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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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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (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 (cg-RX-API-DMAC7.html)
EP (2) EP1921073A1 (cg-RX-API-DMAC7.html)
JP (1) JP2010509280A (cg-RX-API-DMAC7.html)
KR (1) KR20090087031A (cg-RX-API-DMAC7.html)
CN (1) CN101595098B (cg-RX-API-DMAC7.html)
AU (1) AU2007316605B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0718587A2 (cg-RX-API-DMAC7.html)
CA (1) CA2668994A1 (cg-RX-API-DMAC7.html)
ES (1) ES2453497T3 (cg-RX-API-DMAC7.html)
MX (1) MX2009004746A (cg-RX-API-DMAC7.html)
NZ (1) NZ577557A (cg-RX-API-DMAC7.html)
RU (1) RU2451015C2 (cg-RX-API-DMAC7.html)
WO (1) WO2008055932A1 (cg-RX-API-DMAC7.html)

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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
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
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
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
CA2885148A1 (en) * 2012-09-21 2014-03-27 Uwm Research Foundation, Inc. Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma
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
CN105339369B (zh) 2013-04-23 2017-12-22 埃斯蒂维实验室股份有限公司 一种吡嗪并[1,2‑a]吲哚化合物及其制备方法和在药物中的应用
WO2014173901A1 (en) 2013-04-23 2014-10-30 Laboratorios Del Dr. Esteve, S.A. 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
JP2016540771A (ja) 2013-12-17 2016-12-28 ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ セロトニン−ノルアドレナリン再取り込み阻害薬（ｓｎｒｉ）およびシグマ受容体リガンドの組み合わせ
MA41177A (fr) * 2014-12-15 2017-10-24 Esteve Labor Dr Utilisation de ligands des récepteurs sigma dans l'arthrose
JP6728198B2 (ja) 2015-01-30 2020-07-22 ニューロクライン バイオサイエンシーズ，インコーポレイテッド 置換トリアゾールおよびそれに関する方法
AU2016270373A1 (en) * 2015-06-05 2018-01-04 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
US11666554B2 (en) 2017-11-14 2023-06-06 Sk Biopharmaceuticals Co., Ltd. Use of a carbamate compound to prevent, alleviate or treat visceralgia or pain arising from visceral disease
WO2019098632A1 (ko) * 2017-11-14 2019-05-23 에스케이바이오팜 주식회사 근긴장증의 예방, 경감 또는 치료를 위한 카바메이트 화합물의 용도
EP3711761A4 (en) * 2017-11-14 2021-11-24 SK Biopharmaceuticals Co., Ltd. USE OF A CARBAMATE COMPOUND TO REDUCE OR TREAT DEVELOPMENTAL DISORDERS, INCLUDING FRAGILE X SYNDROME, ANGELMAN'S SYNDROME, OR RETT'S SYNDROME
JP7355747B2 (ja) * 2017-11-14 2023-10-03 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 カルバメート化合物を含む統合失調症の予防、軽減又は治療用配合物
EP3893892A4 (en) * 2018-12-12 2022-09-14 Rutgers, the State University of New Jersey Organic compounds

Citations (1)

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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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CA2071897A1 (en) 1989-12-28 1991-06-29 Richard A. Glennon 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
JP2007513872A (ja) 2003-10-24 2007-05-31 ゾルファイ　ファーマスーティカルズ　ゲゼルシャフト　ミット　ベシュレンクテル　ハフツング Ｃｂ１拮抗作用を示す化合物の新規の医学的用途および前記化合物を伴う組み合わせ治療
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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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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BRPI0718587A2 (pt) 2014-03-11
NZ577557A (en) 2011-12-22
MX2009004746A (es) 2009-05-22
CN101595098A (zh) 2009-12-02
US20100004224A1 (en) 2010-01-07
EP2097394A1 (en) 2009-09-09
CA2668994A1 (en) 2008-05-15
RU2009122197A (ru) 2010-12-20
US8039497B2 (en) 2011-10-18
RU2451015C2 (ru) 2012-05-20
AU2007316605B2 (en) 2012-02-09
KR20090087031A (ko) 2009-08-14
AU2007316605A1 (en) 2008-05-15
WO2008055932A1 (en) 2008-05-15
EP1921073A1 (en) 2008-05-14
US8349878B2 (en) 2013-01-08
JP2010509280A (ja) 2010-03-25
ES2453497T3 (es) 2014-04-08
EP2097394B1 (en) 2013-12-25
US20120004211A1 (en) 2012-01-05

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