NO20063866L - 1,3,5-trisubstituerte 4,5-di hydro-1 H-pyrazolderivater med CB1-antagonistisk aktivitet. - Google Patents
1,3,5-trisubstituerte 4,5-di hydro-1 H-pyrazolderivater med CB1-antagonistisk aktivitet.Info
- Publication number
- NO20063866L NO20063866L NO20063866A NO20063866A NO20063866L NO 20063866 L NO20063866 L NO 20063866L NO 20063866 A NO20063866 A NO 20063866A NO 20063866 A NO20063866 A NO 20063866A NO 20063866 L NO20063866 L NO 20063866L
- Authority
- NO
- Norway
- Prior art keywords
- pyrazole derivatives
- trisubstituted
- hydro
- antagonistic activity
- compounds
- Prior art date
Links
- -1 1,3,5-trisubstituted 4,5-di hydro-1H-pyrazole Chemical class 0.000 title abstract 2
- 230000003042 antagnostic effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229940124802 CB1 antagonist Drugs 0.000 abstract 1
- 230000009286 beneficial effect Effects 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 150000003217 pyrazoles Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A61P1/12—Antidiarrhoeals
-
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Virology (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Addiction (AREA)
- Otolaryngology (AREA)
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Abstract
der symbolene har betydningene som er angitt i beskrivelsen. Den foreliggende oppfinnelsen vedrører 1,3,5-trisubstituerte 4,5-dihydro-lH-pyrazol derivater som CB1-antagonister, fremgangsmåte for fremstilling av disse forbindelsene og nye mellomprodukter som er nyttige i syntesen av de nevnte pyrazolderivatene. Oppfinnelsen vedrører også anvendelsen av en forbindelse som her er beskrevet for fremstilling av et medikament som gir en fordelaktig effekt. Forbindelsene har den generelle formel (I)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53998304P | 2004-01-30 | 2004-01-30 | |
| EP04100338 | 2004-01-30 | ||
| PCT/EP2005/050339 WO2005074920A1 (en) | 2004-01-30 | 2005-01-27 | 1,3,5-trisubstituted 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NO20063866L true NO20063866L (no) | 2006-10-27 |
Family
ID=34839806
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20063866A NO20063866L (no) | 2004-01-30 | 2006-08-30 | 1,3,5-trisubstituerte 4,5-di hydro-1 H-pyrazolderivater med CB1-antagonistisk aktivitet. |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1713475B1 (no) |
| JP (1) | JP4693787B2 (no) |
| KR (1) | KR20060131861A (no) |
| CN (1) | CN100563651C (no) |
| AT (1) | ATE402697T1 (no) |
| AU (1) | AU2005210163B2 (no) |
| BR (1) | BRPI0507005A (no) |
| CA (1) | CA2552940A1 (no) |
| DE (1) | DE602005008555D1 (no) |
| DK (1) | DK1713475T3 (no) |
| ES (1) | ES2311972T3 (no) |
| HR (1) | HRP20080549T3 (no) |
| IL (1) | IL176547A (no) |
| MX (1) | MXPA06008593A (no) |
| NO (1) | NO20063866L (no) |
| PL (1) | PL1713475T3 (no) |
| PT (1) | PT1713475E (no) |
| RU (1) | RU2360904C2 (no) |
| SI (1) | SI1713475T1 (no) |
| WO (1) | WO2005074920A1 (no) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200533657A (en) * | 2004-02-17 | 2005-10-16 | Esteve Labor Dr | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1743892A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1849784A1 (en) * | 2006-04-26 | 2007-10-31 | Laboratorios Del Dr. Esteve, S.A. | Indoline-substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1849776A1 (en) * | 2006-04-26 | 2007-10-31 | Laboratorios Del Dr. Esteve, S.A. | Azepane- or Azocane-substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1757588A1 (en) * | 2005-07-29 | 2007-02-28 | Laboratorios Del Dr. Esteve, S.A. | Polymorph of N-Piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide and its use as a cannabinoid receptor modulator |
| EP1749820A1 (en) * | 2005-07-15 | 2007-02-07 | Laboratorios Del Dr. Esteve, S.A. | Salts of substituted pyrazoline compounds, their preparation and use as medicaments |
| ES2330993B1 (es) * | 2005-07-15 | 2010-07-06 | Laboratorios Del Dr. Esteve, S.A. | Combinacion de antagonista del receptor de cannabinoides de tipo pirazolina y estatina. |
| ES2327379B1 (es) * | 2005-07-15 | 2010-05-28 | Laboratorios Del Dr. Esteve, S.A. | Compuestos de pirazolina indolinsustituidos, su preparacion y su uso como medicamentos. |
| EP1743888A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | Carbonyl substituted pyrazoline compounds, their preparation and use as CB1 receptor modulators |
| ES2326952B1 (es) * | 2005-07-15 | 2010-05-28 | Laboratorios Del Dr. Esteve, S.A. | Hidratos de (rac) -n-piperidinil-5-(4-clorofenil)-1-(2,4-diclorofenil)4,5-dihidro-1h-pirazol-3-carboxamida. |
| WO2007009687A1 (en) * | 2005-07-15 | 2007-01-25 | Laboratorios Del Dr. Esteve, S.A. | Carbonyl substituted pyrazoline compounds, their preparation and use as cb1 receptor modulators |
| WO2007009690A1 (en) * | 2005-07-15 | 2007-01-25 | Laboratorios Del Dr. Esteve, S.A | Heterocyclyl-substituted pyrazoline compounds, their preparation and use as medicaments |
| WO2007009720A2 (en) * | 2005-07-15 | 2007-01-25 | Laboratorios Del Dr. Esteve S.A. | Prodrugs of pyrazoline compounds, their preparation and use as medicaments |
| EP1745783A1 (en) * | 2005-07-15 | 2007-01-24 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1749819A1 (en) * | 2005-07-15 | 2007-02-07 | Laboratorios Del Dr. Esteve, S.A. | (rac)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide hydrates |
| WO2007009682A1 (en) * | 2005-07-15 | 2007-01-25 | Laboratorios Del Dr. Esteve, S.A. | Oral pharmaceutical formulations comprising substituted pyrazoline compounds |
| EP1745781A1 (en) * | 2005-07-15 | 2007-01-24 | Laboratorios Del Dr. Esteve, S.A. | Combination of pyrazoline type cannabinoid receptor antagonist and statin |
| WO2007009699A2 (en) * | 2005-07-15 | 2007-01-25 | Laboratorios Del Dr. Esteve, S.A | Use of substituted pyrazoline compounds and their derivatives for the treatment of cannabinoid system-associated diseases |
| ES2337005B1 (es) * | 2005-07-15 | 2011-01-10 | Laboratorios Del Dr. Esteve, S.A. | Compuestos de pirazolina azepan o azocansustituidos, su preparacion ysu uso como medicamentos. |
| EP1743642A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | Use of substituted pyrazoline compounds and their derivatives for the treatment of cannabinoid system-associated diseases |
| ES2348374B1 (es) * | 2005-07-15 | 2011-08-02 | Laboratorios Del Dr Esteve, S.A. | Formulaciones farmaceuticas orales que comprenden compuestos de pirazolina sustituidos. |
| EP1743890A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments |
| EP1757589A1 (en) * | 2005-07-29 | 2007-02-28 | Laboratorios Del Dr. Esteve, S.A. | Amorphous phase of a substituted pyrazoline, its preparation and use as medicament |
| WO2007017124A1 (en) * | 2005-07-29 | 2007-02-15 | Laboratorios Del Dr. Esteve, S.A. | Amorphous phase of a substituted pyrazoline, its preparation and use as medicament |
| WO2007017126A2 (en) * | 2005-07-29 | 2007-02-15 | Laboratorios Del Dr. Esteve, S.A. | POLYMORPH OF N-PIPERIDINYL-5- (4-CHLOROPHENYL) -1- (2, 4-DICHLOROPHENYL) -4, 5-DIHYDRO-lH-PYRAZOLE- 3 -CARBOXAMIDE AND ITS USE AS A CAMNABINOID RECEPTOR MODULATOR |
| EP1911747A1 (en) | 2006-10-11 | 2008-04-16 | Laboratorios del Dr. Esteve S.A. | Sulfonamide substituted pyrazoline compounds, their preparation and use as CB1 modulators |
| EP1946778A1 (en) * | 2007-01-16 | 2008-07-23 | Laboratorios del Dr. Esteve S.A. | Active substance combination for the treatment of diabetes |
| ES2330071B1 (es) * | 2007-01-15 | 2010-07-05 | Laboratorios Del Dr. Esteve, S.A. | Combinacion de sustancias activas. |
| EP1946777A1 (en) * | 2007-01-16 | 2008-07-23 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline for preventing weight gain |
| EP1944295A1 (en) * | 2007-01-15 | 2008-07-16 | Laboratorios del Dr. Esteve S.A. | Non-racemic mixtures of (R)-N-piperidinyl-5-(4-chlorophenyl)1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide and (S)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide |
| ES2328653B1 (es) * | 2007-01-15 | 2010-05-28 | Laboratorios Del Dr. Esteve S.A. | Combinacion de sustancias activas para el tratamiento de la diabetes. |
| EP1946779A1 (en) * | 2007-01-16 | 2008-07-23 | Laboratorios del Dr. Esteve S.A. | Combination of substituted pyrazolines and agent for treating dyslipidemia |
| EP1947089A1 (en) * | 2007-01-18 | 2008-07-23 | Laboratorios del Dr. Esteve S.A. | A-polymorph of a substituted pyrazoline, its preparation and use as medicaments |
| JP2010530367A (ja) * | 2007-06-15 | 2010-09-09 | ソルベイ・フアーマシユーチカルズ・ベー・ブイ | カンナビノイドcb1受容体モジュレーターとしての4,5−ジヒドロ−(1h)−ピラゾール誘導体 |
| US8410135B2 (en) | 2007-06-15 | 2013-04-02 | Solvay Pharmaceuticals B.V. | 4,5 dihydro-(1H)-pyrazole derivatives as cannabinoid CB1 receptor modulators |
| KR20100072037A (ko) * | 2007-09-20 | 2010-06-29 | 애보트 헬스케어 프로덕츠 비.브이. | 칸나비노이드 cb₁수용체 효능제로서의 5-아릴-4,5-디하이드로-(1h)-피라졸 |
| EP2042175A1 (en) * | 2007-09-21 | 2009-04-01 | Laboratorios del Dr. Esteve S.A. | Dose regimens of CB1-Receptor ligands in the treatment of obesity |
| AR071487A1 (es) * | 2008-04-23 | 2010-06-23 | Solvay Pharm Bv | Derivados de (5r)-1,5-diaril-4,5-dihidro-1h-pirazol-3-carboxamidina que tienen actividad antagonista cb1 |
| EP2919779B1 (en) | 2012-11-13 | 2021-01-06 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Cannabinoid receptor mediating compounds |
| US11155521B2 (en) | 2012-11-13 | 2021-10-26 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Cannabinoid receptor mediating compounds |
| WO2014208939A1 (en) * | 2013-06-28 | 2014-12-31 | Hanmi Pharm. Co., Ltd. | 1,5-diaryl-4,5-dihydro-1h-pyrazole-3-carboxamidine derivatives as cannabinoid cb1 receptor antagonist, method for preparing same, and pharmaceutical composition comprising same |
| AU2015255765A1 (en) * | 2014-05-09 | 2016-11-24 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Pyrazole derivatives and their use as cannabinoid receptor mediators |
| CN115536649B (zh) * | 2022-10-27 | 2024-12-20 | 成都中医药大学 | 一种多取代吡唑啉类化合物及其合成方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3765782D1 (de) * | 1987-01-05 | 1990-11-29 | Du Pont | Pyrazolin mit insektizidischer aktivitaet. |
| EP0543930A1 (en) * | 1990-08-17 | 1993-06-02 | E.I. Du Pont De Nemours And Company | Arthropodicidal pyrazolines, pyrazolidines and hydrazines |
| JPH07504658A (ja) * | 1992-03-02 | 1995-05-25 | イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー | 殺節足動物性アミド類 |
| FR2713225B1 (fr) * | 1993-12-02 | 1996-03-01 | Sanofi Sa | N-pipéridino-3-pyrazolecarboxamide substitué. |
| UA74367C2 (uk) * | 2000-03-23 | 2005-12-15 | Сольве Фармас'Ютікалз Б.В. | ПОХІДНІ 4,5-ДИГІДРО-1Н-ПІРАЗОЛУ, ЩО ВИЯВЛЯЮТЬ АНТАГОНІСТИЧНУ АКТИВНІСТЬ ЩОДО СВ<sub>1</sub>, СПОСІБ ЇХ ОДЕРЖАННЯ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ЇЇ ВИГОТОВЛЕННЯ, СПОСІБ ЛІКУВАННЯ ЗАХВОРЮВАНЬ (ВАРІАНТИ) |
| SK287592B6 (sk) * | 2001-03-22 | 2011-03-04 | Solvay Pharmaceuticals B. V. | 4,5-Dihydro-1H-pyrazolové deriváty, ktoré majú CB1-antagonistickú účinnosť, spôsob ich prípravy a použitie |
| HUP0401567A3 (en) * | 2001-09-21 | 2005-06-28 | Solvay Pharm Bv | Novel 4,5-dyhydro-1h-pyrazole derivatives having cb1-antagonistic activity, their use and pharmaceutical compositions containing them |
| HRP20030913A2 (en) * | 2001-09-21 | 2004-06-30 | Solvay Pharm Bv | 4,5-dihydro-1h-pyrazole derivatives having potent cb1-antagonistic activity |
-
2005
- 2005-01-27 HR HR20080549T patent/HRP20080549T3/xx unknown
- 2005-01-27 DK DK05707857T patent/DK1713475T3/da active
- 2005-01-27 KR KR1020067017475A patent/KR20060131861A/ko not_active Ceased
- 2005-01-27 CA CA002552940A patent/CA2552940A1/en not_active Abandoned
- 2005-01-27 PL PL05707857T patent/PL1713475T3/pl unknown
- 2005-01-27 WO PCT/EP2005/050339 patent/WO2005074920A1/en not_active Ceased
- 2005-01-27 BR BRPI0507005-8A patent/BRPI0507005A/pt not_active IP Right Cessation
- 2005-01-27 AU AU2005210163A patent/AU2005210163B2/en not_active Ceased
- 2005-01-27 SI SI200530419T patent/SI1713475T1/sl unknown
- 2005-01-27 ES ES05707857T patent/ES2311972T3/es not_active Expired - Lifetime
- 2005-01-27 MX MXPA06008593A patent/MXPA06008593A/es active IP Right Grant
- 2005-01-27 RU RU2006131132/04A patent/RU2360904C2/ru not_active IP Right Cessation
- 2005-01-27 EP EP05707857A patent/EP1713475B1/en not_active Expired - Lifetime
- 2005-01-27 DE DE602005008555T patent/DE602005008555D1/de not_active Expired - Lifetime
- 2005-01-27 JP JP2006550185A patent/JP4693787B2/ja not_active Expired - Fee Related
- 2005-01-27 AT AT05707857T patent/ATE402697T1/de active
- 2005-01-27 PT PT05707857T patent/PT1713475E/pt unknown
- 2005-01-27 CN CNB2005800034967A patent/CN100563651C/zh not_active Expired - Fee Related
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2006
- 2006-06-26 IL IL176547A patent/IL176547A/en not_active IP Right Cessation
- 2006-08-30 NO NO20063866A patent/NO20063866L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| JP4693787B2 (ja) | 2011-06-01 |
| CN1913885A (zh) | 2007-02-14 |
| ATE402697T1 (de) | 2008-08-15 |
| CN100563651C (zh) | 2009-12-02 |
| DE602005008555D1 (de) | 2008-09-11 |
| RU2360904C2 (ru) | 2009-07-10 |
| AU2005210163B2 (en) | 2010-05-13 |
| SI1713475T1 (sl) | 2008-12-31 |
| HK1099688A1 (en) | 2007-08-24 |
| WO2005074920A1 (en) | 2005-08-18 |
| MXPA06008593A (es) | 2006-08-28 |
| DK1713475T3 (da) | 2008-12-01 |
| IL176547A (en) | 2010-06-30 |
| CA2552940A1 (en) | 2005-08-18 |
| ES2311972T3 (es) | 2009-02-16 |
| BRPI0507005A (pt) | 2007-06-05 |
| KR20060131861A (ko) | 2006-12-20 |
| PT1713475E (pt) | 2008-11-10 |
| AU2005210163A1 (en) | 2005-08-18 |
| IL176547A0 (en) | 2006-10-31 |
| EP1713475B1 (en) | 2008-07-30 |
| RU2006131132A (ru) | 2008-03-10 |
| JP2007519686A (ja) | 2007-07-19 |
| EP1713475A1 (en) | 2006-10-25 |
| HRP20080549T3 (en) | 2008-11-30 |
| PL1713475T3 (pl) | 2009-03-31 |
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