ATE304532T1 - Inhibitoren von serin proteasen - Google Patents

Inhibitoren von serin proteasen

Info

Publication number
ATE304532T1
ATE304532T1 AT01940716T AT01940716T ATE304532T1 AT E304532 T1 ATE304532 T1 AT E304532T1 AT 01940716 T AT01940716 T AT 01940716T AT 01940716 T AT01940716 T AT 01940716T AT E304532 T1 ATE304532 T1 AT E304532T1
Authority
AT
Austria
Prior art keywords
inhibitors
sub
serine proteases
factor
compounds
Prior art date
Application number
AT01940716T
Other languages
English (en)
Inventor
John Walter Liebeschuetz
Christopher William Murray
Stephen Clinton Young
Nicholas Paul Camp
Stuart Donald Jones
William Alexander Wylie
John Joseph Masters
Michael Robert Wiley
Scott Martin Sheehan
David Birenbaum Engel
Brian Morgan Watson
Original Assignee
Lilly Co Eli
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
Priority claimed from PCT/GB2000/002302 external-priority patent/WO2000076971A2/en
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Application granted granted Critical
Publication of ATE304532T1 publication Critical patent/ATE304532T1/de

Links

Classifications

    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—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 no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • C07D401/06—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 only aliphatic carbon 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
    • C07D401/02—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
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
AT01940716T 2000-06-13 2001-06-12 Inhibitoren von serin proteasen ATE304532T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/GB2000/002302 WO2000076971A2 (en) 1999-06-14 2000-06-13 Serine protease inhibitors
GBGB0030305.7A GB0030305D0 (en) 2000-12-13 2000-12-13 Compounds
PCT/GB2001/002551 WO2001096303A1 (en) 2000-06-13 2001-06-12 Serine protease inhibitors

Publications (1)

Publication Number Publication Date
ATE304532T1 true ATE304532T1 (de) 2005-09-15

Family

ID=9904938

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01940716T ATE304532T1 (de) 2000-06-13 2001-06-12 Inhibitoren von serin proteasen

Country Status (8)

Country Link
US (2) US7053078B2 (de)
EP (1) EP1289954B1 (de)
AT (1) ATE304532T1 (de)
AU (1) AU2001274220A1 (de)
DE (1) DE60113412T2 (de)
ES (1) ES2248341T3 (de)
GB (1) GB0030305D0 (de)
WO (1) WO2001096303A1 (de)

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DE60224805T2 (de) 2001-07-26 2009-01-22 Eli Lilly And Co., Indianapolis 1-glycinyl-4-(1-methylpiperidin-4-yl)piperazine und -piperidine als faktor-xa-antagonisten
MY130373A (en) * 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
ES2242086T3 (es) * 2001-12-12 2005-11-01 Eli Lilly And Company Ciertos derivados de glicina como inhibidores del factor xa para el tratamiento de trastornos tromboticos.
WO2003074478A1 (en) 2002-03-05 2003-09-12 Sumitomo Chemical Company, Limited Process for the preparation of biaryl compounds
BR0308870A (pt) 2002-04-01 2005-01-04 Lilly Co Eli Composto, composição farmacêutica, processo para preparar um composto, uso de um composto, e método para tratar um distúrbio trombótico em um paciente
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
EP1581493A1 (de) 2002-12-30 2005-10-05 Eli Lilly And Company Faktor-xa-inhibitoren
US7157471B2 (en) * 2003-08-25 2007-01-02 Boehringer Ingelheim International Gmbh Haloalkyl- and piperidine-substituted benzimidazole-derivatives
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
CA2564207A1 (en) * 2004-05-13 2005-11-24 Boehringer Ingelheim International Gmbh Novel substituted thiophenecarboxamides, their production and their use as medicaments
WO2005111013A1 (de) * 2004-05-13 2005-11-24 Boehringer Ingelheim International Gmbh Substituierte thiophen-2-carbonsäureamide, deren herstellung und deren verwendung als arzneimittel
DE102004047840A1 (de) * 2004-09-29 2006-03-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Thiophencarbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel
US20060079522A1 (en) * 2004-10-08 2006-04-13 Marzabadi Mohammad R Amino substituted aryloxybenzylpiperidine derivatives
EP1724269A1 (de) 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroarylcarbonsäure-sulfamoylalkylamidderivate als Faktor Xa-Inhibitoren
US20090012010A1 (en) * 2007-05-18 2009-01-08 Neuromed Phramaceuticals Ltd. Amino acid derivatives as calcium channel blockers
CA2722923C (en) * 2008-04-29 2016-08-02 Boehringer Ingelheim International Gmbh Indazole compounds as ccr1 receptor antagonists
CA2722811C (en) * 2008-05-06 2016-07-05 Boehringer Ingelheim International Gmbh Pyrazole compounds as ccr1 antagonists
NZ591115A (en) * 2008-09-26 2012-10-26 Boehringer Ingelheim Int Azaindazole compounds as ccr1 receptor antagonists
PH12012500775A1 (en) 2009-10-21 2012-11-26 Boehringer Ingelheim Int Indazole and pyrazolopyridine compounds as ccr1 receptor antagonists
US8927550B2 (en) 2009-10-27 2015-01-06 Boehringer Ingelheim International Gmbh Heterocyclic compounds as CCR1 receptor antagonists
WO2011071730A1 (en) * 2009-12-08 2011-06-16 Boehringer Ingelheim International Gmbh Process for synthesis of intermediates useful for making substituted indazole and azaindazole compounds
US8871786B2 (en) 2010-04-30 2014-10-28 Boehringer Ingelheim International Gmbh Azaindazole amide compounds as CCR1 receptor antagonists
WO2012087782A1 (en) 2010-12-23 2012-06-28 Boehringer Ingelheim International Gmbh Pyrazolopiperidine compounds as ccr1 receptor antagonists
ES2896487T3 (es) 2016-09-01 2022-02-24 Mebias Discovery Llc Derivados de urea sustituidos para el tratamiento del dolor
KR102603671B1 (ko) 2017-01-17 2023-11-17 메비아스 디스커버리 인코포레이티드 치환된 3-디알킬아미노메틸-피페리딘-4-일-벤즈아미드 및 이를 제조 및 사용하는 방법
BR112022001054A2 (pt) * 2019-08-21 2022-03-15 Kalvista Pharmaceuticals Ltd Inibidores enzimáticos
CN112409199B (zh) * 2020-11-26 2022-07-12 山东普洛汉兴医药有限公司 一种氨基酸甲酯连续化生产工艺及装置

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US5346907A (en) * 1988-04-05 1994-09-13 Abbott Laboratories Amino acid analog CCK antagonists
IE902295A1 (en) 1989-07-07 1991-01-16 Abbott Lab Amino acid analog cck antagonists
CA2200163A1 (en) 1996-03-22 1997-09-22 Michael Robert Wiley Antithrombotic diamides
JP2000514788A (ja) 1996-06-25 2000-11-07 イーライ・リリー・アンド・カンパニー 抗凝固剤
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
ES2241151T3 (es) 1997-06-26 2005-10-16 Eli Lilly And Company Agentes antitromboticos.
EP1007037A4 (de) 1997-06-26 2004-10-06 Lilly Co Eli Antithrombose mittel
JP2002512633A (ja) 1997-06-26 2002-04-23 イーライ・リリー・アンド・カンパニー 抗血栓剤
US6313151B1 (en) 1997-06-26 2001-11-06 Eli Lilly And Company Antithrombotic agents
WO2000077027A2 (en) 1999-06-14 2000-12-21 Tularik Limited Serine protease inhibitors
US6262069B1 (en) * 1997-08-29 2001-07-17 Protherics Molecular Design Limited 1-amino-7-isoquinoline derivatives as serine protease inhibitors
SK285729B6 (sk) * 1997-11-18 2007-07-06 Teijin Pharma Limited Zlúčenina derivátov cyklických amínov a jej použitie
AU2055500A (en) 1998-12-23 2000-07-31 Eli Lilly And Company Aromatic amides
CA2358095A1 (en) 1998-12-23 2000-07-06 Eli Lilly And Company Heteroroaromatic amides as inhibitor of factor xa
JP2004522689A (ja) 1998-12-23 2004-07-29 イーライ・リリー・アンド・カンパニー 抗血栓アミド類
AU2364000A (en) 1998-12-24 2000-07-31 Eli Lilly And Company Heterocyclic amides as inhibitors of factor xa
CA2374947A1 (en) 1999-05-24 2000-11-30 Robert M. Scarborough Inhibitors of factor xa
JP2003500382A (ja) 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Ｘａ因子の阻害剤
JP2003502314A (ja) 1999-06-14 2003-01-21 イーライ・リリー・アンド・カンパニー 化合物

Also Published As

Publication number Publication date
US20040259868A1 (en) 2004-12-23
DE60113412T2 (de) 2006-06-29
EP1289954B1 (de) 2005-09-14
GB0030305D0 (en) 2001-01-24
AU2001274220A1 (en) 2001-12-24
ES2248341T3 (es) 2006-03-16
US6900196B2 (en) 2005-05-31
DE60113412D1 (de) 2005-10-20
US7053078B2 (en) 2006-05-30
EP1289954A1 (de) 2003-03-12
WO2001096303A1 (en) 2001-12-20
US20030109706A1 (en) 2003-06-12

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