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AR018010A1 - Secretagogos de la hormona del crecimiento y compuestos intermediarios utiles en la preparacion de dichos compuestos - Google Patents

Secretagogos de la hormona del crecimiento y compuestos intermediarios utiles en la preparacion de dichos compuestos

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Publication number
AR018010A1
AR018010A1 ARP980104068A ARP980104068A AR018010A1 AR 018010 A1 AR018010 A1 AR 018010A1 AR P980104068 A ARP980104068 A AR P980104068A AR P980104068 A ARP980104068 A AR P980104068A AR 018010 A1 AR018010 A1 AR 018010A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
cyclohexyl
alkylidenyl
nhr1
Prior art date
Application number
ARP980104068A
Other languages
English (en)
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
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR018010A1 publication Critical patent/AR018010A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/30Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic 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 two 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
    • C07D207/36Oxygen or sulfur atoms
    • C07D207/402,5-Pyrrolidine-diones
    • C07D207/4162,5-Pyrrolidine-diones 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/30Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic 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 two 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
    • C07D207/42Nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/88Nitrogen atoms, e.g. allantoin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Se trata de compuestos no péptidos denominados genéricamente secretagogos que poseen actividad secretora de la hormona del crecimiento de formula (I) en laque: A es alquilo C1-6, arilo, (alquil C1-6)arilo, (alquil C1-6)(O)(alquil C1-6)arilo, -SH, -OH, indolilo, indolinilo, tienilo, benzotienilo, benzofuranilo,naftanilo, ciclohexilo, (alquil C1-6)indol-3-ilo, (alquil C1-6)benzotien-3-ilo, (alquil C1-6)naftan-2-ilo, (alquil C1-6)benzofuran-3-ilo y (alquil C1-6)ciclohexilo; B es NH2, NHR1, (alquilC1-6)-NH2, (alquil C1-6)-NHR1, (alquil C1-6)aril-NH2, (alquil C1-6)aril-NR1, (alquil C1-6)ciclohexil NH2, (alquil C1-6)ciclohexil NHR1, R1-piperidin-3-il,(alquil C1-6), R1-piperidin-2-il, (alquil C1-6), R1-piperidin-4-il (alquil C1-6), R1-quinolin-2-il,(alquil C1-6),R1-(2,4-dihidroquinolin-2-il,(alquil C1-6),R1-isoquinolin-2-il, (alquil C1-6) y R1-(2,4-dihidroisoquinolin-2-il), (alquil C1-6); R1 es hidrogeno,alquilo C1-6 (alquilC1-6)OH o (alquilidenil C1-6)(OH); R2 es alquilo C1-6 alquenilo C1-6(alquil C1-6)(O)(alquilo C1-6), C(O)-O-alquilo C1-6, arilo o (alquil C1-6)arilo; X es unenlace, alquilidenilo C1-6 O, S, NH o N(alquilo C1-6); V es un grupo de formulas (I), W es S. O, NH o CH2; Y es N o Ch; Z es N o CH; Y es N, S, CH2, O; Z esN, CH2; R4 y R5 son, de forma independiente, hidrogeno, alquilo C1-6, arilo, (alquil C1-C6)arilo, C(O)O(alquilo C1-6), C(O)ON(alquilo C1-6)2 o (alquil C1-6)COR7; R7 es hidrogeno, alquilo C1-6, pirrolidinilo, peperidinilo, homoprolina o prolina; D es C(O)R6, (alquil C1-6)OH, (alquil C1-6)C(O)R6, (alquil C1-6)R6,arilo, CH2NHSO2(alquilo C1-6), R6 es H, alquilo C1-6, arilo, (alquil C1-6)arilo, acetilo, NH2, NH(alquilo C1-6), NH(alquilidenil C1-6)OCH3, NH(alquil C1-6)arilo, N(alquilo C1-6)2, N(alquil C1-6)arilo, N(alquil C1-6)(alquil C1-6)arilo, O(alquilo C1-6), piperidinilo o piperidinilo opcionalmente sustituido,pirrolidinilo o pirrolidinilo opcionalmente sustituido, pirrolinilo o pirrolinilo opcionalmente sustituido, morfolino, hexametilenimino, heptametilenimino,quinolinilo, 2,4-dihidroquinolinilo, isoquinolinilo, 2,4-dihidroisoquinolinilo, un aminoácido seleccionado entre el grupo de prolina, homoprolina, glicina,
ARP980104068A 1997-08-19 1998-08-18 Secretagogos de la hormona del crecimiento y compuestos intermediarios utiles en la preparacion de dichos compuestos AR018010A1 (es)

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Application Number Priority Date Filing Date Title
US5614297P 1997-08-19 1997-08-19

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Publication Number Publication Date
AR018010A1 true AR018010A1 (es) 2001-10-31

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ARP980104068A AR018010A1 (es) 1997-08-19 1998-08-18 Secretagogos de la hormona del crecimiento y compuestos intermediarios utiles en la preparacion de dichos compuestos

Country Status (24)

Country Link
EP (1) EP0933365A3 (es)
JP (1) JP2001515046A (es)
KR (1) KR20010027947A (es)
CN (1) CN1243567C (es)
AR (1) AR018010A1 (es)
AU (1) AU738204B2 (es)
BR (1) BR9811948A (es)
CA (1) CA2302467A1 (es)
CO (1) CO5121066A1 (es)
EA (1) EA002746B1 (es)
HR (1) HRP20000090A2 (es)
HU (1) HUP0002392A3 (es)
ID (1) ID25000A (es)
IL (1) IL134596A0 (es)
MY (1) MY138258A (es)
NO (1) NO20000823L (es)
NZ (1) NZ502947A (es)
PE (1) PE115999A1 (es)
PL (1) PL338883A1 (es)
TR (1) TR200000930T2 (es)
TW (1) TW577879B (es)
UA (1) UA58472C2 (es)
WO (1) WO1999008699A1 (es)
ZA (1) ZA987385B (es)

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US6639076B1 (en) 1998-08-18 2003-10-28 Eli Lilly And Company Growth hormone secretagogues
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US6828331B1 (en) 1999-02-19 2004-12-07 Eli Lilly And Company Growth hormone secretagogues
US6417397B1 (en) 1999-10-04 2002-07-09 The Regents Of The University Of California, San Diego N-substituted alkylamino acids for use as amino-protecting groups
WO2001091752A1 (en) 2000-05-30 2001-12-06 Merck & Co., Inc. Melanocortin receptor agonists
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US7125840B2 (en) 2001-10-09 2006-10-24 Eli Lilly And Company Substituted dipeptides as growth hormone secretagogues
AU2003218337A1 (en) 2002-04-09 2003-10-27 Eli Lilly And Company Growth hormone secretagogues
JP2006511621A (ja) * 2002-12-18 2006-04-06 エフ エム シー コーポレーション N―(置換アリールメチル)―4―(二置換メチル)ピペリジン及びピペラジン
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US7615556B2 (en) 2006-01-27 2009-11-10 Bristol-Myers Squibb Company Piperazinyl derivatives as modulators of chemokine receptor activity
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ES2602789T3 (es) 2007-02-09 2017-02-22 Ocera Therapeutics, Inc. Productos intermedios conectores para la síntesis de moduladores macrocíclicos del receptor de la grelina
TWI433838B (zh) 2008-06-25 2014-04-11 必治妥美雅史谷比公司 作為趨化因子受體活性調節劑之六氫吡啶衍生物
US8642622B2 (en) 2010-06-16 2014-02-04 Bristol-Myers Squibb Company Piperidinyl compound as a modulator of chemokine receptor activity
UY34094A (es) 2011-05-27 2013-01-03 Novartis Ag Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina
EP2852591A1 (en) 2012-05-03 2015-04-01 Novartis AG L-malate salt of 2, 7 - diaza - spiro [4.5]dec- 7 - yle derivatives and crystalline forms thereof as ghrelin receptor agonists
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KR102179510B1 (ko) * 2014-08-29 2020-11-16 도쿄 오카 고교 가부시키가이샤 이미다졸 화합물, 금속 표면 처리액, 금속의 표면 처리 방법 및 적층체의 제조 방법
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CN107286041A (zh) * 2016-04-01 2017-10-24 成都川科化工有限公司 一种n,n-二乙基甲酰胺的制备方法
CN108299218A (zh) * 2017-01-12 2018-07-20 南京红杉生物科技有限公司 一种4-溴-d-苯丙氨酸的合成方法
CN110128285B (zh) * 2019-06-24 2022-03-01 华北制药股份有限公司 D-苯甘氨酸甲酯盐酸盐/d-二氢苯基甘氨酸甲酯盐酸盐的制备方法

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TR200000930T2 (tr) 2000-11-21
TW577879B (en) 2004-03-01
EA002746B1 (ru) 2002-08-29
AU738204B2 (en) 2001-09-13
NZ502947A (en) 2001-11-30
ZA987385B (en) 2000-04-18
JP2001515046A (ja) 2001-09-18
HRP20000090A2 (en) 2001-04-30
CA2302467A1 (en) 1999-02-25
MY138258A (en) 2009-05-29
WO1999008699A1 (en) 1999-02-25
UA58472C2 (uk) 2003-08-15
NO20000823D0 (no) 2000-02-18
EA200000239A1 (ru) 2000-10-30
ID25000A (id) 2000-09-07
BR9811948A (pt) 2000-08-22
EP0933365A3 (en) 2003-03-19
CO5121066A1 (es) 2002-01-30
CN1276727A (zh) 2000-12-13
NO20000823L (no) 2000-04-12
AU9025698A (en) 1999-03-08
KR20010027947A (ko) 2001-04-06
HUP0002392A3 (en) 2000-11-28
PE115999A1 (es) 1999-11-26
PL338883A1 (en) 2000-11-20
EP0933365A2 (en) 1999-08-04
CN1243567C (zh) 2006-03-01
IL134596A0 (en) 2001-04-30
HUP0002392A2 (hu) 2000-10-28

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