CN100364971C - 作为因子Xa抑制剂的吡咯烷-2-酮类 - Google Patents

作为因子Xa抑制剂的吡咯烷-2-酮类 Download PDF

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Publication number
CN100364971C
CN100364971C CNB028282248A CN02828224A CN100364971C CN 100364971 C CN100364971 C CN 100364971C CN B028282248 A CNB028282248 A CN B028282248A CN 02828224 A CN02828224 A CN 02828224A CN 100364971 C CN100364971 C CN 100364971C
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China
Prior art keywords
fluoro
oxopyrrolidin
chloro
sulfonamide
alkyl
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Expired - Fee Related
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CNB028282248A
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English (en)
Chinese (zh)
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CN1620434A (zh
Inventor
艾伦·D·博思威克
陈�全
亨利·A·凯利
奈杰尔·P·金
萨瓦斯·克莱恩索斯
安德鲁·M·马森
伊凡·L·平托
德里克·R·波拉德
斯蒂芬·森杰
吉塔·P·沙
奈杰尔·S·沃森
罗伯特·J·扬
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Glaxo Group Ltd
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Glaxo Group Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • 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
    • 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
    • A61P25/28—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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D409/12—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 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • 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
    • C07D417/04—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 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CNB028282248A 2001-12-21 2002-12-20 作为因子Xa抑制剂的吡咯烷-2-酮类 Expired - Fee Related CN100364971C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0130705.7A GB0130705D0 (en) 2001-12-21 2001-12-21 Chemical compounds
GB0130705.7 2001-12-21

Publications (2)

Publication Number Publication Date
CN1620434A CN1620434A (zh) 2005-05-25
CN100364971C true CN100364971C (zh) 2008-01-30

Family

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CNB028282248A Expired - Fee Related CN100364971C (zh) 2001-12-21 2002-12-20 作为因子Xa抑制剂的吡咯烷-2-酮类

Country Status (23)

Country Link
US (1) US20050059726A1 (https=)
EP (1) EP1456172A1 (https=)
JP (1) JP2005519885A (https=)
KR (1) KR20040072666A (https=)
CN (1) CN100364971C (https=)
AR (1) AR037928A1 (https=)
AU (1) AU2002366747A1 (https=)
BR (1) BR0215200A (https=)
CA (1) CA2471461A1 (https=)
CO (1) CO5590896A2 (https=)
GB (1) GB0130705D0 (https=)
HU (1) HUP0500137A2 (https=)
IL (1) IL162454A0 (https=)
IS (1) IS7316A (https=)
MX (1) MXPA04006139A (https=)
MY (1) MY141579A (https=)
NO (1) NO20042990L (https=)
NZ (1) NZ533129A (https=)
PL (1) PL371008A1 (https=)
RU (1) RU2318807C2 (https=)
TW (1) TWI262075B (https=)
WO (1) WO2003053925A1 (https=)
ZA (1) ZA200404147B (https=)

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Publication number Priority date Publication date Assignee Title
TW200307667A (en) 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
GB0314299D0 (en) * 2003-06-19 2003-07-23 Glaxo Group Ltd Chemical compounds
GB0314373D0 (en) * 2003-06-19 2003-07-23 Glaxo Group Ltd Chemical compounds
EP1641752A1 (en) 2003-06-19 2006-04-05 Glaxo Group Limited 3- sulfonylamino- pyrrolidine- 2- one derivatives as inhibitors of factor xa
GB0314370D0 (en) * 2003-06-19 2003-07-23 Glaxo Group Ltd Chemical compounds
US7169795B2 (en) 2003-09-30 2007-01-30 Bristol Myers Squibb Company Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
US7381728B2 (en) 2004-07-28 2008-06-03 Glaxo Group Limited Piperazine derivatives useful for the treatment of gastrointestinal disorders
DE102004062544A1 (de) 2004-12-24 2006-07-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Pyrrolidinone, deren Herstellung und deren Verewendung als Arzneimittel
DE102005008649A1 (de) 2005-02-25 2006-09-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Pyrrolidinone, deren Herstellung und deren Verwendung als Arzneimittel
EP1869010A1 (en) * 2005-04-11 2007-12-26 Glaxo Group Limited 3-sulfonylamino-pyrrolidine-2-one derivatives as factor xa inhibitors
WO2006137527A1 (ja) 2005-06-23 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. チアゾール誘導体
DK1921077T3 (en) 2005-08-02 2017-10-23 Kyowa Hakko Kirin Co Ltd Means for treating and / or preventing sleep disorders
US7622492B2 (en) 2005-08-31 2009-11-24 Hoffmann-La Roche Inc. Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase
JP2009517351A (ja) * 2005-11-24 2009-04-30 グラクソ グループ リミテッド 化学物質
DK2012839T3 (da) 2006-04-07 2012-04-10 Bactiguard Ab Hidtil ukendte antimikrobielle substrater og anvendelser deraf
KR20090053923A (ko) * 2006-09-22 2009-05-28 노파르티스 아게 헤테로시클릭 유기 화합물
CN116003280B (zh) * 2022-12-30 2024-11-19 合肥工业大学 一种芳基甲酰胺类化合物的光化学合成方法
CN116712596A (zh) * 2023-05-30 2023-09-08 北京福爱乐科技发展有限公司 一种用于体内创面喷涂型医用胶及其制备方法

Citations (1)

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WO1999064397A1 (en) * 1998-06-11 1999-12-16 G.D. Searle & Co. DOUBLE PRODRUGS OF POTENT GPIIb/IIIa ANTAGONISTS

Family Cites Families (10)

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US5202344A (en) * 1990-12-11 1993-04-13 G. D. Searle & Co. N-substituted lactams useful as cholecystokinin antagonists
SI9520044B (sl) * 1994-04-26 2004-08-31 Aventis Pharmaceuticals Inc. Inhibitorji Xa faktorja
US6034093A (en) * 1995-06-07 2000-03-07 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds
US5731315A (en) * 1995-06-07 1998-03-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted sulfonic acid n- (aminoiminomethyl)phenylalkyl!-azaheterocyclamide compounds
AU4064597A (en) * 1996-08-16 1998-03-06 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
GB9715894D0 (en) * 1997-07-29 1997-10-01 Zeneca Ltd Heterocyclic derivatives
US6403632B1 (en) * 2000-03-01 2002-06-11 Bristol Myers Squibb Pharma Co Lactam metalloprotease inhibitors
GB0114005D0 (en) * 2001-06-08 2001-08-01 Glaxo Group Ltd Chemical compounds
TW200307667A (en) * 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
US7169795B2 (en) * 2003-09-30 2007-01-30 Bristol Myers Squibb Company Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999064397A1 (en) * 1998-06-11 1999-12-16 G.D. Searle & Co. DOUBLE PRODRUGS OF POTENT GPIIb/IIIa ANTAGONISTS

Also Published As

Publication number Publication date
WO2003053925A1 (en) 2003-07-03
US20050059726A1 (en) 2005-03-17
JP2005519885A (ja) 2005-07-07
MXPA04006139A (es) 2004-11-01
TWI262075B (en) 2006-09-21
IL162454A0 (en) 2005-11-20
GB0130705D0 (en) 2002-02-06
NZ533129A (en) 2006-12-22
EP1456172A1 (en) 2004-09-15
CA2471461A1 (en) 2003-07-03
KR20040072666A (ko) 2004-08-18
AU2002366747A1 (en) 2003-07-09
IS7316A (is) 2004-06-16
RU2004122427A (ru) 2006-01-20
HUP0500137A2 (en) 2006-02-28
NO20042990L (no) 2004-09-20
AR037928A1 (es) 2004-12-22
CO5590896A2 (es) 2005-12-30
CN1620434A (zh) 2005-05-25
BR0215200A (pt) 2004-10-13
PL371008A1 (en) 2005-06-13
ZA200404147B (en) 2005-06-21
MY141579A (en) 2010-05-14
RU2318807C2 (ru) 2008-03-10
TW200306178A (en) 2003-11-16

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