방법 및 이를유효성분으로 하는 항생제용 약학 조성물 |
| JP5383037B2 (ja) | 2004-02-27 | 2014-01-08 | リブ−エックス ファーマシューティカルズ，インコーポレイテッド | 大環状化合物およびそれらを製造し使用する方法 |
| EP1685841A1 (en) | 2005-01-31 | 2006-08-02 | Bayer Health Care Aktiengesellschaft | Prevention and treatment of thromboembolic disorders |
| EP3290427A1 (en) | 2005-08-24 | 2018-03-07 | Melinta Therapeutics, Inc. | Triazole compounds and methods of making and using the same |
| JP2009506063A (ja) | 2005-08-24 | 2009-02-12 | リブ−エックス ファーマシューティカルズ，インコーポレイテッド | トリアゾール化合物ならびにこれを作製する方法および使用する方法 |
| DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
| US8188270B2 (en) | 2005-10-04 | 2012-05-29 | Bayer Schering Pharma Aktiengesellschaft | Polymorphous form of 5-chloro-N-({(5S)-2-oxo-3[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide |
| JP4012239B2 (ja) * | 2006-01-11 | 2007-11-21 | 生化学工業株式会社 | オキサゾロン誘導体 |
| US7776855B2 (en) * | 2006-07-27 | 2010-08-17 | Janssen Pharmaceutica N.V. | Antimicrobial oxazolidinone prodrugs |
| WO2008045473A1 (en) * | 2006-10-11 | 2008-04-17 | Transform Pharmaceuticals, Inc. | Novel crystal of n-[[(5s)-3-[4-(2,6-dihydro-2-methylpyrolo[3,4-c] pyrazol-5(4h)-yl)-3-fluoropheny]-2-oxo-5-oxazolidinyl]methyl] acetamide |
| US8124623B2 (en) | 2006-11-10 | 2012-02-28 | Actelion Pharmaceuticals Ltd. | 5-hydroxymethyl-oxazolidin-2-one-derivatives and their uses as antibacterials |
| RU2453546C2 (ru) * | 2006-11-10 | 2012-06-20 | Актелион Фармасьютиклз Лтд | Производные 5-гидроксиметилоксазолидин-2-она |
| CN101084901B (zh) * | 2007-06-22 | 2011-12-21 | 复旦大学 | 一种葡萄球菌抑制剂 |
| US8218847B2 (en) | 2008-06-06 | 2012-07-10 | Superdimension, Ltd. | Hybrid registration method |
| CN103030634B (zh) * | 2011-09-30 | 2015-07-15 | 山东轩竹医药科技有限公司 | 含有并环的噁唑烷酮类抗菌素 |
| JP6162704B2 (ja) * | 2011-10-11 | 2017-07-12 | カウンシル オブ サイエンティフィク アンド インダストリアル リサーチ | オキサゾリジノン誘導体のシラアナログ及びその合成 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996023788A1 (en) * | 1995-02-03 | 1996-08-08 | Pharmacia + Upjohn Company | Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials |
| RU2105003C1 (ru) * | 1992-05-08 | 1998-02-20 | Дзе Апджон Компани | Производное оксазолидинона или его фармацевтически приемлемая соль, способ лечения микробных инфекций у теплокровных животных |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE146783T1 (de) | 1991-11-01 | 1997-01-15 | Upjohn Co | Substituierte aryl- und heteroaryl- phenyloxazolidinone |
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- 2000-07-21 US US09/621,814 patent/US6413981B1/en not_active Expired - Lifetime
- 2000-08-02 CA CA002378183A patent/CA2378183C/en not_active Expired - Lifetime
- 2000-08-02 BR BR0013237-3A patent/BR0013237A/pt not_active Application Discontinuation
- 2000-08-02 ES ES00957285T patent/ES2215713T3/es not_active Expired - Lifetime
- 2000-08-02 WO PCT/US2000/021093 patent/WO2001042242A1/en not_active Ceased
- 2000-08-02 JP JP2001543541A patent/JP2003516404A/ja active Pending
- 2000-08-02 DK DK00957285T patent/DK1206469T3/da active
- 2000-08-02 AU AU68928/00A patent/AU783088B2/en not_active Ceased
- 2000-08-02 HU HU0202447A patent/HUP0202447A3/hu unknown
- 2000-08-02 AT AT00957285T patent/ATE260276T1/de active
- 2000-08-02 MX MXPA02001559A patent/MXPA02001559A/es active IP Right Grant
- 2000-08-02 KR KR10-2002-7001679A patent/KR100463634B1/ko not_active Expired - Fee Related
- 2000-08-02 RU RU2002103379/04A patent/RU2278117C2/ru not_active IP Right Cessation
- 2000-08-02 IL IL14786800A patent/IL147868A0/xx unknown
- 2000-08-02 EP EP00957285A patent/EP1206469B1/en not_active Expired - Lifetime
- 2000-08-02 CZ CZ2002882A patent/CZ2002882A3/cs unknown
- 2000-08-02 PL PL354200A patent/PL198558B1/pl not_active IP Right Cessation
- 2000-08-02 DE DE60008545T patent/DE60008545T2/de not_active Expired - Lifetime
- 2000-08-02 CN CNB008178763A patent/CN1330647C/zh not_active Expired - Fee Related
- 2000-08-02 PT PT00957285T patent/PT1206469E/pt unknown
- 2000-08-10 MY MYPI20003657 patent/MY125359A/en unknown
- 2000-08-11 AR ARP000104161A patent/AR025225A1/es not_active Application Discontinuation
- 2000-09-18 TW TW089116145A patent/TW593313B/zh not_active IP Right Cessation
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2002
- 2002-01-10 US US10/043,747 patent/US20030171366A1/en not_active Abandoned
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| RU2105003C1 (ru) * | 1992-05-08 | 1998-02-20 | Дзе Апджон Компани | Производное оксазолидинона или его фармацевтически приемлемая соль, способ лечения микробных инфекций у теплокровных животных |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2556234C2 (ru) * | 2008-10-10 | 2015-07-10 | Траюс Терапьютикс | Способы получения оксазолидинонов и содержащих их композиций |
| US9328087B2 (en) | 2008-10-10 | 2016-05-03 | Merck Sharp & Dohme Corp. | Methods for preparing oxazolidinones and compositions containing them |
| RU2659792C1 (ru) * | 2008-10-10 | 2018-07-04 | Мерк Шарп Энд Домэ Корп. | Оксазолидиноны и способ их очистки |
| US9624250B2 (en) | 2009-02-03 | 2017-04-18 | Merck Sharp & Dohme Corp. | Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate |
| US9988406B2 (en) | 2009-02-03 | 2018-06-05 | Merck Sharp & Dohme Corp. | Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate |
| US10065947B1 (en) | 2009-02-03 | 2018-09-04 | Merck Sharp & Dohme Corp. | Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate |
| US10442829B2 (en) | 2009-02-03 | 2019-10-15 | Merck Sharp & Dohme Corp. | Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| US10913752B2 (en) | 2015-11-25 | 2021-02-09 | Dana-Farber Cancer Institute, Inc. | Bivalent bromodomain inhibitors and uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| KR100463634B1 (ko) | 2004-12-30 |
| PL198558B1 (pl) | 2008-06-30 |
| ES2215713T3 (es) | 2004-10-16 |
| PL354200A1 (en) | 2003-12-29 |
| KR20020016652A (ko) | 2002-03-04 |
| DK1206469T3 (da) | 2004-05-10 |
| US20030171366A1 (en) | 2003-09-11 |
| MY125359A (en) | 2006-07-31 |
| HUP0202447A2 (en) | 2002-10-28 |
| AU783088B2 (en) | 2005-09-22 |
| WO2001042242A1 (en) | 2001-06-14 |
| CZ2002882A3 (cs) | 2002-06-12 |
| IL147868A0 (en) | 2002-08-14 |
| AU6892800A (en) | 2001-06-18 |
| DE60008545D1 (de) | 2004-04-01 |
| EP1206469B1 (en) | 2004-02-25 |
| CN1414964A (zh) | 2003-04-30 |
| DE60008545T2 (de) | 2004-12-23 |
| US6413981B1 (en) | 2002-07-02 |
| ATE260276T1 (de) | 2004-03-15 |
| HUP0202447A3 (en) | 2003-10-28 |
| CN1330647C (zh) | 2007-08-08 |
| AR025225A1 (es) | 2002-11-13 |
| BR0013237A (pt) | 2003-07-15 |
| CA2378183A1 (en) | 2001-06-14 |
| EP1206469A1 (en) | 2002-05-22 |
| MXPA02001559A (es) | 2003-10-14 |
| RU2002103379A (ru) | 2003-09-20 |
| JP2003516404A (ja) | 2003-05-13 |
| PT1206469E (pt) | 2004-06-30 |
| CA2378183C (en) | 2009-10-20 |
| TW593313B (en) | 2004-06-21 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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Effective date: 20051208 |
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| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20090803 |