EA200000702A1 - Пролекарства ингибиторов аспартилпротеаз - Google Patents
Пролекарства ингибиторов аспартилпротеазInfo
- Publication number
- EA200000702A1 EA200000702A1 EA200000702A EA200000702A EA200000702A1 EA 200000702 A1 EA200000702 A1 EA 200000702A1 EA 200000702 A EA200000702 A EA 200000702A EA 200000702 A EA200000702 A EA 200000702A EA 200000702 A1 EA200000702 A1 EA 200000702A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- prodrugs
- relates
- inhibitors
- pharmaceutical compositions
- procaraments
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 239000000651 prodrug Substances 0.000 abstract 5
- 229940002612 prodrug Drugs 0.000 abstract 5
- 102000004580 Aspartic Acid Proteases Human genes 0.000 abstract 2
- 108010017640 Aspartic Acid Proteases Proteins 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
- 150000003456 sulfonamides Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4172—Imidazole-alkanecarboxylic acids, e.g. histidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7024—Esters of saccharides
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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
- C07D307/20—Oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
- C07D317/32—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings 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
- C07D317/34—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
- C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
- C07F9/65842—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
- C07F9/65844—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a five-membered ring which may be condensed with another ring system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Enzymes And Modification Thereof (AREA)
- Furan Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
(57) Настоящее изобретение относится к пролекарствам класса сульфонамидов, которые представляют собой ингибиторы аспартилпротеаз. В одном из воплощений данное изобретение относится к новому классу пролекарств, являющихся ингибиторами аспартилпротеаз ВИЧ, характеризующихся хорошей водорастворимостью, высокой биологической доступностью при пероральном применении и легким воспроизведением in vivo активного компонента. Данное изобретение также относится к фармацевтическим композициям, содержащим данные пролекарства. Пролекарство и фармацевтические препараты по данному изобретению особенно хорошо подходят для снижения лекарственной нагрузки и повышения удобства пациентов. Данное изобретение также относится к способам лечения млекопитающих данными пролекарствами и фармацевтическими композициями.Отчет о международном поиске был опубликован 1999.09.10.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US6888997P | 1997-12-24 | 1997-12-24 | |
PCT/US1998/027424 WO1999033793A2 (en) | 1997-12-24 | 1998-12-23 | Prodrugs of aspartyl protease inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
EA200000702A1 true EA200000702A1 (ru) | 2000-12-25 |
Family
ID=22085350
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200000702A EA200000702A1 (ru) | 1997-12-24 | 1998-12-23 | Пролекарства ингибиторов аспартилпротеаз |
Country Status (21)
Country | Link |
---|---|
US (2) | US20020082249A1 (ru) |
EP (1) | EP1042280A2 (ru) |
JP (1) | JP2001527062A (ru) |
KR (1) | KR20010033595A (ru) |
CN (1) | CN1110492C (ru) |
AP (1) | AP2000001856A0 (ru) |
AU (1) | AU2092599A (ru) |
BR (1) | BR9814484A (ru) |
CA (1) | CA2316218A1 (ru) |
EA (1) | EA200000702A1 (ru) |
EE (1) | EE200000386A (ru) |
HR (1) | HRP20000499A2 (ru) |
HU (1) | HUP0101598A3 (ru) |
ID (1) | ID25551A (ru) |
IL (1) | IL136940A0 (ru) |
IS (1) | IS5547A (ru) |
NO (1) | NO20003332L (ru) |
PL (1) | PL341762A1 (ru) |
SK (1) | SK9672000A3 (ru) |
TR (1) | TR200002402T2 (ru) |
WO (1) | WO1999033793A2 (ru) |
Families Citing this family (79)
Publication number | Priority date | Publication date | Assignee | Title |
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US6436989B1 (en) * | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
GB9815567D0 (en) * | 1998-07-18 | 1998-09-16 | Glaxo Group Ltd | Antiviral compound |
EE05385B1 (et) | 2001-02-14 | 2011-02-15 | Tibotec�Pharmaceuticals�Ltd. | LaiaspektrilisedÁ2-(asendatudÁamino)bensotiasoolsulfoonamiididÁkuiÁHIVÁproteaasiÁinhibiitorid,ÁnendeÁvalmistamismeetodÁjaÁkasutamineÁningÁfarmatseutilineÁkompositsioon |
CN100491360C (zh) | 2001-04-09 | 2009-05-27 | 泰博特克药品有限公司 | 广谱2-(取代的-氨基)-苯并唑磺酰胺hiv蛋白酶抑制剂 |
AU2002256418A1 (en) * | 2001-04-27 | 2002-11-11 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
AU2002310818B2 (en) | 2001-05-11 | 2007-12-13 | Tibotec Pharmaceuticals Ltd. | Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors |
BR0215260A (pt) | 2001-12-21 | 2004-12-07 | Tibotec Pharm Ltd | Inibidores de hiv protease de sulfonamida contendo fenila substituìda heterocìclica de amplo espectro |
MY142238A (en) | 2002-03-12 | 2010-11-15 | Tibotec Pharm Ltd | Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors |
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DE10259245A1 (de) | 2002-12-17 | 2004-07-01 | Merck Patent Gmbh | Derivate des Asimadolins mit kovalent gebundenen Säuren |
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NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
EP1938691A3 (en) | 2004-12-17 | 2009-07-22 | Devgen NV | Nematicidal compositions |
US8003627B2 (en) | 2005-10-21 | 2011-08-23 | Universiteit Antwerpen | Urokinase inhibitors |
AR058238A1 (es) | 2005-11-28 | 2008-01-23 | Tibotec Pharm Ltd | Compuestos y derivados de aminofenilsulfonamida sustituida como inhibidores de proteasa del vih |
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Family Cites Families (3)
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WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
IS2334B (is) * | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
US5691372A (en) * | 1995-04-19 | 1997-11-25 | Vertex Pharmaceuticals Incorporated | Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease |
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1998
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- 1998-12-23 EA EA200000702A patent/EA200000702A1/ru unknown
- 1998-12-23 BR BR9814484-7A patent/BR9814484A/pt not_active Application Discontinuation
- 1998-12-23 EP EP98965466A patent/EP1042280A2/en not_active Withdrawn
- 1998-12-23 SK SK967-2000A patent/SK9672000A3/sk unknown
- 1998-12-23 ID IDW20001410A patent/ID25551A/id unknown
- 1998-12-23 CN CN98813313A patent/CN1110492C/zh not_active Expired - Fee Related
- 1998-12-23 AP APAP/P/2000/001856A patent/AP2000001856A0/en unknown
- 1998-12-23 WO PCT/US1998/027424 patent/WO1999033793A2/en not_active Application Discontinuation
- 1998-12-23 HU HU0101598A patent/HUP0101598A3/hu unknown
- 1998-12-23 JP JP2000526477A patent/JP2001527062A/ja active Pending
- 1998-12-23 EE EEP200000386A patent/EE200000386A/xx unknown
- 1998-12-23 TR TR2000/02402T patent/TR200002402T2/xx unknown
- 1998-12-23 KR KR1020007007108A patent/KR20010033595A/ko not_active Application Discontinuation
- 1998-12-23 CA CA002316218A patent/CA2316218A1/en not_active Abandoned
- 1998-12-23 IL IL13694098A patent/IL136940A0/xx unknown
- 1998-12-23 AU AU20925/99A patent/AU2092599A/en not_active Withdrawn
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2000
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2001
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2002
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US20030144217A1 (en) | 2003-07-31 |
AP2000001856A0 (en) | 2000-09-30 |
WO1999033793A3 (en) | 1999-09-10 |
NO20003332D0 (no) | 2000-06-26 |
BR9814484A (pt) | 2000-10-10 |
AU2092599A (en) | 1999-07-19 |
HUP0101598A3 (en) | 2002-08-28 |
SK9672000A3 (en) | 2001-04-09 |
HUP0101598A2 (hu) | 2002-04-29 |
IS5547A (is) | 2000-06-22 |
CN1284072A (zh) | 2001-02-14 |
WO1999033793A2 (en) | 1999-07-08 |
CA2316218A1 (en) | 1999-07-08 |
NO20003332L (no) | 2000-08-18 |
TR200002402T2 (tr) | 2001-01-22 |
HRP20000499A2 (en) | 2001-04-30 |
PL341762A1 (en) | 2001-05-07 |
EE200000386A (et) | 2001-12-17 |
JP2001527062A (ja) | 2001-12-25 |
ID25551A (id) | 2000-10-12 |
KR20010033595A (ko) | 2001-04-25 |
IL136940A0 (en) | 2001-06-14 |
CN1110492C (zh) | 2003-06-04 |
EP1042280A2 (en) | 2000-10-11 |
US20020082249A1 (en) | 2002-06-27 |
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