HRP20070393T3 - 4-(aminometil)-piperidin benzamidi kao 5ht4-antagonisti - Google Patents

4-(aminometil)-piperidin benzamidi kao 5ht4-antagonisti

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Publication number
HRP20070393T3
HRP20070393T3 HR20070393T HRP20070393T HRP20070393T3 HR P20070393 T3 HRP20070393 T3 HR P20070393T3 HR 20070393 T HR20070393 T HR 20070393T HR P20070393 T HRP20070393 T HR P20070393T HR P20070393 T3 HRP20070393 T3 HR P20070393T3
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Croatia
Prior art keywords
6alkyl
substituted
hydrogen
hydroxy
halo
Prior art date
Application number
HR20070393T
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English (en)
Inventor
Ren� Marie Andr� Bosmans Jean-Paul
Jacobus Henricus
Anne Laurence
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Janssen Pharmaceutica N.V.
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Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HRP20070393T3 publication Critical patent/HRP20070393T3/hr

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • 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
    • A61P1/04Drugs 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
    • 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
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/10Laxatives
    • 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
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/06Anti-spasmodics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • 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
    • A61P25/14Drugs 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
    • A61P25/18Antipsychotics, 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
    • A61P25/20Hypnotics; Sedatives
    • 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
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    • 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
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Spoj s formulom (I) njegov stereokemijski izomemioblik, njegov N-oksidni oblik ili njegova farmaceutski prihvatljiva kisela ili bazna adicijska sol,naznačen time, da-R1-R2 je dvovalentni radikal s formulom-O-CH2-O- (a-1) -O-CH2-CH2- (a-2) -O-CH2-CH2-O- (a-3) -O-CH2-CH2-CH2- (a-4) -O-CH2-CH2-CH2-O- (a-5) -O-CH2-CH2-CH2-CH2- (a-6) -O-CH2-CH2-CH2-CH2-O- (a-7) -O-CH2-CH2-CH2-CH2-CH2- (a-8), gdje u rečenim dvovalentnim radikalima jedan ili dva vodikova atoma na istom ili različitom ugljikovom atomu ponekad mogu biti zamijenjeni s C1-6alkilom ili hidroksiR3 je vodik, halo, C1-4alkil; R4 je C1-6alkil; C1-6alkil zamijenjen s cijano ili C1-6alkiloksi; C1-6alkilaoki; cijano; amino ili mono ili di(C1-6alkil)amino; R5 je vodik ili C1-6alkil, a -OR5 radikal se nalazi na položaju 3- ili 4-piperidinskog ostatka; L je vodik ili L je radikal s formulom-Alk-R6 (b-1), -Alk-X-R7 (b-2), -Alk-Y-C(=O)-R9 (b-3) ili-Alk-Z-C(=O)-NR11R12 (b-4), gdje svaki Alk je C1-12alkandiil; iR6 je vodik; hidroksi; cijano;C3-6cikloalkil; C1-6alkilsulfonilamino; aril ili Het; R7 je C1-6alkil; C1-6alkil supstituiran s hidroksi; C3-6cikloalkil; aril ili Het; X je O, S, SO2 ili NR8; spomenuti R8 je vodik ili C1-6alkil; R9 je vodik, C1-6alkil, C3-6cikloalkil, hidroksi iliaril; Y je izravna veza ili NR10 gdje R10 je vodik ili C1-6alkil; Z je izravna veza, O, S ili NR10 gdje R10 je vodik ili C1-6alkil; R11 i R12, svaki zasebno su vodici, C1-6alkil, C3-6cikloalkil ili R11 i R12 skupa s dušikovim atomom koji nosi R11 i R12 mogu oblikovati pirolidinilni, piperidinilni, piperazinilni ili 4-morfohalinilni prsten, a pri tome oba mogu biti ponekad supstituirana s C1-6alkilom; Aril predstavlja nesupstituirani fenil ili fenil koji je supstituirani s 1, 2 ili 3 supstituenta svaki neovisno izabran između halo, hidroksi, C1-6alkila, C1-6alkiloksi, C1-6alkilkarbomla, nitro,trifluorometana, amino, aminokarbonila i aminosulfonila; iHet je furanil supstituiran s C1-6alkil ili halo; tetrahidrofuranil; tetrahidrofuranil supstituiran s C1-6alkilom; dioksolanil; dioksolanil supstituiran s C1-6alkilora; dioksanil; dioksanil supstituiran s C1-6alkilom; tetrahidropiranil; tetrahidropiranil supstituiran s C1-6alkilom; 2,3-dihidro-2-okso-1H-imidazolil; 2,3-dihidro-2-okso-1H-imidazolil supstituiran s jednim ili dva supstituenta, svaki neovisno izabran između halo ili C1-6alkila; pirolidinil; pirolidinil supstituiran s jednim ili dva supstituenta, svaki zasebno izabran između halo, hidroksi ili C1-6alkila; piridinil; piridinil supstituiran s jednim ili dva supstituenta, svaki zasebno izabran između halo, hidroksi ili C1-6alkila; pirimidinil; pirimidinil supstituiran s jednim ili dva supstituenta, svaki zasebno izabran između halo, hidroksi ili C1-6alkila; piridazinil;piridazinil supstituiran s jednim ili dva supstituenta, svaki zasebno izabran između hidroksi, C1-6alkiloksi, C1-6alkila ili halo; pirazinil; pirazinil supstituiran s jednim ili dva supstituenta, svaki zasebno izabran između hidroksi, C1-6alkiloksi,C1-6alk
HR20070393T 2003-06-19 2007-09-10 4-(aminometil)-piperidin benzamidi kao 5ht4-antagonisti HRP20070393T3 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0350236 2003-06-19
PCT/EP2004/006285 WO2005000838A1 (en) 2003-06-19 2004-06-10 4-(aminomethyl)-piperidine benzamides as 5ht4-antagonists

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HRP20070393T3 true HRP20070393T3 (hr) 2007-10-31

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US (1) US7638535B2 (hr)
EP (1) EP1641784B1 (hr)
JP (1) JP4688800B2 (hr)
KR (1) KR101151645B1 (hr)
CN (1) CN100537565C (hr)
AR (1) AR044821A1 (hr)
AT (1) ATE364602T1 (hr)
AU (1) AU2004251825B2 (hr)
BR (1) BRPI0411603B1 (hr)
CA (1) CA2528590C (hr)
CY (1) CY1106857T1 (hr)
DE (1) DE602004006997T2 (hr)
DK (1) DK1641784T3 (hr)
EA (1) EA008504B1 (hr)
ES (1) ES2288258T3 (hr)
HK (1) HK1095327A1 (hr)
HR (1) HRP20070393T3 (hr)
IL (1) IL172604A (hr)
JO (1) JO2478B1 (hr)
MX (1) MXPA05013772A (hr)
MY (1) MY139454A (hr)
NZ (1) NZ544592A (hr)
PA (1) PA8605101A1 (hr)
PL (1) PL1641784T3 (hr)
PT (1) PT1641784E (hr)
SI (1) SI1641784T1 (hr)
TW (1) TWI346107B (hr)
UA (1) UA88607C2 (hr)
WO (1) WO2005000838A1 (hr)

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TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
US7728006B2 (en) 2004-04-07 2010-06-01 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
JP5042028B2 (ja) 2004-11-05 2012-10-03 セラヴァンス, インコーポレーテッド キノリノン−カルボキサミド化合物
ATE441646T1 (de) 2004-11-05 2009-09-15 Theravance Inc 5-ht4-rezeptoragonistenverbindungen
ATE469897T1 (de) 2004-12-22 2010-06-15 Theravance Inc Indazolcarbonsäureamidverbindungen
ES2523851T3 (es) 2005-03-02 2014-12-02 Theravance Biopharma R&D Ip, Llc Compuestos de quinolinona como agonistas de los receptores 5-HT4
US9101160B2 (en) 2005-11-23 2015-08-11 The Coca-Cola Company Condiments with high-potency sweetener
US8017168B2 (en) 2006-11-02 2011-09-13 The Coca-Cola Company High-potency sweetener composition with rubisco protein, rubiscolin, rubiscolin derivatives, ace inhibitory peptides, and combinations thereof, and compositions sweetened therewith
US20100081981A1 (en) * 2008-10-01 2010-04-01 Cheng Shien-Che Wrist support
GB0901487D0 (en) 2009-01-30 2009-03-11 Movetis N V Asthma Therapy
CA2854266A1 (en) 2011-11-30 2013-06-06 Actelion Pharmaceuticals Ltd 3,7-disubstituted octahydro-2h-pyrido[4,3-e][1,3]oxazin-2-one antibiotics
GB201403093D0 (en) 2014-02-21 2014-04-09 Cancer Rec Tech Ltd Therapeutic compounds and their use
US10323024B2 (en) 2016-01-15 2019-06-18 Sumitomo Dainippon Pharma Co., Ltd. Biheterocyclic compound
GB201715194D0 (en) 2017-09-20 2017-11-01 Carrick Therapeutics Ltd Compounds and their therapeutic use
CN115974856B (zh) * 2022-12-28 2023-08-11 北京康立生医药技术开发有限公司 一种治疗成人t细胞白血病淋巴瘤药物伐美妥司他的制备方法

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US4186135A (en) * 1976-08-04 1980-01-29 Societe D'etudes Scientifiques Et Industrielles De L'ile-De-France Substituted 2,3-alkylene bis (oxy) benzamides and derivatives and method of preparation
US5374637A (en) * 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
TW402591B (en) * 1997-07-11 2000-08-21 Janssen Pharmaceutica Nv Monocyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
TW570920B (en) * 1998-12-22 2004-01-11 Janssen Pharmaceutica Nv 4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders

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TW200517376A (en) 2005-06-01
CA2528590C (en) 2012-04-03
SI1641784T1 (sl) 2007-10-31
HK1095327A1 (en) 2007-05-04
JO2478B1 (en) 2009-01-20
KR101151645B1 (ko) 2012-06-08
UA88607C2 (en) 2009-11-10
PL1641784T3 (pl) 2007-11-30
DE602004006997D1 (de) 2007-07-26
JP4688800B2 (ja) 2011-05-25
CA2528590A1 (en) 2005-01-06
MY139454A (en) 2009-10-30
MXPA05013772A (es) 2006-03-08
CN100537565C (zh) 2009-09-09
EA200600061A1 (ru) 2006-06-30
BRPI0411603B1 (pt) 2017-10-31
IL172604A (en) 2010-12-30
ATE364602T1 (de) 2007-07-15
TWI346107B (en) 2011-08-01
BRPI0411603A (pt) 2006-08-08
PT1641784E (pt) 2007-08-28
DE602004006997T2 (de) 2008-05-15
US20060281753A1 (en) 2006-12-14
DK1641784T3 (da) 2007-09-24
IL172604A0 (en) 2006-04-10
JP2006527716A (ja) 2006-12-07
CY1106857T1 (el) 2012-05-23
KR20060018263A (ko) 2006-02-28
ES2288258T3 (es) 2008-01-01
AR044821A1 (es) 2005-10-05
EA008504B1 (ru) 2007-06-29
US7638535B2 (en) 2009-12-29
WO2005000838A1 (en) 2005-01-06
EP1641784A1 (en) 2006-04-05
NZ544592A (en) 2008-05-30
PA8605101A1 (es) 2005-02-04
AU2004251825A1 (en) 2005-01-06
AU2004251825B2 (en) 2009-11-26
EP1641784B1 (en) 2007-06-13
CN1809558A (zh) 2006-07-26

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