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MXPA02006329A - 8-arilquinolinas sustituidas que son inhibidores de fosfodiesterasa-4. - Google Patents

8-arilquinolinas sustituidas que son inhibidores de fosfodiesterasa-4.

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Publication number
MXPA02006329A
MXPA02006329A MXPA02006329A MXPA02006329A MXPA02006329A MX PA02006329 A MXPA02006329 A MX PA02006329A MX PA02006329 A MXPA02006329 A MX PA02006329A MX PA02006329 A MXPA02006329 A MX PA02006329A MX PA02006329 A MXPA02006329 A MX PA02006329A
Authority
MX
Mexico
Prior art keywords
c1c6alkyl
c0c6alkyl
aryl
heteroaryl
son
Prior art date
Application number
MXPA02006329A
Other languages
English (en)
Inventor
Denis Deschenes
Original Assignee
Merck Frosst Canada Inc
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 Merck Frosst Canada Inc filed Critical Merck Frosst Canada Inc
Publication of MXPA02006329A publication Critical patent/MXPA02006329A/es

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    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P11/06—Antiasthmatics
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
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    • 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
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    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
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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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • 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
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

8-arilquinolinas sustituidas novedosas representadas por la formula (l), o una sal farmaceuticamente aceptable del mismo, en donde S1, S2 y S3 son independientemente H, -OH, halogeno, alquilo de C1-C6, -NO2, -CN o alcoxi de C1-C6, en donde los grupos alquilo y alcoxi son opcionalmente sustituidos con 1-5 sustituyentes; en donde cada sustituyente es independientemente un halogeno u OH; R1 es un grupo H, -OH, halogeno, carbonilo, o alquilo de C1-C6, cicloalquilo de C3-C6, alquenilo de C1-C6, alcoxi de C1-C6, arilo, heteroarilo, -CN, heterocicloalquilo de C3-C6, -amino, alquilamino de C1-C6, -(alquilo de C1-C6)(alquilo de C1-C6)amino, alquilo de C1-C6(oxi) alquilo de C1-C6, -C(O)NH(arilo), -(O)NH(heteroarilo), -SOnNH(arilo), SOnNH(heteroarilo), SOnNH(alquilo de C1-C6), -C(O)N(alquilo de C0-C6)(alquilo de C0-C6), -NH-SOn-(alquilo de C1-C6), SOn-(alquilo de C1-C6), -(alquilo de C1-C6)-O-C(CN)dialquilamino, o -(alquilo de C1-C6)SOn-(alquilo de C1-C6), en donde cualquiera de los grupos es opcionalmente sustituido con 1-5 sustituyentes, en donde cada sustituyente es independientemente un halogeno, -OH, -CN, alquilo de C1-C6, cicloalquilo de C3-C6, -C(O)(heterocicloalquilo de C3-C6), -C(O)-O-(alquilo de C0-C6), -C(O)(aroiloxi), alcoxi de C1-C6, -(alquilo de C0-C6)(alquilo de C0-C6)amino, cicloalquiloxi, acilo, aciloxi, -cicloalquilo de C3-C6, heterocicloalquilo de C3-C6, arilo, heteroarilo, carbonilo, carbamoilo o SOn-(alquilo de C1-C6); A es CH, C-ester o CR4; R2 y R3 son independientemente un grupo arilo, heteroarilo, H, halogeno, -CN, alquilo de C1-C6, heterocicloalquilo de C3-C6, alcoxi de C1-C6, carbonilo, carbamoilo, -C(O)-OH, -(alquilo de C1-C6)SOn-(alquilo de C1-C6), -C(O)N(alquilo de C0-C6) (alquilo de C0-C6), o alquilacilamino de C1-C6, en donde cualquiera de los grupos es opcionalmente sustituido con 1-5 sustituyentes, en donde cada sustituyente es independientemente un grupo sustituyente arilo, heteroarilo, halogeno, -NO2, -C(O)-OH, carbonilo, -CN, alquilo de C1-C6, SOn-(alquilo de C1-C6), SOn-(arilo), ariloxi, heteroariloxi, alcoxi de C1-C6, N-oxido, -C(O)(heterocicloalquilo de C3-C6), -NH-cicloalquilo de C3-C6, amino, -OH, o -(alquilo de C0-C6)(alquilo de C0-C6)amino, -C(O)-N(alquilo de C0-C6) (alquilo de C0-C6), en donde cada sustituyente independientemente es opcionalmente sustituido con -OH, alcoxi de C1-C6, alquilo de C1-C6, cicloalquilo de C3-C6, ariloxi, -C(O)-OH, -C(O)-O-(alquilo de C1-C6), halogeno, -NO2, -CN, -SOn-(alquilo de C1-C6), o -C(O)-N(alquilo de C0-C6) (alquilo de C0-C6); uno de R2 y R3 debe ser un arilo o heteroarilo, opcionalmente sustituido; cuando R2 y R3 son ambos un arilo o heteroarilo, entonces R2 y R3 pueden ser opcionalmente conectados por un puente de tio, oxi o alquilo de C1-C4, para formar un sistema de tres anillos fusionados; son inhibidores de PDE4.
MXPA02006329A 1999-12-22 2000-12-20 8-arilquinolinas sustituidas que son inhibidores de fosfodiesterasa-4. MXPA02006329A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17152299P 1999-12-22 1999-12-22
PCT/CA2000/001559 WO2001046151A1 (en) 1999-12-22 2000-12-20 Substituted 8-arylquinoline phosphodiesterase-4 inhibitors

Publications (1)

Publication Number Publication Date
MXPA02006329A true MXPA02006329A (es) 2004-05-14

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MXPA02006329A MXPA02006329A (es) 1999-12-22 2000-12-20 8-arilquinolinas sustituidas que son inhibidores de fosfodiesterasa-4.

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EP (1) EP1244628A1 (es)
JP (1) JP3782011B2 (es)
KR (1) KR20020082839A (es)
CN (1) CN1221534C (es)
AR (1) AR029214A1 (es)
AU (1) AU778531B2 (es)
BG (1) BG65403B1 (es)
BR (1) BR0016651A (es)
CA (1) CA2393749C (es)
CO (1) CO5261613A1 (es)
CZ (1) CZ20022171A3 (es)
DZ (1) DZ3244A1 (es)
EA (1) EA004747B1 (es)
EE (1) EE200200342A (es)
GE (1) GEP20053626B (es)
HR (1) HRP20020545A2 (es)
HU (1) HUP0203896A3 (es)
IL (1) IL150114A0 (es)
IS (1) IS6413A (es)
MX (1) MXPA02006329A (es)
MY (1) MY134008A (es)
NO (1) NO20023013L (es)
NZ (1) NZ520258A (es)
PE (1) PE20010989A1 (es)
PL (1) PL355752A1 (es)
SK (1) SK8972002A3 (es)
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WO (1) WO2001046151A1 (es)
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NZ526143A (en) * 2000-12-20 2004-05-28 Merck & Co Inc Process for making substituted 8-arylquinolinium benzenesulfonate
US6740666B2 (en) * 2000-12-20 2004-05-25 Merck & Co., Inc. Substituted 8-arylquinoline phosphodiesterase-4 inhibitors
ES2242036T3 (es) 2001-06-27 2005-11-01 MERCK FROSST CANADA & CO. Inhibidores pde4 de arilquinolina 8-sustituida.
US7009055B2 (en) * 2001-07-24 2006-03-07 Merck & Co., Inc. Preparation of Sulfonyl quinoline
WO2003024488A2 (en) * 2001-09-19 2003-03-27 Altana Pharma Ag Combination of a pde inhibitor and a leukotriene receptor antagonist
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MXPA05009434A (es) * 2003-03-05 2005-11-23 Celgene Corp Compuestos de difeniletileno y usos de los mismos.
CA2560895A1 (en) * 2004-03-25 2005-10-06 Synta Pharmaceuticals Corp. Acrylonitrile derivatives for inflammation and immune-related uses
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CN102772411A (zh) 2006-07-05 2012-11-14 奈科明有限责任公司 用于治疗炎症性肺部疾病的HMG-CoA还原酶抑制剂与磷酸二酯酶4抑制剂的组合
CA2657093A1 (en) * 2006-07-07 2008-01-10 Steven P. Govek Bicyclic heteroaryl inhibitors of pde4
EP2076288A2 (en) * 2006-09-22 2009-07-08 Braincells, Inc. Combination comprising an hmg-coa reductase inhibitor and a second neurogenic agent for treating a nervous system disorder and increasing neurogenesis
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UA74815C2 (en) 2006-02-15
KR20020082839A (ko) 2002-10-31
WO2001046151A1 (en) 2001-06-28
NO20023013D0 (no) 2002-06-21
AU2336201A (en) 2001-07-03
NO20023013L (no) 2002-08-22
AR029214A1 (es) 2003-06-18
BG106840A (en) 2003-01-31
HUP0203896A2 (hu) 2003-04-28
JP3782011B2 (ja) 2006-06-07
HUP0203896A3 (en) 2003-05-28
YU47102A (sh) 2005-06-10
TWI280240B (en) 2007-05-01
BG65403B1 (bg) 2008-06-30
GEP20053626B (en) 2005-10-10
EA004747B1 (ru) 2004-08-26
EE200200342A (et) 2003-06-16
EP1244628A1 (en) 2002-10-02
HK1057560A1 (en) 2004-04-08
DZ3244A1 (fr) 2001-06-28
AU778531B2 (en) 2004-12-09
IL150114A0 (en) 2002-12-01
MY134008A (en) 2007-11-30
SK8972002A3 (en) 2002-11-06
EA200200702A1 (ru) 2003-02-27
NZ520258A (en) 2004-05-28
CA2393749A1 (en) 2001-06-28
PL355752A1 (en) 2004-05-17
BR0016651A (pt) 2002-09-10
CZ20022171A3 (cs) 2002-11-13
ZA200204862B (en) 2003-03-17
CO5261613A1 (es) 2003-03-31
CN1434801A (zh) 2003-08-06
PE20010989A1 (es) 2001-10-01
HRP20020545A2 (en) 2005-10-31
IS6413A (is) 2002-06-11
CN1221534C (zh) 2005-10-05
CA2393749C (en) 2008-06-17
JP2003531112A (ja) 2003-10-21

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