PE97499A1 - Derivados de 5h-tiazolo [3,2-a] pirimidina - Google Patents

Derivados de 5h-tiazolo [3,2-a] pirimidina

Info

Publication number
PE97499A1
PE97499A1 PE1998000625A PE00062598A PE97499A1 PE 97499 A1 PE97499 A1 PE 97499A1 PE 1998000625 A PE1998000625 A PE 1998000625A PE 00062598 A PE00062598 A PE 00062598A PE 97499 A1 PE97499 A1 PE 97499A1
Authority
PE
Peru
Prior art keywords
alkyl
refers
compound
alcoxyl
cycloalkyl
Prior art date
Application number
PE1998000625A
Other languages
English (en)
Inventor
Jurgen Wichmann
Vincent Mutel
Geo Adam
Thomas Johannes Woltering
Sabine Kolczewski
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 PE97499A1 publication Critical patent/PE97499A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • 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]
    • AHUMAN NECESSITIES
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/38One sulfur atom
    • C07D239/40One sulfur atom as doubly bound sulfur atom or as unsubstituted mercapto radical

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • 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)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Addiction (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) O SUS SALES, DONDE R1 ES H, ALQUILO, BENCILO; R2 ES ALQUILO, ALCOXILO, -O(CH2)nN(R13)(R14), ENTRE OTROS; R3 A R12 SON H, HALOGENO, TRIFLUOROMETILO, ALQUILO, CICLOALQUILO, ALCOXILO, HIDROXILO, ENTRE OTROS; o R6 Y R7 FORMAN UN ANILLO DE BENCENO; R13 A R15 SON H, ALQUILO, CICLOALQUILO; n ES 1-5. UN COMPUESTO PREFERIDO ES (RS)-2-(2,6-DICLOROFENIL)-5-(2-METOXIFENIL)-7-METIL-5H-TIAZOLO[3,2-a]PIRIMIDIN-6-CARBOXILATO DE 2-DIMETILAMINO-ETILO, ENTRE OTROS. TAMBIEN SE REFIERE A COMPUESTOS DE FORMULA (II). TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO (I) PUEDE SER UTIL PARA EL CONTROL O PREVENCION DE TRASTORNOS NEUROLOGICOS COMO FUNCION CEREBRAL LIMITADA CAUSADA POR OPERACIONES DE BYPASS O TRASPLANTES, LESIONES DE LA MEDULA ESPINAL, HIPOXIA CAUSADA POR GESTACION; O FUNCIONES GLUTAMATO DEFICIENTES COMO ESPASMOS, CONVULSIONES, MIGRANA, INCONTINENCIA URINARIA
PE1998000625A 1997-07-18 1998-07-15 Derivados de 5h-tiazolo [3,2-a] pirimidina PE97499A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP97112324 1997-07-18

Publications (1)

Publication Number Publication Date
PE97499A1 true PE97499A1 (es) 1999-10-12

Family

ID=8227080

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1998000625A PE97499A1 (es) 1997-07-18 1998-07-15 Derivados de 5h-tiazolo [3,2-a] pirimidina

Country Status (33)

Country Link
US (1) US5958931A (es)
EP (1) EP0891978B1 (es)
JP (1) JP3100573B2 (es)
KR (1) KR100296837B1 (es)
CN (1) CN1102596C (es)
AR (1) AR016129A1 (es)
AT (1) ATE214704T1 (es)
AU (1) AU738207B2 (es)
BR (1) BR9802482A (es)
CA (1) CA2243234C (es)
CO (1) CO5210884A1 (es)
CZ (1) CZ288944B6 (es)
DE (1) DE69804273T2 (es)
DK (1) DK0891978T3 (es)
ES (1) ES2172840T3 (es)
HK (1) HK1018439A1 (es)
HR (1) HRP980398B1 (es)
HU (1) HUP9801587A3 (es)
ID (1) ID21824A (es)
IL (1) IL125358A (es)
MA (1) MA26520A1 (es)
NO (1) NO310512B1 (es)
NZ (1) NZ330988A (es)
PE (1) PE97499A1 (es)
PL (1) PL190218B1 (es)
PT (1) PT891978E (es)
RU (1) RU2197493C2 (es)
SI (1) SI0891978T1 (es)
TR (1) TR199801367A2 (es)
TW (1) TW523518B (es)
UY (1) UY25095A1 (es)
YU (1) YU29798A (es)
ZA (1) ZA986250B (es)

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EP1074549B1 (en) * 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
CA2438582C (en) * 2001-01-31 2012-06-26 Synaptic Pharmaceutical Corporation Use of gal3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
WO2002102807A1 (fr) * 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Nouveaux derives d'isoxazolopyridone et leur utilisation
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
RU2378277C2 (ru) * 2004-06-21 2010-01-10 Ф. Хоффманн-Ля Рош Аг Производные пиразолпиримидина
KR100847160B1 (ko) * 2004-06-21 2008-07-17 에프. 호프만-라 로슈 아게 피라졸로 피리미딘 유도체
ES2365406T3 (es) 2005-02-11 2011-10-04 F. Hoffmann-La Roche Ag Derivados de pirazolo-pirimidina como antagonistas de mglur2.
MX2007011483A (es) 2005-03-23 2007-10-12 Hoffmann La Roche Derivados de acetilenil-pirazolo-pirimidina como antagonistas de glutamato metabotropico 2.
CA2623721C (en) 2005-09-27 2014-05-13 F. Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
TW200845978A (en) * 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
EA019085B1 (ru) 2007-09-14 2014-01-30 Янссен Фармасьютикалз, Инк. 1',3-двузамещенные 4-(арил-х-фенил)-1н-пиридин-2-оны
EP2205565B1 (en) * 2007-09-14 2013-04-17 Janssen Pharmaceuticals, Inc. 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones
NZ584145A (en) 2007-09-14 2012-03-30 Ortho Mcneil Janssen Pharm 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1,4'] bipyridinyl-2'-ones
MX2010005110A (es) * 2007-11-14 2010-09-09 Ortho Mcneil Janssen Pharm Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2.
ES2439291T3 (es) 2008-09-02 2014-01-22 Janssen Pharmaceuticals, Inc. Derivados de 3-azabiciclo[3.1.0]hexilo como moduladores de receptores de glutamato metabotrópicos
US8697689B2 (en) 2008-10-16 2014-04-15 Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
MX2011005242A (es) 2008-11-28 2011-09-06 Ortho Mcneil Janssen Pharm Derivados de indol y benzoxazina como moduladores de los receptores de glutamato metabotropicos.
CN101503414B (zh) * 2009-03-04 2013-10-30 沈阳药科大学 噻唑并[3,2-b]-1,2,4-三嗪衍生物及其应用
MY161325A (en) 2009-05-12 2017-04-14 Janssen Pharmaceuticals Inc 1, 2, 4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
CA2760259C (en) 2009-05-12 2018-05-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
ES2536433T3 (es) 2010-11-08 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
JP5852664B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド 1,2,4−トリアゾロ[4,3−a]ピリジン誘導体およびmGluR2受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
CN103298809B (zh) 2010-11-08 2016-08-31 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
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ME03518B (me) 2014-01-21 2020-04-20 Janssen Pharmaceutica Nv Kombinacije koje obuhvataju pozitivne alosterične modulatore ili ortosterične agoniste metabotropnog glutamatergičnog receptora podtipa 2 i njihova primjena
WO2015110435A1 (en) 2014-01-21 2015-07-30 Janssen Pharmaceutica Nv Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
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EP0524055A1 (fr) * 1991-07-19 1993-01-20 Synthelabo Dérivés d'imidazo[2,1-b]benzothiazole-3-acétamide, leur préparation et leur application en thérapeutique
PL182285B1 (pl) * 1994-08-12 2001-12-31 Lilly Co Eli Syntetyczne aminokwasy oraz ich estry i srodki farmaceutyczne je zawierajace PL PL PL PL PL PL PL
GB9609976D0 (en) * 1996-05-13 1996-07-17 Lilly Industries Ltd Pharmaceutical compounds
WO1998006724A1 (fr) * 1996-08-09 1998-02-19 Yamanouchi Pharmaceutical Co., Ltd. Agonistes du recepteur du glutamate metabotropique

Also Published As

Publication number Publication date
ATE214704T1 (de) 2002-04-15
HRP980398A2 (en) 1999-04-30
EP0891978A3 (en) 1999-02-03
CZ288944B6 (cs) 2001-10-17
HU9801587D0 (en) 1998-09-28
EP0891978A2 (en) 1999-01-20
DK0891978T3 (da) 2002-07-01
IL125358A0 (en) 1999-03-12
DE69804273T2 (de) 2002-10-31
CZ223998A3 (cs) 1999-02-17
CA2243234C (en) 2007-09-18
CN1206010A (zh) 1999-01-27
TR199801367A3 (tr) 1999-02-22
IL125358A (en) 2002-09-12
ZA986250B (en) 1999-01-22
NO983244D0 (no) 1998-07-14
HUP9801587A3 (en) 2001-09-28
BR9802482A (pt) 2000-03-14
KR19990013919A (ko) 1999-02-25
RU2197493C2 (ru) 2003-01-27
NO983244L (no) 1999-01-19
ID21824A (id) 1999-07-29
HUP9801587A2 (hu) 1999-11-29
JP3100573B2 (ja) 2000-10-16
PT891978E (pt) 2002-07-31
AR016129A1 (es) 2001-06-20
CA2243234A1 (en) 1999-01-18
PL190218B1 (pl) 2005-11-30
TW523518B (en) 2003-03-11
EP0891978B1 (en) 2002-03-20
NO310512B1 (no) 2001-07-16
CO5210884A1 (es) 2002-10-30
UY25095A1 (es) 2001-01-31
CN1102596C (zh) 2003-03-05
PL327532A1 (en) 1999-02-01
ES2172840T3 (es) 2002-10-01
HRP980398B1 (en) 2002-06-30
SI0891978T1 (en) 2002-06-30
HK1018439A1 (en) 1999-12-24
YU29798A (sh) 2001-12-26
JPH1171380A (ja) 1999-03-16
US5958931A (en) 1999-09-28
KR100296837B1 (ko) 2001-10-26
MA26520A1 (fr) 2004-12-20
NZ330988A (en) 1999-03-29
DE69804273D1 (de) 2002-04-25
AU7730298A (en) 1999-01-28
AU738207B2 (en) 2001-09-13
TR199801367A2 (xx) 1999-02-22

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