ZA200408151B - New pharmaceutical compositions containing flibanserin polymorph A - Google Patents
New pharmaceutical compositions containing flibanserin polymorph A Download PDFInfo
- Publication number
- ZA200408151B ZA200408151B ZA200408151A ZA200408151A ZA200408151B ZA 200408151 B ZA200408151 B ZA 200408151B ZA 200408151 A ZA200408151 A ZA 200408151A ZA 200408151 A ZA200408151 A ZA 200408151A ZA 200408151 B ZA200408151 B ZA 200408151B
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- ZA
- South Africa
- Prior art keywords
- core
- pharmaceutical composition
- film
- composition according
- lactose
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- PPRRDFIXUUSXRA-UHFFFAOYSA-N flibanserin Chemical compound FC(F)(F)C1=CC=CC(N2CCN(CCN3C(NC4=CC=CC=C43)=O)CC2)=C1 PPRRDFIXUUSXRA-UHFFFAOYSA-N 0.000 title claims abstract description 44
- 229960002053 flibanserin Drugs 0.000 title claims abstract description 44
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 19
- 239000000203 mixture Substances 0.000 claims description 59
- 238000009472 formulation Methods 0.000 claims description 27
- 239000000945 filler Substances 0.000 claims description 19
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 18
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 18
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 18
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 239000007888 film coating Substances 0.000 claims description 15
- 238000009501 film coating Methods 0.000 claims description 15
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 14
- 229960001021 lactose monohydrate Drugs 0.000 claims description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 14
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 14
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 14
- 239000011230 binding agent Substances 0.000 claims description 13
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 12
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 11
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- -1 poly(ethylacrylate) Polymers 0.000 claims description 9
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- 229910052623 talc Inorganic materials 0.000 claims description 9
- 235000012222 talc Nutrition 0.000 claims description 9
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 7
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 229960001375 lactose Drugs 0.000 claims description 7
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- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- 229920002261 Corn starch Polymers 0.000 claims description 6
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 6
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- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 5
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- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 5
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 5
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- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 2
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- 238000000034 method Methods 0.000 abstract description 17
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- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 14
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- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 9
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- 208000006262 Psychological Sexual Dysfunctions Diseases 0.000 description 8
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- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 4
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- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 229920003091 Methocel™ Polymers 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 238000000634 powder X-ray diffraction Methods 0.000 description 3
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- 235000021355 Stearic acid Nutrition 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 238000012512 characterization method Methods 0.000 description 2
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
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- DMBUODUULYCPAK-UHFFFAOYSA-N 1,3-bis(docosanoyloxy)propan-2-yl docosanoate Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCCCCCC DMBUODUULYCPAK-UHFFFAOYSA-N 0.000 description 1
- 102000056834 5-HT2 Serotonin Receptors Human genes 0.000 description 1
- 108091005479 5-HT2 receptors Proteins 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 102220487426 Actin-related protein 2/3 complex subunit 3_K15M_mutation Human genes 0.000 description 1
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
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- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
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- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 1
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- NEDGUIRITORSKL-UHFFFAOYSA-N butyl 2-methylprop-2-enoate;2-(dimethylamino)ethyl 2-methylprop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound COC(=O)C(C)=C.CCCCOC(=O)C(C)=C.CN(C)CCOC(=O)C(C)=C NEDGUIRITORSKL-UHFFFAOYSA-N 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
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- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
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- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Gynecology & Obstetrics (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02011224 | 2002-05-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200408151B true ZA200408151B (en) | 2006-06-28 |
Family
ID=29433081
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200408151A ZA200408151B (en) | 2002-05-22 | 2004-10-08 | New pharmaceutical compositions containing flibanserin polymorph A |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP1511489B1 (uk) |
| JP (1) | JP3919788B2 (uk) |
| KR (1) | KR101054237B1 (uk) |
| CN (3) | CN101002780A (uk) |
| AT (1) | ATE499939T1 (uk) |
| BR (1) | BRPI0311189B8 (uk) |
| CA (1) | CA2483597C (uk) |
| CY (1) | CY1111470T1 (uk) |
| DE (1) | DE60336225D1 (uk) |
| DK (1) | DK1511489T3 (uk) |
| EA (1) | EA007185B1 (uk) |
| EC (1) | ECSP045493A (uk) |
| ES (1) | ES2361994T3 (uk) |
| HR (1) | HRP20041092B1 (uk) |
| IL (1) | IL164440A0 (uk) |
| ME (1) | MEP55308A (uk) |
| MX (1) | MXPA04011487A (uk) |
| NO (1) | NO329414B1 (uk) |
| NZ (1) | NZ537253A (uk) |
| PL (1) | PL211062B1 (uk) |
| RS (1) | RS51718B (uk) |
| SI (1) | SI1511489T1 (uk) |
| UA (1) | UA80135C2 (uk) |
| WO (1) | WO2003097058A1 (uk) |
| ZA (1) | ZA200408151B (uk) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10675280B2 (en) | 2001-10-20 | 2020-06-09 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| UA78974C2 (en) | 2001-10-20 | 2007-05-10 | Boehringer Ingelheim Pharma | Use of flibanserin for treating disorders of sexual desire |
| US20050239798A1 (en) * | 2004-04-22 | 2005-10-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Method for the treatment of premenstrual and other female sexual disorders |
| WO2006096439A2 (en) * | 2005-03-04 | 2006-09-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for the treatment and/or prevention of schizophrenia and related diseases |
| EP1888070A1 (en) * | 2005-05-19 | 2008-02-20 | Boehringer Ingelheim International GmbH | Method for the treatment of sexual dysfunctions due to medical conditions |
| WO2006125042A1 (en) * | 2005-05-19 | 2006-11-23 | Boehringer Ingelheim International Gmbh | Method for the treatment of drug-induced sexual dysfunction |
| US8227476B2 (en) | 2005-08-03 | 2012-07-24 | Sprout Pharmaceuticals, Inc. | Use of flibanserin in the treatment of obesity |
| US7923449B2 (en) | 2005-10-29 | 2011-04-12 | Boehringer Ingelheim International Gmbh | Benzimidazolone derivatives for the treatment of premenstrual and other female sexual disorders |
| US20070105869A1 (en) * | 2005-11-08 | 2007-05-10 | Stephane Pollentier | Use of flibanserin for the treatment of pre-menopausal sexual desire disorders |
| ES2336719T3 (es) | 2006-06-30 | 2010-04-15 | Boehringer Ingelheim International Gmbh | Flibanserina para el tratamiento de la incontinencia urinaria y las enfermedades relacionadas. |
| CA2660476C (en) | 2006-08-14 | 2015-11-17 | Boehringer Ingelheim International Gmbh | Formulations of flibanserin and method for manufacturing the same |
| CL2007002214A1 (es) | 2006-08-14 | 2008-03-07 | Boehringer Ingelheim Int | Composicion farmaceutica en la forma de comprimido, donde al menos la longitud del comprimido en el estado anterior de la aplicacion es al menos 7/12 del diametro pilorico del paciente y despues de ingerirlo en estado alimentado, la longitud del comp |
| CA2661613C (en) | 2006-08-25 | 2016-01-26 | Boehringer Ingelheim International Gmbh | Controlled release system and method for manufacturing the same |
| EP2097389B1 (en) | 2006-12-20 | 2011-09-14 | Boehringer Ingelheim International GmbH | Sulfated benzimidazolone derivatives having mixed serotonine receptor affinity |
| EP1955699A1 (en) * | 2007-02-08 | 2008-08-13 | Boehringer Ingelheim Pharma GmbH & Co. KG | Use of flibanserin for the treatment of insomnia |
| UY31335A1 (es) | 2007-09-12 | 2009-04-30 | Tratamiento de sintomas vasomotores | |
| EP2090297A1 (en) * | 2008-02-13 | 2009-08-19 | Boehringer Ingelheim International GmbH | Formulations of flibanserin |
| DE102008047910A1 (de) | 2008-09-19 | 2010-03-25 | Molkerei Meggle Wasserburg Gmbh & Co. Kg | Tablettierhilfsstoff auf Laktose- und Cellulosebasis |
| US20120010216A1 (en) * | 2010-07-06 | 2012-01-12 | Brown Arthur M | Pharmaceutical compositions containing vanoxerine |
| CN104926734B (zh) * | 2015-07-07 | 2017-04-05 | 苏州立新制药有限公司 | 氟班色林的制备方法 |
| CN108699007A (zh) * | 2016-01-31 | 2018-10-23 | 孟晓明 | 氟班色林的新晶型及其制备方法及其用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1251144B (it) * | 1991-07-30 | 1995-05-04 | Boehringer Ingelheim Italia | Derivati del benzimidazolone |
| MXPA04000913A (es) * | 2001-08-02 | 2004-10-27 | Bidachem Spa | Compuesto polimorfo estable de flibanserina, procedimiento industrial para su preparacion, y uso del mismo para preparar medicamentos. |
| DE10138273A1 (de) * | 2001-08-10 | 2003-02-27 | Boehringer Ingelheim Pharma | Arzneimittel mit neuroprotektiver Wirkung |
-
2003
- 2003-05-19 BR BRPI0311189A patent/BRPI0311189B8/pt not_active IP Right Cessation
- 2003-05-19 DE DE60336225T patent/DE60336225D1/de not_active Expired - Lifetime
- 2003-05-19 PL PL372457A patent/PL211062B1/pl unknown
- 2003-05-19 JP JP2004505057A patent/JP3919788B2/ja not_active Expired - Fee Related
- 2003-05-19 DK DK03730069.6T patent/DK1511489T3/da active
- 2003-05-19 UA UA20041210555A patent/UA80135C2/uk unknown
- 2003-05-19 NZ NZ537253A patent/NZ537253A/en not_active IP Right Cessation
- 2003-05-19 CA CA2483597A patent/CA2483597C/en not_active Expired - Fee Related
- 2003-05-19 EP EP03730069A patent/EP1511489B1/en not_active Expired - Lifetime
- 2003-05-19 WO PCT/EP2003/005226 patent/WO2003097058A1/en active Application Filing
- 2003-05-19 RS YU98704A patent/RS51718B/en unknown
- 2003-05-19 KR KR1020047018741A patent/KR101054237B1/ko active IP Right Grant
- 2003-05-19 ES ES03730069T patent/ES2361994T3/es not_active Expired - Lifetime
- 2003-05-19 AT AT03730069T patent/ATE499939T1/de active
- 2003-05-19 SI SI200331994T patent/SI1511489T1/sl unknown
- 2003-05-19 EA EA200401515A patent/EA007185B1/ru not_active IP Right Cessation
- 2003-05-19 CN CNA2007100014771A patent/CN101002780A/zh active Pending
- 2003-05-19 CN CN201110122058XA patent/CN102240289A/zh active Pending
- 2003-05-19 MX MXPA04011487A patent/MXPA04011487A/es active IP Right Grant
- 2003-05-19 CN CNA038117029A patent/CN1655789A/zh active Pending
- 2003-05-19 ME MEP-553/08A patent/MEP55308A/xx unknown
-
2004
- 2004-10-05 IL IL16444004A patent/IL164440A0/xx unknown
- 2004-10-08 ZA ZA200408151A patent/ZA200408151B/en unknown
- 2004-10-22 NO NO20044547A patent/NO329414B1/no not_active IP Right Cessation
- 2004-11-19 HR HRP20041092AA patent/HRP20041092B1/hr not_active IP Right Cessation
- 2004-12-13 EC EC2004005493A patent/ECSP045493A/es unknown
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2011
- 2011-05-17 CY CY20111100475T patent/CY1111470T1/el unknown
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