ATE322496T1 - 4-phenylpyridin-derivate als neurokinin-1- rezeptor-antagonisten - Google Patents

4-phenylpyridin-derivate als neurokinin-1- rezeptor-antagonisten

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Publication number
ATE322496T1
ATE322496T1 AT01960529T AT01960529T ATE322496T1 AT E322496 T1 ATE322496 T1 AT E322496T1 AT 01960529 T AT01960529 T AT 01960529T AT 01960529 T AT01960529 T AT 01960529T AT E322496 T1 ATE322496 T1 AT E322496T1
Authority
AT
Austria
Prior art keywords
neurokinin
receptor antagonists
phenylpyridine derivatives
phenylpyridine
derivatives
Prior art date
Application number
AT01960529T
Other languages
English (en)
Inventor
Torsten Hoffmann
Patrick Schnider
Heinz Stadler
Original Assignee
Hoffmann La Roche
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Application granted granted Critical
Publication of ATE322496T1 publication Critical patent/ATE322496T1/de

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P1/08Drugs 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • 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
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    • A61P17/00Drugs for dermatological disorders
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
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    • 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
    • A61P25/22Anxiolytics
    • 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
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    • 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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    • 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
    • A61P25/36Opioid-abuse
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • 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]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AT01960529T 2000-07-24 2001-07-20 4-phenylpyridin-derivate als neurokinin-1- rezeptor-antagonisten ATE322496T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00115846 2000-07-24

Publications (1)

Publication Number Publication Date
ATE322496T1 true ATE322496T1 (de) 2006-04-15

Family

ID=8169331

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01960529T ATE322496T1 (de) 2000-07-24 2001-07-20 4-phenylpyridin-derivate als neurokinin-1- rezeptor-antagonisten

Country Status (37)

Country Link
US (2) US6576762B2 (de)
EP (1) EP1305319B1 (de)
JP (1) JP4118673B2 (de)
KR (1) KR100527214B1 (de)
CN (1) CN1192032C (de)
AR (1) AR029875A1 (de)
AT (1) ATE322496T1 (de)
AU (2) AU2001282005B2 (de)
BR (1) BR0112695A (de)
CA (1) CA2416874C (de)
CY (1) CY1106113T1 (de)
CZ (1) CZ2003528A3 (de)
DE (1) DE60118569T2 (de)
DK (1) DK1305319T3 (de)
EC (1) ECSP034446A (de)
ES (1) ES2260265T3 (de)
GT (1) GT200100148A (de)
HR (1) HRP20030031A2 (de)
HU (1) HU229231B1 (de)
IL (2) IL153837A0 (de)
JO (1) JO2321B1 (de)
MA (1) MA26933A1 (de)
MX (1) MXPA03000367A (de)
MY (1) MY129224A (de)
NO (1) NO20030353D0 (de)
NZ (1) NZ523452A (de)
PA (1) PA8522801A1 (de)
PE (1) PE20020258A1 (de)
PL (1) PL366173A1 (de)
PT (1) PT1305319E (de)
RU (1) RU2276139C2 (de)
SI (1) SI1305319T1 (de)
TW (1) TWI287003B (de)
UY (1) UY26851A1 (de)
WO (1) WO2002008232A1 (de)
YU (1) YU2803A (de)
ZA (1) ZA200300219B (de)

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ES2208205T3 (es) * 1999-11-29 2004-06-16 F. Hoffmann-La Roche Ag 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-otolil-piridin-3-il)-isobutiramida.
WO2003091227A1 (en) 2002-04-26 2003-11-06 Eli Lilly And Company Tachykinin receptor antagonists
AU2003230829B8 (en) 2002-04-26 2008-12-11 Eli Lilly And Company Triazole derivatives as tachykinin receptor antagonists
WO2004032875A2 (en) * 2002-10-11 2004-04-22 Bristol-Myers Squibb Company Process for the preparation of tri-nitrogen containing heteroaryl-diamine derivatives useful as pharmaceutical agents and methods of producing pharmaceutical agents
EP1638944A1 (de) * 2003-06-12 2006-03-29 Eli Lilly And Company Tachykininrezeptor-antagonisten
JP4490421B2 (ja) 2003-07-03 2010-06-23 エフ.ホフマン−ラ ロシュ アーゲー 統合失調症を処置するデュアルnk1/nk3アンタゴニスト
US7288658B2 (en) * 2003-07-15 2007-10-30 Hoffmann-La Roche Inc. Process for preparation of pyridine derivatives
EP1776342B1 (de) 2004-07-06 2011-03-02 F. Hoffmann-La Roche AG Herstellungsverfahren für carboxamid-pyridin-derivate als zwischenprodukte bei der synthese von nk-1-rezeptor-antagonisten
US20060030600A1 (en) * 2004-08-06 2006-02-09 Patrick Schnider Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
JP2008514612A (ja) * 2004-09-23 2008-05-08 ミシャロウ、アレクサンダー 対抗適応を誘発することにより神経伝達物質系を調節する方法
CN101128189A (zh) 2005-02-25 2008-02-20 弗·哈夫曼-拉罗切有限公司 药物物质分散性改善的片剂
US8067662B2 (en) 2009-04-01 2011-11-29 Aalnex, Inc. Systems and methods for wound protection and exudate management
US7816577B2 (en) 2006-02-13 2010-10-19 Aalnex, Inc. Wound shield
KR101119365B1 (ko) 2006-05-31 2012-03-07 에프. 호프만-라 로슈 아게 아릴-4-에틴일-아이속사졸 유도체
JP2010516734A (ja) 2007-01-24 2010-05-20 グラクソ グループ リミテッド 3,5−ジアミノ−6−(2,3−ジクロロフェニル)−1,2,4−トリアジンまたはr(−)−2,4−ジアミノ−5−(2,3−ジクロロフェニル)−6−フルオロメチルピリミジンを含む医薬組成物
GB0808747D0 (en) 2008-05-14 2008-06-18 Glaxo Wellcome Mfg Pte Ltd Novel compounds
US8426450B1 (en) 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
CA2930008A1 (en) 2013-11-08 2015-05-14 Kissei Pharmaceutical Co., Ltd. Carboxymethyl piperidine derivative
TWI649307B (zh) 2014-05-07 2019-02-01 日商橘生藥品工業股份有限公司 Cyclohexylpyridine derivative
US10538491B2 (en) 2015-03-16 2020-01-21 Vanderbilt University 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators
CA3009325A1 (en) * 2015-12-22 2017-06-29 Takeda Pharmaceutical Company Limited Tripartite modulators of endosomal g protein-coupled receptors
US20210015834A1 (en) 2018-02-26 2021-01-21 Ospedale San Raffaele S.R.L. Nk-1 antagonists for use in the treatment of ocular pain

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IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
DE69428913T2 (de) 1993-12-29 2002-05-29 Merck Sharp & Dohme Ltd., Hoddesdon Substituierte morpholinderivate und ihre verwendung als arzneimittel
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US6303790B1 (en) * 1999-11-29 2001-10-16 Hoffman-La Roche Inc. Process for the preparation of pyridine derivatives
CA2415890C (en) * 2000-07-14 2009-04-07 F. Hoffmann-La Roche Ag N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives

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PL366173A1 (en) 2005-01-24
NO20030353L (no) 2003-01-23
MXPA03000367A (es) 2003-05-27
MA26933A1 (fr) 2004-12-20
US20020038030A1 (en) 2002-03-28
UY26851A1 (es) 2002-01-31
MY129224A (en) 2007-03-30
AU2001282005B2 (en) 2006-10-19
GT200100148A (es) 2002-05-16
HU229231B1 (en) 2013-09-30
CZ2003528A3 (cs) 2003-09-17
PA8522801A1 (es) 2002-09-30
NO20030353D0 (no) 2003-01-23
US20030130508A1 (en) 2003-07-10
JP4118673B2 (ja) 2008-07-16
CA2416874A1 (en) 2002-01-31
JP2004504400A (ja) 2004-02-12
DE60118569D1 (de) 2006-05-18
AR029875A1 (es) 2003-07-16
YU2803A (sh) 2006-01-16
HK1058360A1 (en) 2004-05-14
EP1305319B1 (de) 2006-04-05
US6624176B2 (en) 2003-09-23
IL153837A (en) 2008-06-05
IL153837A0 (en) 2003-07-31
ZA200300219B (en) 2004-04-08
NZ523452A (en) 2004-07-30
US6576762B2 (en) 2003-06-10
SI1305319T1 (sl) 2006-08-31
JO2321B1 (en) 2005-09-12
CY1106113T1 (el) 2011-06-08
PT1305319E (pt) 2006-08-31
DE60118569T2 (de) 2007-02-15
CA2416874C (en) 2011-01-18
BR0112695A (pt) 2003-04-22
CN1444589A (zh) 2003-09-24
PE20020258A1 (es) 2002-04-02
KR20030015898A (ko) 2003-02-25
DK1305319T3 (da) 2006-08-14
HUP0301272A2 (hu) 2003-08-28
TWI287003B (en) 2007-09-21
AU8200501A (en) 2002-02-05
CN1192032C (zh) 2005-03-09
EP1305319A1 (de) 2003-05-02
HRP20030031A2 (en) 2004-02-29
KR100527214B1 (ko) 2005-11-08
WO2002008232A1 (en) 2002-01-31
ES2260265T3 (es) 2006-11-01
RU2276139C2 (ru) 2006-05-10
ECSP034446A (es) 2003-03-10

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