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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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45922803P | 2003-03-31 | 2003-03-31 |
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|---|---|
| ZA200507896B true ZA200507896B (en) | 2007-03-28 |
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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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| EA009035B1 (ru) * | 2000-12-13 | 2007-10-26 | Уиет | Получение гетероциклических сульфонамидных ингибиторов бета-амилоида |
| ATE430727T1 (de) * | 2001-12-20 | 2009-05-15 | Bristol Myers Squibb Co | Alpha-(n-sulfonamid)acetamidderivate als beta- amyloidinhibitoren |
| IL165265A0 (en) * | 2002-06-11 | 2005-12-18 | Wyeth Corp | Substituted phenylsulfonamide inhibitors of beta amyloid production |
| CL2004000647A1 (es) * | 2003-03-31 | 2005-02-04 | Wyeth Corp | Compuestos derivados de heterociclicos de sulfonamida que contienen fluoro y trifluoro alquilo; composicion farmaceutica; kit farmaceutico; procedimiento de preparacion; y su uso como inhibidores de beta amiloides para tratar alzheimer, angiopatia am |
| US7399778B2 (en) * | 2004-01-16 | 2008-07-15 | Wyeth | Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole |
| PE20080109A1 (es) | 2006-02-17 | 2008-04-01 | Wyeth Corp | N-sulfonilacion selectiva de alcoholes sustituidos con 2-aminotrifluoralquilo |
| CA2641013A1 (en) * | 2006-02-17 | 2007-08-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
| BRPI0710470A2 (pt) * | 2006-04-21 | 2011-08-16 | Wyeth Corp | métodos para preparar seletivamente um aminoálcool quiral e uma sulfonamida quiral |
| 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 |
| US20080233132A1 (en) * | 2006-11-03 | 2008-09-25 | Miller Stephen D | Multiple sclerosis therapy |
| PA8789701A1 (es) * | 2007-07-16 | 2009-04-23 | Wyeth Corp | Inhibidores de producción de beta amiloide |
| WO2009012203A1 (en) * | 2007-07-16 | 2009-01-22 | Wyeth | Processes and intermediates for the preparation of heterocyclic sulfonamide compounds |
| CL2008002058A1 (es) * | 2007-07-16 | 2008-11-14 | Wyeth Corp | Metodo para la preparacion de trifluoralquil-fenil-sulfonamidas y de sulfonamidas heterociclicas usando n-trifluoroacteilmorfolina; su metodo de preparacion y su uso. |
| 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 |
| CN102088855A (zh) * | 2008-05-08 | 2011-06-08 | 百时美施贵宝公司 | 2-芳基甘氨酰胺衍生物 |
| CN102143928A (zh) * | 2008-09-05 | 2011-08-03 | 马克斯普朗克科学促进协会 | 利用两个连续的结晶步骤对化合物形成的手性体系进行对映体拆分的方法 |
| 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 |
| US9223217B2 (en) * | 2010-02-19 | 2015-12-29 | International Business Machines Corporation | Sulfonamide-containing topcoat and photoresist additive compositions and methods of use |
| US9223209B2 (en) * | 2010-02-19 | 2015-12-29 | International Business Machines Corporation | Sulfonamide-containing photoresist compositions and methods of use |
| WO2011112858A1 (en) * | 2010-03-10 | 2011-09-15 | North Carolina Central University | Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase |
| US20150209406A1 (en) | 2012-09-07 | 2015-07-30 | Massachusetts Eye And Ear Infirmary | Methods and compositions for regenerating hair cells and/or supporting cells |
| WO2014039781A1 (en) | 2012-09-07 | 2014-03-13 | Massachusetts Eye & Ear Infirmary | Treating hearing loss |
| EP2987496B1 (en) | 2013-04-19 | 2018-08-08 | National University Corporation Okayama University | Treatment agent for cognitive disorders, induced by amyloid -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 |
| KR102362222B1 (ko) | 2016-05-16 | 2022-02-11 | 더 제너럴 하스피탈 코포레이션 | 폐 상피 공학에서 인간 기도 줄기 세포 |
| US11590152B2 (en) | 2018-01-26 | 2023-02-28 | Massachusetts Eye And 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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| US5514691A (en) | 1993-05-20 | 1996-05-07 | Immunopharmaceutics, Inc. | N-(4-halo-isoxazolyl)-sulfonamides and derivatives thereof that modulate the activity of endothelin |
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| EP0510700A3 (en) | 1991-04-26 | 1992-12-16 | Takeda Chemical Industries, Ltd. | Azole compounds, their production and use |
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| ATE377006T1 (de) | 1995-11-28 | 2007-11-15 | Cephalon Inc | Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer |
| NZ333825A (en) | 1996-07-22 | 2000-10-27 | Monsanto Co | Metalloprotease inhibitors particularly MMP-13 |
| US5703129A (en) | 1996-09-30 | 1997-12-30 | Bristol-Myers Squibb Company | 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production |
| US5985930A (en) | 1996-11-21 | 1999-11-16 | Pasinetti; Giulio M. | Treatment of neurodegenerative conditions with nimesulide |
| EP0942923A2 (en) | 1996-11-22 | 1999-09-22 | Elan Pharmaceuticals, Inc. | N-(ARYL/HETEROARYL) AMINO ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING $g(b)-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS |
| 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 |
| US5981168A (en) | 1998-05-15 | 1999-11-09 | The University Of British Columbia | Method and composition for modulating amyloidosis |
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| US6967196B1 (en) | 1999-02-26 | 2005-11-22 | Bristol-Myers Squibb Company | Sulfonamide compounds and uses thereof |
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| EP1088821A1 (en) | 1999-09-28 | 2001-04-04 | Applied Research Systems ARS Holding N.V. | Pharmaceutically active sulfonamide derivatives |
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| WO2001027108A1 (en) | 1999-10-08 | 2001-04-19 | Bristol-Myers Squibb Pharma Company | AMINO LACTAM SULFONAMIDES AS INHIBITORS OF Aβ PROTEIN PRODUCTION |
| ES2275657T3 (es) | 2000-03-20 | 2007-06-16 | MERCK SHARP & DOHME LTD. | Derivados de bicicloalquilo puenteados sulfonamido sustituidos. |
| EA009035B1 (ru) * | 2000-12-13 | 2007-10-26 | Уиет | Получение гетероциклических сульфонамидных ингибиторов бета-амилоида |
| US6657070B2 (en) | 2000-12-13 | 2003-12-02 | Wyeth | Production of chirally pure α-amino acids and N-sulfonyl α-amino acids |
| PL370859A1 (en) | 2001-12-11 | 2005-05-30 | Wyeth | Process for the synthesis of chirally pure beta-amino-alcohols |
| CA2470111A1 (en) | 2001-12-11 | 2003-06-19 | Wyeth | Production of chirally pure .alpha.-amino acids and n-sulfonyl .alpha.-amino acids |
| IL165265A0 (en) | 2002-06-11 | 2005-12-18 | Wyeth Corp | Substituted phenylsulfonamide inhibitors of beta amyloid production |
| CL2004000647A1 (es) | 2003-03-31 | 2005-02-04 | Wyeth Corp | Compuestos derivados de heterociclicos de sulfonamida que contienen fluoro y trifluoro alquilo; composicion farmaceutica; kit farmaceutico; procedimiento de preparacion; y su uso como inhibidores de beta amiloides para tratar alzheimer, angiopatia am |
| US7399778B2 (en) | 2004-01-16 | 2008-07-15 | Wyeth | Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole |
| CA2641013A1 (en) | 2006-02-17 | 2007-08-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
| PE20080109A1 (es) | 2006-02-17 | 2008-04-01 | Wyeth Corp | N-sulfonilacion selectiva de alcoholes sustituidos con 2-aminotrifluoralquilo |
| US7550629B2 (en) | 2006-04-21 | 2009-06-23 | Wyeth | Trifluoromethyl-containing phenylsulfonamide beta amyloid inhibitors |
| BRPI0710470A2 (pt) | 2006-04-21 | 2011-08-16 | Wyeth Corp | métodos para preparar seletivamente um aminoálcool quiral e uma sulfonamida quiral |
| US7476762B2 (en) | 2006-04-21 | 2009-01-13 | Wyeth | Methods for preparing sulfonamide compounds |
| PA8789701A1 (es) | 2007-07-16 | 2009-04-23 | Wyeth Corp | Inhibidores de producción de beta amiloide |
| CL2008002058A1 (es) | 2007-07-16 | 2008-11-14 | Wyeth Corp | Metodo para la preparacion de trifluoralquil-fenil-sulfonamidas y de sulfonamidas heterociclicas usando n-trifluoroacteilmorfolina; su metodo de preparacion y su uso. |
| WO2009012203A1 (en) | 2007-07-16 | 2009-01-22 | Wyeth | Processes and intermediates for the preparation of heterocyclic sulfonamide compounds |
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2004
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- 2004-03-26 UA UAA200510177A patent/UA82093C2/uk unknown
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- 2004-03-26 CN CNA2008100013400A patent/CN101274926A/zh active Pending
- 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 BR BRPI0408962-6A patent/BRPI0408962A/pt not_active IP Right Cessation
- 2004-03-26 JP JP2006509331A patent/JP2006522126A/ja active Pending
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- 2004-03-26 RU RU2005133434/04A patent/RU2342374C2/ru not_active IP Right Cessation
- 2004-03-26 CA CA002517155A patent/CA2517155A1/en not_active Abandoned
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- 2004-03-26 KR KR1020057018637A patent/KR20060002908A/ko not_active Ceased
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2005
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2007
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2009
- 2009-05-05 US US12/435,442 patent/US7858658B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| ECSP056128A (es) | 2006-03-01 |
| KR20060002908A (ko) | 2006-01-09 |
| CO5640049A2 (es) | 2006-05-31 |
| BRPI0408962A (pt) | 2006-04-04 |
| RU2342374C2 (ru) | 2008-12-27 |
| TWI336698B (en) | 2011-02-01 |
| CN1780829A (zh) | 2006-05-31 |
| CN1780829B (zh) | 2010-12-29 |
| UA82093C2 (uk) | 2008-03-11 |
| CA2517155A1 (en) | 2004-10-28 |
| US7858658B2 (en) | 2010-12-28 |
| NO20054263D0 (no) | 2005-09-15 |
| AU2004230844A1 (en) | 2004-10-28 |
| JP2006522126A (ja) | 2006-09-28 |
| AU2004230844B2 (en) | 2010-12-09 |
| CN101274926A (zh) | 2008-10-01 |
| NO20054263L (no) | 2005-12-14 |
| CR7951A (es) | 2008-10-29 |
| US7300951B2 (en) | 2007-11-27 |
| US20040198778A1 (en) | 2004-10-07 |
| US7547725B2 (en) | 2009-06-16 |
| WO2004092155A1 (en) | 2004-10-28 |
| MXPA05010368A (es) | 2005-11-17 |
| US20070254929A1 (en) | 2007-11-01 |
| AR043940A1 (es) | 2005-08-17 |
| CL2004000647A1 (es) | 2005-02-04 |
| RU2005133434A (ru) | 2006-07-10 |
| NZ542468A (en) | 2009-01-31 |
| US20090227667A1 (en) | 2009-09-10 |
| EP1608638A1 (en) | 2005-12-28 |
| TW200504047A (en) | 2005-02-01 |
| SG167669A1 (en) | 2011-01-28 |
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