ZA200507896B - Fluoro-and trifluoroalkyl-containing heterocylclic sulfonamide inhibitors of beta amyloid production and derivatives thereof - Google Patents
Fluoro-and trifluoroalkyl-containing heterocylclic sulfonamide inhibitors of beta amyloid production and derivatives thereof Download PDFInfo
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- ZA200507896B ZA200507896B ZA200507896A ZA200507896A ZA200507896B ZA 200507896 B ZA200507896 B ZA 200507896B ZA 200507896 A ZA200507896 A ZA 200507896A ZA 200507896 A ZA200507896 A ZA 200507896A ZA 200507896 B ZA200507896 B ZA 200507896B
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- ZA
- South Africa
- Prior art keywords
- sulfonamide
- trifluoro
- thiophene
- chloro
- compound according
- Prior art date
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- 102000013455 Amyloid beta-Peptides Human genes 0.000 title claims description 25
- 108010090849 Amyloid beta-Peptides Proteins 0.000 title claims description 25
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- 238000004519 manufacturing process Methods 0.000 title claims description 10
- 125000004950 trifluoroalkyl group Chemical group 0.000 title description 10
- 239000003112 inhibitor Substances 0.000 title description 6
- 125000003709 fluoroalkyl group Chemical group 0.000 title description 2
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- 238000000034 method Methods 0.000 claims description 56
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- -1 CFs Chemical group 0.000 claims description 49
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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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
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- 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
- A61P25/28—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/18—One oxygen or sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/30—Hetero atoms other than halogen
- C07D333/34—Sulfur atoms
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- Chemical & Material Sciences (AREA)
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- Health & Medical Sciences (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)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45922803P | 2003-03-31 | 2003-03-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200507896B true ZA200507896B (en) | 2007-03-28 |
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| Application Number | Title | Priority Date | Filing Date |
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| ZA200507896A ZA200507896B (en) | 2003-03-31 | 2005-09-29 | Fluoro-and trifluoroalkyl-containing heterocylclic sulfonamide inhibitors of beta amyloid production and derivatives thereof |
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Families Citing this family (35)
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| ATE330950T1 (de) * | 2000-12-13 | 2006-07-15 | Wyeth Corp | Heterocyclische sulfonamide als inhibitoren der beta-amyloid-produktion |
| RS51155B (sr) * | 2001-12-20 | 2010-10-31 | Bristol-Myers Squibb Company | DERIVATI α -(N-SULFONAMIDO)ACETAMIDA KAO INHIBITORI β -AMILOIDA |
| AU2003237518B8 (en) * | 2002-06-11 | 2009-03-12 | Arqule, Inc. | Substituted phenylsulfonamide inhibitors of beta amyloid production |
| KR20060002908A (ko) * | 2003-03-31 | 2006-01-09 | 와이어쓰 | 베타 아밀로이드 생산 억제제인 플루오로- 및트리플루오로알킬-함유 헤테로사이클릭 설폰아미드 및 이의유도체 |
| ATE443701T1 (de) * | 2004-01-16 | 2009-10-15 | Wyeth Corp | Heterocyclische, ein azol enthaltende sulfonamidinhibitoren der beta-amyloid-produktion |
| CA2637615A1 (en) * | 2006-02-17 | 2007-08-30 | Wyeth | Selective n-sulfonylation of 2-amino trifluoroalkyl substituted alcohols |
| CA2641013A1 (en) * | 2006-02-17 | 2007-08-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
| US7476762B2 (en) | 2006-04-21 | 2009-01-13 | Wyeth | Methods for preparing sulfonamide compounds |
| US7550629B2 (en) | 2006-04-21 | 2009-06-23 | Wyeth | Trifluoromethyl-containing phenylsulfonamide beta amyloid inhibitors |
| CN101472877A (zh) | 2006-04-21 | 2009-07-01 | 惠氏公司 | 制备手性纯氨基醇中间体、其衍生物及其用途 |
| JP2010509235A (ja) * | 2006-11-03 | 2010-03-25 | ノースウェスタン ユニバーシティ | 多発性硬化症の治療 |
| PA8789701A1 (es) * | 2007-07-16 | 2009-04-23 | Wyeth Corp | Inhibidores de producción de beta amiloide |
| PA8789601A1 (es) * | 2007-07-16 | 2009-02-09 | Wyeth Corp | Proceso para la preparación de trifluoralquil-fenil sulfonamidas y de sulfonamidas heterocíclicas |
| PE20090810A1 (es) * | 2007-07-16 | 2009-07-20 | Wyeth Corp | Procesos e intermediarios para la preparacion de compuestos de sulfonamida heterociclica |
| US8093276B2 (en) * | 2007-10-31 | 2012-01-10 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| US8084477B2 (en) | 2007-10-31 | 2011-12-27 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| WO2009089237A1 (en) * | 2008-01-11 | 2009-07-16 | Wyeth | Compositions containing o-sulfate and o-phosphate containing aryl sulfonamide derivatives useful as beta-amyloid inhibitors |
| US20110059940A1 (en) * | 2008-05-08 | 2011-03-10 | Bristol- Myers Squibb Company | 2-Aryl Glycinamide Derivatives |
| WO2010025968A2 (en) * | 2008-09-05 | 2010-03-11 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e. V. | Process for enantioseparation of chiral systems with compound formation using two subsequent crystallization steps |
| US8044077B2 (en) * | 2009-03-19 | 2011-10-25 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production |
| US20110071199A1 (en) * | 2009-03-20 | 2011-03-24 | Bristol-Myers Squibb Company | Thiophenyl Sulfonamides for the Treatment of Alzheimer's Disease |
| US7977362B2 (en) * | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
| TW201043269A (en) * | 2009-04-14 | 2010-12-16 | Bristol Myers Squibb Co | Bioavailable compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| US8252821B2 (en) * | 2009-04-14 | 2012-08-28 | Bristol-Myers Squibb Company | Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| WO2010126002A1 (ja) * | 2009-04-28 | 2010-11-04 | 塩野義製薬株式会社 | ヘテロ環スルホンアミド化合物を含有する医薬 |
| WO2011084503A1 (en) * | 2009-12-16 | 2011-07-14 | North Carolina Central University | Phenoxy thiophene sulfonamides and their use in the treatment of neurodegenerative diseases |
| US9223209B2 (en) * | 2010-02-19 | 2015-12-29 | International Business Machines Corporation | Sulfonamide-containing photoresist compositions and methods of use |
| US9223217B2 (en) * | 2010-02-19 | 2015-12-29 | International Business Machines Corporation | Sulfonamide-containing topcoat and photoresist additive compositions and methods of use |
| US9617239B2 (en) | 2010-03-10 | 2017-04-11 | North Carolina Central University | Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| US20150209367A1 (en) | 2012-09-07 | 2015-07-30 | Massachusetts Eye & Ear Infirmary | Treating Hearing Loss |
| US20160067306A1 (en) | 2013-04-19 | 2016-03-10 | National University Corporation Hokkaido University | Treatment agent for cognitive impairment induced by amyloid beta-protein, therapeutic agent for alzheimer's disease, and treatment method and pathological analysis method related to these |
| EP3212773B1 (en) | 2014-10-29 | 2021-09-15 | Massachusetts Eye and Ear Infirmary | Efficient delivery of therapeutic molecules to cells of the inner ear |
| EP3458076A4 (en) | 2016-05-16 | 2020-01-22 | The General Hospital Corporation | HUMAN RESPIRATORY STEM CELLS IN BREEDING LUNG EPITHEL |
| EP3743057A4 (en) | 2018-01-26 | 2021-11-17 | Massachusetts Eye & Ear Infirmary | TREATMENT OF HEARING LOSS |
| EP4299062A1 (en) | 2022-06-30 | 2024-01-03 | Vilnius University | Inhibition of protein amyloid aggregation using fluorinated benzenesulfonamides |
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| ID22275A (id) | 1996-11-22 | 1999-09-23 | Elan Pharm Inc | Komposisi farmasi yang terdiri dari derivat asam amino n-(aril atau heteroaril) dan metode untuk menghambat pelepasan b-amiloid peptida dan atau sintesisnya dengan menggunakan senyawa tersebut |
| DE19650196A1 (de) * | 1996-12-04 | 1998-06-10 | Bayer Ag | Thienylsulfonylamino(thio)carbonylverbindungen |
| JPH11343279A (ja) | 1998-03-16 | 1999-12-14 | Shionogi & Co Ltd | スルホンアミド誘導体およびそれらを含有するＴＮＦ―α産生抑制剤 |
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| EP1088815A1 (en) | 1999-09-28 | 2001-04-04 | Applied Research Systems ARS Holding N.V. | Pharmaceutically active sulfonyl amino acid derivatives |
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| CA2404125C (en) | 2000-03-20 | 2011-01-25 | Merck Sharp & Dohme Limited | Sulphonamido-substituted bridged bicycloalkyl derivatives |
| US6657070B2 (en) * | 2000-12-13 | 2003-12-02 | Wyeth | Production of chirally pure α-amino acids and N-sulfonyl α-amino acids |
| ATE330950T1 (de) * | 2000-12-13 | 2006-07-15 | Wyeth Corp | Heterocyclische sulfonamide als inhibitoren der beta-amyloid-produktion |
| MXPA04005570A (es) | 2001-12-11 | 2004-12-06 | Wyeth Corp | Proceso para sintesis de beta-amino-alcoholes quiralmente puros. |
| CA2470111A1 (en) | 2001-12-11 | 2003-06-19 | Wyeth | Production of chirally pure .alpha.-amino acids and n-sulfonyl .alpha.-amino acids |
| AU2003237518B8 (en) * | 2002-06-11 | 2009-03-12 | Arqule, Inc. | Substituted phenylsulfonamide inhibitors of beta amyloid production |
| KR20060002908A (ko) * | 2003-03-31 | 2006-01-09 | 와이어쓰 | 베타 아밀로이드 생산 억제제인 플루오로- 및트리플루오로알킬-함유 헤테로사이클릭 설폰아미드 및 이의유도체 |
| ATE443701T1 (de) | 2004-01-16 | 2009-10-15 | Wyeth Corp | Heterocyclische, ein azol enthaltende sulfonamidinhibitoren der beta-amyloid-produktion |
| CA2637615A1 (en) * | 2006-02-17 | 2007-08-30 | Wyeth | Selective n-sulfonylation of 2-amino trifluoroalkyl substituted alcohols |
| CA2641013A1 (en) * | 2006-02-17 | 2007-08-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
| US7476762B2 (en) * | 2006-04-21 | 2009-01-13 | Wyeth | Methods for preparing sulfonamide compounds |
| US7550629B2 (en) * | 2006-04-21 | 2009-06-23 | Wyeth | Trifluoromethyl-containing phenylsulfonamide beta amyloid inhibitors |
| CN101472877A (zh) * | 2006-04-21 | 2009-07-01 | 惠氏公司 | 制备手性纯氨基醇中间体、其衍生物及其用途 |
| PA8789601A1 (es) * | 2007-07-16 | 2009-02-09 | Wyeth Corp | Proceso para la preparación de trifluoralquil-fenil sulfonamidas y de sulfonamidas heterocíclicas |
| PA8789701A1 (es) * | 2007-07-16 | 2009-04-23 | Wyeth Corp | Inhibidores de producción de beta amiloide |
| PE20090810A1 (es) * | 2007-07-16 | 2009-07-20 | Wyeth Corp | Procesos e intermediarios para la preparacion de compuestos de sulfonamida heterociclica |
-
2004
- 2004-03-26 KR KR1020057018637A patent/KR20060002908A/ko not_active Application Discontinuation
- 2004-03-26 RU RU2005133434/04A patent/RU2342374C2/ru not_active IP Right Cessation
- 2004-03-26 WO PCT/US2004/009268 patent/WO2004092155A1/en active Application Filing
- 2004-03-26 BR BRPI0408962-6A patent/BRPI0408962A/pt not_active IP Right Cessation
- 2004-03-26 JP JP2006509331A patent/JP2006522126A/ja active Pending
- 2004-03-26 AU AU2004230844A patent/AU2004230844B2/en not_active Expired - Fee Related
- 2004-03-26 EP EP04758978A patent/EP1608638A1/en not_active Withdrawn
- 2004-03-26 UA UAA200510177A patent/UA82093C2/uk unknown
- 2004-03-26 CN CNA2008100013400A patent/CN101274926A/zh active Pending
- 2004-03-26 NZ NZ542468A patent/NZ542468A/en not_active IP Right Cessation
- 2004-03-26 SG SG200708961-8A patent/SG167669A1/en unknown
- 2004-03-26 CN CN2004800087813A patent/CN1780829B/zh not_active Expired - Fee Related
- 2004-03-26 AR ARP040101022A patent/AR043940A1/es unknown
- 2004-03-26 US US10/810,517 patent/US7300951B2/en not_active Expired - Fee Related
- 2004-03-26 MX MXPA05010368A patent/MXPA05010368A/es active IP Right Grant
- 2004-03-26 CL CL200400647A patent/CL2004000647A1/es unknown
- 2004-03-26 CA CA002517155A patent/CA2517155A1/en not_active Abandoned
- 2004-03-26 TW TW093108219A patent/TWI336698B/zh not_active IP Right Cessation
-
2005
- 2005-08-19 CR CR7951A patent/CR7951A/es unknown
- 2005-09-15 NO NO20054263A patent/NO20054263L/no not_active Application Discontinuation
- 2005-09-29 ZA ZA200507896A patent/ZA200507896B/en unknown
- 2005-10-26 CO CO05109226A patent/CO5640049A2/es not_active Application Discontinuation
- 2005-10-28 EC EC2005006128A patent/ECSP056128A/es unknown
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2007
- 2007-06-15 US US11/818,630 patent/US7547725B2/en not_active Expired - Fee Related
-
2009
- 2009-05-05 US US12/435,442 patent/US7858658B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20070254929A1 (en) | 2007-11-01 |
| UA82093C2 (uk) | 2008-03-11 |
| CA2517155A1 (en) | 2004-10-28 |
| AR043940A1 (es) | 2005-08-17 |
| AU2004230844B2 (en) | 2010-12-09 |
| CR7951A (es) | 2008-10-29 |
| NO20054263D0 (no) | 2005-09-15 |
| US7300951B2 (en) | 2007-11-27 |
| CN1780829A (zh) | 2006-05-31 |
| US7858658B2 (en) | 2010-12-28 |
| NZ542468A (en) | 2009-01-31 |
| ECSP056128A (es) | 2006-03-01 |
| JP2006522126A (ja) | 2006-09-28 |
| AU2004230844A1 (en) | 2004-10-28 |
| TWI336698B (en) | 2011-02-01 |
| CN1780829B (zh) | 2010-12-29 |
| BRPI0408962A (pt) | 2006-04-04 |
| CN101274926A (zh) | 2008-10-01 |
| SG167669A1 (en) | 2011-01-28 |
| RU2005133434A (ru) | 2006-07-10 |
| RU2342374C2 (ru) | 2008-12-27 |
| US7547725B2 (en) | 2009-06-16 |
| EP1608638A1 (en) | 2005-12-28 |
| TW200504047A (en) | 2005-02-01 |
| US20090227667A1 (en) | 2009-09-10 |
| US20040198778A1 (en) | 2004-10-07 |
| MXPA05010368A (es) | 2005-11-17 |
| KR20060002908A (ko) | 2006-01-09 |
| CL2004000647A1 (es) | 2005-02-04 |
| NO20054263L (no) | 2005-12-14 |
| WO2004092155A1 (en) | 2004-10-28 |
| CO5640049A2 (es) | 2006-05-31 |
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