EA200501241A1 - ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 8'-ПИРИДИНИЛ-ДИГИДРОСПИРО-[ЦИКЛОАЛКИЛ]-ПИРИМИДО [1,2-a]ПИРИМИДИН-6-ОНА И 8'-ПИРИМИДИНИЛ-ДИГИДРОСПИРО-[ЦИКЛОАЛКИЛ]-ПИРИМИДО [1,2-a]ПИРИМИДИН-6-ОНА И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ НЕЙРОДЕГЕНЕРАТИВНЫХ ЗАБОЛЕВАНИЙ - Google Patents
ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 8'-ПИРИДИНИЛ-ДИГИДРОСПИРО-[ЦИКЛОАЛКИЛ]-ПИРИМИДО [1,2-a]ПИРИМИДИН-6-ОНА И 8'-ПИРИМИДИНИЛ-ДИГИДРОСПИРО-[ЦИКЛОАЛКИЛ]-ПИРИМИДО [1,2-a]ПИРИМИДИН-6-ОНА И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ НЕЙРОДЕГЕНЕРАТИВНЫХ ЗАБОЛЕВАНИЙInfo
- Publication number
- EA200501241A1 EA200501241A1 EA200501241A EA200501241A EA200501241A1 EA 200501241 A1 EA200501241 A1 EA 200501241A1 EA 200501241 A EA200501241 A EA 200501241A EA 200501241 A EA200501241 A EA 200501241A EA 200501241 A1 EA200501241 A1 EA 200501241A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- dihydrospyro
- cyclo
- ring
- syndyrohydroxyldyl
- Prior art date
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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
- C07D487/10—Spiro-condensed systems
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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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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
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- A61P25/16—Anti-Parkinson drugs
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- 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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- Health & Medical Sciences (AREA)
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- Engineering & Computer Science (AREA)
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- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
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- Ophthalmology & Optometry (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Данное изобретение относится к производному дигидроспиро[циклоалкил]пиримидона, представленному формулой (I), или его соли, где X представляет собой два атома водорода, атом серы, атом кислорода или Cалкильную группу и атом водорода; Y представляет собой связь, карбонильную группу, метиленовую группу, возможно замещенную; R1 представляет собой 2-, 3- или 4-пиридиновое кольцо или 2-, 4- или 5-пиримидиновое кольцо, причем кольцо возможно замещено; R2 представляет собой бензольное кольцо или нафталиновое кольцо; при этом кольца возможно замещены; R3 представляет собой атом водорода, Cалкильную группу или атом галогена; m означает 1-4; n означает 0-3; p означает 0-2; q означает 0-2, при этом p+q меньше 4. Данное изобретение также относится к лекарственному средству, включающему в качестве активного ингредиента указанное производное или его соль, используемому для профилактического и/или терапевтического лечения нейродегенеративного заболевания, вызванного аномальной активностью GSK3β, такого как болезнь Альцгеймера.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03290569A EP1454909B1 (en) | 2003-03-07 | 2003-03-07 | 8'-pyridinyl-dihydrospiro (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro (cycloalkyl) pyrimido (1,2-a) pyrimidin-6 derivatives -one and their use against neurodegenerative diseases |
| PCT/EP2004/003051 WO2004078760A1 (en) | 2003-03-07 | 2004-03-05 | SUBSTITUTED 8'-PYRIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE AND 8'-PYRIMIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200501241A1 true EA200501241A1 (ru) | 2006-04-28 |
| EA008172B1 EA008172B1 (ru) | 2007-04-27 |
Family
ID=32799103
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200501241A EA008172B1 (ru) | 2003-03-07 | 2004-03-05 | ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 8'-ПИРИДИНИЛДИГИДРОСПИРО[ЦИКЛОАЛКИЛ]ПИРИМИДО[1,2-а]ПИРИМИДИН-6-ОНА И 8'-ПИРИМИДИНИЛДИГИДРОСПИРО[ЦИКЛОАЛКИЛ]ПИРИМИДО[1,2-а]ПИРИМИДИН-6-ОНА И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ НЕЙРОДЕГЕНЕРАТИВНЫХ ЗАБОЛЕВАНИЙ |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7294632B2 (ru) |
| EP (2) | EP1454909B1 (ru) |
| JP (1) | JP4639182B2 (ru) |
| KR (1) | KR101069984B1 (ru) |
| CN (1) | CN100463908C (ru) |
| AR (1) | AR043485A1 (ru) |
| AT (1) | ATE469153T1 (ru) |
| AU (1) | AU2004218250B2 (ru) |
| BR (1) | BRPI0408189A (ru) |
| CA (1) | CA2516937C (ru) |
| CY (1) | CY1111057T1 (ru) |
| DE (1) | DE602004027354D1 (ru) |
| DK (1) | DK1603915T3 (ru) |
| EA (1) | EA008172B1 (ru) |
| ES (1) | ES2346311T3 (ru) |
| HK (1) | HK1085740A1 (ru) |
| IL (1) | IL170461A (ru) |
| MX (1) | MXPA05009574A (ru) |
| NO (1) | NO20054140L (ru) |
| NZ (1) | NZ542135A (ru) |
| PL (1) | PL1603915T3 (ru) |
| PT (1) | PT1603915E (ru) |
| SI (1) | SI1603915T1 (ru) |
| TW (1) | TWI320785B (ru) |
| WO (1) | WO2004078760A1 (ru) |
| ZA (1) | ZA200507107B (ru) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1891021B1 (en) * | 2005-06-14 | 2019-01-23 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
| CA2620333A1 (en) | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP2377530A3 (en) | 2005-10-21 | 2012-06-20 | Braincells, Inc. | Modulation of neurogenesis by PDE inhibition |
| WO2007053596A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| JP2009536669A (ja) | 2006-05-09 | 2009-10-15 | ブレインセルス，インコーポレイティド | アンジオテンシン調節による神経新生 |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| EP1992624A1 (en) | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Heteroarylamide pyrimidone compounds |
| EP1992620A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Arylamide pyrimidone derivatives for the treatment of neurodegenerative diseases |
| EP1992621A1 (en) | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Heteroarylamide-substituted pyrimidone derivatives for the treatment of neurodegenerative diseases |
| EP1992625A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Arylamide pyrimidone compounds |
| EP2138494A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted alkyl pyrimidin-4-one derivatives |
| EP2138495A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives |
| EP2138498A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted tricyclic derivatives against neurodegenerative diseases |
| EP2138492A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidin-4-one derivatives |
| EP2138488A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases |
| EP2138485A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted N-Oxide pyrazine derivatives |
| EP2138493A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidone derivatives |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| JP5655070B2 (ja) | 2009-07-02 | 2015-01-14 | サノフイ | 新規６，７，８，９−テトラヒドロピリミド｛１，２−ａ｝ピリミジン−４−オン誘導体、これらの調製およびこれらの医薬的使用 |
| PL2655375T3 (pl) | 2010-12-23 | 2015-05-29 | Sanofi Sa | Pochodne pirymidynonu, ich wytwarzanie i ich farmaceutyczne zastosowanie |
| FR2992314B1 (fr) | 2012-06-22 | 2015-10-16 | Sanofi Sa | Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique |
| FR2992316A1 (fr) | 2012-06-22 | 2013-12-27 | Sanofi Sa | Derives de pyrimidinones, leur preparation et leur application en therapeutique |
| CA2945263A1 (en) | 2014-04-09 | 2015-10-15 | Christopher Rudd | Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2812636A1 (fr) * | 2000-08-02 | 2002-02-08 | Novapharme | Nouveaux derives 2-phenyl imidazo[1.2-a]pyrimidin-5-ones et 2-phenyl 2,3-dihydro imidazo[1,2-a]pyrimidin-5-ones |
| WO2002018386A1 (en) * | 2000-09-01 | 2002-03-07 | Sanofi-Synthelabo | 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a]PYRIMIDIN-4-ONE AND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO[1,2-a]PYRIMIDIN-5(1H)ONE DERIVATI VES |
| EP1184385A1 (en) * | 2000-09-01 | 2002-03-06 | Sanofi-Synthelabo | 1-[Alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-pyridin-4-yl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one derivatives |
| EP1184383A1 (en) * | 2000-09-01 | 2002-03-06 | Sanofi-Synthelabo | 9-[Alkyl], 9-[(heteroaryl)alkyl] and 9-[(aryl)alkyl]-2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives |
| AU2002342798C1 (en) * | 2001-09-21 | 2008-09-25 | Mitsubishi Pharma Corporation | Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders |
| EP1295885A1 (en) * | 2001-09-21 | 2003-03-26 | Sanofi-Synthelabo | Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido(1,2-a)pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo(1,2-a)pyrimidin-5(1H)one derivatives |
| MXPA04002629A (es) * | 2001-09-21 | 2005-02-17 | Sanofi Aventis | Derivados de 2-piridinil-6, 7, 8, 9-tetrahidropirimido [1, 2-a] pirimidin-4-ona y 7-piridinil-2, 3-dihidroimidazo [1, 2-a] pirimidin-5(1h) -ona. |
| EP1295884A1 (en) * | 2001-09-21 | 2003-03-26 | Sanofi-Synthelabo | 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 7-Pyrimidinyl-2,3-Dihydroimidazo[1,2-a]Pyrimidin-5(1H)one derivatives |
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2003
- 2003-03-07 EP EP03290569A patent/EP1454909B1/en not_active Withdrawn - After Issue
-
2004
- 2004-03-05 NZ NZ542135A patent/NZ542135A/en not_active IP Right Cessation
- 2004-03-05 SI SI200431465T patent/SI1603915T1/sl unknown
- 2004-03-05 WO PCT/EP2004/003051 patent/WO2004078760A1/en active Application Filing
- 2004-03-05 DK DK04717643.3T patent/DK1603915T3/da active
- 2004-03-05 CN CNB2004800109973A patent/CN100463908C/zh not_active Expired - Fee Related
- 2004-03-05 EP EP04717643A patent/EP1603915B1/en not_active Expired - Lifetime
- 2004-03-05 ZA ZA200507107A patent/ZA200507107B/en unknown
- 2004-03-05 CA CA2516937A patent/CA2516937C/en not_active Expired - Fee Related
- 2004-03-05 AR ARP040100694A patent/AR043485A1/es not_active Application Discontinuation
- 2004-03-05 MX MXPA05009574A patent/MXPA05009574A/es active IP Right Grant
- 2004-03-05 DE DE602004027354T patent/DE602004027354D1/de not_active Expired - Lifetime
- 2004-03-05 EA EA200501241A patent/EA008172B1/ru not_active IP Right Cessation
- 2004-03-05 AU AU2004218250A patent/AU2004218250B2/en not_active Ceased
- 2004-03-05 AT AT04717643T patent/ATE469153T1/de active
- 2004-03-05 JP JP2006504813A patent/JP4639182B2/ja not_active Expired - Fee Related
- 2004-03-05 ES ES04717643T patent/ES2346311T3/es not_active Expired - Lifetime
- 2004-03-05 PT PT04717643T patent/PT1603915E/pt unknown
- 2004-03-05 PL PL04717643T patent/PL1603915T3/pl unknown
- 2004-03-05 TW TW093105914A patent/TWI320785B/zh not_active IP Right Cessation
- 2004-03-05 BR BRPI0408189-7A patent/BRPI0408189A/pt not_active IP Right Cessation
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2005
- 2005-08-23 IL IL170461A patent/IL170461A/en not_active IP Right Cessation
- 2005-09-06 NO NO20054140A patent/NO20054140L/no not_active Application Discontinuation
- 2005-09-06 KR KR1020057016622A patent/KR101069984B1/ko not_active IP Right Cessation
- 2005-09-07 US US11/220,999 patent/US7294632B2/en not_active Expired - Fee Related
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2006
- 2006-07-14 HK HK06107902.6A patent/HK1085740A1/xx not_active IP Right Cessation
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2007
- 2007-10-02 US US11/866,142 patent/US7507743B2/en not_active Expired - Fee Related
-
2010
- 2010-08-17 CY CY20101100761T patent/CY1111057T1/el unknown
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