ZA200501227B - Aryl-substituted diazabicycloalkanes as nicotinic acetylcholine agonists - Google Patents
Aryl-substituted diazabicycloalkanes as nicotinic acetylcholine agonists Download PDFInfo
- Publication number
- ZA200501227B ZA200501227B ZA200501227A ZA200501227A ZA200501227B ZA 200501227 B ZA200501227 B ZA 200501227B ZA 200501227 A ZA200501227 A ZA 200501227A ZA 200501227 A ZA200501227 A ZA 200501227A ZA 200501227 B ZA200501227 B ZA 200501227B
- Authority
- ZA
- South Africa
- Prior art keywords
- diazabicyclo
- methanone
- oxygen
- sulfur
- propenone
- Prior art date
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- 239000000064 cholinergic agonist Substances 0.000 title description 2
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims abstract description 9
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims abstract description 9
- 150000001875 compounds Chemical class 0.000 claims description 48
- -1 Cy_salkynyl Chemical group 0.000 claims description 33
- 229910052760 oxygen Inorganic materials 0.000 claims description 27
- 239000001301 oxygen Substances 0.000 claims description 27
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 25
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 25
- 229910052717 sulfur Inorganic materials 0.000 claims description 25
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 22
- 239000011593 sulfur Substances 0.000 claims description 22
- 125000005842 heteroatom Chemical group 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 19
- FTTATHOUSOIFOQ-UHFFFAOYSA-N 1,2,3,4,6,7,8,8a-octahydropyrrolo[1,2-a]pyrazine Chemical compound C1NCCN2CCCC21 FTTATHOUSOIFOQ-UHFFFAOYSA-N 0.000 claims description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- 239000000203 mixture Substances 0.000 claims description 13
- 230000006735 deficit Effects 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 11
- CKJNUZNMWOVDFN-UHFFFAOYSA-N methanone Chemical compound O=[CH-] CKJNUZNMWOVDFN-UHFFFAOYSA-N 0.000 claims description 11
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
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- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
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- 150000002431 hydrogen Chemical class 0.000 claims description 8
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- YYUJHPFFBNOQAE-UHFFFAOYSA-N 1,4-diazabicyclo[3.2.2]nonan-4-yl-(4-methoxyphenyl)methanone Chemical compound C1=CC(OC)=CC=C1C(=O)N1C(CC2)CCN2CC1 YYUJHPFFBNOQAE-UHFFFAOYSA-N 0.000 claims description 4
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- QAQZGYOOSFWULK-UHFFFAOYSA-N 1,4-diazabicyclo[3.2.2]nonan-4-yl(furan-2-yl)methanone Chemical compound C1CN(CC2)CCC2N1C(=O)C1=CC=CO1 QAQZGYOOSFWULK-UHFFFAOYSA-N 0.000 claims description 2
- UCLKOOMKBIIIOY-UHFFFAOYSA-N 1,4-diazabicyclo[3.2.2]nonan-4-yl(naphthalen-2-yl)methanone Chemical compound C=1C=C2C=CC=CC2=CC=1C(=O)N1CCN2CCC1CC2 UCLKOOMKBIIIOY-UHFFFAOYSA-N 0.000 claims description 2
- KSQYHMYVSVAPGG-UHFFFAOYSA-N 1,4-diazabicyclo[3.2.2]nonan-4-yl(phenyl)methanone Chemical compound C1CN(CC2)CCC2N1C(=O)C1=CC=CC=C1 KSQYHMYVSVAPGG-UHFFFAOYSA-N 0.000 claims description 2
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- HAXPXNGBJPFDGV-UHFFFAOYSA-N 1,4-diazabicyclo[3.2.2]nonan-4-yl-(4-iodophenyl)methanone Chemical compound C1=CC(I)=CC=C1C(=O)N1C(CC2)CCN2CC1 HAXPXNGBJPFDGV-UHFFFAOYSA-N 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- ZWUSBSHBFFPRNE-UHFFFAOYSA-N 3,4-dichlorobenzaldehyde Chemical compound ClC1=CC=C(C=O)C=C1Cl ZWUSBSHBFFPRNE-UHFFFAOYSA-N 0.000 claims description 2
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- BEOBZEOPTQQELP-UHFFFAOYSA-N 4-(trifluoromethyl)benzaldehyde Chemical compound FC(F)(F)C1=CC=C(C=O)C=C1 BEOBZEOPTQQELP-UHFFFAOYSA-N 0.000 claims description 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000004532 benzofuran-3-yl group Chemical group O1C=C(C2=C1C=CC=C2)* 0.000 claims description 2
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Classifications
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- 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
- C07D471/08—Bridged 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
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- 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
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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Landscapes
- Health & Medical Sciences (AREA)
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- Organic Chemistry (AREA)
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Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0202465A SE0202465D0 (sv) | 2002-08-14 | 2002-08-14 | New compounds |
Publications (1)
| Publication Number | Publication Date |
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| ZA200501227B true ZA200501227B (en) | 2006-07-26 |
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| ZA200501227A ZA200501227B (en) | 2002-08-14 | 2005-02-10 | Aryl-substituted diazabicycloalkanes as nicotinic acetylcholine agonists |
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| Country | Link |
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| US (1) | US20060052368A1 (es) |
| EP (1) | EP1539764B1 (es) |
| JP (1) | JP2005539030A (es) |
| KR (1) | KR20060005334A (es) |
| CN (1) | CN100436453C (es) |
| AT (1) | ATE430152T1 (es) |
| AU (1) | AU2003248590B2 (es) |
| BR (1) | BR0313233A (es) |
| CA (1) | CA2493246A1 (es) |
| DE (1) | DE60327441D1 (es) |
| IL (1) | IL166425A0 (es) |
| MX (1) | MXPA05001584A (es) |
| NO (1) | NO20051260L (es) |
| SE (1) | SE0202465D0 (es) |
| WO (1) | WO2004016616A1 (es) |
| ZA (1) | ZA200501227B (es) |
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| SE521512C2 (sv) | 2001-06-25 | 2003-11-11 | Niconovum Ab | Anordning för administrering av en substans till främre delen av en individs munhåla |
| DE10164139A1 (de) | 2001-12-27 | 2003-07-10 | Bayer Ag | 2-Heteroarylcarbonsäureamide |
| SE0202430D0 (sv) * | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | New Compounds |
| CA2499128C (en) | 2002-09-25 | 2012-07-31 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, and benzoisothiazoles, and preparation and uses thereof |
| US7456171B2 (en) * | 2002-10-08 | 2008-11-25 | Sanofi-Aventis | 1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof |
| PT1578422E (pt) | 2002-12-20 | 2007-06-14 | Niconovum Ab | Material particulado contendo nicotina fisicamente e quimicamente estável |
| DE602004023586D1 (de) * | 2003-02-27 | 2009-11-26 | Neurosearch As | Neue diazabicyclische arylderivate |
| RS20060391A (en) | 2003-12-22 | 2008-11-28 | Memory Pharmaceuticals Corporation, | Indoles, 1h-indazoles, 1,2-benzisoxazoles, and 1,2- benzisothiazoles, and preparation and uses thereof |
| TW200529860A (en) * | 2003-12-22 | 2005-09-16 | Astrazeneca Ab | Nicotinic acetylcholine receptor ligands |
| CN100445285C (zh) * | 2003-12-22 | 2008-12-24 | 阿斯利康(瑞典)有限公司 | 烟碱性乙酰胆碱受体配体 |
| FR2865208B1 (fr) * | 2004-01-16 | 2009-01-16 | Sanofi Synthelabo | Derives de 1,4-diazabicyclo[3.2.1]octanecarboxmique, leur preparation et leur application en therapeutique |
| CA2555311A1 (en) * | 2004-02-04 | 2005-08-18 | Neurosearch A/S | Diazabicyclic aryl derivatives as nicotinic acetylcholine receptor ligands |
| EP1725236A4 (en) * | 2004-03-11 | 2009-05-13 | Glaxo Group Ltd | NEW M3 MUSCARIN ACETYLCHOLINE RECEPTOR ANTAGONISTS |
| MXPA06010852A (es) | 2004-03-25 | 2007-01-16 | Memory Pharm Corp | Indazoles, benzotiazoles, benzoisotiazoles, bencisoxazoles y preparacion y usos de los mismos. |
| WO2006001894A1 (en) | 2004-04-22 | 2006-01-05 | Memory Pharmaceutical Corporation | Indoles, 1h-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof |
| DE602005027452D1 (de) * | 2004-05-07 | 2011-05-26 | Memory Pharm Corp | 1h-indazole, benzothiazole, 1,2-benzisoxazole, 1,2-benzisothiazole und chromone und deren herstellung und verwendungen |
| US7612074B2 (en) | 2004-11-30 | 2009-11-03 | Neurosearch A/S | Diazabicyclic aryl derivatives as cholinergy ligands |
| PL1828179T3 (pl) | 2004-12-22 | 2010-08-31 | Memory Pharm Corp | Ligandy dla receptorów nikotynowych alfa-7 przeciwko chorobom związanym z OUN |
| CA2627089A1 (en) * | 2005-11-09 | 2007-05-18 | Memory Pharmaceuticals Corporation | 1 h-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof |
| US7855208B2 (en) | 2006-02-14 | 2010-12-21 | Neurosearch A/S | 3, 9-diazabicyclo(3.3.1)non-3-yl-aryl methanone derivatives as nicotinic acetylcholine receptor agonists |
| JP5694645B2 (ja) | 2006-03-16 | 2015-04-01 | ニコノヴァム エービーＮｉｃｏｎｏｖｕｍ Ａｂ | 改善された嗅ぎたばこ組成物 |
| TWI454262B (zh) * | 2006-11-02 | 2014-10-01 | Targacept Inc | 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺 |
| SA08290475B1 (ar) | 2007-08-02 | 2013-06-22 | Targacept Inc | (2s، 3r)-n-(2-((3-بيردينيل)ميثيل)-1-آزا بيسيكلو[2، 2، 2]أوكت-3-يل)بنزو فيوران-2-كربوكساميد، وصور أملاحه الجديدة وطرق استخدامه |
| CA2716863A1 (en) * | 2008-03-05 | 2009-09-11 | Targacept, Inc. | Sub-type selective amides of diazabicycloalkanes |
| DK2307389T3 (da) | 2008-06-20 | 2013-04-02 | Astrazeneca Ab | Dibenzothiazepinderivat og anvendelser deraf |
| TW201031664A (en) | 2009-01-26 | 2010-09-01 | Targacept Inc | Preparation and therapeutic applications of (2S,3R)-N-2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)-3,5-difluorobenzamide |
| CN103221411B (zh) | 2010-05-17 | 2016-05-11 | 富瑞姆制药公司 | (R)-7-氯-N-(奎宁环-3-基)苯并[b]噻吩-2-甲酰胺盐酸盐单水合物的晶型 |
| PL2657237T3 (pl) * | 2010-12-22 | 2015-11-30 | Tosoh Corp | Cykliczny związek aminowy i proces produkcji żywicy poliuretanowej z jego zastosowaniem |
| GB201111705D0 (en) | 2011-07-07 | 2011-08-24 | Takeda Pharmaceutical | Compounds and their use |
| GB201111704D0 (en) | 2011-07-07 | 2011-08-24 | Takeda Pharmaceutical | Novel compounds |
| JO3115B1 (ar) | 2011-08-22 | 2017-09-20 | Takeda Pharmaceuticals Co | مركبات بيريدازينون واستخدامها كمثبطات daao |
| EP2797886A2 (fr) | 2011-12-30 | 2014-11-05 | Ecole Nationale Superieure de Chimie de Clermont Ferrand | Composes anti-douleur |
| AU2013259871A1 (en) | 2012-05-08 | 2014-11-20 | Forum Pharmaceuticals Inc. | Methods of maintaining, treating or improving cognitive function |
| GB201209587D0 (en) | 2012-05-30 | 2012-07-11 | Takeda Pharmaceutical | Therapeutic compounds |
| US8609162B2 (en) * | 2012-10-04 | 2013-12-17 | Invivo Beverages Llc | Integrated neuromodulation system for mood enhancement of a living human subject |
| WO2014122474A1 (en) | 2013-02-07 | 2014-08-14 | Takeda Pharmaceutical Company Limited | Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists |
| CA2914263C (en) | 2013-06-21 | 2021-05-18 | Takeda Pharmaceutical Company Limited | 1-sulfonyl piperidine derivatives as modulators of prokineticin receptors |
| GB201314286D0 (en) | 2013-08-08 | 2013-09-25 | Takeda Pharmaceutical | Therapeutic Compounds |
| GB201318222D0 (en) | 2013-10-15 | 2013-11-27 | Takeda Pharmaceutical | Novel compounds |
| GB201320905D0 (en) | 2013-11-27 | 2014-01-08 | Takeda Pharmaceutical | Therapeutic compounds |
| TW201613864A (en) | 2014-02-20 | 2016-04-16 | Takeda Pharmaceutical | Novel compounds |
| GB201616839D0 (en) | 2016-10-04 | 2016-11-16 | Takeda Pharmaceutical Company Limited | Therapeutic compounds |
| GB201619514D0 (en) | 2016-11-18 | 2017-01-04 | Takeda Pharmaceuticals Co | Novel compounds |
| WO2019005874A1 (en) | 2017-06-26 | 2019-01-03 | The Trustees Of Columbia University In The City Of New York | CHOLINERGIC AGONISM FOR THE TREATMENT OF PANCREATIC CANCER |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3281423A (en) * | 1964-02-03 | 1966-10-25 | Merck & Co Inc | 1, 3-ethanopiperazines and process |
| US4895943A (en) * | 1988-10-25 | 1990-01-23 | Pfizer Inc. | Preparation of 1,4-diazabicyclo(3.2.2)nonane |
| US5679673A (en) * | 1992-09-24 | 1997-10-21 | The United States Of America, Represented By The Department Of Health And Human Services | Aralkyl bridged diazabicycloalkane derivatives for CNS disorders |
| FR2791678B1 (fr) * | 1999-03-30 | 2001-05-04 | Synthelabo | Derives de 1,4-diazabicyclo [3.2.2] nonane-4-carboxylates et -carboxamides, leur preparation et leur application en therapeutique |
| FR2809732B1 (fr) * | 2000-05-31 | 2002-07-19 | Sanofi Synthelabo | DERIVES DE 4(-2-PHENYLTHIAZOL-5-yl)-1,4-DIAZABICYCLO-[3.2.2] NONANE, LEUR PREPARATION ET LEUR APPLICATION ENTHERAPEUTIQUE |
| FR2809731B1 (fr) * | 2000-05-31 | 2002-07-19 | Sanofi Synthelabo | Derives de 1,4-diazabicyclo-[3.2.2] nonane-pheylisoxazole, leur preparation et leur application en therapeutique |
| FR2809730B1 (fr) * | 2000-05-31 | 2002-07-19 | Sanofi Synthelabo | Derives de 1,4-diazabicyclo[3.2.2] nonanebenzoxazole, -benzothiazole et -benzimidazole, leur preparation et leur application therapeutique |
| US20020086871A1 (en) * | 2000-12-29 | 2002-07-04 | O'neill Brian Thomas | Pharmaceutical composition for the treatment of CNS and other disorders |
| SE0202430D0 (sv) * | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | New Compounds |
| DE602004023586D1 (de) * | 2003-02-27 | 2009-11-26 | Neurosearch As | Neue diazabicyclische arylderivate |
| CN100445285C (zh) * | 2003-12-22 | 2008-12-24 | 阿斯利康(瑞典)有限公司 | 烟碱性乙酰胆碱受体配体 |
| TW200529860A (en) * | 2003-12-22 | 2005-09-16 | Astrazeneca Ab | Nicotinic acetylcholine receptor ligands |
-
2002
- 2002-08-14 SE SE0202465A patent/SE0202465D0/xx unknown
-
2003
- 2003-08-13 AU AU2003248590A patent/AU2003248590B2/en not_active Expired - Fee Related
- 2003-08-13 CA CA002493246A patent/CA2493246A1/en not_active Abandoned
- 2003-08-13 KR KR1020057002266A patent/KR20060005334A/ko not_active Application Discontinuation
- 2003-08-13 CN CNB038192578A patent/CN100436453C/zh not_active Expired - Fee Related
- 2003-08-13 BR BR0313233-1A patent/BR0313233A/pt not_active IP Right Cessation
- 2003-08-13 US US10/524,482 patent/US20060052368A1/en not_active Abandoned
- 2003-08-13 DE DE60327441T patent/DE60327441D1/de not_active Expired - Fee Related
- 2003-08-13 EP EP03788213A patent/EP1539764B1/en not_active Expired - Lifetime
- 2003-08-13 JP JP2004529001A patent/JP2005539030A/ja active Pending
- 2003-08-13 WO PCT/SE2003/001276 patent/WO2004016616A1/en active Application Filing
- 2003-08-13 MX MXPA05001584A patent/MXPA05001584A/es unknown
- 2003-08-13 AT AT03788213T patent/ATE430152T1/de not_active IP Right Cessation
-
2005
- 2005-01-20 IL IL16642505A patent/IL166425A0/xx unknown
- 2005-02-10 ZA ZA200501227A patent/ZA200501227B/en unknown
- 2005-03-11 NO NO20051260A patent/NO20051260L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20060005334A (ko) | 2006-01-17 |
| NO20051260L (no) | 2005-05-10 |
| US20060052368A1 (en) | 2006-03-09 |
| CN100436453C (zh) | 2008-11-26 |
| AU2003248590A1 (en) | 2004-03-03 |
| CA2493246A1 (en) | 2004-02-26 |
| BR0313233A (pt) | 2005-06-14 |
| SE0202465D0 (sv) | 2002-08-14 |
| WO2004016616A1 (en) | 2004-02-26 |
| JP2005539030A (ja) | 2005-12-22 |
| IL166425A0 (en) | 2006-01-15 |
| CN1675215A (zh) | 2005-09-28 |
| AU2003248590B2 (en) | 2008-03-20 |
| EP1539764A1 (en) | 2005-06-15 |
| DE60327441D1 (de) | 2009-06-10 |
| ATE430152T1 (de) | 2009-05-15 |
| EP1539764B1 (en) | 2009-04-29 |
| MXPA05001584A (es) | 2005-04-25 |
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