ZA200501332B - Vanilloid receptor ligands and their use in treatments - Google Patents

Vanilloid receptor ligands and their use in treatments Download PDF

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Publication number
ZA200501332B
ZA200501332B ZA200501332A ZA200501332A ZA200501332B ZA 200501332 B ZA200501332 B ZA 200501332B ZA 200501332 A ZA200501332 A ZA 200501332A ZA 200501332 A ZA200501332 A ZA 200501332A ZA 200501332 B ZA200501332 B ZA 200501332B
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ZA
South Africa
Prior art keywords
pyrimidin
phenyl
trifluoromethyl
oxy
dihydro
Prior art date
Application number
ZA200501332A
Other languages
English (en)
Inventor
Partha P Chakrabarti
Chen Ning
Elizabeth M Doherty
Dominguez Celia
Falsey James Richard
Christopher H Fotsch
Hulme Christopher
Katon Jodie
Nixey Thomas
Mark H Norman
Vassil I Ognyanov
Liping H Pettus
Rzasa Robert Michael
Stec Markian
Wang Hui-Ling
Zhu Jiawang
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Amgen Inc
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Application filed by Amgen Inc filed Critical Amgen Inc
Publication of ZA200501332B publication Critical patent/ZA200501332B/en

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Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7351719B2 (en) * 2002-10-31 2008-04-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds
CA2512899A1 (fr) 2003-01-14 2004-08-05 Arena Pharmaceuticals Inc. Derives aryles et heteroaryles tri-substitues en position 1,2,3 en tant que modulateurs de metabolisme et prophylaxie et traitement de troubles lies au metabolisme
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
EP2287166A3 (fr) 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Dérivés d'hétéroaryle et aryle fusionné en tant que modulateurs du métabolisme et prophylaxie et traitement des troubles associés
US7390907B2 (en) 2003-09-30 2008-06-24 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7592373B2 (en) * 2003-12-23 2009-09-22 Boehringer Ingelheim International Gmbh Amide compounds with MCH antagonistic activity and medicaments comprising these compounds
MY139645A (en) * 2004-02-11 2009-10-30 Amgen Inc Vanilloid receptor ligands and their use in treatments
EP1745034A1 (fr) * 2004-02-11 2007-01-24 Amgen Inc. Ligands du recepteur vanilloide et leurs applications dans des traitements
EP1775283A4 (fr) * 2004-07-14 2008-12-10 Japan Tobacco Inc Compose 3-aminobenamide et inhibiteur d'activite a recepteur vanilloide 1 (vr1)
KR101042490B1 (ko) * 2004-07-15 2011-06-16 니뽄 다바코 산교 가부시키가이샤 축합 벤즈아미드 화합물 및 바닐로이드 수용체 1형(ｖｒ1)활성 저해제
CN101090724A (zh) * 2004-09-20 2007-12-19 泽农医药公司 用于抑制人硬脂酰CoA去饱和酶的吡啶衍生物
CN101084207A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
CA2580857A1 (fr) 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Derives heterocycliques et leur utilisation en tant qu'agents therapeutiques
WO2006034474A2 (fr) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Composes a base de pyridine, leur procede de preparation et compositions les contenant
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
KR20060087386A (ko) 2005-01-28 2006-08-02 주식회사 대웅제약 신규 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물
US7301022B2 (en) 2005-02-15 2007-11-27 Amgen Inc. Vanilloid receptor ligands and their use in treatments
CA2606288A1 (fr) * 2005-04-18 2006-10-26 Neurogen Corporation Antagonistes cb1 heteroaryle substitue
MX2007013931A (es) * 2005-05-12 2008-01-11 Amgen Inc Agentes antipireticos contra incrementos en la temperatura corporal inducidos por antagonista del receptor vainilloide 1.
AU2006343359A1 (en) 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
US20090181991A1 (en) * 2005-11-03 2009-07-16 Irm Llc Compounds and compositions as protein kinase inhibitors
US7709501B2 (en) * 2005-12-23 2010-05-04 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7906508B2 (en) * 2005-12-28 2011-03-15 Japan Tobacco Inc. 3,4-dihydrobenzoxazine compounds and inhibitors of vanilloid receptor subtype 1 (VRI) activity
DE102006008880A1 (de) * 2006-02-27 2007-09-06 Merck Patent Gmbh Aminopyrimidinderivate
MX2008013427A (es) * 2006-04-19 2008-11-04 Novartis Ag Compuestos de benzoxazole y benzotiazole sustituidos-6-0 y metodos para inhibir la señalizacion csf-1r.
US20080051453A1 (en) * 2006-08-22 2008-02-28 Annette Bak Sorbic acid analog co-crystals
BRPI0721169A2 (pt) 2006-12-15 2014-03-18 Janssen Pharmaceutica Nv Inibidores de benzimidazol trpv1
CN101925575B (zh) 2008-01-28 2014-06-18 株式会社爱茉莉太平洋 作为香草酸受体拮抗剂的化合物、其异构体或其药物学可接受的盐、及包含这些化合物的药物组合物
CN101983197B (zh) 2008-04-18 2015-04-22 大熊制药株式会社 新型苯并噁嗪苯并咪唑衍生物、含有该衍生物的药物组合物及其用途
KR101449785B1 (ko) 2008-04-21 2014-10-14 오토노미, 인코포레이티드 귀 질환 및 병태를 치료하기 위한 귀 조제물
US11969501B2 (en) 2008-04-21 2024-04-30 Dompé Farmaceutici S.P.A. Auris formulations for treating otic diseases and conditions
CN102137851B (zh) 2008-07-02 2014-08-27 株式会社爱茉莉太平洋 作为香草素受体拮抗剂的化合物、其异构体或其药学可接受的盐以及包含它们的药物组合物
CA2731769C (fr) 2008-07-21 2013-09-10 Otonomy, Inc. Compositions a liberation controlee modulant la structure otique et modulant le systeme immunitaire naturel et procedes de traitement de troubles otiques
TW201008933A (en) * 2008-08-29 2010-03-01 Hutchison Medipharma Entpr Ltd Pyrimidine compounds
CA2744935A1 (fr) * 2008-12-19 2010-06-24 Boehringer Ingelheim International Gmbh Nouveaux composes
AU2010206161B2 (en) 2009-01-21 2014-08-07 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
WO2011103091A1 (fr) * 2010-02-18 2011-08-25 Transtech Pharma, Inc. Dérivés de phényl-hétéroaryle et procédés d'utilisation de ceux-ci
CN103539791B (zh) 2010-09-22 2017-01-11 艾尼纳制药公司 Gpr119 受体调节剂和对与其相关的障碍的治疗
KR101293384B1 (ko) 2010-10-13 2013-08-05 주식회사 대웅제약 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도
CN102020647B (zh) * 2010-11-18 2013-09-11 孙智华 1-(2,2-二氟乙氧基)-6-三氟甲基-n-([1,2,4]三氮唑[1,5-c]嘧啶-2-)苯磺酰胺的制备方法
ITMI20110362A1 (it) * 2011-03-09 2012-09-10 F I S Fabbrica Italiana Sint P A Procedimento per la preparazione di 1-(6-metilpiridin-3-il)-2-[4-(metilsolfonil)fenil]etanone, un intermedio dell'etoricoxib.
US9822108B2 (en) 2012-01-13 2017-11-21 Rutgers, The State University Of New Jersey Antimicrobial agents
ITMI20120394A1 (it) * 2012-03-14 2013-09-15 Zach System Spa Processo di sintesi di un chetosolfone derivato
WO2013175415A1 (fr) * 2012-05-23 2013-11-28 Piramal Enterprises Limited Composés de pyrimidine substituée et leurs utilisations
CA3002540C (fr) 2015-01-06 2023-11-07 Arena Pharmaceuticals, Inc. Utilisation de (r)-2-(7-(4-cyclopentyl-3(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acide acetique pour le traitement de conditions liees au recepteur s1p1
KR20170122782A (ko) * 2015-02-27 2017-11-06 난트바이오사이언스 인코포레이티드 키나아제 억제제로서의 피리미딘 유도체 및 그 치료적 용도
WO2016209809A1 (fr) 2015-06-22 2016-12-29 Arena Pharmaceuticals, Inc. Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
US11571564B2 (en) 2016-06-02 2023-02-07 Battelle Memorial Institute Flexible sheet for neuromuscular stimulation
CN109689027A (zh) 2016-06-29 2019-04-26 奥德纳米有限公司 甘油三酯耳用制剂及其用途
WO2018101793A2 (fr) * 2016-12-01 2018-06-07 서울대학교 산학협력단 Composé dérivé d'amide, stéréo-isomère de celui-ci, ou sel pharmaceutiquement acceptable de celui-ci, et composition pharmaceutique ou cosmétique comprenant celui-ci permettant de supprimer le vieillissement de la peau, d'atténuer les rides, ou de cicatriser les plaies cutanées
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
KR102039608B1 (ko) 2017-11-03 2019-11-01 주식회사 셀버틱스 미도드린을 포함하는 조성물 및 이의 용도
ES2987794T3 (es) 2018-06-06 2024-11-18 Arena Pharm Inc Procedimientos de tratamiento de afecciones relacionadas con el receptor S1P1
AU2022405116A1 (en) 2021-12-09 2024-07-11 Deciphera Pharmaceuticals, Llc Raf kinase inhibitors and methods of use thereof
DE102022104759A1 (de) 2022-02-28 2023-08-31 SCi Kontor GmbH Co-Kristall-Screening Verfahren, insbesondere zur Herstellung von Co-Kristallen
CN120092008A (zh) * 2022-10-20 2025-06-03 上海瑛派药业有限公司 取代的杂芳基双环化合物作为usp1抑制剂及其应用

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3940395A (en) * 1969-08-29 1976-02-24 American Home Products Corporation 4-Amino-2-phenyl-6-thiopryimidines
JPS54115384A (en) * 1978-02-28 1979-09-07 Hokko Chem Ind Co Ltd Ryrazolyl pyrimidine derivative, and agricultural and horticultural fungicides
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US4725600A (en) * 1984-07-13 1988-02-16 Fujisawa Pharmaceutical Co., Ltd. Pyrimidine compounds having activity as a cardiotonic anti-hypertensive cerebrovascular vasodilator and anti-platelet aggregation agent
GB8417852D0 (en) * 1984-07-13 1984-08-15 Fujisawa Pharmaceutical Co Pyrimidine derivatives
US5750532A (en) 1986-12-10 1998-05-12 Schering Corporation Pharmaceutically active compounds
US5272167A (en) 1986-12-10 1993-12-21 Schering Corporation Pharmaceutically active compounds
KR930702312A (ko) 1990-08-31 1993-09-08 아만 히데아키 피리미딘 유도체 및 의약
IL118469A (en) 1995-06-15 2000-08-13 Tanabe Seiyaku Co Naphthalene derivatives their preparation and intermediates thereof
HUP9901228A3 (en) * 1995-06-20 2001-11-28 Du Pont Cyclic amides, their intermediates, arthropodicide and fungicide compositions containing theses compounds as active ingredients and use thereof
ES2100129B1 (es) 1995-10-11 1998-02-16 Medichem Sa Nuevos compuestos aminopiridinicos policiclicos inhibidores de acetilcolinesterasa, procedimiento para su preparacion y su utilizacion.
YU48398A (sh) 1996-05-01 2000-12-28 Eli Lily And Company Inhibitori halo-supstituisane protein kinaze c
DE69711926D1 (de) 1996-09-23 2002-05-16 Naeja Pharmaceutical Inc 3,4-disubstituierte azetidin-2-on-derivate die als cystein-proteinase regulatoren nuetzlich sind
US5916887A (en) 1996-09-23 1999-06-29 National Research Council Of Canada 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives as cysteine proteinase regulators
CZ184599A3 (cs) * 1996-11-26 1999-09-15 E. I. Du Pont De Nemours And Company Methylem substituované fungicidy a artropodicidy
WO1998023155A1 (fr) 1996-11-26 1998-06-04 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides
US5932590A (en) 1996-12-05 1999-08-03 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU6013998A (en) 1996-12-30 1998-07-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1999009140A1 (fr) 1997-08-20 1999-02-25 The Regents Of The University Of California Sequences nucleotidiques codant pour le recepteur de la capsicine, polypeptides lies au recepteur de la capsicine et leur utilisation
HUP0004063A3 (en) 1997-09-05 2002-11-28 Basf Ag Method for producing (hetero)aromatic hydroxylamines
CA2260499A1 (fr) 1998-01-29 1999-07-29 Sumitomo Pharmaceuticals Company Limited Compositions pharmaceutiques pour le traitement de dommages ischemiques au cerveau
EP1054882A1 (fr) 1998-02-13 2000-11-29 Aventis Pharma S.A. Derives de systemes heterocycliques condenses, leur preparation, les compositions pharmaceutiques qui les contiennent
US6306866B1 (en) * 1998-03-06 2001-10-23 American Cyanamid Company Use of aryl-substituted pyrimidines as insecticidal and acaricidal agents
EP0943683A1 (fr) 1998-03-10 1999-09-22 Smithkline Beecham Plc Homologue humain du récepteur vanilloide Vanilrep1
AR014975A1 (es) 1998-04-08 2001-04-11 Nps Pharma Inc Compuestos calciliticos, una composicion farmaceutica que los comprende, y el uso de los mismos para la fabricacion de un medicamento
US6562847B1 (en) 1998-08-25 2003-05-13 Ortho-Mcneil Pharmaceutical, Inc. Pyridyl ethers and thioethers as ligands for nicotinic acetylcholine receptor and its therapeutic application
US6127376A (en) * 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
KR100514236B1 (ko) 1999-02-24 2005-09-13 에프. 호프만-라 로슈 아게 페닐 유도체 및 피리디닐 유도체
GB9907097D0 (en) 1999-03-26 1999-05-19 Novartis Ag Organic compounds
GB9907683D0 (en) 1999-04-06 1999-05-26 Synphar Lab Inc Substituted azetidin-2-ones as cysteine protease inhibitors
EP1219606A4 (fr) 1999-07-19 2005-08-31 Shionogi & Co Composes tricycliques porteurs de pendants acyloxymethoxycarbonyle
AU6016000A (en) 1999-07-23 2001-02-13 Shionogi & Co., Ltd. Tricyclic compounds and drug compositions containing the same
BR0012697A (pt) 1999-07-23 2002-04-09 Shionogi & Co Inibidores da diferenciação de th2
WO2001014331A2 (fr) 1999-08-24 2001-03-01 Regents Of The University Of California Inhibiteurs exempts de quinoline de parasites du paludisme
US20020151712A1 (en) 1999-09-14 2002-10-17 Nan-Horng Lin 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission
WO2001019817A2 (fr) 1999-09-14 2001-03-22 Abbott Laboratories Composes d'ether 3-pyrrolidinyloxy-3'-pyridyle utilises comme regulateurs de la transmission synaptique chimique
WO2001021606A1 (fr) 1999-09-21 2001-03-29 Qinetiq Limited Composes cristaux liquides
US6602872B1 (en) * 1999-12-13 2003-08-05 Merck & Co., Inc. Substituted pyridazines having cytokine inhibitory activity
HUP0202263A3 (en) * 1999-12-27 2003-02-28 Japan Tobacco Inc Benzimidazole, indole and imidazo-pyridine derivatives and pharmaceutical compositions containing them
EA200200688A1 (ru) * 2000-01-18 2003-02-27 Пфайзер Продактс Инк. Антагонисты фактора, высвобождающего кортикотропин
WO2001054503A1 (fr) 2000-01-28 2001-08-02 Akkadix Corporation Procedes de destruction des nematodes et des oeufs de nematodes a l'aide de derives 4-phenoxy-6-aminopyrimidine
GB0005789D0 (en) 2000-03-11 2000-05-03 Knoll Ag Therapeutic agents
CA2404381A1 (fr) 2000-04-04 2002-09-26 Shionogi & Co., Ltd. Compositions huileuses contenant des medicaments solubles dans des graisses
WO2001076582A1 (fr) 2000-04-05 2001-10-18 Shionogi & Co., Ltd. Micro-emulsions huile dans eau contenant des composes tricycliques ou des preconcentres de ceux-ci
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
US6664256B1 (en) * 2000-07-10 2003-12-16 Kowa Co., Ltd. Phenylpyridazine compounds and medicines containing the same
TWI259180B (en) 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
EP1313704A2 (fr) 2000-08-30 2003-05-28 Dow AgroSciences LLC Composes utiles en tant qu'insecticides, acaricides, et procedes d'utilisation et de preparation de ces derniers
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20040067938A1 (en) 2000-09-29 2004-04-08 Penglie Zhang Quaternary amines and related inhibitors of factor xa
DE60137273D1 (de) * 2000-10-20 2009-02-12 Eisai R&D Man Co Ltd Verfahren zur Herstellung von 4-Phenoxy chinolin Derivaten
SE0004053D0 (sv) 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
SE0004245D0 (sv) 2000-11-20 2000-11-20 Pharmacia Ab Novel compounds and their use
AU2002224942A1 (en) 2000-12-20 2002-07-01 Syngenta Participations Ag N-acyl aminoacetonitriles having pesticidal properties
ES2292753T4 (es) 2001-03-29 2009-02-16 Vertex Pharmaceuticals Incorporated Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas.
US6790845B2 (en) 2001-04-09 2004-09-14 Bristol-Myers Squibb Pharma Company Fused heterocyclic inhibitors of factor Xa
EP1389616B1 (fr) 2001-04-27 2011-07-27 Mitsubishi Tanabe Pharma Corporation Dérivés de 3,4-dihalobenzylpipéridine et leur utilisation médicale
JP2003212846A (ja) * 2001-06-26 2003-07-30 Japan Tobacco Inc 縮合環化合物及びｃ型肝炎治療剤
IL159811A0 (en) 2001-07-13 2004-06-20 Neurogen Corp Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands
US7105559B2 (en) 2001-10-03 2006-09-12 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
MXPA04003169A (es) 2001-10-03 2004-07-08 Pharmacia Corp Profarmacos de compuestos policiclicos sustituidos utiles para inhibicion selectiva de la cascada de coagulacion.
CA2462289C (fr) 2001-10-04 2010-02-23 Nicholas D. Cosford Composes de tetrazole substitues par heteroaryle, modulateurs du recepteur-5 metabotropique du glutamate
AU2002352663B2 (en) 2001-11-13 2007-06-21 Axys Pharmaceuticals, Inc. Cyanoalkylamino derivatives as protease inhibitors
AU2002364549B2 (en) * 2001-12-10 2007-11-22 Amgen, Inc Vanilloid receptor ligands and their use in treatments
PE20040522A1 (es) * 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
WO2004005283A1 (fr) 2002-07-09 2004-01-15 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles et thiazoles presentant des activites d'inhibition des proteines kinases
US7419984B2 (en) 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
GB0226724D0 (en) 2002-11-15 2002-12-24 Merck Sharp & Dohme Therapeutic agents
CA2512646A1 (fr) 2003-01-17 2004-08-05 Warner-Lambert Company Llc Heterocycles 2-aminopyridines substitues utilises comme inhibiteurs de la proliferation cellulaire
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors

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BR0313255A (pt) 2005-07-12
EA200500168A1 (ru) 2005-08-25
CN1694873A (zh) 2005-11-09
US7332511B2 (en) 2008-02-19
EP1546116A1 (fr) 2005-06-29
KR20050055694A (ko) 2005-06-13
IL166396A0 (en) 2006-01-15
CA2493667C (fr) 2010-04-27
AU2003264047B2 (en) 2008-06-26
US20040082780A1 (en) 2004-04-29
EP1717220A2 (fr) 2006-11-02
AU2008202517A1 (en) 2008-06-26
MXPA05001456A (es) 2005-06-06
AU2003264047A1 (en) 2004-02-25
NZ537952A (en) 2008-04-30
CA2493667A1 (fr) 2004-02-19
PL376372A1 (en) 2005-12-27
NO20051193L (no) 2005-05-04
EP2270006A1 (fr) 2011-01-05
EA010380B1 (ru) 2008-08-29
EP1717220A3 (fr) 2007-08-22
US20050277631A1 (en) 2005-12-15
US20050272777A1 (en) 2005-12-08
JP2006504670A (ja) 2006-02-09
TW200410945A (en) 2004-07-01
US7148221B2 (en) 2006-12-12
WO2004014871A1 (fr) 2004-02-19
AR041191A1 (es) 2005-05-04
US7144888B2 (en) 2006-12-05
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JP4555082B2 (ja) 2010-09-29
RS20050161A (sr) 2007-09-21

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