DK1272505T3 - 8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater - Google Patents

8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater

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Publication number
DK1272505T3
DK1272505T3 DK01940331T DK01940331T DK1272505T3 DK 1272505 T3 DK1272505 T3 DK 1272505T3 DK 01940331 T DK01940331 T DK 01940331T DK 01940331 T DK01940331 T DK 01940331T DK 1272505 T3 DK1272505 T3 DK 1272505T3
Authority
DK
Denmark
Prior art keywords
sup
8beta
11beta
substituted
compounds
Prior art date
Application number
DK01940331T
Other languages
Danish (da)
English (en)
Inventor
Alexander Hillisch
Karl-Heinrich Fritzemeier
Olaf Peters
Nico Braeuer
Christa Hegele-Hartung
Original Assignee
Schering Ag
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 DE10019167A external-priority patent/DE10019167A1/de
Application filed by Schering Ag filed Critical Schering Ag
Application granted granted Critical
Publication of DK1272505T3 publication Critical patent/DK1272505T3/da

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P25/20—Hypnotics; Sedatives
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
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    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P9/10—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
    • 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
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0062—Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074—Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Toxicology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pregnancy & Childbirth (AREA)
  • Anesthesiology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DK01940331T 2000-04-12 2001-04-12 8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater DK1272505T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10019167A DE10019167A1 (de) 2000-04-12 2000-04-12 Substituierte Estratriene als selektiv wirksame Estrogene
US20737000P 2000-05-26 2000-05-26

Publications (1)

Publication Number Publication Date
DK1272505T3 true DK1272505T3 (da) 2005-11-07

Family

ID=26005365

Family Applications (2)

Application Number Title Priority Date Filing Date
DK01940331T DK1272505T3 (da) 2000-04-12 2001-04-12 8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater
DK01931609T DK1272504T3 (da) 2000-04-12 2001-04-12 8.Beta-hydrocarbylsubstituerede östradiener til anvendelse som selektive östrogener

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK01931609T DK1272504T3 (da) 2000-04-12 2001-04-12 8.Beta-hydrocarbylsubstituerede östradiener til anvendelse som selektive östrogener

Country Status (26)

Country Link
US (3) US7378404B2 (fr)
EP (2) EP1272505B1 (fr)
JP (2) JP3828423B2 (fr)
CN (1) CN100453549C (fr)
AT (2) ATE302790T1 (fr)
AU (3) AU5834101A (fr)
BG (1) BG107173A (fr)
BR (1) BR0109983A (fr)
CA (1) CA2406177C (fr)
CZ (1) CZ20023382A3 (fr)
DE (1) DE50112561D1 (fr)
DK (2) DK1272505T3 (fr)
EA (1) EA006299B1 (fr)
EE (1) EE200200589A (fr)
ES (2) ES2287127T3 (fr)
HK (1) HK1057219A1 (fr)
HR (1) HRP20020892B1 (fr)
HU (1) HUP0300335A2 (fr)
IL (2) IL152248A0 (fr)
MX (1) MXPA02010066A (fr)
NO (2) NO325337B1 (fr)
NZ (1) NZ543724A (fr)
PL (1) PL207488B1 (fr)
PT (1) PT1272504E (fr)
SK (1) SK14632002A3 (fr)
WO (2) WO2001077139A1 (fr)

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CZ20023382A3 (cs) * 2000-04-12 2003-02-12 Schering Aktiengesellschaft Substituované estratrieny jako selektivně účinné estrogeny
DE10027887A1 (de) 2000-05-31 2001-12-13 Jenapharm Gmbh Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
DE10039199A1 (de) * 2000-08-10 2002-02-21 Schering Ag Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen
GB0020498D0 (en) 2000-08-18 2000-10-11 Sterix Ltd Compound
DE10151363A1 (de) * 2001-10-17 2003-05-08 Schering Ag Somatotrope Therapie
DE10226326A1 (de) * 2002-06-11 2004-01-15 Schering Ag 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
ES2315455T3 (es) * 2003-03-27 2009-04-01 Pantarhei Bioscience B.V. Uso de estrogenos para el tratamiento de infertilidad en maniferos machos.
DE10318896A1 (de) * 2003-04-22 2004-11-25 Schering Ag 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene
DK1689410T3 (da) * 2003-11-26 2008-09-08 Bayer Schering Pharma Ag Forebyggelse og behandling af hypertensive hjertesygdomme ved de selektive östrogener 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol og 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057225A1 (de) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
DE102005057224A1 (de) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
EP2014672A1 (fr) * 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft Estratriènes 8 bêta substitués servant d'oestrogènes sélectivement actifs
MX2010008945A (es) * 2008-02-13 2010-09-07 Bayer Schering Pharma Ag Sistema de administracion de drogas con efecto estabilizante.
EP2249803A2 (fr) * 2008-02-13 2010-11-17 Bayer Schering Pharma Aktiengesellschaft Système de distribution de médicaments contenant de l'oestradiol
EP2143432A1 (fr) 2008-07-11 2010-01-13 Bayer Schering Pharma AG Dérivés d'estratriènes 9-alpha en tant que ligands sélectifs ER-beta pour la prévention et le traitement du cancer intestinal
WO2010057594A1 (fr) * 2008-11-21 2010-05-27 Bayer Schering Pharma Aktiengesellschaft Système d'administration de médicament
PT2782584T (pt) 2011-11-23 2021-09-02 Therapeuticsmd Inc Preparações e terapias de substituição para hormonoterapias naturais combinadas
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
CA2947767A1 (fr) 2014-05-22 2015-11-26 Therapeuticsmd, Inc. Formulations d'hormones substitutives combinees naturelles et traitement hormonal substitutif
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
WO2017173044A1 (fr) 2016-04-01 2017-10-05 Therapeuticsmd Inc. Compositions d'hormones stéroïdes dans des huiles à chaîne moyenne
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CA2406177A1 (fr) 2001-10-18
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PL207488B1 (pl) 2010-12-31
CA2406177C (fr) 2010-06-22
SK14632002A3 (sk) 2003-03-04
NO20024907D0 (no) 2002-10-11
BR0109983A (pt) 2003-02-25
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IL152248A0 (en) 2003-05-29
US20030176405A1 (en) 2003-09-18
EA200201052A1 (ru) 2003-04-24
BG107173A (bg) 2003-05-30
ATE302790T1 (de) 2005-09-15
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ES2287127T3 (es) 2007-12-16
HK1057219A1 (en) 2004-03-19
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