PE20000276A1 - Derivados fusionados de pirrolidina o piperidina con un anillo de oxazol y procedimiento para su preparacion - Google Patents

Derivados fusionados de pirrolidina o piperidina con un anillo de oxazol y procedimiento para su preparacion

Info

Publication number
PE20000276A1
PE20000276A1 PE1999000101A PE00010199A PE20000276A1 PE 20000276 A1 PE20000276 A1 PE 20000276A1 PE 1999000101 A PE1999000101 A PE 1999000101A PE 00010199 A PE00010199 A PE 00010199A PE 20000276 A1 PE20000276 A1 PE 20000276A1
Authority
PE
Peru
Prior art keywords
pyrrolidine
alcoxyl
procedure
preparation
piperidine
Prior art date
Application number
PE1999000101A
Other languages
English (en)
Inventor
Bernd Buttelmann
Alexander Alanine
Emmanuel Pinard
Marie-Paule Heitz Neidhart
Rene Wyler
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20000276A1 publication Critical patent/PE20000276A1/es

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Classifications

    • 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
    • C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE AL USO DE DERIVADOS DE PIRROLIDINA Y PIPERIDINA DE FORMULAS I Y II; R1 Y R2 SON H, ALCOXILO, HIDROXILO, HALOGENO, ENTRE OTROS; R3 Y R4 SON H, ALCOXILO, BENCILOXILO, HALOGENO, ENTRE OTROS; R5 ES H, ALQUILO; X E Y SON -CH(OH)-, -(CH2)n, -C(O)-, -CH(ALCOXILO)-; m, n Y p SON 1 o 2. SON COMPUESTOS PREFERIDOS 4-[(RS)-HIDROXI-[(2SR, 5RS)-5-FENETIL-PIRROLIDIN-2-IL]-METIL]-FENOL; (1RS,5SR,7aRS)-4-(5-FENETIL-TETRAHIDRO-PIRROLO[1,2-c]OXAZOL-1-IL)FENOL, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON BLOQUEADORES SELECTIVOS DE RECEPTORES DE NMDA (METIL-D-ASPARTATO), LOS QUE MODULAN LA ACTIVIDAD NEURONAL Y PLASTICIDAD Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE NEURODEGENERACION CAUSADA POR ATAQUE O TRAUMA RECEREBRAL, FORMAS CRONICAS DE NEURODEGENERACION TAL COMO ENFERMEDAD DE ALZHEIMER, ENFERMEDAD DE PARKINSON, ENFERMEDAD DE HUNTINGTON, ESCLEROSIS LATERAL AMIOTROFICA, ESQUIZOFRENIA, ANSIEDAD Y DEPRESION
PE1999000101A 1998-02-10 1999-02-08 Derivados fusionados de pirrolidina o piperidina con un anillo de oxazol y procedimiento para su preparacion PE20000276A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP98102246 1998-02-10

Publications (1)

Publication Number Publication Date
PE20000276A1 true PE20000276A1 (es) 2000-04-18

Family

ID=8231382

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1999000101A PE20000276A1 (es) 1998-02-10 1999-02-08 Derivados fusionados de pirrolidina o piperidina con un anillo de oxazol y procedimiento para su preparacion

Country Status (28)

Country Link
US (2) US6015824A (es)
EP (1) EP0937458B1 (es)
JP (1) JP3142527B2 (es)
KR (1) KR100319249B1 (es)
CN (1) CN1144789C (es)
AR (1) AR018077A1 (es)
AT (1) ATE285766T1 (es)
AU (1) AU748335B2 (es)
BR (1) BR9900742A (es)
CA (1) CA2260698A1 (es)
CZ (1) CZ41099A3 (es)
DE (1) DE69922858T2 (es)
DK (1) DK0937458T3 (es)
ES (1) ES2245808T3 (es)
HR (1) HRP990042A2 (es)
HU (1) HUP9900275A3 (es)
ID (1) ID23456A (es)
IL (2) IL128389A0 (es)
MA (1) MA26607A1 (es)
NO (1) NO990609L (es)
NZ (1) NZ334081A (es)
PE (1) PE20000276A1 (es)
PL (1) PL331336A1 (es)
PT (1) PT937458E (es)
SG (1) SG74120A1 (es)
TR (1) TR199900286A2 (es)
YU (1) YU5899A (es)
ZA (1) ZA991038B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2793245B1 (fr) * 1999-05-05 2002-10-11 Adir Nouveaux composes pyridiniques ou piperidiniques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6369078B1 (en) * 1999-08-31 2002-04-09 J. Phillip Bowen Solenopsin derivatives and analogues as fire ant suppressants
EP1278728B1 (en) * 2000-04-20 2004-08-25 F. Hoffmann-La Roche Ag Pyrrolidine and piperidine derivatives and their use for the treatment of neurodegenerative disorders
WO2002050070A2 (en) 2000-12-21 2002-06-27 Warner-Lambert Company Llc Piperidine derivatives as subtype selective n-methyl-d-aspartate antagonists
MXPA02002749A (es) 2001-03-27 2002-10-28 Warner Lambert Co Derivados de ciclohexilamina como antagonistas del subtipo selectivo del n-metil-d-aspartato.
US7005432B2 (en) 2002-05-16 2006-02-28 Hoffman-La Roche Inc. Substituted imidazol-pyridazine derivatives
JP2011516417A (ja) * 2008-03-27 2011-05-26 エヴォテック・ノイロサイエンシーズ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング Ｎｍｄａｎｒ２ｂ−サブタイプ選択的アンタゴニストを使用する障害の処置方法
IN2012DN00971A (es) * 2009-08-27 2015-04-10 Merck Sharp & Dohme
EP2470021B1 (en) * 2009-08-27 2014-10-22 Merck Sharp & Dohme Corp. Novel pyrrolidine derived beta 3 adrenergic receptor agonists

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3941796A (en) * 1970-05-21 1976-03-02 Minnesota Mining And Manufacturing Company α-(Hydroxy and alkoxy substituted)phenyl-α-(2-piperidinyl)-methanols
US4407670A (en) * 1980-02-28 1983-10-04 National Research Development Corporation Biocidal compounds and compositions
US4342692A (en) * 1980-10-20 1982-08-03 Usv Pharmaceutical Corporation Pyrrolidines
ZA825227B (en) * 1981-07-22 1984-03-28 Syntex Inc Substituted pyrrolidine cardiovascular system regulators antihypertensives
CA1227490A (en) * 1983-01-24 1987-09-29 Joseph M. Muchowski ¬(3,4-METHYLENEDIOXY) PHENETHYL|-5-¬ 3- CARBOXAMIDO-4-HYDROXY)-.alpha.-HYDROXYBENZYL| PYRROLIDINES
JPS59161380A (ja) * 1983-01-24 1984-09-12 シンテツクス・（ユ−・エス・エイ）・インコ−ポレ−テツド ±２−〔（３，４−メチレンジオキシ）フエネチル〕−５−〔（３−カルボキシアミド−４−ヒドロキシ）−α−ヒドロキシベンジル〕ピロリジン類
US4569941A (en) * 1983-03-21 1986-02-11 Usv Pharmaceutical Corp. Method of using phenyl-alkylene-2-pyridyl derivatives to increase cardiac contractility in a mammal
US4548951A (en) * 1983-04-21 1985-10-22 Syntex (U.S.A.) Inc. Hypotensive benzoxathiole pyrrolidines
US4558066A (en) * 1984-05-17 1985-12-10 Syntex (U.S.A.) Inc. Treatment and prevention of ocular hypertension
US4632929A (en) * 1985-01-17 1986-12-30 Usv Pharmaceutical Corp. Method of hypertensive treatment using phenyl-alkylene-2-pyridyl derivatives

Also Published As

Publication number Publication date
CA2260698A1 (en) 1999-08-10
ID23456A (id) 2000-04-27
IL144456A0 (en) 2002-05-23
ES2245808T3 (es) 2006-01-16
EP0937458A3 (en) 2001-05-23
IL128389A0 (en) 2000-01-31
ATE285766T1 (de) 2005-01-15
EP0937458A2 (en) 1999-08-25
CN1144789C (zh) 2004-04-07
US6015824A (en) 2000-01-18
DK0937458T3 (da) 2005-05-17
NO990609L (no) 1999-08-11
AU748335B2 (en) 2002-05-30
AR018077A1 (es) 2001-10-31
ZA991038B (en) 1999-08-10
TR199900286A3 (tr) 1999-09-21
KR19990072459A (ko) 1999-09-27
HUP9900275A2 (hu) 1999-12-28
CZ41099A3 (cs) 1999-09-15
HU9900275D0 (en) 1999-04-28
BR9900742A (pt) 2000-05-09
CN1232025A (zh) 1999-10-20
DE69922858D1 (de) 2005-02-03
NZ334081A (en) 2000-07-28
HUP9900275A3 (en) 2001-08-28
DE69922858T2 (de) 2006-04-13
PT937458E (pt) 2005-04-29
AU1635499A (en) 1999-08-26
JP2000063384A (ja) 2000-02-29
SG74120A1 (en) 2000-07-18
JP3142527B2 (ja) 2001-03-07
KR100319249B1 (ko) 2002-01-05
TR199900286A2 (xx) 1999-09-21
US6153624A (en) 2000-11-28
MA26607A1 (fr) 2004-12-20
PL331336A1 (en) 1999-08-16
NO990609D0 (no) 1999-02-09
EP0937458B1 (en) 2004-12-29
HRP990042A2 (en) 2000-02-29
YU5899A (sh) 2001-07-10

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