JP2006517221A - ネルフィナビル用の投与レジメン - Google Patents
ネルフィナビル用の投与レジメン Download PDFInfo
- Publication number
- JP2006517221A JP2006517221A JP2006502411A JP2006502411A JP2006517221A JP 2006517221 A JP2006517221 A JP 2006517221A JP 2006502411 A JP2006502411 A JP 2006502411A JP 2006502411 A JP2006502411 A JP 2006502411A JP 2006517221 A JP2006517221 A JP 2006517221A
- Authority
- JP
- Japan
- Prior art keywords
- nelfinavir
- fat
- administration
- food
- auc
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- QAGYKUNXZHXKMR-HKWSIXNMSA-N nelfinavir Chemical compound CC1=C(O)C=CC=C1C(=O)N[C@H]([C@H](O)CN1[C@@H](C[C@@H]2CCCC[C@@H]2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 QAGYKUNXZHXKMR-HKWSIXNMSA-N 0.000 title claims abstract description 181
- QAGYKUNXZHXKMR-UHFFFAOYSA-N CPD000469186 Natural products CC1=C(O)C=CC=C1C(=O)NC(C(O)CN1C(CC2CCCCC2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 QAGYKUNXZHXKMR-UHFFFAOYSA-N 0.000 title claims abstract description 175
- 229960000884 nelfinavir Drugs 0.000 title claims abstract description 175
- 241000725303 Human immunodeficiency virus Species 0.000 claims abstract description 51
- 238000000034 method Methods 0.000 claims abstract description 42
- 235000013305 food Nutrition 0.000 claims abstract description 40
- 238000011282 treatment Methods 0.000 claims abstract description 33
- 241000124008 Mammalia Species 0.000 claims abstract description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
- 235000012631 food intake Nutrition 0.000 claims description 14
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- 239000000203 mixture Substances 0.000 claims description 9
- 238000013213 extrapolation Methods 0.000 claims description 7
- 229940002612 prodrug Drugs 0.000 claims description 5
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- 150000003839 salts Chemical class 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 235000019197 fats Nutrition 0.000 description 93
- 235000012054 meals Nutrition 0.000 description 28
- 230000036470 plasma concentration Effects 0.000 description 28
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- 230000000694 effects Effects 0.000 description 22
- 230000037213 diet Effects 0.000 description 18
- 235000009200 high fat diet Nutrition 0.000 description 16
- 235000015263 low fat diet Nutrition 0.000 description 16
- 235000021152 breakfast Nutrition 0.000 description 15
- 238000002474 experimental method Methods 0.000 description 14
- GLWHPRRGGYLLRV-XLPZGREQSA-N [[(2s,3s,5r)-3-azido-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](N=[N+]=[N-])C1 GLWHPRRGGYLLRV-XLPZGREQSA-N 0.000 description 13
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- 229940124158 Protease/peptidase inhibitor Drugs 0.000 description 5
- XNKLLVCARDGLGL-JGVFFNPUSA-N Stavudine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1C=C[C@@H](CO)O1 XNKLLVCARDGLGL-JGVFFNPUSA-N 0.000 description 5
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- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 description 5
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- 208000034332 Body integrity dysphoria Diseases 0.000 description 3
- BXZVVICBKDXVGW-NKWVEPMBSA-N Didanosine Chemical compound O1[C@H](CO)CC[C@@H]1N1C(NC=NC2=O)=C2N=C1 BXZVVICBKDXVGW-NKWVEPMBSA-N 0.000 description 3
- 208000031886 HIV Infections Diseases 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- WREGKURFCTUGRC-POYBYMJQSA-N Zalcitabine Chemical compound O=C1N=C(N)C=CN1[C@@H]1O[C@H](CO)CC1 WREGKURFCTUGRC-POYBYMJQSA-N 0.000 description 3
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- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 description 3
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- CBVCZFGXHXORBI-PXQQMZJSSA-N indinavir Chemical compound C([C@H](N(CC1)C[C@@H](O)C[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H]2C3=CC=CC=C3C[C@H]2O)C(=O)NC(C)(C)C)N1CC1=CC=CN=C1 CBVCZFGXHXORBI-PXQQMZJSSA-N 0.000 description 3
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- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 description 2
- 241000713772 Human immunodeficiency virus 1 Species 0.000 description 2
- 241000713340 Human immunodeficiency virus 2 Species 0.000 description 2
- VSNHCAURESNICA-UHFFFAOYSA-N Hydroxyurea Chemical compound NC(=O)NO VSNHCAURESNICA-UHFFFAOYSA-N 0.000 description 2
- KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 description 2
- 239000004743 Polypropylene Substances 0.000 description 2
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 description 2
- 244000269722 Thea sinensis Species 0.000 description 2
- 241000700605 Viruses Species 0.000 description 2
- WOZSCQDILHKSGG-UHFFFAOYSA-N adefovir depivoxil Chemical compound N1=CN=C2N(CCOCP(=O)(OCOC(=O)C(C)(C)C)OCOC(=O)C(C)(C)C)C=NC2=C1N WOZSCQDILHKSGG-UHFFFAOYSA-N 0.000 description 2
- 229960001830 amprenavir Drugs 0.000 description 2
- YMARZQAQMVYCKC-OEMFJLHTSA-N amprenavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1COCC1)C1=CC=CC=C1 YMARZQAQMVYCKC-OEMFJLHTSA-N 0.000 description 2
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- 235000014121 butter Nutrition 0.000 description 2
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- 235000021245 dietary protein Nutrition 0.000 description 2
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- 229960003804 efavirenz Drugs 0.000 description 2
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- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 229960001936 indinavir Drugs 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 230000002458 infectious effect Effects 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 229960004525 lopinavir Drugs 0.000 description 2
- 235000004213 low-fat Nutrition 0.000 description 2
- 235000013336 milk Nutrition 0.000 description 2
- 239000008267 milk Substances 0.000 description 2
- 210000004080 milk Anatomy 0.000 description 2
- 229940025676 nelfinavir 250 mg Drugs 0.000 description 2
- 229960005230 nelfinavir mesylate Drugs 0.000 description 2
- NQHXCOAXSHGTIA-SKXNDZRYSA-N nelfinavir mesylate Chemical compound CS(O)(=O)=O.CC1=C(O)C=CC=C1C(=O)N[C@H]([C@H](O)CN1[C@@H](C[C@@H]2CCCC[C@@H]2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 NQHXCOAXSHGTIA-SKXNDZRYSA-N 0.000 description 2
- 239000002777 nucleoside Substances 0.000 description 2
- 150000003833 nucleoside derivatives Chemical class 0.000 description 2
- 235000016709 nutrition Nutrition 0.000 description 2
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- 229920001155 polypropylene Polymers 0.000 description 2
- 238000009597 pregnancy test Methods 0.000 description 2
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- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 229960000311 ritonavir Drugs 0.000 description 2
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 description 2
- 238000005070 sampling Methods 0.000 description 2
- 229960001852 saquinavir Drugs 0.000 description 2
- QWAXKHKRTORLEM-UGJKXSETSA-N saquinavir Chemical compound C([C@@H]([C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)C=1N=C2C=CC=CC2=CC=1)C1=CC=CC=C1 QWAXKHKRTORLEM-UGJKXSETSA-N 0.000 description 2
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- 244000105624 Arachis hypogaea Species 0.000 description 1
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- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
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- 206010012735 Diarrhoea Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010048474 Fat redistribution Diseases 0.000 description 1
- 208000037357 HIV infectious disease Diseases 0.000 description 1
- 229940122440 HIV protease inhibitor Drugs 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010022489 Insulin Resistance Diseases 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 229960004748 abacavir Drugs 0.000 description 1
- MCGSCOLBFJQGHM-SCZZXKLOSA-N abacavir Chemical compound C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 MCGSCOLBFJQGHM-SCZZXKLOSA-N 0.000 description 1
- WMHSRBZIJNQHKT-FFKFEZPRSA-N abacavir sulfate Chemical compound OS(O)(=O)=O.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 WMHSRBZIJNQHKT-FFKFEZPRSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 229960001997 adefovir Drugs 0.000 description 1
- 229960003205 adefovir dipivoxil Drugs 0.000 description 1
- 230000036436 anti-hiv Effects 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 235000013351 cheese Nutrition 0.000 description 1
- 229940014461 combivir Drugs 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
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- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 1
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- 230000036512 infertility Effects 0.000 description 1
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- 231100000535 infertility Toxicity 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 235000015094 jam Nutrition 0.000 description 1
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
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- 238000012544 monitoring process Methods 0.000 description 1
- NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 description 1
- 125000003729 nucleotide group Chemical group 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 244000052769 pathogen Species 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 235000020232 peanut Nutrition 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 230000001323 posttranslational effect Effects 0.000 description 1
- 230000003334 potential effect Effects 0.000 description 1
- 229940064914 retrovir Drugs 0.000 description 1
- 238000010839 reverse transcription Methods 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
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- 235000011888 snacks Nutrition 0.000 description 1
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- 229960001203 stavudine Drugs 0.000 description 1
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- 210000002700 urine Anatomy 0.000 description 1
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- 229940052255 ziagen Drugs 0.000 description 1
Images
Classifications
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/30—Dietetic or nutritional methods, e.g. for losing weight
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Organic Chemistry (AREA)
- Mycology (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44644403P | 2003-02-10 | 2003-02-10 | |
| US52425803P | 2003-11-21 | 2003-11-21 | |
| PCT/IB2004/000313 WO2004069251A1 (en) | 2003-02-10 | 2004-01-29 | Regimen of administration for nelfinavir |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2006517221A true JP2006517221A (ja) | 2006-07-20 |
Family
ID=32853430
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006502411A Pending JP2006517221A (ja) | 2003-02-10 | 2004-01-29 | ネルフィナビル用の投与レジメン |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1605942A1 (es) |
| JP (1) | JP2006517221A (es) |
| AR (1) | AR043133A1 (es) |
| BR (1) | BRPI0407174A (es) |
| CA (1) | CA2515095A1 (es) |
| CL (1) | CL2004000202A1 (es) |
| MX (1) | MXPA05008425A (es) |
| NL (1) | NL1025449C2 (es) |
| PA (1) | PA8595301A1 (es) |
| PE (1) | PE20040948A1 (es) |
| TW (1) | TW200423922A (es) |
| UY (1) | UY28183A1 (es) |
| WO (1) | WO2004069251A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7157455B2 (en) | 2003-02-10 | 2007-01-02 | Hoffmann-La Roche Inc. | 4-Aminopyrimidine-5-one derivatives |
-
2004
- 2004-01-29 CA CA002515095A patent/CA2515095A1/en not_active Abandoned
- 2004-01-29 MX MXPA05008425A patent/MXPA05008425A/es unknown
- 2004-01-29 EP EP04706250A patent/EP1605942A1/en not_active Withdrawn
- 2004-01-29 JP JP2006502411A patent/JP2006517221A/ja active Pending
- 2004-01-29 WO PCT/IB2004/000313 patent/WO2004069251A1/en not_active Application Discontinuation
- 2004-01-29 BR BR0407174-3A patent/BRPI0407174A/pt not_active IP Right Cessation
- 2004-02-05 CL CL200400202A patent/CL2004000202A1/es unknown
- 2004-02-09 AR ARP040100399A patent/AR043133A1/es unknown
- 2004-02-09 PE PE2004000146A patent/PE20040948A1/es not_active Application Discontinuation
- 2004-02-09 PA PA20048595301A patent/PA8595301A1/es unknown
- 2004-02-09 TW TW093102921A patent/TW200423922A/zh unknown
- 2004-02-10 UY UY28183A patent/UY28183A1/es not_active Application Discontinuation
- 2004-02-10 NL NL1025449A patent/NL1025449C2/nl not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| TW200423922A (en) | 2004-11-16 |
| CL2004000202A1 (es) | 2005-03-18 |
| EP1605942A1 (en) | 2005-12-21 |
| CA2515095A1 (en) | 2004-08-19 |
| NL1025449A1 (nl) | 2004-08-12 |
| PE20040948A1 (es) | 2004-12-27 |
| WO2004069251A1 (en) | 2004-08-19 |
| UY28183A1 (es) | 2004-09-30 |
| BRPI0407174A (pt) | 2006-02-07 |
| NL1025449C2 (nl) | 2005-03-15 |
| MXPA05008425A (es) | 2005-10-19 |
| AR043133A1 (es) | 2005-07-20 |
| PA8595301A1 (es) | 2005-08-04 |
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