CN101595098B - 作为σ受体抑制剂的1,2,4-三唑衍生物 - Google Patents

作为σ受体抑制剂的1,2,4-三唑衍生物 Download PDF

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Publication number
CN101595098B
CN101595098B CN2007800418720A CN200780041872A CN101595098B CN 101595098 B CN101595098 B CN 101595098B CN 2007800418720 A CN2007800418720 A CN 2007800418720A CN 200780041872 A CN200780041872 A CN 200780041872A CN 101595098 B CN101595098 B CN 101595098B
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China
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methyl
triazol
dichlorophenyl
ethyl
alkyl
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Expired - Fee Related
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CN2007800418720A
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Chinese (zh)
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CN101595098A (zh
Inventor
纳丁·贾戈洛维克
约瑟·玛利亚·库米拉-蒙坦彻兹
玛利亚·皮拉尔·戈雅-拉扎
埃尔伯特·多达尔卓尔拉斯
玛莉亚·罗萨·库韦莱斯-阿尔蒂森特
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Esteve Pharmaceuticals SA
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Laboratorios del Dr Esteve SA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2007800418720A 2006-11-10 2007-11-07 作为σ受体抑制剂的1,2,4-三唑衍生物 Expired - Fee Related CN101595098B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP06380291A EP1921073A1 (en) 2006-11-10 2006-11-10 1,2,4-Triazole derivatives as sigma receptor inhibitors
EP06380291.2 2006-11-10
PCT/EP2007/062006 WO2008055932A1 (en) 2006-11-10 2007-11-07 1,2,4-triazole derivatives as sigma receptor inhibitors

Publications (2)

Publication Number Publication Date
CN101595098A CN101595098A (zh) 2009-12-02
CN101595098B true CN101595098B (zh) 2012-07-18

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CN2007800418720A Expired - Fee Related CN101595098B (zh) 2006-11-10 2007-11-07 作为σ受体抑制剂的1,2,4-三唑衍生物

Country Status (13)

Country Link
US (2) US8039497B2 (enExample)
EP (2) EP1921073A1 (enExample)
JP (1) JP2010509280A (enExample)
KR (1) KR20090087031A (enExample)
CN (1) CN101595098B (enExample)
AU (1) AU2007316605B2 (enExample)
BR (1) BRPI0718587A2 (enExample)
CA (1) CA2668994A1 (enExample)
ES (1) ES2453497T3 (enExample)
MX (1) MX2009004746A (enExample)
NZ (1) NZ577557A (enExample)
RU (1) RU2451015C2 (enExample)
WO (1) WO2008055932A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0507602D0 (en) * 2005-04-14 2005-05-18 Glaxo Group Ltd Compounds
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
US20100273805A1 (en) * 2009-04-23 2010-10-28 Astrazeneca Ab Sulphide bridged derivatives as modulators of mglur5 733
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP2015529254A (ja) * 2012-09-21 2015-10-05 ユーダブリューエム・リサーチ・ファウンデーション，インコーポレーテッド 喘息における気道の過敏症及び炎症を制御するための新規なｇａｂａａアゴニスト及び使用方法
EP2752411A1 (en) 2013-01-07 2014-07-09 Laboratorios Del Dr. Esteve, S.A. 1,2,3-triazole-4-amine derivatives for the treatment of sigma receptor related diseases and disorders
MX2015014905A (es) 2013-04-23 2016-03-07 Esteve Labor Dr Compuestos de pirazino - [1,2-a] indol, su preparacion y su uso en medicamentos.
TN2015000474A1 (en) 2013-04-23 2017-04-06 Esteve Labor Dr PYRAZINO[1,2-a]INDOLE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS
EP2832720A1 (en) 2013-07-30 2015-02-04 Laboratorios Del. Dr. Esteve, S.A. 1,2-disubstituted cyclobutyl compounds
TW201607538A (zh) 2013-12-17 2016-03-01 以斯提夫博士實驗室股份有限公司 血清素－去甲腎上腺素再攝取抑制劑（ＳＮＲＩＳ）和σ受體配體組合物
MA41177A (fr) * 2014-12-15 2017-10-24 Esteve Labor Dr Utilisation de ligands des récepteurs sigma dans l'arthrose
CN107406420B (zh) 2015-01-30 2020-11-06 纽罗克里生物科学有限公司 取代的三唑及与其相关的方法
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
JP7258902B2 (ja) * 2017-11-14 2023-04-17 エスケー バイオファーマスティカルズ カンパニー リミテッド 脆弱ｘ症候群、アンジェルマン症候群又はレット症候群を含む発達障害の軽減又は治療のためのカルバメート化合物の使用
KR102900177B1 (ko) * 2017-11-14 2025-12-16 에스케이바이오팜 주식회사 내장통 또는 내장 질환에서 기인한 통증을 예방, 경감 또는 치료하기 위한 카바메이트 화합물의 용도
WO2019098634A1 (ko) 2017-11-14 2019-05-23 에스케이바이오팜 주식회사 카바메이트 화합물을 포함하는 조현병의 예방, 경감 또는 치료용 배합물
US11389429B2 (en) 2017-11-14 2022-07-19 Sk Biopharmaceuticals Co., Ltd. Use of carbamate compound for preventing, alleviating or treating myotonia
EP3893892A4 (en) * 2018-12-12 2022-09-14 Rutgers, the State University of New Jersey ORGANIC COMPOUNDS

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WO2002036119A1 (en) * 2000-11-02 2002-05-10 K And K Biosciences, Inc. Δ2,-1,2,3-triazoline anticonvulsants and their active metabolite analogues, the aminoalkylpyridines, are excitatory amino acid antagonists and antiischemic agents, useful in the treatment of cerebral ischemia resulting from stroke

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DE1547640A1 (de) * 1967-04-10 1969-12-04 Agfa Gevaert Ag Verbessertes photographisches Material
AU658134B2 (en) 1989-12-28 1995-04-06 Virginia Commonwealth University Sigma receptor ligands and the use thereof
US6797722B2 (en) 2002-05-03 2004-09-28 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Use of 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole for the treatment of autoimmune diseases
SE0301232D0 (sv) 2003-04-25 2003-04-25 Astrazeneca Ab Novel use
JP2007509045A (ja) 2003-10-18 2007-04-12 バイエル・ヘルスケア・アクチェンゲゼルシャフト 尿失禁および関連疾患の処置用のｇａｂａアゴニストとしての５−置換２−（フェニルメチル）チオ−４−フェニル−４ｈ−１，２，４−トリアゾール誘導体および関連化合物
CA2543338A1 (en) 2003-10-24 2005-05-06 Solvay Pharmaceuticals Gmbh Novel medical uses of compounds showing cb1-antagonistic activity and combination treatment involving said compounds
DE102005007304A1 (de) * 2005-02-17 2006-08-24 Merck Patent Gmbh Triazolderivate
GB0504556D0 (en) 2005-03-04 2005-04-13 Pfizer Ltd Novel pharmaceuticals

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2002036119A1 (en) * 2000-11-02 2002-05-10 K And K Biosciences, Inc. Δ2,-1,2,3-triazoline anticonvulsants and their active metabolite analogues, the aminoalkylpyridines, are excitatory amino acid antagonists and antiischemic agents, useful in the treatment of cerebral ischemia resulting from stroke
US6638954B2 (en) * 2000-11-02 2003-10-28 K And K Biosciences, Inc. Δ2-1,2,3-triazoline anticonvulsants and their active metabolite analogues, the aminoalkylpyridines, are excitatory amino acid antagonists and antiischemic agents, useful in the treatment of cerebral ischemia resulting from stroke

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Publication number Publication date
JP2010509280A (ja) 2010-03-25
WO2008055932A1 (en) 2008-05-15
RU2451015C2 (ru) 2012-05-20
AU2007316605B2 (en) 2012-02-09
US8349878B2 (en) 2013-01-08
US8039497B2 (en) 2011-10-18
RU2009122197A (ru) 2010-12-20
BRPI0718587A2 (pt) 2014-03-11
CN101595098A (zh) 2009-12-02
CA2668994A1 (en) 2008-05-15
EP1921073A1 (en) 2008-05-14
US20100004224A1 (en) 2010-01-07
EP2097394B1 (en) 2013-12-25
KR20090087031A (ko) 2009-08-14
NZ577557A (en) 2011-12-22
MX2009004746A (es) 2009-05-22
EP2097394A1 (en) 2009-09-09
AU2007316605A1 (en) 2008-05-15
US20120004211A1 (en) 2012-01-05
ES2453497T3 (es) 2014-04-08

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