PE20050245A1 - Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidos - Google Patents

Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidos

Info

Publication number
PE20050245A1
PE20050245A1 PE2004000552A PE2004000552A PE20050245A1 PE 20050245 A1 PE20050245 A1 PE 20050245A1 PE 2004000552 A PE2004000552 A PE 2004000552A PE 2004000552 A PE2004000552 A PE 2004000552A PE 20050245 A1 PE20050245 A1 PE 20050245A1
Authority
PE
Peru
Prior art keywords
aril
pyrimidin
fluoro
methyl
nonaryl
Prior art date
Application number
PE2004000552A
Other languages
English (en)
Inventor
Nigel J Liverton
David A Claremon
John A Mccauley
Christopher F Claiborne
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33511734&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20050245(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20050245A1 publication Critical patent/PE20050245A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Addiction (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
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Abstract

REFERIDA A UN COMPUESTO DE FORMULA I DONDE HetAr ES UN ANILLO HETEROAROMATICO CON 1-2 ATOMOS DE N EN EL ANILLO, TIAZOLILO, TIADIAZOLILO; HetAr ESTA OPCIONALMENTE TIENE 1-2 SUSTITUYENTES TALES COMO ALQUILC1-C4, FLUORO, CLORO; BROMO, YODO; A ES UN ENLACE O ALQUIL-C1-C2; B ES ARIL(CH2)0-3-O-C(O)-, ARIL(CH2)1-3-C(O)-, ARIL-CICLOPROPIL-C(O)-, ENTRE OTROS. TAMBIEN REFERIDA A UNA COMPOSICION FARMACEUTICA QUE CONTIENE DICHO COMPUESTO CUYOS PREFERIDOS SON: (3R,4S)3-FLUORO-4-[(PIRIMIDIN-2-ILAMINO)METIL]PIPERIDINA-1-CARBOXILATO DE 4-METILBENCILO; 3-FLUORO-4-[(PIRIMIDIN-2-ILAMINO)METIL]PIPERIDINA-1-CARBOXILATO DE (-)-TRANS-4-METILBENCILO Y (3R,4S)-N-[(3-CIS-FLUORO-1-{[(1R,2R)-2-FENILCICLOPROPIL]CARBONIL}PIPERIDIN-4-IL)METIL]PIRIMIDIN-2-AMINA; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE PARKINSON, DE DOLORES CRONICOS, VISCERALES, INFLAMATORIOS Y NEUROPATICOS, ENTRE OTROS
PE2004000552A 2003-06-04 2004-06-01 Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidos PE20050245A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US47593803P 2003-06-04 2003-06-04

Publications (1)

Publication Number Publication Date
PE20050245A1 true PE20050245A1 (es) 2005-04-13

Family

ID=33511734

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000552A PE20050245A1 (es) 2003-06-04 2004-06-01 Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidos

Country Status (30)

Country Link
EP (1) EP1648882B1 (es)
JP (1) JP3927228B2 (es)
KR (1) KR20060017839A (es)
CN (1) CN1798744A (es)
AR (1) AR044579A1 (es)
AT (1) ATE403651T1 (es)
AU (1) AU2004245522B2 (es)
BR (1) BRPI0410837A (es)
CA (1) CA2527093C (es)
CL (1) CL2004001365A1 (es)
CO (1) CO5700762A2 (es)
DE (1) DE602004015610D1 (es)
DK (1) DK1648882T3 (es)
EC (1) ECSP056192A (es)
ES (1) ES2309540T3 (es)
HR (1) HRP20080490T3 (es)
IS (1) IS8117A (es)
MA (1) MA27781A1 (es)
MX (1) MXPA05013151A (es)
MY (1) MY138547A (es)
NO (1) NO20060020L (es)
PE (1) PE20050245A1 (es)
PL (1) PL1648882T3 (es)
PT (1) PT1648882E (es)
RU (1) RU2339630C2 (es)
SI (1) SI1648882T1 (es)
TW (1) TW200510378A (es)
UA (1) UA81319C2 (es)
WO (1) WO2004108705A1 (es)
ZA (1) ZA200509000B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009535364A (ja) * 2006-05-03 2009-10-01 シーエヌエスバイオ ピーティーワイ リミテッド 炎症性疼痛の治療のための方法および組成物
KR101506156B1 (ko) * 2007-04-23 2015-03-26 얀센 파마슈티카 엔.브이. 속해리성 도파민 2 수용체 길항제로서의 티아(디아)졸
WO2009000038A1 (en) * 2007-06-28 2008-12-31 Cnsbio Pty Ltd Combination methods and compositions for treatment of neuropathic pain
CN102762554A (zh) 2010-02-16 2012-10-31 辉瑞大药厂 5-ht4受体的部分激动剂(r)-4-((4-((4-(四氢呋喃-3-基氧基)苯并[d]异*唑-3-基氧基)甲基)哌啶-1-基)甲基)四氢-2h-吡喃-4-醇
JP6042968B2 (ja) 2012-04-20 2016-12-14 ユセベ ファルマ ソシエテ アノニム パーキンソン病の処置方法
CN103936663B (zh) * 2013-01-23 2016-12-28 艾琪康医药科技(上海)有限公司 一种1-r1-3,3-二氟(或3-氟)-4-r2-4-氨甲基哌啶及其衍生物的制备方法
US9187506B2 (en) 2014-01-09 2015-11-17 Bristol-Myers Squibb Company (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders
US9221796B2 (en) 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists
US10030026B2 (en) 2014-06-04 2018-07-24 Rugen Holdings (Cayman) Limited Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists
CN106715435B (zh) 2014-09-15 2019-10-01 卢郡控股(开曼)有限公司 作为nr2b nmda受体拮抗剂的吡咯并嘧啶衍生物
WO2016049048A1 (en) * 2014-09-22 2016-03-31 Rugen Holdings (Cayman) Limited Treatment of anxiety disorders and autism spectrum disorders
BR112017013593A2 (pt) * 2014-12-23 2018-06-19 Cerecor, Inc. compostos, composições e métodos
US10221182B2 (en) 2015-02-04 2019-03-05 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists
JP6876625B2 (ja) 2015-06-01 2021-05-26 リューゲン ホールディングス (ケイマン) リミテッド Nr2bnmdaレセプターアンタゴニストとしての3,3−ジフルオロピペリジンカルバメート複素環式化合物
WO2017066368A1 (en) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Selective nr2b antagonists
CN108137543B (zh) 2015-10-14 2021-11-23 百时美施贵宝公司 选择性nr2b拮抗剂
AU2017319080B2 (en) 2016-08-31 2020-12-17 Eisai R&D Management Co., Ltd. Pyrazolo[1,5-a]pyrimidine compound
EP3544610A1 (en) 2016-11-22 2019-10-02 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1379520T1 (sl) * 2001-02-23 2006-08-31 Merck & Co Inc N-substituirani nonaril-heterociklicni NMDA/NR2B antagonisti

Also Published As

Publication number Publication date
WO2004108705A1 (en) 2004-12-16
ES2309540T3 (es) 2008-12-16
MXPA05013151A (es) 2006-03-17
RU2339630C2 (ru) 2008-11-27
JP2006526650A (ja) 2006-11-24
MY138547A (en) 2009-06-30
AU2004245522A1 (en) 2004-12-16
HRP20080490T3 (en) 2008-11-30
AU2004245522B2 (en) 2009-10-29
SI1648882T1 (sl) 2009-02-28
ATE403651T1 (de) 2008-08-15
CN1798744A (zh) 2006-07-05
CL2004001365A1 (es) 2005-05-06
PL1648882T3 (pl) 2008-12-31
DK1648882T3 (da) 2008-11-24
CA2527093A1 (en) 2004-12-16
IS8117A (is) 2005-11-07
BRPI0410837A (pt) 2006-06-27
CA2527093C (en) 2009-10-20
UA81319C2 (en) 2007-12-25
RU2005137704A (ru) 2006-05-27
KR20060017839A (ko) 2006-02-27
DE602004015610D1 (de) 2008-09-18
NO20060020L (no) 2006-03-03
CO5700762A2 (es) 2006-11-30
ZA200509000B (en) 2006-12-27
JP3927228B2 (ja) 2007-06-06
ECSP056192A (es) 2006-04-19
AR044579A1 (es) 2005-09-21
MA27781A1 (fr) 2006-02-01
PT1648882E (pt) 2008-10-20
EP1648882A1 (en) 2006-04-26
EP1648882B1 (en) 2008-08-06
TW200510378A (en) 2005-03-16

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