CO4870779A1 - Nuevas sulfonamidas que inhiben la proteasa aspartilo - Google Patents
Nuevas sulfonamidas que inhiben la proteasa aspartiloInfo
- Publication number
- CO4870779A1 CO4870779A1 CO93406779A CO93406779A CO4870779A1 CO 4870779 A1 CO4870779 A1 CO 4870779A1 CO 93406779 A CO93406779 A CO 93406779A CO 93406779 A CO93406779 A CO 93406779A CO 4870779 A1 CO4870779 A1 CO 4870779A1
- Authority
- CO
- Colombia
- Prior art keywords
- compound
- group
- het
- hiv aspartyl
- aspartyl protease
- Prior art date
Links
- 108091005804 Peptidases Proteins 0.000 title abstract 3
- 239000004365 Protease Substances 0.000 title abstract 3
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title 1
- 150000003456 sulfonamides Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 22
- 108010017640 Aspartic Acid Proteases Proteins 0.000 abstract 15
- 102000004580 Aspartic Acid Proteases Human genes 0.000 abstract 15
- 229910052739 hydrogen Inorganic materials 0.000 abstract 14
- 239000001257 hydrogen Substances 0.000 abstract 11
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 230000002209 hydrophobic effect Effects 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 229940122440 HIV protease inhibitor Drugs 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 102000035195 Peptidases Human genes 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 230000009881 electrostatic interaction Effects 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 239000004030 hiv protease inhibitor Substances 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- -1 methylenedioxyl Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000000758 substrate Substances 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 101710193123 Death domain-containing membrane protein NRADD Proteins 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- 239000002671 adjuvant Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005605 benzo group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 238000011156 evaluation Methods 0.000 abstract 1
- 230000002349 favourable effect Effects 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000007935 neutral effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229920001184 polypeptide Polymers 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
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- 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
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- A—HUMAN NECESSITIES
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C307/04—Diamides of sulfuric acids
- C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
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- C—CHEMISTRY; METALLURGY
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- 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
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
- C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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- 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
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- C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
- C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
- C07C311/46—Y being a hydrogen or a carbon atom
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- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen 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
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
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- 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
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- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
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- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
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- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K38/00—Medicinal preparations containing peptides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
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- Chemical & Material Sciences (AREA)
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- General Health & Medical Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Tropical Medicine & Parasitology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Furan Compounds (AREA)
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Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US94198292A | 1992-09-08 | 1992-09-08 |
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CO4870779A1 true CO4870779A1 (es) | 1999-12-27 |
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CO93406779A CO4870779A1 (es) | 1992-09-08 | 1993-09-07 | Nuevas sulfonamidas que inhiben la proteasa aspartilo |
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-
1993
- 1993-08-31 IS IS4068A patent/IS2334B/is unknown
- 1993-09-01 LT LTIP917A patent/LT3302B/lt not_active IP Right Cessation
- 1993-09-01 TW TW082107130A patent/TW254927B/zh not_active IP Right Cessation
- 1993-09-06 IL IL10692793A patent/IL106927A/en not_active IP Right Cessation
- 1993-09-07 KR KR1019950700920A patent/KR100262056B1/ko not_active Expired - Lifetime
- 1993-09-07 EP EP98113921A patent/EP0885887B1/en not_active Expired - Lifetime
- 1993-09-07 AT AT98113921T patent/ATE241602T1/de active
- 1993-09-07 ES ES93921428T patent/ES2131589T3/es not_active Expired - Lifetime
- 1993-09-07 GE GEAP19932481A patent/GEP20012579B/en unknown
- 1993-09-07 EP EP93921428A patent/EP0659181B1/en not_active Expired - Lifetime
- 1993-09-07 DE DE69324369T patent/DE69324369T2/de not_active Expired - Lifetime
- 1993-09-07 UA UA95048318A patent/UA44694C2/uk unknown
- 1993-09-07 SK SK293-95A patent/SK281360B6/sk not_active IP Right Cessation
- 1993-09-07 CA CA002143208A patent/CA2143208C/en not_active Expired - Lifetime
- 1993-09-07 PL PL93307858A patent/PL185635B1/pl unknown
- 1993-09-07 DE DE2001199024 patent/DE10199024I2/de active Active
- 1993-09-07 NZ NZ256238A patent/NZ256238A/en not_active IP Right Cessation
- 1993-09-07 PT PT98113921T patent/PT885887E/pt unknown
- 1993-09-07 WO PCT/US1993/008458 patent/WO1994005639A1/en not_active Application Discontinuation
- 1993-09-07 US US08/142,327 patent/US5585397A/en not_active Expired - Lifetime
- 1993-09-07 DK DK93921428T patent/DK0659181T3/da active
- 1993-09-07 RO RO95-00479A patent/RO118747B1/ro unknown
- 1993-09-07 DK DK98113921T patent/DK0885887T3/da active
- 1993-09-07 ES ES98113921T patent/ES2200243T3/es not_active Expired - Lifetime
- 1993-09-07 DE DE69333012T patent/DE69333012T2/de not_active Expired - Lifetime
- 1993-09-07 CZ CZ1995587A patent/CZ289475B6/cs not_active IP Right Cessation
- 1993-09-07 PH PH46835A patent/PH31251A/en unknown
- 1993-09-07 JP JP6507525A patent/JP3012002B2/ja not_active Expired - Lifetime
- 1993-09-07 HU HU9500685A patent/HU228198B1/hu unknown
- 1993-09-07 AU AU48520/93A patent/AU691160B2/en not_active Expired
- 1993-09-07 CO CO93406779A patent/CO4870779A1/es unknown
- 1993-09-07 NZ NZ314376A patent/NZ314376A/xx not_active IP Right Cessation
- 1993-09-07 AT AT93921428T patent/ATE178598T1/de active
- 1993-09-07 SG SG1996003219A patent/SG43862A1/en unknown
- 1993-09-07 RU RU95109928A patent/RU2135496C1/ru active
- 1993-09-08 MY MYPI93001823A patent/MY142901A/en unknown
- 1993-09-08 CN CN93117370A patent/CN1061339C/zh not_active Expired - Lifetime
- 1993-09-08 AP APAP/P/1993/000572A patent/AP390A/en active
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1995
- 1995-03-07 FI FI951059A patent/FI120685B/fi not_active IP Right Cessation
- 1995-03-07 NO NO950876A patent/NO303444B1/no not_active IP Right Cessation
- 1995-04-03 BG BG99540A patent/BG62488B1/bg unknown
- 1995-06-07 US US08/484,326 patent/US6372778B1/en not_active Expired - Lifetime
- 1995-06-07 US US08/477,937 patent/US5856353A/en not_active Expired - Lifetime
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1997
- 1997-05-12 BR BR1100824-5A patent/BR1100824A/pt active IP Right Grant
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1999
- 1999-07-07 GR GR990401802T patent/GR3030719T3/el unknown
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2000
- 2000-01-01 NL NL300039C patent/NL300039I2/nl unknown
- 2000-03-31 CY CY0000008A patent/CY2164B1/xx unknown
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2001
- 2001-03-07 LU LU90736C patent/LU90736I2/fr unknown
- 2001-07-03 NO NO2001012C patent/NO2001012I1/no unknown
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2002
- 2002-03-08 US US10/094,790 patent/US20030069222A1/en not_active Abandoned
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2003
- 2003-11-17 MX MXPA03010538A patent/MXPA03010538A/es active IP Right Grant
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2006
- 2006-04-19 US US11/408,287 patent/US7608632B2/en not_active Expired - Fee Related
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2007
- 2007-12-12 US US12/001,993 patent/US20080293727A1/en not_active Abandoned
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2009
- 2009-09-11 US US12/558,051 patent/US20100210603A1/en not_active Abandoned
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