PE20011215A1 - STRATRENS SUBSTITUTED AS SELECTIVELY ACTIVE ESTROGENS - Google Patents

STRATRENS SUBSTITUTED AS SELECTIVELY ACTIVE ESTROGENS

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Publication number
PE20011215A1
PE20011215A1 PE2001000335A PE2001000335A PE20011215A1 PE 20011215 A1 PE20011215 A1 PE 20011215A1 PE 2001000335 A PE2001000335 A PE 2001000335A PE 2001000335 A PE2001000335 A PE 2001000335A PE 20011215 A1 PE20011215 A1 PE 20011215A1
Authority
PE
Peru
Prior art keywords
halogen
link
hydrocarbon
substituted
stratrens
Prior art date
Application number
PE2001000335A
Other languages
Spanish (es)
Inventor
Karl-Heinrich Fritzemeier
Christa Hegele-Hartung
Walter Elger
Alexander Hillisch
Uwe Kollenkirchen
Ina Thieme
Vladimir Patchev
Olaf Peters
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
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20011215A1 publication Critical patent/PE20011215A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • 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
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0062Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074Esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072Normal 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

Abstract

SE REFIERE A DERIVADOS DE ESTRA-1,3,5(10-TRIENO 8ß SUSTITUIDOS DE FORMULA I' DONDE R2 ES H, HALOGENO, R18-O, R18 ES H, HIDROCARBURO C1-C6, TRIFLUOROMETILO, R19SO2-O-; R19 ES R20R21N; R20 Y R21 SON H, ALQUILO C1-C5, COR22; R22 ES HIDROCARBURO C1-C10 OPCIONALMENTE HALOGENADO, CICLOALQUILO C3-C7, ENTRE OTROS; R3 ES R18-O, R19SO2-O, O-COR22, ENTRE OTROS; R6 Y R7 SON H O JUNTOS SON UN ENLACE; R6' Y R7' SON H, HALOGENO, R18-O-, ENTRE OTROS; R8 ES ALQUILO, ALQUENILO C1-C5 OPCIONALMENTE HALOGENADO, ETINILO, PROP-1-INILO; R9 ES H, HIDROCARBURO C1-C5 O JUNTO A R11 ES UN ENLACE; R11 ES H O JUNTO A R12 O R9 SON UN ENLACE; R12 ES H; R11' ES H, HALOGENO, HIDROCARBURO PARCIALMENTE HALOGENADO, ENTRE OTROS; R14 ES ES H O JUNTO A R15 ES UN ENLACE; R15 ES H, O JUNTO A R16 ES UN ENLACE, R15 Y R16 SON H, HALOGENO, R18-O-, ENTRE OTROS; R15' Y R16' SON H, HALOGENO, R18-O-, ENTRE OTROS; R17 Y R17' SON H, H Y HALOGENO; H Y BENCILOXI, ENTRE OTROS; R3 ES OH, METOXI, ACETILO; R2 ES H; R6, R6', R7, R7' SON H; R8 ES METILO, R9 ES H; R9 Y R11 SON JUNTOS UN ENLACE; R11' Y R12 SON H. SON COMPUESTOS PREFERIDOS : 8ß-VINIL-ESTRA-1,3,5(10), 9(11)-TETRAEN-3,17ß-DIOL, ENTRE OTROS. LOS COMPUESTOS PUEDEN SER UTILES PARA EL TRATAMIENTO DE TRASTORNOS PERI U POSTMENOPAUSICOS, PERI U POSTANDROPAUSICOS, TRASTORNOS DE SUENO, IRRITABILIDAD, CAMBIOS DE ANIMO, INCONTINENCIA, ATROFIA VAGINAL, ENFERMEDADES DEL TRACTO UROGENITALREFERS TO DERIVATIVES OF ESTRA-1,3,5 (10-TRIENE 8ß SUBSTITUTED FOR FORMULA I 'WHERE R2 IS H, HALOGEN, R18-O, R18 IS H, HYDROCARBON C1-C6, TRIFLUOROMETHYL, R19SO2-O-; R19 IS R20R21N; R20 AND R21 ARE H, C1-C5 ALKYL, COR22; R22 IS C1-C10 HYDROCARBON OPTIONALLY HALOGENATED, C3-C7 CYCLOALKYL, AMONG OTHERS; R3 IS R18-O, R19SO2-O, O-COR22, AMONG OTHERS; R6 AND R7 ARE HO TOGETHER THEY ARE A LINK; R6 'AND R7' ARE H, HALOGEN, R18-O-, AMONG OTHERS; R8 IS ALKYL, C1-C5 OPTIONALLY HALOGENATED, ETHINYL, PROP-1-YELLOW; R9 IS H , C1-C5 HYDROCARBON OR TOGETHER WITH R11 IS A LINK; R11 IS HO TOGETHER TO R12 OR R9 ARE A LINK; R12 IS H; R11 'IS H, HALOGEN, PARTIALLY HALOGENATED HYDROCARBON, AMONG OTHERS; R14 IS IS HO TOGETHER TO R15 IT IS A LINK; R15 IS H, OR TOGETHER WITH R16 IS A LINK, R15 AND R16 ARE H, HALOGEN, R18-O-, AMONG OTHERS; R15 'AND R16' ARE H, HALOGEN, R18-O-, AMONG OTHERS; R17 AND R17 'ARE H, HY HALOGEN; HY BENZYLOXY, AMONG OTHERS; R3 IS OH, METHYL, ACETYL; R2 IS H; R6, R6', R7, R7 'ARE H; R8 E S METHYL, R9 IS H; R9 AND R11 ARE TOGETHER A LINK; R11 'AND R12 ARE H. PREFERRED COMPOUNDS ARE: 8ß-VINYL-ESTRA-1,3,5 (10), 9 (11) -TETRAEN-3,17ß-DIOL, AMONG OTHERS. THE COMPOUNDS MAY BE USEFUL FOR THE TREATMENT OF PERI OR POSTMENOPAUSAL, PERI OR POSTANDROPAUSIC DISORDERS, SLEEP DISORDERS, IRRITABILITY, MOOD CHANGES, INCONTINENCE, VAGINAL ATROPHY, DISEASES OF THE UROGITAL TRACT

PE2001000335A 2000-04-12 2001-04-11 STRATRENS SUBSTITUTED AS SELECTIVELY ACTIVE ESTROGENS PE20011215A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10019167A DE10019167A1 (en) 2000-04-12 2000-04-12 New 8 beta-substituted 11 beta-(pentyl or hexyl)-estra-1,3,5(10)-triene derivatives, are ovary-selective estrogen receptor ligands useful e.g. as female or male contraceptives or for treating ovarian carcinoma

Publications (1)

Publication Number Publication Date
PE20011215A1 true PE20011215A1 (en) 2001-11-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000335A PE20011215A1 (en) 2000-04-12 2001-04-11 STRATRENS SUBSTITUTED AS SELECTIVELY ACTIVE ESTROGENS

Country Status (11)

Country Link
JP (1) JP4860880B2 (en)
KR (1) KR100825534B1 (en)
AR (1) AR028329A1 (en)
DE (2) DE10019167A1 (en)
PE (1) PE20011215A1 (en)
SI (1) SI1272504T1 (en)
TW (1) TWI288138B (en)
UA (1) UA79073C2 (en)
UY (1) UY26665A1 (en)
YU (1) YU77302A (en)
ZA (1) ZA200209149B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7378404B2 (en) * 2000-04-12 2008-05-27 Schering Aktiengesellschaft 8β-hydrocarbyl-substituted estratrienes for use as selective estrogens
DE10151114A1 (en) * 2001-10-15 2003-04-17 Schering Ag New 8 beta-substituted-11 beta-aryl-estra-2,3,5(10)-triene derivatives, are tissue-selective estrogens useful e.g. as female or male contraceptives or for treating ovarian carcinoma
PL1689410T3 (en) * 2003-11-26 2008-10-31 Bayer Schering Pharma Ag Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
US7714012B2 (en) * 2006-11-17 2010-05-11 Trustees Of Dartmouth University Synthesis and biological activities of new tricyclic-bis-enones (TBEs)
EP2014672A1 (en) * 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft 8-beta-substituted estratrienes as selectively active estrogens
CA2744127A1 (en) * 2008-11-21 2010-05-27 Bayer Schering Pharma Aktiengesellschaft Drug delivery system

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3681407A (en) 1969-06-18 1972-08-01 American Cyanamid Co 3-methoxy 8{62 -methylestra 1,3,5(10),9(11)-tetraene-17{62 -carboxylic acid lower alkyl ester and intermediates in the preparation thereof
US3806546A (en) 1969-06-18 1974-04-23 American Cyanamid Co Steroid-like compounds and method of synthesis
US3736345A (en) 1971-05-18 1973-05-29 American Cyanamid Co Steroid-like compounds and method of synthesis

Also Published As

Publication number Publication date
UY26665A1 (en) 2001-11-30
DE10019167A1 (en) 2001-10-18
JP2003534248A (en) 2003-11-18
SI1272504T1 (en) 2007-10-31
KR20030028734A (en) 2003-04-10
KR100825534B1 (en) 2008-04-25
DE50107204D1 (en) 2005-09-29
JP4860880B2 (en) 2012-01-25
UA79073C2 (en) 2007-05-25
YU77302A (en) 2005-11-28
TWI288138B (en) 2007-10-11
ZA200209149B (en) 2007-10-31
AR028329A1 (en) 2003-05-07

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