PE20010203A1 - Derivados de 5-fenil-pirimidina como antagonistas del receptor de la neuroquinina 1 - Google Patents

Derivados de 5-fenil-pirimidina como antagonistas del receptor de la neuroquinina 1

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Publication number
PE20010203A1
PE20010203A1 PE2000000509A PE0005092000A PE20010203A1 PE 20010203 A1 PE20010203 A1 PE 20010203A1 PE 2000000509 A PE2000000509 A PE 2000000509A PE 0005092000 A PE0005092000 A PE 0005092000A PE 20010203 A1 PE20010203 A1 PE 20010203A1
Authority
PE
Peru
Prior art keywords
phenyl
alkyl
alcoxyl
trifluoromethyl
halogen
Prior art date
Application number
PE2000000509A
Other languages
English (en)
Inventor
Michael Boes
Guido Galley
Torsten Hoffmann
Walter Hunkeler
Heinz Stadler
Thierry Godel
Patrick Schnider
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
Publication of PE20010203A1 publication Critical patent/PE20010203A1/es

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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/06—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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms

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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)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE 5-FENIL-PIRIMIDINA DE FORMULA I, DONDE: R1 ES H, HALOGENO; R2 ES H, HALOGENO, ALQUILO, ALCOXILO; R3 ES HALOGENO, TRIFLUOROMETILO, ALCOXILO, ALQUILO; R4 Y R4` SON H, ALQUILO; R5 ES ALQUILO, ALCOXILO, AMINO, HIDROXILO, HIDROXIALQUILO, -(CH2)n-PIPERAZINILO, -(CH2)n-MORFOLINILO, -(CH2)n+1-IMIDAZOLILO, -O-(CH2)n+1(NR4")2, ENTRE OTROS, R4" ES H, ALQUILO; R6 ES H; R2 Y R6 O R1 Y R6 PUEDEN SER JUNTO A DOS ATOMOS DE C DEL ANILLO -CH=CH-CH=CH-, CON LA CONDICION QUE n PARA R1 SEA 1; n ES 0-2; X ES -C(O)N(R4")-, -N(R4")C(O)-. SON COMPUESTOS PREFERIDOS (3,5-BIS-TRIFLUOROMETIL-BENCIL)-METIL-AMIDA DEL ACIDO 5-(2-CLORO-FENIL)-2-(4-METIL-PIPERAZIN-1-IL)-PIRIMIDIN-4-CARBOXILICO, (3,5-BIS-TRIFLUOROMETIL-BENCIL)-METIL-AMIDA DEL ACIDO 5-(2-CLORO-FENIL)-2-(2-MORFOLIN-4-IL-ETOXI)-PIRIMIDIN-4-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION Y A COMPUESTOS INTERMEDIOS. LOS DERIVADOS DE 5-FENIL-PIRIMIDINA DE FORMULA I SON ANTAGONISTAS DEL RECEPTOR DE LA NEUROQUININA 1 (NK-1), SUSTANCIA P) POR LO QUE PUEDEN SER UTILES EN ENFERMEDADES INFLAMATORIA, MIGRANA, ARTRITIS REUMATOIDEA, ASMA
PE2000000509A 1999-05-31 2000-05-26 Derivados de 5-fenil-pirimidina como antagonistas del receptor de la neuroquinina 1 PE20010203A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP99110482 1999-05-31

Publications (1)

Publication Number Publication Date
PE20010203A1 true PE20010203A1 (es) 2001-02-15

Family

ID=8238270

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000509A PE20010203A1 (es) 1999-05-31 2000-05-26 Derivados de 5-fenil-pirimidina como antagonistas del receptor de la neuroquinina 1

Country Status (36)

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US (1) US6756380B1 (es)
EP (1) EP1187814B1 (es)
JP (1) JP3590591B2 (es)
KR (1) KR100478369B1 (es)
CN (1) CN1187338C (es)
AR (1) AR024145A1 (es)
AT (1) ATE273962T1 (es)
AU (1) AU769265B2 (es)
BR (1) BR0011097A (es)
CA (1) CA2375670C (es)
CO (1) CO5170529A1 (es)
CZ (1) CZ20014273A3 (es)
DE (1) DE60013127T2 (es)
DK (1) DK1187814T3 (es)
ES (1) ES2225144T3 (es)
GC (1) GC0000338A (es)
HK (1) HK1046411B (es)
HR (1) HRP20010867A2 (es)
HU (1) HU225016B1 (es)
IL (2) IL146519A0 (es)
JO (1) JO2308B1 (es)
MA (1) MA26794A1 (es)
MX (1) MXPA01011704A (es)
MY (1) MY136258A (es)
NO (1) NO321334B1 (es)
NZ (1) NZ515408A (es)
PE (1) PE20010203A1 (es)
PL (1) PL353492A1 (es)
PT (1) PT1187814E (es)
RU (1) RU2244710C2 (es)
SI (1) SI1187814T1 (es)
TR (1) TR200103460T2 (es)
TW (1) TWI263638B (es)
WO (1) WO2000073278A2 (es)
YU (1) YU85001A (es)
ZA (1) ZA200109496B (es)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AUPQ514600A0 (en) 2000-01-18 2000-02-10 James Cook University Brain injury treatment
CA2412010A1 (en) * 2000-06-13 2001-12-20 Basf Aktiengesellschaft Fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines
CA2432642A1 (en) 2000-12-21 2002-08-08 Subhash P. Khanapure Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
MXPA04012345A (es) 2002-07-02 2005-02-25 Hoffmann La Roche Derivados de pirimidina 2,5-substituida como antagonistas ix del receptor ccr-3.
WO2005046604A2 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Heteroaryl-hydrazone compounds
JP2007217282A (ja) * 2004-03-04 2007-08-30 Astellas Pharma Inc 置換ピリミジン誘導体
CA2586870A1 (en) * 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Il-12 modulatory compounds
CA2598762A1 (en) 2005-02-25 2006-08-31 F. Hoffmann-La Roche Ag Tablets with improved drug substance dispersibility
US9013997B2 (en) 2012-06-01 2015-04-21 Broadcom Corporation System for performing distributed data cut-through
SG11201507459YA (en) 2013-03-15 2015-10-29 Epigen Biosciences Inc Heterocyclic compounds useful in the treatment of disease
GB201316600D0 (en) * 2013-09-18 2013-10-30 Redx Pharma Ltd Agricultural chemicals
JP6609253B2 (ja) * 2014-08-06 2019-11-20 キッセイ薬品工業株式会社 シアノチオフェン誘導体
EP3250034B1 (en) * 2015-01-30 2020-03-11 Basf Se Herbicidal phenylpyrimidines
AU2017298874A1 (en) 2016-07-20 2019-01-03 Basf Se Herbicidal compositions comprising phenylpyrimidines
WO2018019552A1 (en) 2016-07-25 2018-02-01 Basf Se Herbicidal pyrimidine compounds
CN109561685A (zh) 2016-07-25 2019-04-02 巴斯夫欧洲公司 除草的嘧啶化合物
BR112018077111A2 (pt) 2016-07-26 2019-04-02 Basf Se uso de compostos de pirimidina, compostos de pirimidina, mistura herbicida, composições herbicidas, método para controlar vegetação indesejada e uso das composições
WO2018019765A1 (en) 2016-07-27 2018-02-01 Basf Se Herbicidal pyrimidine compounds
EA201990342A1 (ru) 2016-07-28 2019-08-30 Басф Се Гербицидные пиримидиновые соединения
WO2018229041A1 (en) 2017-06-14 2018-12-20 Basf Se Herbicidal pyrimidine compounds
WO2019121408A1 (en) 2017-12-20 2019-06-27 Basf Se Herbicidal pyrimidine compounds
WO2019121373A1 (en) 2017-12-20 2019-06-27 Basf Se Herbicidal pyrimidine compounds
WO2019121374A1 (en) 2017-12-20 2019-06-27 Basf Se Herbicidal pyrimidine compounds
WO2019121352A1 (en) 2017-12-20 2019-06-27 Basf Se Herbicidal pyrimidine compounds
WO2020058062A1 (de) * 2018-09-19 2020-03-26 Bayer Aktiengesellschaft Herbizid wirksame substituierte phenylpyrimidinhydrazide

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AR208171A1 (es) 1972-09-29 1976-12-09 Ciba Geigy Ag Procedimiento para la obtencion de nuevos derivados del acido cef-3-em-4-carboxilico
SG52217A1 (en) 1993-12-29 1998-09-28 Merck Sharp & Dohme Substituted morpholine derivatives and their use as therapeutic agents
EP0850228A1 (en) 1995-09-01 1998-07-01 Signal Pharmaceuticals, Inc. Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions

Also Published As

Publication number Publication date
HUP0201527A3 (en) 2005-01-28
AU769265B2 (en) 2004-01-22
HUP0201527A2 (en) 2002-08-28
NO321334B1 (no) 2006-04-24
US6756380B1 (en) 2004-06-29
MA26794A1 (fr) 2004-12-20
TR200103460T2 (tr) 2002-05-21
TWI263638B (en) 2006-10-11
EP1187814B1 (en) 2004-08-18
NO20015701L (no) 2001-11-22
AU5070800A (en) 2000-12-18
KR20020003399A (ko) 2002-01-12
MY136258A (en) 2008-09-30
NZ515408A (en) 2004-02-27
HK1046411A1 (en) 2003-01-10
IL146519A0 (en) 2002-07-25
ZA200109496B (en) 2003-02-17
JO2308B1 (en) 2005-09-12
BR0011097A (pt) 2002-03-19
CZ20014273A3 (cs) 2002-05-15
IL146519A (en) 2006-12-10
ATE273962T1 (de) 2004-09-15
AR024145A1 (es) 2002-09-04
PT1187814E (pt) 2004-10-29
CN1187338C (zh) 2005-02-02
CA2375670A1 (en) 2000-12-07
JP2003500477A (ja) 2003-01-07
WO2000073278A2 (en) 2000-12-07
RU2244710C2 (ru) 2005-01-20
CN1353696A (zh) 2002-06-12
DE60013127D1 (de) 2004-09-23
DE60013127T2 (de) 2005-09-08
WO2000073278A3 (en) 2001-07-05
EP1187814A2 (en) 2002-03-20
NO20015701D0 (no) 2001-11-22
HRP20010867A2 (en) 2003-04-30
DK1187814T3 (da) 2004-12-20
CA2375670C (en) 2009-09-29
SI1187814T1 (en) 2004-12-31
YU85001A (sh) 2004-09-03
MXPA01011704A (es) 2002-05-14
KR100478369B1 (ko) 2005-03-24
HK1046411B (zh) 2005-05-27
ES2225144T3 (es) 2005-03-16
HU225016B1 (en) 2006-05-29
CO5170529A1 (es) 2002-06-27
JP3590591B2 (ja) 2004-11-17
GC0000338A (en) 2007-03-31
PL353492A1 (en) 2003-11-17

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