HUP0203131A2 - Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents
Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásukInfo
- Publication number
- HUP0203131A2 HUP0203131A2 HU0203131A HUP0203131A HUP0203131A2 HU P0203131 A2 HUP0203131 A2 HU P0203131A2 HU 0203131 A HU0203131 A HU 0203131A HU P0203131 A HUP0203131 A HU P0203131A HU P0203131 A2 HUP0203131 A2 HU P0203131A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- cycloalkyl
- group
- carbon atoms
- nr8r9
- Prior art date
Links
- 125000003277 amino group Chemical group 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- JUXWUYWPUDKPSD-UHFFFAOYSA-N pyrazolo[1,5-a][1,3,5]triazine Chemical class N1=CN=CN2N=CC=C21 JUXWUYWPUDKPSD-UHFFFAOYSA-N 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 8
- 229910052799 carbon Inorganic materials 0.000 abstract 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 cyano- Chemical class 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 101150027439 NPY1 gene Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000002093 peripheral effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
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- 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
- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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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
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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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
- A61P25/06—Antimigraine agents
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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
- A61P25/08—Antiepileptics; Anticonvulsants
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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
- A61P25/20—Hypnotics; Sedatives
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—Antidepressants
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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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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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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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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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
- A61P9/12—Antihypertensives
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/575—Hormones
- G01N2333/5755—Neuropeptide Y
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
- G01N2333/70571—Assays involving receptors, cell surface antigens or cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor
Abstract
A találmány (I) általános képletű vegyületekre vonatkozik, amelyekképletében R1, R2, R3, R4, R5, R6 és X jelentése az alábbiakbanmegadott. E vegyületek szelektív NPY1 receptormodulátorok. Ezek avegyületek számos CNS rendellenesség, anyagcserezavarok, perifériásrendellenességek, különösen táplálkozási zavarok és magas vérnyomáskezelésére alkalmasak. A találmány tárgyát képezik továbbá az ilyenrendellenességek kezelésére szolgáló kezelési eljárások, valamintezeket tartalmazó gyógyszerkészítmények. X jelentése N vagy CHR14; R1jelentése hidrogénatom, 1-6 szénatomszámú alkil-, 3-10 szénatomszámúcikloalkil-, (3-10 szénatomszámú cikloalkil)-(1-6 szén<- >atomszámúalkil)-, 2-6 szénatomszámú alkenil, 2-6 szén<- >atomszámú alkinil-,ciano-, halo-, 1-6 szénatomszámú halo-alkil-, -OR7, -(1-6szénatomszámú alkil)-OR7, 1-6 szénatomszámú ciano-alkil-, -NR8R9, és -(1-6 szénatomszámú alkil)-NR8R9 közül választott csoport; R2 jelentésehidrogénatom, 1-6 szénatomszámú alkilcsoport, amely adott esetben az Avagy a B csoporttal 3-6 szénatomszámú amino-karbociklust vagy 2-5szénatomszámú amino-heterociklust képez, amelyek mindegyike adottesetben R7 csoporttal helyettesített, 3-10 szénatomszámú cikloalkil-vagy (3-10 szénatomszámú cikloalkil)-(1-6 szénatomszámú alkil)-csoport; vagy R2 és R6 együttesen azzal a két nitrogénatommal,amelyhez kapcsolódnak 2-5 szénatomszámú amino- heterociklust képez,amely adott esetben R7 csoporttal helyettesített; A jelentése (CH2)mcsoport, amelyben m értéke 1, 2 vagy 3 és mindegyik szénatom adottesetben 1-6 szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10 szénatomszámú ciklo-alkil)-(1-6 szénatomszámú alkil)-, 2-6szénatomszámú alkenil, 2-6 szénatomszámú alkinil-, ciano-, halo-, 1-6szénatom-számú halo-alkil-, -OR7, -(1-6 szénatomszámú alkil)-OR7, 1-6szénatomszámú ciano-alkil-, -NR8R9, vagy -(1-6 szénatomszámú alkil)-NR8R9 csoporttal helyettesített, B jelentése (CH2)m csoport, amelybenm értéke 1, 2 vagy 3 és mindegyik szénatom adott esetben 1-6szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10szénatomszámú ciklo-alkil)-<- >(1-6 szénatomszámú alkil)-, 2-6szénatomszámú alkenil, 2-6 szénatomszámú alkinil-, ciano-, halo-, 1-6szénatomszámú haloalkil-, -OR7, -(1-6 szénatomszámú alkil)-OR7, 1-6szénatomszámú ciano-alkil-, -NR8R9, vagy -(1-6 szénatomszámú alkil)-NR8R9 csoporttal helyettesített, R3 jelentése hidrogénatom, 1-6szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10szénatomszámú cikloalkil)-(1-6 szén<- >atomszámú alkil)-, 2-6szénatomszámú alkenilcsoport; R4 jelentése aril- vagyheteroarilcsoport, amely adott esetben 1-6 szénatomszámú alkil-, 3-10szénatomszámú cikloalkil-, (3-10 szénatomszámú cikloalkil)-(1-6szénatomszámú alkil)-, 2-6 szénatomszámú alkenil, 2-6 szénatomszámúalkinil-, halo-, 1-6 szénatomszámú halo-alkil-, tri
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US15686899P | 1999-09-30 | 1999-09-30 | |
PCT/US2000/026885 WO2001023388A2 (en) | 1999-09-30 | 2000-09-29 | AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0203131A2 true HUP0203131A2 (hu) | 2003-01-28 |
HUP0203131A3 HUP0203131A3 (en) | 2004-06-28 |
Family
ID=22561433
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0203131A HUP0203131A3 (en) | 1999-09-30 | 2000-09-29 | Amino substituted pyrazolo[1,5-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines, pharmaceutical compositions containing them and their use |
Country Status (21)
Country | Link |
---|---|
US (1) | US6476038B1 (hu) |
EP (1) | EP1218381B1 (hu) |
JP (2) | JP2003510326A (hu) |
KR (1) | KR20020047201A (hu) |
CN (1) | CN1377355A (hu) |
AT (1) | ATE347553T1 (hu) |
AU (1) | AU7737900A (hu) |
BG (1) | BG106507A (hu) |
CA (1) | CA2379633C (hu) |
CZ (1) | CZ20021089A3 (hu) |
DE (1) | DE60032249T2 (hu) |
EA (1) | EA200200421A1 (hu) |
ES (1) | ES2277855T3 (hu) |
HU (1) | HUP0203131A3 (hu) |
IL (1) | IL148904A0 (hu) |
NO (1) | NO20021357L (hu) |
OA (1) | OA12049A (hu) |
PL (1) | PL354982A1 (hu) |
WO (1) | WO2001023388A2 (hu) |
YU (1) | YU23602A (hu) |
ZA (1) | ZA200202517B (hu) |
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FR2842809A1 (fr) * | 2002-07-26 | 2004-01-30 | Greenpharma Sas | NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION |
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2000
- 2000-09-29 AU AU77379/00A patent/AU7737900A/en not_active Abandoned
- 2000-09-29 EP EP00967132A patent/EP1218381B1/en not_active Expired - Lifetime
- 2000-09-29 OA OA1200200088A patent/OA12049A/en unknown
- 2000-09-29 CZ CZ20021089A patent/CZ20021089A3/cs unknown
- 2000-09-29 US US09/676,972 patent/US6476038B1/en not_active Expired - Fee Related
- 2000-09-29 IL IL14890400A patent/IL148904A0/xx unknown
- 2000-09-29 YU YU23602A patent/YU23602A/sh unknown
- 2000-09-29 AT AT00967132T patent/ATE347553T1/de not_active IP Right Cessation
- 2000-09-29 WO PCT/US2000/026885 patent/WO2001023388A2/en active IP Right Grant
- 2000-09-29 JP JP2001526540A patent/JP2003510326A/ja not_active Ceased
- 2000-09-29 HU HU0203131A patent/HUP0203131A3/hu unknown
- 2000-09-29 CN CN00813627A patent/CN1377355A/zh active Pending
- 2000-09-29 DE DE60032249T patent/DE60032249T2/de not_active Expired - Fee Related
- 2000-09-29 KR KR1020027004178A patent/KR20020047201A/ko not_active Application Discontinuation
- 2000-09-29 EA EA200200421A patent/EA200200421A1/ru unknown
- 2000-09-29 PL PL00354982A patent/PL354982A1/xx not_active Application Discontinuation
- 2000-09-29 CA CA002379633A patent/CA2379633C/en not_active Expired - Fee Related
- 2000-09-29 ES ES00967132T patent/ES2277855T3/es not_active Expired - Lifetime
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2002
- 2002-03-11 BG BG106507A patent/BG106507A/xx unknown
- 2002-03-19 NO NO20021357A patent/NO20021357L/no not_active Application Discontinuation
- 2002-03-28 ZA ZA200202517A patent/ZA200202517B/xx unknown
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2006
- 2006-09-06 JP JP2006241067A patent/JP2007077144A/ja active Pending
Also Published As
Publication number | Publication date |
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WO2001023388A2 (en) | 2001-04-05 |
CN1377355A (zh) | 2002-10-30 |
CA2379633A1 (en) | 2001-04-05 |
NO20021357D0 (no) | 2002-03-19 |
DE60032249D1 (de) | 2007-01-18 |
EP1218381A2 (en) | 2002-07-03 |
KR20020047201A (ko) | 2002-06-21 |
ATE347553T1 (de) | 2006-12-15 |
CA2379633C (en) | 2006-06-20 |
JP2003510326A (ja) | 2003-03-18 |
EP1218381B1 (en) | 2006-12-06 |
BG106507A (en) | 2002-12-29 |
PL354982A1 (en) | 2004-03-22 |
DE60032249T2 (de) | 2007-07-19 |
YU23602A (sh) | 2004-09-03 |
JP2007077144A (ja) | 2007-03-29 |
OA12049A (en) | 2006-05-02 |
HUP0203131A3 (en) | 2004-06-28 |
CZ20021089A3 (cs) | 2002-11-13 |
EA200200421A1 (ru) | 2002-10-31 |
ZA200202517B (en) | 2003-05-28 |
ES2277855T3 (es) | 2007-08-01 |
NO20021357L (no) | 2002-05-23 |
AU7737900A (en) | 2001-04-30 |
US6476038B1 (en) | 2002-11-05 |
IL148904A0 (en) | 2002-09-12 |
WO2001023388A3 (en) | 2001-10-18 |
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