HUP0303108A2 - Szubsztituált pirazolok és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Szubsztituált pirazolok és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0303108A2 HUP0303108A2 HU0303108A HUP0303108A HUP0303108A2 HU P0303108 A2 HUP0303108 A2 HU P0303108A2 HU 0303108 A HU0303108 A HU 0303108A HU P0303108 A HUP0303108 A HU P0303108A HU P0303108 A2 HUP0303108 A2 HU P0303108A2
- Authority
- HU
- Hungary
- Prior art keywords
- optionally substituted
- group
- independently
- hydrogen atom
- alkyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Chemical class 0.000 title 1
- 150000003217 pyrazoles Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 108090000613 Cathepsin S Proteins 0.000 abstract 1
- 102100035654 Cathepsin S Human genes 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 125000003435 aroyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N sulfur dioxide Inorganic materials O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/275—Nitriles; Isonitriles
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
Abstract
A találmány tárgya az (I) általános képletű vegyületek vagygyógyászatilag elfogadható sói, amidjai vagy észterei, illetvesztereoizomer formái, ahol a képletben Ar2 jelentése adott esetbenszubsztituált monociklusos vagy biciklusos gyűrűrendszer, ami adottesetben kondenzált, és adott esetben 1-5 heteroatomot tartalmazgyűrűtagonként, amelyek egymástól függetlenül O, S, N, SO2 és C=Olehetnek; R5 és R6 jelentése egymástól függetlenül hidrogénatom vagyalkilcsoport; R7 és R8 jelentése egymástól függetlenül hidrogénatom,alkil-, alkenil-, alkoxi-, alkiltiocsoport, halogénatom vagy 4-7 tagúkarbociklusos vagy heterociklusos csoport; vagy R7 és R8 jelentéseegyütt egy adott esetben szubsztituált 5-7 tagú karbociklusos vagyheterociklusos gyűrű; n értéke 0, 1 vagy 2; G jelentése adott esetbenszubsztituált alkéndiil- vagy alkándiilcsoport; Ar jelentése adottesetben szubsztituált monociklusos- vagy biciklusos aril- vagyheteroaril gyűrű; W jelentése O, S, NR27, C=O, (C=O)NH, NH(C=O), CHR28vagy egy kovalens kötés, RZ jelentése hidrogénatom vagyhidroxilcsoport és a szaggatott vonal nincs jelen; vagy RZ nincs jelenés a szaggatott vonal egy sp2 kötést jelent; R27 jelentése többekközött hidrogénatom, alkil-, alkenil-, fenil-, naftil-, benzil-,fenetil-, heterociklusos csoport, acil-, aroilcsoport, vagy R27 és azAr2 egy része együttesen egy adott esetben szubsztituált 5 vagy 6 tagúheterociklusos gyűrűt alkothat. A találmány tárgya továbbá fentivegyületeket tartalmazó gyógyászati készítmény. A találmány szerintivegyületek a cathepsin S-sel mediált állapotok, így például azautoimmun-betegség kezelésére alkalmasak. Ó
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22517800P | 2000-08-14 | 2000-08-14 | |
US60/225,178 | 2000-08-14 | ||
PCT/US2001/025290 WO2002014315A2 (en) | 2000-08-14 | 2001-08-10 | Substituted pyrazoles |
US09/927,324 | 2001-08-10 | ||
US09/927,324 US6953793B2 (en) | 2000-08-14 | 2001-08-10 | Substituted pyrazoles |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0303108A2 true HUP0303108A2 (hu) | 2004-01-28 |
HUP0303108A3 HUP0303108A3 (en) | 2012-10-29 |
HU230538B1 HU230538B1 (hu) | 2016-11-28 |
Family
ID=26919364
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0303108A HU230538B1 (hu) | 2000-08-14 | 2001-08-10 | Szubsztituált pirazolok és ezeket tartalmazó gyógyszerkészítmények |
Country Status (20)
Country | Link |
---|---|
US (2) | US6953793B2 (hu) |
EP (1) | EP1309593B1 (hu) |
JP (1) | JP5049447B2 (hu) |
KR (1) | KR100837193B1 (hu) |
AT (1) | ATE320427T1 (hu) |
AU (2) | AU8645401A (hu) |
BR (1) | BRPI0113286B8 (hu) |
CA (1) | CA2419552C (hu) |
CZ (1) | CZ307185B6 (hu) |
DE (1) | DE60118004T2 (hu) |
DK (1) | DK1309593T3 (hu) |
ES (1) | ES2261463T3 (hu) |
HK (1) | HK1055422A1 (hu) |
HU (1) | HU230538B1 (hu) |
MX (1) | MXPA03001422A (hu) |
NZ (1) | NZ524191A (hu) |
PL (1) | PL213103B1 (hu) |
PT (1) | PT1309593E (hu) |
RU (1) | RU2317988C2 (hu) |
WO (1) | WO2002014315A2 (hu) |
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PT1309591E (pt) * | 2000-08-14 | 2007-04-30 | Ortho Mcneil Pharm Inc | Pirazoles substituídos |
MXPA03001422A (es) * | 2000-08-14 | 2004-01-26 | Johnson & Johnson | Pirazoles substituidos. |
US20050101587A9 (en) * | 2000-08-14 | 2005-05-12 | Butler Christopher R. | Method for treating allergies using substituted pyrazoles |
WO2002051983A2 (en) * | 2000-12-22 | 2002-07-04 | Axys Pharmaceuticals, Inc. | Novel compounds and compositions as cathepsin inhibitors |
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US20040147503A1 (en) * | 2002-06-04 | 2004-07-29 | Sheila Zipfeil | Novel compounds and compositions as cathepsin inhibitors |
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US9643922B2 (en) | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
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US9540322B2 (en) | 2008-08-18 | 2017-01-10 | Yale University | MIF modulators |
TWI475020B (zh) * | 2009-03-12 | 2015-03-01 | The substituted nicotine amide as a KCNQ2 / 3 modifier | |
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JPS5640714B2 (hu) * | 1974-03-04 | 1981-09-22 | ||
DK27383A (da) | 1982-02-17 | 1983-08-18 | Lepetit Spa | Fremgangsmaade til fremstilling af pyrazol(4,3-c)pyridiner |
JPH0615542B2 (ja) * | 1986-07-22 | 1994-03-02 | 吉富製薬株式会社 | ピラゾロピリジン化合物 |
FR2642759B1 (fr) | 1989-02-09 | 1991-05-17 | Laboratorios Esteve Sa | Derives de pyrimidyl-piperazinyl-alkyl azoles avec activite anxiolytique et/ou tranquillisante |
FR2673628B1 (fr) | 1991-03-07 | 1993-07-09 | Esteve Labor Dr | Procede de preparation de derives d'aryl (ou heteroaryl)-piperazinyl-butyl-azoles. |
US5264576A (en) | 1992-10-22 | 1993-11-23 | Hoechst-Roussel Pharmaceuticals Incorporated | Pyrazolo[4,3-c]pyridines which are intermediates |
FR2705962B1 (fr) * | 1993-06-03 | 1995-07-13 | Rhone Poulenc Agrochimie | Arylpyrazoles fongicides. |
FR2712808B1 (fr) | 1993-11-25 | 1996-02-16 | Esteve Labor Dr | Utilisation des dérivés de 1-{4-[4-aryl(ou hétéroaryl)-1-pipérazinyl]-butyl}-1-H-azole pour la préparation de médicaments destinés au traitement des troubles de la sécrétion gastrique . |
IL112759A0 (en) | 1994-02-25 | 1995-05-26 | Khepri Pharmaceuticals Inc | Novel cysteine protease inhibitors |
US5776718A (en) | 1995-03-24 | 1998-07-07 | Arris Pharmaceutical Corporation | Reversible protease inhibitors |
AU713492B2 (en) | 1995-03-24 | 1999-12-02 | Axys Pharmaceuticals, Inc. | Reversible protease inhibitors |
TW438591B (en) | 1995-06-07 | 2001-06-07 | Arris Pharm Corp | Reversible cysteine protease inhibitors |
FR2742052B1 (fr) | 1995-12-12 | 1998-04-10 | Esteve Labor Dr | Utilisation des derives 1-(4-(4-aryl (ou heteroaryl)-1-piper azinyl)-buty)-1h-azole pour le traitement de la depression, des troubles obsessifs compulsifs, l'apnee du sommeil, les dysfonctions sexuelles, l'emese et le mal des transports |
PT912601E (pt) | 1996-04-22 | 2004-04-30 | Massachusetts Inst Technology | Supressao da resposta imune via inibicao da catepsina s |
AU7553198A (en) | 1997-06-12 | 1998-12-30 | Sumitomo Pharmaceuticals Company, Limited | Pyrazole derivatives |
DE69841871D1 (en) | 1997-11-05 | 2010-10-14 | Novartis Ag | Dipeptide nitrile |
GB9806287D0 (en) | 1998-03-24 | 1998-05-20 | Synphar Lab Inc | Monobactam enzyme inhibitors |
WO1999058153A1 (en) | 1998-05-08 | 1999-11-18 | Brigham & Women's Hospital | Methods of diagnosing and modulating autoimmunity |
AU2560000A (en) | 1999-02-20 | 2000-09-04 | Astrazeneca Ab | Di- and tripeptide nitrile derivatives as inhibitors of cathepsin l and cathepsin |
EP1159273A1 (en) | 1999-03-02 | 2001-12-05 | Boehringer Ingelheim Pharmaceuticals Inc. | Compounds useful as reversible inhibitors of cathepsin s |
TW200404789A (en) | 1999-03-15 | 2004-04-01 | Axys Pharm Inc | Novel compounds and compositions as protease inhibitors |
ATE326454T1 (de) | 1999-07-30 | 2006-06-15 | Boehringer Ingelheim Pharma | Neue bernsteinsäure derivative als cysteine- protease-inhibitoren |
EP1212302A1 (en) | 1999-09-16 | 2002-06-12 | Axys Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions as cathepsin s inhibitors |
WO2001040204A1 (fr) | 1999-12-03 | 2001-06-07 | Ono Pharmaceutical Co., Ltd. | Derives de 1.3.4-oxadiazoline et medicaments contenant ces derives utiles comme ingredients actifs |
MXPA03001422A (es) * | 2000-08-14 | 2004-01-26 | Johnson & Johnson | Pirazoles substituidos. |
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2001
- 2001-08-10 MX MXPA03001422A patent/MXPA03001422A/es active IP Right Grant
- 2001-08-10 NZ NZ524191A patent/NZ524191A/en not_active IP Right Cessation
- 2001-08-10 EP EP01965898A patent/EP1309593B1/en not_active Expired - Lifetime
- 2001-08-10 PL PL360696A patent/PL213103B1/pl unknown
- 2001-08-10 RU RU2003107016/04A patent/RU2317988C2/ru not_active Application Discontinuation
- 2001-08-10 US US09/927,324 patent/US6953793B2/en not_active Expired - Lifetime
- 2001-08-10 AT AT01965898T patent/ATE320427T1/de active
- 2001-08-10 DE DE60118004T patent/DE60118004T2/de not_active Expired - Lifetime
- 2001-08-10 KR KR1020037002163A patent/KR100837193B1/ko not_active Expired - Lifetime
- 2001-08-10 HU HU0303108A patent/HU230538B1/hu not_active IP Right Cessation
- 2001-08-10 AU AU8645401A patent/AU8645401A/xx active Pending
- 2001-08-10 BR BRPI0113286A patent/BRPI0113286B8/pt not_active IP Right Cessation
- 2001-08-10 DK DK01965898T patent/DK1309593T3/da active
- 2001-08-10 JP JP2002519455A patent/JP5049447B2/ja not_active Expired - Lifetime
- 2001-08-10 PT PT01965898T patent/PT1309593E/pt unknown
- 2001-08-10 CA CA2419552A patent/CA2419552C/en not_active Expired - Lifetime
- 2001-08-10 AU AU2001286454A patent/AU2001286454B2/en not_active Expired
- 2001-08-10 CZ CZ2003-429A patent/CZ307185B6/cs not_active IP Right Cessation
- 2001-08-10 ES ES01965898T patent/ES2261463T3/es not_active Expired - Lifetime
- 2001-08-10 WO PCT/US2001/025290 patent/WO2002014315A2/en active IP Right Grant
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2003
- 2003-07-10 HK HK03104996A patent/HK1055422A1/xx not_active IP Right Cessation
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2005
- 2005-06-30 US US11/174,077 patent/US20050245576A1/en not_active Abandoned
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