ES2152496T3 - Compuestos pentaciclicos, intermediarios, procesos, composiciones y procedimientos. - Google Patents

Compuestos pentaciclicos, intermediarios, procesos, composiciones y procedimientos.

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Publication number
ES2152496T3
ES2152496T3 ES96306351T ES96306351T ES2152496T3 ES 2152496 T3 ES2152496 T3 ES 2152496T3 ES 96306351 T ES96306351 T ES 96306351T ES 96306351 T ES96306351 T ES 96306351T ES 2152496 T3 ES2152496 T3 ES 2152496T3
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Spain
Prior art keywords
sub
sup
compounds
rent
procedures
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Expired - Lifetime
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ES96306351T
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English (en)
Inventor
Timothy Alan Grese
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Eli Lilly and Co
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Eli Lilly and Co
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Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
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Publication of ES2152496T3 publication Critical patent/ES2152496T3/es
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/20Heterocyclic 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 singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic 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 singly bound oxygen or sulphur atoms by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • C07D221/18Ring systems of four or more rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/78Ring systems having three or more relevant rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Mechanical Pencils And Projecting And Retracting Systems Therefor, And Multi-System Writing Instruments (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A COMPUESTOS DE FORMULAS I Y II; DONDE X ES -O-, -S-, O -NR{SUP,5}-; Y ES -O-, -S-, -CH{SUB,2}-, -CH{SUB,2}CH{SUB,2}-, -CH=CH-, O -NR{SUP,5}-; B ES -CH{SUB,2}- O -CO-; R{SUP,1}, R{SUP,2} Y R{SUP,3} SON CADA UNO INDEPENDIENTEMENTE -H, -OH, -O(ALQUILO C{SUB,1}-C{SUB,4}), -OCO(ALQUILO C{SUB,1}C{SUB,6}), -OSO{SUB,2}(ALQUILO C{SUB,4}-C{SUB,6}, OSO{SUB,2}CF{SUB,3}, CL O F; N ES 1 O 2; W ES CH{SUB,2} O C=O; R{SUP,4} ES 1-PIPERIDINIL, 2-OXO-1-PIPERIDINIL, 1-PIRROLIDINIL, METIL-1-PIRROLIDINIL, DIMETIL-1-PIRROLIDINIL, 2-OXO-1PIRROLIDINIL, 4-MORFOLINO, DIMETILAMINO, DIETILAMINO, O 1HEXAMETILENOIMINO; R{SUP,5} ES ALQUILO C{SUB,1}-C{SUB,3}, -COC{SUB,6}H{SUB,5}, CO(ALQUILO C{SUB,1}-C{SUB,6}), -C(O)OC{SUB,6}H{SUB,5}, -C(O)O(ALQUILO C{SUB,1}-C{SUB,6}), -SO{SUB,2}C{SUB,6}H{SUB,5}, O -SO{SUB,2}CF{SUB,3}, O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO. TAMBIEN SE PROPORCIONAN EN LA PRESENTE INVENCION COMPUESTOS INTERMEDIOS; PROCEDIMIENTOS DE PREPARACION DE LOS COMPUESTOS DE FORMULAS I Y II; Y METODOS FARMACEUTICOS Y FORMULACIONES QUE EMPLEAN DICHOS COMPUESTOS.
ES96306351T 1995-09-08 1996-09-02 Compuestos pentaciclicos, intermediarios, procesos, composiciones y procedimientos. Expired - Lifetime ES2152496T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US349695P 1995-09-08 1995-09-08

Publications (1)

Publication Number Publication Date
ES2152496T3 true ES2152496T3 (es) 2001-02-01

Family

ID=21706148

Family Applications (1)

Application Number Title Priority Date Filing Date
ES96306351T Expired - Lifetime ES2152496T3 (es) 1995-09-08 1996-09-02 Compuestos pentaciclicos, intermediarios, procesos, composiciones y procedimientos.

Country Status (25)

Country Link
US (3) US5726186A (es)
EP (1) EP0761669B1 (es)
JP (1) JP3688299B2 (es)
KR (1) KR19990044422A (es)
CN (1) CN1201392A (es)
AT (1) ATE197712T1 (es)
AU (1) AU705454B2 (es)
BR (1) BR9610356A (es)
CA (1) CA2230974A1 (es)
CZ (1) CZ286236B6 (es)
DE (1) DE69611015T2 (es)
DK (1) DK0761669T3 (es)
EA (1) EA001649B1 (es)
ES (1) ES2152496T3 (es)
GR (1) GR3035253T3 (es)
HU (1) HUP9802213A3 (es)
IL (1) IL123560A (es)
MX (1) MX9801734A (es)
NO (1) NO980936L (es)
NZ (1) NZ318183A (es)
PL (1) PL325479A1 (es)
PT (1) PT761669E (es)
SI (1) SI0761669T1 (es)
TR (1) TR199800387T1 (es)
WO (1) WO1997009044A1 (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6515009B1 (en) 1991-09-27 2003-02-04 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5811447A (en) 1993-01-28 1998-09-22 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US6251920B1 (en) 1993-05-13 2001-06-26 Neorx Corporation Prevention and treatment of cardiovascular pathologies
US6491938B2 (en) 1993-05-13 2002-12-10 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
JPH11510479A (ja) 1995-06-07 1999-09-14 ネオルックス コーポレイション タモキシフェン類似体による心臓血管疾病の予防及び治療
WO2000037083A1 (en) * 1998-12-18 2000-06-29 Schering Corporation Oral antiestrogen pharmaceutical composition
US7105679B2 (en) 2001-12-19 2006-09-12 Kanojia Ramesh M Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
US7329654B2 (en) * 2001-12-19 2008-02-12 Janssen Pharmaceutica N.V. Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
WO2004009578A2 (en) * 2002-07-24 2004-01-29 Eli Lilly And Company Pentacyclic oxepines and derivatives thereof, process for their preparation and pharmaceutical compositions containing them
WO2004009603A1 (en) * 2002-07-24 2004-01-29 Eli Lilly And Company Dihydro-dibenzo[b,e]oxepine based selective estrogen receptor modulators, compositions and methods
JP3887588B2 (ja) * 2002-08-30 2007-02-28 株式会社リガク X線回折による応力測定法
BR0314594A (pt) * 2002-09-25 2005-08-09 Lilly Co Eli Composto ou um seu sal farmaceuticamente aceitável, composição farmacêutica, método para inibir uma doença associada com deprivação de estrogênio, método para inibir uma doença associada com uma resposta fisiológica aberrante a estrogênio endógeno, e, uso de um composto
US6894061B2 (en) 2002-12-04 2005-05-17 Wyeth Substituted dihydrophenanthridinesulfonamides
US7074779B2 (en) * 2003-07-02 2006-07-11 Ortho-Mcneil Pharmaceutical, Inc. Estrieno[3,2-b]/[3,4-c]pyrrole derivatives useful as modulators of the estrogen receptors
UA85862C2 (uk) 2004-01-22 2009-03-10 Елі Ліллі Енд Компані Селективні модулятори рецепторів естрогену для лікування вазомоторних симптомів
CN1910167B (zh) * 2004-01-22 2011-08-10 伊莱利利公司 用于治疗血管舒缩症状的选择性雌激素受体调节剂
WO2005073244A1 (en) * 2004-01-22 2005-08-11 Eli Lilly And Company Selective estrogen receptor modulators
KR20150039882A (ko) 2010-06-16 2015-04-13 앙도르쉐르슈 인코포레이티드 에스트로겐-관련 질병의 치료 또는 예방 방법
WO2013064206A1 (de) * 2011-11-01 2013-05-10 Merck Patent Gmbh Organische elektrolumineszenzvorrichtung
US8829993B2 (en) 2012-10-30 2014-09-09 Eta Devices, Inc. Linearization circuits and methods for multilevel power amplifier systems
CN109678878A (zh) * 2019-02-27 2019-04-26 陕西科技大学 一种苯并噻吩并香豆素类化合物及其合成方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2884427A (en) * 1958-01-22 1959-04-28 Oliver H Emerson Synthesis of coumestrol and its esters
US2987398A (en) * 1958-05-12 1961-06-06 Emanuel M Bickoff Coumestrol ethers and use thereof
US3912740A (en) * 1974-02-28 1975-10-14 Us Health Method for the preparation of oxygenated benzo{8 c{9 phenanthridine compounds
US4230862A (en) * 1975-10-28 1980-10-28 Eli Lilly And Company Antifertility compounds
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
US4659671A (en) * 1983-07-01 1987-04-21 Massachusetts Institute Of Technology Enzymatic separation of racemic mixtures of hydroxy compounds
CA2054569A1 (en) * 1990-11-07 1992-05-08 Masanobu Suzuki Process for preparing benzo¬c|phenanthridinium derivatives, and novel compounds prepared by said process
US5147880A (en) * 1991-07-22 1992-09-15 Eli Lilly And Company Benzo[a]fluorene compounds
TW366342B (en) * 1992-07-28 1999-08-11 Lilly Co Eli The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
US5336687A (en) * 1993-08-04 1994-08-09 American Home Products Corporation Inhibition of bone loss by 4-aryloxy-5-hydroxy-2(5H)-furanones

Also Published As

Publication number Publication date
KR19990044422A (ko) 1999-06-25
DE69611015D1 (de) 2000-12-28
NZ318183A (en) 1998-09-24
US6004971A (en) 1999-12-21
SI0761669T1 (en) 2001-04-30
NO980936D0 (no) 1998-03-04
BR9610356A (pt) 1999-07-06
IL123560A (en) 2002-02-10
DE69611015T2 (de) 2001-05-10
ATE197712T1 (de) 2000-12-15
GR3035253T3 (en) 2001-04-30
US5726186A (en) 1998-03-10
AU705454B2 (en) 1999-05-20
CZ67898A3 (cs) 1998-06-17
JP3688299B2 (ja) 2005-08-24
TR199800387T1 (xx) 1998-05-21
NO980936L (no) 1998-05-07
PT761669E (pt) 2001-04-30
EA001649B1 (ru) 2001-06-25
US6133288A (en) 2000-10-17
CN1201392A (zh) 1998-12-09
EP0761669A2 (en) 1997-03-12
EP0761669A3 (en) 1997-10-29
CA2230974A1 (en) 1997-03-13
PL325479A1 (en) 1998-07-20
JPH11514347A (ja) 1999-12-07
EA199800278A1 (ru) 1998-08-27
EP0761669B1 (en) 2000-11-22
IL123560A0 (en) 1998-10-30
HUP9802213A2 (hu) 1999-02-01
WO1997009044A1 (en) 1997-03-13
AU6959096A (en) 1997-03-27
CZ286236B6 (cs) 2000-02-16
HUP9802213A3 (en) 2000-03-28
MX9801734A (es) 1998-08-30
DK0761669T3 (da) 2000-12-11

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