SK9592002A3 - A method for reduction or elimination of the incidence of menopausal symptoms, method of treatment or decreasing the risk of an acquiring disease, a pharmaceutical composition and a kit - Google Patents
A method for reduction or elimination of the incidence of menopausal symptoms, method of treatment or decreasing the risk of an acquiring disease, a pharmaceutical composition and a kit Download PDFInfo
- Publication number
- SK9592002A3 SK9592002A3 SK959-2002A SK9592002A SK9592002A3 SK 9592002 A3 SK9592002 A3 SK 9592002A3 SK 9592002 A SK9592002 A SK 9592002A SK 9592002 A3 SK9592002 A3 SK 9592002A3
- Authority
- SK
- Slovakia
- Prior art keywords
- group
- pharmaceutical composition
- estrogen
- acid
- effective amount
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- 238000011282 treatment Methods 0.000 title claims abstract description 144
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 52
- 230000009467 reduction Effects 0.000 title claims abstract description 9
- 206010027304 Menopausal symptoms Diseases 0.000 title claims abstract description 6
- 238000000034 method Methods 0.000 title abstract description 81
- 201000010099 disease Diseases 0.000 title abstract description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract description 22
- 230000003247 decreasing effect Effects 0.000 title abstract description 14
- 230000008030 elimination Effects 0.000 title abstract 2
- 238000003379 elimination reaction Methods 0.000 title abstract 2
- 239000000262 estrogen Substances 0.000 claims abstract description 146
- 229940011871 estrogen Drugs 0.000 claims abstract description 146
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims abstract description 133
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims abstract description 111
- 150000001875 compounds Chemical class 0.000 claims abstract description 83
- 208000026310 Breast neoplasm Diseases 0.000 claims abstract description 43
- 206010006187 Breast cancer Diseases 0.000 claims abstract description 40
- 210000000481 breast Anatomy 0.000 claims abstract description 24
- 230000001076 estrogenic effect Effects 0.000 claims abstract description 21
- 208000001132 Osteoporosis Diseases 0.000 claims abstract description 19
- 206010060800 Hot flush Diseases 0.000 claims abstract description 17
- 208000033830 Hot Flashes Diseases 0.000 claims abstract description 15
- 201000001320 Atherosclerosis Diseases 0.000 claims abstract description 12
- 208000035150 Hypercholesterolemia Diseases 0.000 claims abstract description 11
- 208000031226 Hyperlipidaemia Diseases 0.000 claims abstract description 11
- 208000008589 Obesity Diseases 0.000 claims abstract description 11
- 235000020824 obesity Nutrition 0.000 claims abstract description 11
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 10
- 206010020772 Hypertension Diseases 0.000 claims abstract description 10
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract description 10
- 206010022489 Insulin Resistance Diseases 0.000 claims abstract description 9
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- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims abstract description 9
- 229940122361 Bisphosphonate Drugs 0.000 claims abstract description 8
- 150000004663 bisphosphonates Chemical class 0.000 claims abstract description 7
- 206010014733 Endometrial cancer Diseases 0.000 claims abstract description 6
- 206010014759 Endometrial neoplasm Diseases 0.000 claims abstract description 6
- 206010047791 Vulvovaginal dryness Diseases 0.000 claims abstract description 4
- 208000037093 Menstruation Disturbances Diseases 0.000 claims abstract description 3
- 206010027339 Menstruation irregular Diseases 0.000 claims abstract description 3
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 claims description 119
- FMGSKLZLMKYGDP-UHFFFAOYSA-N Dehydroepiandrosterone Natural products C1C(O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 FMGSKLZLMKYGDP-UHFFFAOYSA-N 0.000 claims description 116
- 229960002847 prasterone Drugs 0.000 claims description 116
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims description 99
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims description 73
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 73
- 229960003399 estrone Drugs 0.000 claims description 52
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 51
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims description 48
- 239000000203 mixture Substances 0.000 claims description 37
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims description 33
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- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 25
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- 229960005309 estradiol Drugs 0.000 claims description 24
- HJQQVNIORAQATK-DDJBQNAASA-N (e)-3-[4-[(z)-1,2-diphenylbut-1-enyl]phenyl]prop-2-enoic acid Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(\C=C\C(O)=O)=CC=1)/C1=CC=CC=C1 HJQQVNIORAQATK-DDJBQNAASA-N 0.000 claims description 22
- 239000003098 androgen Substances 0.000 claims description 22
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 17
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
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- 230000002357 endometrial effect Effects 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 230000009245 menopause Effects 0.000 claims description 15
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- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 claims description 14
- ZQZFYGIXNQKOAV-OCEACIFDSA-N Droloxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=C(O)C=CC=1)\C1=CC=C(OCCN(C)C)C=C1 ZQZFYGIXNQKOAV-OCEACIFDSA-N 0.000 claims description 13
- 239000003795 chemical substances by application Substances 0.000 claims description 13
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- 238000002657 hormone replacement therapy Methods 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 13
- 239000002253 acid Substances 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 11
- 238000001727 in vivo Methods 0.000 claims description 11
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims description 10
- CZWCKYRVOZZJNM-UHFFFAOYSA-N Prasterone sodium sulfate Natural products C1C(OS(O)(=O)=O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 CZWCKYRVOZZJNM-UHFFFAOYSA-N 0.000 claims description 10
- CZWCKYRVOZZJNM-USOAJAOKSA-N dehydroepiandrosterone sulfate Chemical compound C1[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 CZWCKYRVOZZJNM-USOAJAOKSA-N 0.000 claims description 10
- 150000002148 esters Chemical class 0.000 claims description 10
- 229950009829 prasterone sulfate Drugs 0.000 claims description 10
- 238000002360 preparation method Methods 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
- JJKOTMDDZAJTGQ-DQSJHHFOSA-N Idoxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN2CCCC2)=CC=1)/C1=CC=C(I)C=C1 JJKOTMDDZAJTGQ-DQSJHHFOSA-N 0.000 claims description 8
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 8
- 239000000654 additive Substances 0.000 claims description 7
- 229960005471 androstenedione Drugs 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 7
- IMSSROKUHAOUJS-MJCUULBUSA-N mestranol Chemical compound C1C[C@]2(C)[C@@](C#C)(O)CC[C@H]2[C@@H]2CCC3=CC(OC)=CC=C3[C@H]21 IMSSROKUHAOUJS-MJCUULBUSA-N 0.000 claims description 7
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- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 claims description 6
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- 229940035811 conjugated estrogen Drugs 0.000 claims description 6
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- 230000001457 vasomotor Effects 0.000 claims description 4
- JICOGKJOQXTAIP-UHFFFAOYSA-N 2-(4-hydroxyphenyl)-3-methyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]indol-5-ol Chemical compound C=1C=C(OCCN2CCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 JICOGKJOQXTAIP-UHFFFAOYSA-N 0.000 claims description 3
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Classifications
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
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- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Reproductive Health (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17860100P | 2000-01-28 | 2000-01-28 | |
| PCT/CA2001/000086 WO2001054699A1 (en) | 2000-01-28 | 2001-01-26 | Selective estrogen receptor modulators in combination with estrogens |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK9592002A3 true SK9592002A3 (en) | 2003-12-02 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK959-2002A SK9592002A3 (en) | 2000-01-28 | 2001-01-26 | A method for reduction or elimination of the incidence of menopausal symptoms, method of treatment or decreasing the risk of an acquiring disease, a pharmaceutical composition and a kit |
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| Country | Link |
|---|---|
| US (3) | US20030040510A1 (cs) |
| EP (1) | EP1251855A1 (cs) |
| JP (1) | JP2003520817A (cs) |
| KR (1) | KR20020073566A (cs) |
| CN (1) | CN1400904A (cs) |
| AR (1) | AR035564A1 (cs) |
| AU (1) | AU2991301A (cs) |
| BR (1) | BR0108107A (cs) |
| CA (1) | CA2395730A1 (cs) |
| CZ (1) | CZ20022401A3 (cs) |
| HK (1) | HK1048761A1 (cs) |
| HU (1) | HUP0204211A3 (cs) |
| IL (1) | IL149990A0 (cs) |
| MX (1) | MXPA02007165A (cs) |
| NO (1) | NO20023484L (cs) |
| NZ (1) | NZ534348A (cs) |
| PL (1) | PL357163A1 (cs) |
| RU (1) | RU2342145C2 (cs) |
| SK (1) | SK9592002A3 (cs) |
| WO (1) | WO2001054699A1 (cs) |
| ZA (1) | ZA200205926B (cs) |
Families Citing this family (73)
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| JPH11513390A (ja) * | 1995-10-06 | 1999-11-16 | アーチ デベロップメント コーポレイション | 細胞殺傷のウイルス増強のための方法および組成物 |
| US6358991B2 (en) * | 2000-07-06 | 2002-03-19 | American Home Products Corporation | Methods of treating neuropeptide Y-related conditions |
| CA2414111A1 (en) * | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for increasing nitric oxide synthase activity |
| US6245819B1 (en) | 2000-07-21 | 2001-06-12 | Hormos Medical Oy, Ltd. | Method for the treatment of vaginal dryness and sexual dysfunction in women during or after the menopause |
| US6503894B1 (en) | 2000-08-30 | 2003-01-07 | Unimed Pharmaceuticals, Inc. | Pharmaceutical composition and method for treating hypogonadism |
| IL145838A (en) * | 2000-10-16 | 2008-11-03 | Pfizer Prod Inc | Use of an estrogen agonist/antagonist for the manufacture of a medicament for treating vaginitis |
| WO2003004033A1 (en) * | 2001-07-06 | 2003-01-16 | Penwest Pharmaceuticals Company | Sustained release formulations of oxymorphone |
| SK622004A3 (en) | 2001-07-31 | 2004-08-03 | Pfizer Prod Inc | Pharmaceutical compositions, kits and methods comprising combinations of estrogen agonists/antagonists, estrogens and progestins |
| US20060269611A1 (en) * | 2001-11-29 | 2006-11-30 | Steiner Mitchell S | Prevention and treatment of androgen-deprivation induced osteoporosis |
| US20070197664A1 (en) * | 2001-11-29 | 2007-08-23 | Steiner Mitchell S | Prevention and treatment of androgen-deprivation induced osteoporosis |
| US20080249183A1 (en) * | 2001-11-29 | 2008-10-09 | Steiner Mitchell S | Treatment of androgen-deprivation induced osteoporosis |
| US20040214898A1 (en) * | 2001-11-29 | 2004-10-28 | Steiner Mitchell S. | Methods for treating hot flashes |
| US20050080143A1 (en) * | 2001-11-29 | 2005-04-14 | Steiner Mitchell S. | Treatment of androgen-deprivation induced osteoporosis |
| TW200307553A (en) * | 2002-05-24 | 2003-12-16 | Akzo Nobel Nv | Treatment of post-menopausal complaints in breast cancer patients |
| DK1509215T3 (da) * | 2002-06-06 | 2007-03-12 | Hormos Medical Ltd | Behandling eller forebyggelse af urogenital atrofi og dets symptomer hos kvinder |
| PL1499278T3 (pl) * | 2003-05-23 | 2005-09-30 | Msd Oss Bv | Farmaceutyczna postać użytkowa o natychmiastowym uwalnianiu zawierająca polimorficzny tibolon |
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2001
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- 2001-01-26 HU HU0204211A patent/HUP0204211A3/hu unknown
- 2001-01-26 PL PL01357163A patent/PL357163A1/xx not_active Application Discontinuation
- 2001-01-26 NZ NZ534348A patent/NZ534348A/en active IP Right Revival
- 2001-01-26 JP JP2001554683A patent/JP2003520817A/ja active Pending
- 2001-01-26 RU RU2002123047/14A patent/RU2342145C2/ru not_active IP Right Cessation
- 2001-01-26 WO PCT/CA2001/000086 patent/WO2001054699A1/en not_active Ceased
- 2001-01-26 KR KR1020027009728A patent/KR20020073566A/ko not_active Ceased
- 2001-01-26 CA CA002395730A patent/CA2395730A1/en not_active Abandoned
- 2001-01-26 IL IL14999001A patent/IL149990A0/xx unknown
- 2001-01-26 EP EP01902194A patent/EP1251855A1/en not_active Withdrawn
- 2001-01-26 AU AU29913/01A patent/AU2991301A/en not_active Abandoned
- 2001-01-26 BR BR0108107-1A patent/BR0108107A/pt not_active Application Discontinuation
- 2001-01-26 CZ CZ20022401A patent/CZ20022401A3/cs unknown
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- 2001-01-26 AR ARP010100372A patent/AR035564A1/es unknown
- 2001-01-26 MX MXPA02007165A patent/MXPA02007165A/es not_active Application Discontinuation
- 2001-01-26 HK HK03100850.6A patent/HK1048761A1/zh unknown
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- 2001-11-07 US US10/052,803 patent/US20020198179A1/en not_active Abandoned
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- 2002-07-24 ZA ZA200005926A patent/ZA200205926B/xx unknown
Also Published As
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| BR0108107A (pt) | 2003-03-11 |
| EP1251855A1 (en) | 2002-10-30 |
| CZ20022401A3 (cs) | 2003-10-15 |
| US20020198179A1 (en) | 2002-12-26 |
| US20030040510A1 (en) | 2003-02-27 |
| JP2003520817A (ja) | 2003-07-08 |
| AU2991301A (en) | 2001-08-07 |
| NZ534348A (en) | 2006-06-30 |
| KR20020073566A (ko) | 2002-09-27 |
| AR035564A1 (es) | 2004-06-16 |
| HUP0204211A3 (en) | 2005-06-28 |
| NO20023484D0 (no) | 2002-07-22 |
| HUP0204211A2 (hu) | 2003-04-28 |
| RU2342145C2 (ru) | 2008-12-27 |
| RU2002123047A (ru) | 2004-03-10 |
| MXPA02007165A (es) | 2003-09-22 |
| IL149990A0 (en) | 2002-12-01 |
| CN1400904A (zh) | 2003-03-05 |
| US20030065008A1 (en) | 2003-04-03 |
| CA2395730A1 (en) | 2001-08-02 |
| PL357163A1 (en) | 2004-07-26 |
| ZA200205926B (en) | 2003-07-24 |
| NO20023484L (no) | 2002-07-22 |
| HK1048761A1 (zh) | 2003-04-17 |
| WO2001054699A1 (en) | 2001-08-02 |
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