AR044013A1 - Derivados de acido [2-(8,9-dioxo-2,6-diazabiciclo [5.2.0.] non-1 (7)-en-2-il)alquil]fosfonico, metodos para su uso, composicion y procedimiento de preparacion - Google Patents
Derivados de acido [2-(8,9-dioxo-2,6-diazabiciclo [5.2.0.] non-1 (7)-en-2-il)alquil]fosfonico, metodos para su uso, composicion y procedimiento de preparacionInfo
- Publication number
- AR044013A1 AR044013A1 ARP040101199A ARP040101199A AR044013A1 AR 044013 A1 AR044013 A1 AR 044013A1 AR P040101199 A ARP040101199 A AR P040101199A AR P040101199 A ARP040101199 A AR P040101199A AR 044013 A1 AR044013 A1 AR 044013A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- aryl
- treatment
- mammal
- cycloalkyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title 2
- 239000002253 acid Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 241000124008 Mammalia Species 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 abstract 2
- 208000028017 Psychotic disease Diseases 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 2
- 206010008118 cerebral infarction Diseases 0.000 abstract 2
- 208000026106 cerebrovascular disease Diseases 0.000 abstract 2
- 230000001684 chronic effect Effects 0.000 abstract 2
- 206010015037 epilepsy Diseases 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006564 (C4-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010002660 Anoxia Diseases 0.000 abstract 1
- 241000976983 Anoxia Species 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 201000006474 Brain Ischemia Diseases 0.000 abstract 1
- 206010008120 Cerebral ischaemia Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 208000002249 Diabetes Complications Diseases 0.000 abstract 1
- 206010012655 Diabetic complications Diseases 0.000 abstract 1
- 208000001640 Fibromyalgia Diseases 0.000 abstract 1
- 208000010412 Glaucoma Diseases 0.000 abstract 1
- 208000010496 Heart Arrest Diseases 0.000 abstract 1
- 208000007514 Herpes zoster Diseases 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 208000013016 Hypoglycemia Diseases 0.000 abstract 1
- 206010021143 Hypoxia Diseases 0.000 abstract 1
- 208000007101 Muscle Cramp Diseases 0.000 abstract 1
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 abstract 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000020186 Schizophreniform disease Diseases 0.000 abstract 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 208000030886 Traumatic Brain injury Diseases 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 1
- 230000036592 analgesia Effects 0.000 abstract 1
- 230000007953 anoxia Effects 0.000 abstract 1
- 125000003435 aroyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 230000001149 cognitive effect Effects 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000002996 emotional effect Effects 0.000 abstract 1
- 230000001037 epileptic effect Effects 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002218 hypoglycaemic effect Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 208000001286 intracranial vasospasm Diseases 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 210000000056 organ Anatomy 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 230000036407 pain Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000022610 schizoaffective disease Diseases 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 210000000278 spinal cord Anatomy 0.000 abstract 1
- 125000003003 spiro group Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
-
- 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
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A—HUMAN NECESSITIES
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- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
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- A61P25/12—Antiepileptics; Anticonvulsants for grand-mal
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- 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
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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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Psychology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Los compuestos son antagonistas del receptor de N-metil-D-aspartato (NMDA), y son útiles en el tratamiento de una variedad de afecciones presentes en una mamífero que se benefician con la inhibición del receptor de NMDA. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de dicho compuesto, en donde: R1 es hidrógeno, un grupo alquilo C1-6, un grupo acilo C2-7, un grupo alcanosulfonilo C1-6, o un grupo aroílo C6-14; A es alquileno C1-4, o alquenileno C2- 4; R2 y R3, de manera independiente, se seleccionan entre hidrógeno o un resto de grupo de fórmula (2), con la condición de que por lo menos uno de R2 y R3 no es hidrógeno; R4 y R5, de manera independiente, se seleccionan entre hidrógeno, un grupo alquilo C1-4, un grupo arilo C5-7, un grupo alquilarilo C6-15 que tiene 5 a 7 átomos de carbono en el anillo arilo, un grupo alquenilo C2-7, o un grupo alquinilo C2-7, o R4 y R5 pueden formar juntos un anillo carbocíclico C38 espiro; R6 es un grupo alquilo lineal o ramificado C1-12, un grupo alquenilo o alquinilo lineal o ramificado C2-7, un grupo arilo C5-13, un grupo alquilarilo C6-21 que tiene 5 a 13 átomos de carbono en la porción arilo, un grupo heteroarilo de 5 a 13 miembros, un grupo alquilheteroarilo de 6 a 21 miembros que tiene 5 a 13 miembros en la porción heteroarilo, un grupo cicloalquilo C4-8, un grupo alquilcicloalquilo C5-16 que tiene 4 a 8 átomos de carbono en el anillo cicloalquilo; R7 y R8, se seleccionan de manera independiente entre hidrógeno, un grupo alquilo lineal o ramificado C1-12, un grupo alquenilo o alquinilo lineal o ramificado C2-7, un grupo arilo C5-13, un grupo alquilarilo C6-21 que tiene 5 a 13 átomos de carbono en la porción arilo, un grupo heteroarilo de 5 a 13 miembros, un grupo alquilheteroarilo de 6 a 21 miembros que tiene 5 a 13 miembros en la porción heteroarilo, o R7 y R8 pueden formar juntos un grupo cicloalquilo o heterocicloalquilo que tiene en el anillo C4-8, y opcionalmente, uno o dos átomos seleccionados entre nitrógeno, oxígeno o azufre; en donde cualquier grupo R1 a R8 que tiene una porción arilo, heteroarilo, cicloalquilo o heterocicloalquilo puede estar opcionalmente sustituido en la porción arilo, heteroarilo, cicloalquilo o heterocicloalquilo, con 1 a aproximadamente 5 sustituyentes seleccionados en forma independiente entre un átomo de halógeno, un grupo ciano, nitro o hidroxilo, un grupo alquilo C1-6, o un grupo alcoxi C1- 6. Reivindicación 27: Uso de un compuesto de fórmula (1) según se define en cualquiera de las reivindicaciones 1 a 10, para el tratamiento de por lo menos una afección en mamífero seleccionada entre un trastorno cerebrovascular seleccionado entre isquemia cerebral, infarto cerebral o vasoespasmo cerebral; traumatismo cerebral; calambre muscular; un trastorno convulsivo seleccionado entre epilepsia o estado epiléptico; glaucoma; complicaciones diabéticas de órganos terminales; hipoglucemia, paro cardíaco; anoxia por asfixia; o daño de la médula espinal; o para el tratamiento de por lo menos una afección en un mamífero seleccionada entre trastorno de ansiedad; trastornos del estado emocional; esquizofrenia; trastorno esquizofreniforme; trastorno esquizoafectivo; o daño cognitivo; o para el tratamiento de por lo menos un trastorno neurodegenerativo crónico en un mamífero, seleccionado entre enfermedad de Parkinson, enfermedad de Huntington, enfermedad de Alzheimer, esclerosis lateral amiotrófica, o demencia crónica; o para el tratamiento de por lo menos una afección en un mamífero, seleccionado entre enfermedades inflamatorias; fibromialgia; complicaciones del herpes zoster; prevención de la tolerancia a la analgesia opioidea; o síntomas de abstinencia de drogas adictivas; o para el tratamiento del dolor en un mamífero.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46149003P | 2003-04-09 | 2003-04-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR044013A1 true AR044013A1 (es) | 2005-08-24 |
Family
ID=33299828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101199A AR044013A1 (es) | 2003-04-09 | 2004-04-07 | Derivados de acido [2-(8,9-dioxo-2,6-diazabiciclo [5.2.0.] non-1 (7)-en-2-il)alquil]fosfonico, metodos para su uso, composicion y procedimiento de preparacion |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US7253153B2 (es) |
| EP (1) | EP1611144B1 (es) |
| JP (1) | JP4621659B2 (es) |
| CN (1) | CN1863810B (es) |
| AR (1) | AR044013A1 (es) |
| AT (1) | ATE481103T1 (es) |
| AU (1) | AU2004230895B2 (es) |
| BR (1) | BRPI0409255A (es) |
| CA (1) | CA2521313A1 (es) |
| CL (1) | CL2004000769A1 (es) |
| CY (1) | CY1110863T1 (es) |
| DE (1) | DE602004029146D1 (es) |
| DK (1) | DK1611144T3 (es) |
| ES (1) | ES2350449T3 (es) |
| MX (1) | MXPA05010760A (es) |
| PL (1) | PL1611144T3 (es) |
| PT (1) | PT1611144E (es) |
| TW (1) | TWI349674B (es) |
| WO (1) | WO2004092189A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7687080B2 (en) | 2002-11-25 | 2010-03-30 | Taraxos Inc. | Treatment of neuropathy |
| US7732162B2 (en) | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
| TW200514775A (en) * | 2003-10-22 | 2005-05-01 | Wyeth Corp | Methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl} phosphonic acid and esters thereof |
| JP2008515904A (ja) * | 2004-10-08 | 2008-05-15 | ワイス | ［２−（８，９−ジオキソ−２，６−ジアザビシクロ［５．２．０］ノン−１（７）−エン−２−イル）アルキル］ホスホン酸の誘導体およびその製造方法 |
| WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
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| DK2545047T3 (da) | 2010-03-10 | 2014-07-28 | Probiodrug Ag | Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5) |
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| DK124393D0 (da) | 1993-11-03 | 1993-11-03 | Lundbeck & Co As H | Compounds |
| TW427904B (en) | 1995-12-07 | 2001-04-01 | American Home Prod | Neuroprotective agents |
| UA52698C2 (uk) | 1996-10-04 | 2003-01-15 | Х. Луннбек А/С | Похідні (3-алкоксіізоксазол-4-іл)заміщеної 2-амінокарбонової кислоти та їх сірковмісні аналоги, фармацевтична композиція на їх основі |
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-
2004
- 2004-04-07 PL PL04759168T patent/PL1611144T3/pl unknown
- 2004-04-07 MX MXPA05010760A patent/MXPA05010760A/es active IP Right Grant
- 2004-04-07 EP EP04759168A patent/EP1611144B1/en not_active Expired - Lifetime
- 2004-04-07 BR BRPI0409255-4A patent/BRPI0409255A/pt not_active IP Right Cessation
- 2004-04-07 PT PT04759168T patent/PT1611144E/pt unknown
- 2004-04-07 ES ES04759168T patent/ES2350449T3/es not_active Expired - Lifetime
- 2004-04-07 CN CN200480009542XA patent/CN1863810B/zh not_active Expired - Fee Related
- 2004-04-07 AU AU2004230895A patent/AU2004230895B2/en not_active Ceased
- 2004-04-07 AR ARP040101199A patent/AR044013A1/es not_active Application Discontinuation
- 2004-04-07 CA CA002521313A patent/CA2521313A1/en not_active Abandoned
- 2004-04-07 WO PCT/US2004/010596 patent/WO2004092189A1/en active Application Filing
- 2004-04-07 US US10/820,216 patent/US7253153B2/en not_active Expired - Fee Related
- 2004-04-07 AT AT04759168T patent/ATE481103T1/de active
- 2004-04-07 DK DK04759168.0T patent/DK1611144T3/da active
- 2004-04-07 DE DE602004029146T patent/DE602004029146D1/de not_active Expired - Lifetime
- 2004-04-07 JP JP2006509747A patent/JP4621659B2/ja not_active Expired - Fee Related
- 2004-04-08 CL CL200400769A patent/CL2004000769A1/es unknown
- 2004-04-08 TW TW093109670A patent/TWI349674B/zh not_active IP Right Cessation
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2007
- 2007-06-01 US US11/757,006 patent/US7879825B2/en not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| CN1863810B (zh) | 2010-12-01 |
| TWI349674B (en) | 2011-10-01 |
| DK1611144T3 (da) | 2010-11-22 |
| JP4621659B2 (ja) | 2011-01-26 |
| CN1863810A (zh) | 2006-11-15 |
| US20070225257A1 (en) | 2007-09-27 |
| DE602004029146D1 (de) | 2010-10-28 |
| EP1611144A1 (en) | 2006-01-04 |
| AU2004230895B2 (en) | 2010-09-09 |
| TW200504085A (en) | 2005-02-01 |
| PT1611144E (pt) | 2010-11-12 |
| ATE481103T1 (de) | 2010-10-15 |
| EP1611144B1 (en) | 2010-09-15 |
| CA2521313A1 (en) | 2004-10-28 |
| CL2004000769A1 (es) | 2005-02-04 |
| US7879825B2 (en) | 2011-02-01 |
| JP2006523694A (ja) | 2006-10-19 |
| BRPI0409255A (pt) | 2006-03-28 |
| US7253153B2 (en) | 2007-08-07 |
| CY1110863T1 (el) | 2015-06-10 |
| WO2004092189A1 (en) | 2004-10-28 |
| ES2350449T3 (es) | 2011-01-24 |
| MXPA05010760A (es) | 2005-12-12 |
| AU2004230895A1 (en) | 2004-10-28 |
| PL1611144T3 (pl) | 2011-03-31 |
| US20050004080A1 (en) | 2005-01-06 |
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