AR005278A1 - Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición. - Google Patents

Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición.

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Publication number
AR005278A1
AR005278A1 ARP960105895A ARP960105895A AR005278A1 AR 005278 A1 AR005278 A1 AR 005278A1 AR P960105895 A ARP960105895 A AR P960105895A AR P960105895 A ARP960105895 A AR P960105895A AR 005278 A1 AR005278 A1 AR 005278A1
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AR
Argentina
Prior art keywords
formula
alkyl
radical
preparation
hydrogen
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ARP960105895A
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English (en)
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Janssen Pharmaceutica Nv
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Publication of AR005278A1 publication Critical patent/AR005278A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/20—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Virology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
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  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen derivados 1-(piperidinil 1,2-disustituido)-4- (imidazolfusionado)-piperidina, que comprende un compuesto de la fórmula (I),en forma N-óxido, una sal de adición farmacéuticamente aceptable o una forma estereoquímicamen te isomérica delmismo, donde n es 0,1o 2; m es 1 o 2, siempreque si m es 2, n sea 1; =Q es =O o =NR3; X es un enlace covalente o un radical bivalente de la fórmula -O-, -S-, NR3-; R1 es Ar1.Ar1 alquilo C1-6 o di(Ar1)alquilo C1-6, donde cada grupo a lquilo C1-C6está optaitvamentte sustituido con hidroxi, alquilox C1-C4, oxo o un sustituyente oxo cetalizado de lafórmula -O-CH2-CH2-O o -O-CH2-CH2-CH2-O-; R2 es Ar2, Ar2 alquilo C1-6, Het o Het alquilo C1-6; R3 es hidrógeno o alquilo C1-C6; L es un radicalde lafórmula (a-1) o (a2),en la cual la línea de puntos es un enlace optativo; cada -A-B es, independientemente, un radical bivalente de la fórmula: Y-CR7=CH-(b-1); -CH=CR7-Y (b-2); -CH=CH-CH=CH- (b-3); -CH=CR7-CH=CH- (b-4); -CH=CH-CR7=CH- (b-5); o-CH=CH-CH=CR7 (b-6) en el cual cada Y esindependientemente , alquilo C1-6, halo, etenilo sustituido con carboxilo o alquiloxicarbonilo C1-C6, hidroxialquilo C1-C6; o R7 es hidrógeno en el casoque -A-B- es un radical de fórmula (b-1)o (b-2); R8 eshidrógeno, alquilo C1-C6 o alquilcarbonilo C1-C6; cada Z es, independientemente, Z1 o Z2; dondeZ1 es un radical bivalente de la fórmula -CH2-, -CH2-CH2-,o -CH=Ch-, siempre que cuando L es un radical de la fórmu la (a-1) y la línea de puntos esunenlace adicional, Z1 no sea -CH2-; Z2 es un radical bivalente de la fórmula -CH2-CHOH, -CH2-O-, -CH2C(=O)- o -CH2-C(=NOH)-, siempre que la porción -CH2- dedichos radicales bivalentes esté conectada al nitrógeno del anillo de imidazol; cada R4 es,independientemente, hidrógeno, alquilo C1-C6, halo, etenilo
ARP960105895A 1995-12-27 1996-12-26 Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición. AR005278A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP95203652 1995-12-27

Publications (1)

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AR005278A1 true AR005278A1 (es) 1999-04-28

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ID=8221024

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP960105895A AR005278A1 (es) 1995-12-27 1996-12-26 Derivados de 1- (piperidinil 1,2 - disustituido) -4- (imidazol fusionado) -piperidina, proceso para la preparación de los mismos, composición farmacéutica que los contiene y proceso para la preparación de dicha composición.
ARP050105316A AR051817A2 (es) 1995-12-27 2005-12-16 Derivados de piperidina-1-(1,2-piperidinil disustituidos)-4-(imidazol condensados)

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ARP050105316A AR051817A2 (es) 1995-12-27 2005-12-16 Derivados de piperidina-1-(1,2-piperidinil disustituidos)-4-(imidazol condensados)

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US (1) US6251894B1 (es)
EP (1) EP0843679B1 (es)
JP (1) JP4097043B2 (es)
KR (1) KR100485147B1 (es)
CN (1) CN1066733C (es)
AR (2) AR005278A1 (es)
AT (1) ATE208392T1 (es)
AU (1) AU716071B2 (es)
BR (1) BR9612307A (es)
CA (1) CA2238817C (es)
CY (1) CY2271B1 (es)
CZ (1) CZ295861B6 (es)
DE (1) DE69616802T2 (es)
DK (1) DK0843679T3 (es)
EA (1) EA001374B1 (es)
ES (1) ES2167619T3 (es)
HK (1) HK1011206A1 (es)
HU (1) HU229766B1 (es)
IL (2) IL124641A (es)
MY (1) MY117680A (es)
NO (1) NO310916B1 (es)
NZ (1) NZ325845A (es)
PL (1) PL183767B1 (es)
PT (1) PT843679E (es)
SI (1) SI0843679T1 (es)
SK (1) SK283540B6 (es)
TR (1) TR199801210T2 (es)
TW (1) TW382017B (es)
WO (1) WO1997024356A1 (es)
ZA (1) ZA9610889B (es)

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TW527186B (en) 1996-03-19 2003-04-11 Janssen Pharmaceutica Nv Fused imidazole derivatives as multidrug resistance modulators
US6544979B1 (en) 1997-09-18 2003-04-08 Janssen Pharmaceuticals, N.V. Fused imidazole derivatives for improving oral bioavailability of pharmaceutical agents
HU229406B1 (en) * 1998-12-19 2013-12-30 Janssen Pharmaceutica Nv Antihistaminic spiro compounds
WO2001030348A1 (en) * 1999-10-25 2001-05-03 Janssen Pharmaceutica N.V. Use of substance p antagonists for influencing the circadian timing system
EP1401838B1 (en) 2001-06-12 2014-03-26 Janssen Pharmaceutica NV Novel substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine
US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
NZ550723A (en) * 2001-11-23 2008-06-30 Janssen Pharmaceutica Nv The use of anti-histaminics for acute reduction of elevated intracranial pressure
WO2003050123A1 (fr) * 2001-12-10 2003-06-19 Kyorin Pharmaceutical Co., Ltd. Derives bicycliques fusionnes de pyridine en tant qu'antagonistes du recepteur de la tachykinine
AU2003206722B2 (en) * 2002-01-16 2008-01-24 Mercury Pharma Group Limited Prucalopride-N-oxide
CN1297559C (zh) * 2002-01-18 2007-01-31 杏林制药株式会社 稠合双环嘧啶衍生物
EP1489083B1 (en) * 2002-03-26 2007-06-06 Kyorin Pharmaceutical Co., Ltd. Fused bicyclic pyridine derivative as tachykinin receptor antagonist
WO2004056805A1 (en) * 2002-12-23 2004-07-08 Janssen Pharmaceutica N.V. Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
JO2696B1 (en) 2002-12-23 2013-03-03 شركة جانسين فارماسوتيكا ان. في Derivatives of 1-piperdine-4-yl-4-biprolidine-3-yl-piperazine substituted and used as quinine antagonists
JO2676B1 (en) 2004-04-06 2012-06-17 جانسين فارماسوتيكا ان. في Derivatives of second-aza-spiro- (5,4) -dikan and their use as antihistamines
JO2525B1 (en) * 2004-04-08 2010-03-17 شركة جانسين فارماسوتيكا ان. في Derived 4-alkyl-and-4-canoelperidine derivatives and their use as anti-neroquin
DE602006014531D1 (de) 2005-03-03 2010-07-08 Janssen Pharmaceutica Nv Substituierte oxadiazaspiro-ä5.5ü-undecanonderivate und ihre verwendung als neurokininantagonisten
ES2350647T3 (es) 2005-03-08 2011-01-25 Janssen Pharmaceutica Nv Derivados de diaza-espiro-[4.4]-nonano como antagonistas de neuroquininas (nk1).
AU2008278273A1 (en) * 2007-07-19 2009-01-22 Adelaide Research & Innovation Pty Ltd Method for reducing intracranial pressure
UA105182C2 (ru) 2008-07-03 2014-04-25 Ньюрексон, Інк. Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность
EP2729147B1 (en) 2011-07-04 2017-09-06 IRBM - Science Park S.p.A. Nk-1 receptor antagonists for treating corneal neovascularisation
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
US20230134843A1 (en) 2020-03-11 2023-05-04 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency

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US4329353A (en) 1980-10-22 1982-05-11 Janssen Pharmaceutica, N.V. 1-(4-Aryl-cyclohexyl)piperidine derivatives, method of use thereof and pharmaceutical compositions thereof
DE69110685T2 (de) * 1990-10-10 1995-11-09 Schering Corp Substituierte imidazobenzazepine und imidazopyridoazepine.
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Also Published As

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DE69616802D1 (de) 2001-12-13
EA199800603A1 (ru) 1998-12-24
ATE208392T1 (de) 2001-11-15
CA2238817A1 (en) 1997-07-10
HUP9903948A2 (hu) 2000-03-28
ZA9610889B (en) 1998-06-23
EA001374B1 (ru) 2001-02-26
JP2000506503A (ja) 2000-05-30
NO310916B1 (no) 2001-09-17
TW382017B (en) 2000-02-11
AU1308697A (en) 1997-07-28
SI0843679T1 (en) 2002-06-30
IL124642A (en) 2002-08-14
EP0843679A1 (en) 1998-05-27
KR19990076715A (ko) 1999-10-15
CN1206417A (zh) 1999-01-27
TR199801210T2 (xx) 1999-10-21
SK83098A3 (en) 1999-01-11
AR051817A2 (es) 2007-02-14
CZ295861B6 (cs) 2005-11-16
PL183767B1 (pl) 2002-07-31
EP0843679B1 (en) 2001-11-07
BR9612307A (pt) 1999-07-13
DK0843679T3 (da) 2002-02-25
AU716071B2 (en) 2000-02-17
PL327136A1 (en) 1998-11-23
PT843679E (pt) 2002-04-29
DE69616802T2 (de) 2002-07-04
ES2167619T3 (es) 2002-05-16
NO982405D0 (no) 1998-05-27
NZ325845A (en) 1999-06-29
CZ186598A3 (cs) 1998-11-11
NO982405L (no) 1998-08-19
HK1011206A1 (en) 1999-07-09
IL124642A0 (en) 1998-12-06
HU229766B1 (hu) 2014-06-30
CN1066733C (zh) 2001-06-06
KR100485147B1 (ko) 2005-09-13
JP4097043B2 (ja) 2008-06-04
US6251894B1 (en) 2001-06-26
CY2271B1 (en) 2003-07-04
SK283540B6 (sk) 2003-09-11
IL124641A (en) 2001-11-25
MY117680A (en) 2004-07-31
CA2238817C (en) 2006-10-17
WO1997024356A1 (en) 1997-07-10
HUP9903948A3 (hu) 2000-04-28
IL124641A0 (en) 1998-12-06

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