HRP20120003T1 - Stabilni kompleks aktivnog sastojka soli o-acetilsalicilne kiseline sa osnovnim aminokiselinama i glicinom - Google Patents
Stabilni kompleks aktivnog sastojka soli o-acetilsalicilne kiseline sa osnovnim aminokiselinama i glicinom Download PDFInfo
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- HRP20120003T1 HRP20120003T1 HR20120003T HRP20120003T HRP20120003T1 HR P20120003 T1 HRP20120003 T1 HR P20120003T1 HR 20120003 T HR20120003 T HR 20120003T HR P20120003 T HRP20120003 T HR P20120003T HR P20120003 T1 HRP20120003 T1 HR P20120003T1
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- active ingredient
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- glycine
- basic amino
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- 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
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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- 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
- A61K31/60—Salicylic acid; Derivatives thereof
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- 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
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- 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
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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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
- A61P25/06—Antimigraine agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
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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
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/38—Separation; Purification; Stabilisation; Use of additives
- C07C227/40—Separation; Purification
- C07C227/42—Crystallisation
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
- C07C69/12—Acetic acid esters
- C07C69/14—Acetic acid esters of monohydroxylic compounds
- C07C69/145—Acetic acid esters of monohydroxylic compounds of unsaturated alcohols
- C07C69/157—Acetic acid esters of monohydroxylic compounds of unsaturated alcohols containing six-membered aromatic rings
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- Animal Behavior & Ethology (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Crystallography & Structural Chemistry (AREA)
- Pain & Pain Management (AREA)
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- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract
Kompleks aktivnog sastojka koji se sastoji od soli o-acetilsalicilne kiseline sa jednom osnovnom aminokiselinom i glicinom, naznačen time da raspodjela veličina čestica ima srednju veličinu čestica manju od 100 µm. Patent sadrži još 19 patentnih zahtjeva.
Claims (20)
1. Kompleks aktivnog sastojka koji se sastoji od soli o-acetilsalicilne kiseline sa jednom osnovnom aminokiselinom i glicinom, naznačen time da raspodjela veličina čestica ima srednju veličinu čestica manju od 100 µm.
2. Kompleks aktivnog sastojka prema zahtjevu 1, naznačen time da kompleks aktivnog sastojka sadrži od 8 do 12 težinskih postotaka glicina.
3. Kompleks aktivnog sastojka prema zahtjevima 1 do 2 naznačen time da je sa lizinom kao osnovnom aminokiselinom.
4. Kompleks aktivnog sastojka prema zahtjevima 1 do 3 naznačen time da je sa D,L-lizinom kao osnovnom aminokiselinom.
5. Kompleks aktivnog sastojka prema zahtjevu 4, naznačen time da kompleks aktivnog sastojka sadrži do 10 težinskih postotaka glicina i da u rasponu otapanja kompleks aktivnog sastojka ima jednu endotermnu vršnu temperaturu od 148 ± 2°C i jednu egzotermnu vršnu temperaturu od 153 ± 2°C.
6. Kompleks aktivnog sastojka koji se sastoji od soli o-acetilsalicilne kiseline sa jednom osnovnom kiselinom i glicinom, naznačen time da se dobiva tako da se brzo dodaju o-acetilsalicilna kiselina i jedna osnovna aminokiselina u vodi ili u organskom otapalu koje se može miješati sa vodom pri temperaturi jednakoj ili manjoj od 40°C, homogena mješavina se zatim hladi na -5 do 10°C, nakon čega se dodaju rashlađeni aceton i rashlađena suspenzija glicina i miješaju se barem još 1 dodatni sat, kristalizirana tvar se izolira i tijekom kristalizacije se ne smije prekoračiti temperatura od 5°C; kompleks aktivnog sastojka ima srednju veličinu čestica manju od 100 µm.
7. Kompleks aktivnog sastojka prema zahtjevu 6 naznačen time što kompleks aktivnog sastojka sadrži od 8 do 12 težinskih postotaka glicina.
8. Kompleks aktivnog sastojka prema zahtjevima 6 do 7 naznačen time da je sa lizinom kao osnovnom aminokiselinom.
9. Kompleks aktivnog sastojka prema zahtjevima 6 do 7 naznačen time da je sa D,L-lizinom kao osnovnom aminokiselinom.
10. Kompleks aktivnog sastojka prema zahtjevu 9, naznačen time da kompleks aktivnog sastojka sadrži do 10 težinskih postotaka glicina i da u rasponu otapanja kompleks aktivnog sastojka ima jednu endotermnu vršnu temperaturu od 148 ± 2°C i jednu egzotermnu vršnu temperaturu od 153 ± 2°C.
11. Kompleks aktivnog sastojka prema zahtjevima 6 do 10, naznačen time da energija miješanja tijekom kristalizacije nije veća od 0,1 W po litri reakcijskog sredstva.
12. Kompleks aktivnog sastojka prema zahtjevima 6 do 11, naznačen time da se postupak provodi kod sterilnih uvjeta.
13. Postupak proizvodnje tvari, kao što je navedeno u bilo kojem od zahtjeva 1 do 12, naznačen time da se brzo dodaju o-acetilsalicilna kiselina i jedna osnovna aminokiselina u vodi ili u organskom otapalu koje se može miješati sa vodom pri temperaturi jednakoj ili manjoj od 40°C, te se homogena mješavina zatim hladi na -5 do 10°C, nakon čega se dodaju rashlađeni aceton i rashlađena suspenzija glicina i miješaju se barem još 1 dodatni sat, te se kristalizirana tvar izolira, a tijekom kristalizacije se ne smije prekoračiti temperatura od 5°C.
14. Postupak prema zahtjevu 13, naznačen time da energija miješanja tijekom kristalizacije nije veća od 0,1 W po litri reakcijskog sredstva.
15. Postupak prema zahtjevima 13 do 14, naznačen time da se postupak provodi kod sterilnih uvjeta.
16. Lijek naznačen time što sadrži najmanje jedan kompleks aktivnog sastojka prema bilo kojem od zahtjeva 1 do 12.
17. Lijek prema zahtjevu 16, naznačen time da je u parenteralnom obliku za davanje.
18. Lijek prema zahtjevima 16 do 17, naznačen time da je pripravak za injekcije i infuziju u obliku otopine, suspenzije ili emulzije.
19. Lijek prema bilo kojem od zahtjeva 16 do 18, naznačen time da predstavlja oblik primjene, gdje je kompleks aktivnog sastojka u obliku, na primjer liofilizata ili sterilnog praška, odvojen od otapala za injekcije ili infuzije i gdje se gotov injekcijski ili infuzijski pripravak može dobiti tek neposredno prije davanja, miješanjem sa otapalom.
20. Lijek prema bilo kojem od zahtjeva 16 do 19 naznačen time da se koristi za liječenje artritisa, neuralgija, mijalgija, migrena, infarkta miokarda, moždanog udara, ishemijske bolesti srca, angine pektoris, kod ugradnje PTCA stentova i/ili astme, gdje se astma treba liječiti pomoću inhalacije kompleksa aktivnog sastojka.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005025283A DE102005025283A1 (de) | 2005-06-02 | 2005-06-02 | Stabiler Wirkstoffkomplex von Salzen der o-Acetylsalicylsäure mit basischen Aminosäuren und Glycin |
| PCT/EP2006/004799 WO2006128600A2 (de) | 2005-06-02 | 2006-05-20 | Stabiler wirkstoffkomplex von salzen der o-acetylsalicylsäure mit basischen aminosäuren und glycin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120003T1 true HRP20120003T1 (hr) | 2012-01-31 |
Family
ID=36649662
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20120003T HRP20120003T1 (hr) | 2005-06-02 | 2012-01-02 | Stabilni kompleks aktivnog sastojka soli o-acetilsalicilne kiseline sa osnovnim aminokiselinama i glicinom |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US8063243B2 (hr) |
| EP (1) | EP1890994B1 (hr) |
| JP (1) | JP2008542316A (hr) |
| KR (1) | KR101347522B1 (hr) |
| CN (1) | CN101248036B (hr) |
| AR (1) | AR057341A1 (hr) |
| AT (1) | ATE526974T1 (hr) |
| AU (1) | AU2006254429B2 (hr) |
| BR (1) | BRPI0610734A2 (hr) |
| CA (1) | CA2610194C (hr) |
| CR (1) | CR9556A (hr) |
| CY (1) | CY1112185T1 (hr) |
| DE (1) | DE102005025283A1 (hr) |
| DK (1) | DK1890994T3 (hr) |
| ES (1) | ES2373917T3 (hr) |
| HR (1) | HRP20120003T1 (hr) |
| IL (1) | IL187772A (hr) |
| MA (1) | MA29604B1 (hr) |
| MX (1) | MX2007014988A (hr) |
| NO (1) | NO20076592L (hr) |
| NZ (1) | NZ563871A (hr) |
| PL (1) | PL1890994T3 (hr) |
| PT (1) | PT1890994E (hr) |
| RS (1) | RS52111B (hr) |
| RU (1) | RU2433995C2 (hr) |
| SG (1) | SG162744A1 (hr) |
| SI (1) | SI1890994T1 (hr) |
| TN (1) | TNSN07452A1 (hr) |
| TW (1) | TWI374740B (hr) |
| UA (1) | UA89827C2 (hr) |
| WO (1) | WO2006128600A2 (hr) |
| ZA (1) | ZA200710251B (hr) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102008004386A1 (de) * | 2008-01-14 | 2009-07-23 | Activaero Gmbh | Verwendung eines Acetylsalicylsäuresalzes zur Behandlung viraler Infektionen |
| AU2010263409B2 (en) * | 2009-06-25 | 2013-09-05 | Tetra, Sia | Novel acetylsalicylic acid salts |
| CA2766048A1 (en) | 2009-06-25 | 2010-12-29 | Tetra, Sia | Novel acetylsalicylic acid salts |
| FR2965261B1 (fr) * | 2009-09-30 | 2012-10-26 | Holis Technologies | Procede de preparation d'un sel d'acide o-acetylsalicylique d'un acide amine basique et composition obtenue par ce procede |
| FR2950625B1 (fr) * | 2009-09-30 | 2016-12-02 | Holis Tech | Procede de preparation d'un sel d'acide o-acetylsalicylique d'un acide amine basique et composition obtenue |
| TWI478715B (zh) * | 2010-12-03 | 2015-04-01 | Tetra Sia | 新穎乙醯柳酸鹽 |
| RU2011132483A (ru) * | 2011-08-02 | 2013-02-10 | Елена Александровна Моренко | Биологически активный продукт для применения в ветеринарии и животноводстве, способ его получения и способы повышения выживаемости, стимуляции роста, иммуностимуляции и повышения общей неспецифической резистентности организма сельскохозяйственных животных |
| CN102503845A (zh) * | 2011-09-28 | 2012-06-20 | 广州普星药业有限公司 | 一种dl-赖氨酸阿司匹林盐的制备方法及其应用 |
| ITMI20121144A1 (it) * | 2012-06-28 | 2013-12-29 | Dipharma Francis Srl | Procedimento per la preparazione di un sale di un farmaco antinfiammatorio non steroideo |
| LV14963B (lv) | 2013-06-28 | 2015-10-20 | Tetra, Sia | Endoteliālās disfunkcijas korektors |
| WO2017144149A1 (de) * | 2016-02-23 | 2017-08-31 | Merck Patent Gmbh | Glycin-partikel |
| DK3558920T3 (da) * | 2016-12-23 | 2021-07-05 | Aspiair Gmbh | Forbedret syntese af lysinacetylsalicylat-glycin-partikler |
| CA3064012A1 (en) | 2017-05-30 | 2018-12-06 | Rhoshan Pharmaceuticals, Inc. | In-vial deposition of a stable, sterile and crystalline o-acetyl salicylic acid (aspirin) |
| CN112592286B (zh) * | 2020-11-23 | 2024-02-02 | 蚌埠丰原医药科技发展有限公司 | 一种阿司匹林与碱性氨基酸的络合物的制备方法 |
| JP2025501974A (ja) | 2022-01-05 | 2025-01-24 | アスピエアー ゲーエムベーハー | アセチルサリチル酸リジン・グリシン粒子の改良された合成 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5610110A (en) * | 1979-07-06 | 1981-02-02 | Green Cross Corp:The | Acetyl salicylate salt preparation for injection |
| JPS5665816A (en) * | 1979-11-01 | 1981-06-03 | Green Cross Corp:The | Acetylsalicylate pharmaceutical for injection |
| US4446132A (en) * | 1982-03-11 | 1984-05-01 | Dynatech Laboratories Incorporated | Nontoxic aspirin composition |
| CS247688B1 (cs) * | 1984-12-22 | 1987-01-15 | Evzen Kasafirek | Způsob výroby soli lysinu s kyselinou acetylsalicylovou |
| EP0499142A3 (en) * | 1991-02-09 | 1993-05-05 | Hoechst Aktiengesellschaft | Potentiation of the antireactive-antiasthmatic effect of inhaled loop diuretics by inhaled non steroidal anti-flammatory drugs |
| FR2741534B1 (fr) * | 1995-11-23 | 1998-09-11 | Mazal Pharma | Composition pharmaceutique stable a base d'acide acetylsalicylique et de tocopherol |
| JPH11222425A (ja) * | 1997-10-27 | 1999-08-17 | Ss Pharmaceut Co Ltd | 関節疾患治療用関節内投与製剤 |
| DE10034802A1 (de) | 2000-07-18 | 2002-01-31 | Bayer Ag | Stabile Salze von O-Acetylsalicylsäure mit basischen Aminosäuren |
| RU2203064C2 (ru) * | 2001-03-11 | 2003-04-27 | Каменев Виктор Федорович | Способ лечения аспириновой бронхиальной астмы |
| DE10202019A1 (de) * | 2002-01-18 | 2003-07-24 | Bayer Ag | Stabile Salze von o-Acetylsalicylsäure mit basischen Aminosäuren II |
| DE102004025535A1 (de) * | 2004-05-25 | 2005-12-22 | Bayer Healthcare Ag | Kombination von Salzen der o-Acetylsalicylsäure und Alpha-Glucosidase-Inhibitoren |
-
2005
- 2005-06-02 DE DE102005025283A patent/DE102005025283A1/de not_active Withdrawn
-
2006
- 2006-05-20 WO PCT/EP2006/004799 patent/WO2006128600A2/de active Application Filing
- 2006-05-20 BR BRPI0610734-6A patent/BRPI0610734A2/pt not_active IP Right Cessation
- 2006-05-20 AU AU2006254429A patent/AU2006254429B2/en not_active Ceased
- 2006-05-20 PT PT06743005T patent/PT1890994E/pt unknown
- 2006-05-20 CA CA2610194A patent/CA2610194C/en not_active Expired - Fee Related
- 2006-05-20 MX MX2007014988A patent/MX2007014988A/es active IP Right Grant
- 2006-05-20 AT AT06743005T patent/ATE526974T1/de active
- 2006-05-20 KR KR1020077030689A patent/KR101347522B1/ko not_active Expired - Fee Related
- 2006-05-20 PL PL06743005T patent/PL1890994T3/pl unknown
- 2006-05-20 US US11/921,339 patent/US8063243B2/en not_active Expired - Fee Related
- 2006-05-20 UA UAA200715004A patent/UA89827C2/ru unknown
- 2006-05-20 EP EP06743005A patent/EP1890994B1/de active Active
- 2006-05-20 DK DK06743005.8T patent/DK1890994T3/da active
- 2006-05-20 RU RU2007148709/04A patent/RU2433995C2/ru not_active IP Right Cessation
- 2006-05-20 CN CN200680019089.XA patent/CN101248036B/zh not_active Expired - Fee Related
- 2006-05-20 JP JP2008513970A patent/JP2008542316A/ja active Pending
- 2006-05-20 SI SI200631222T patent/SI1890994T1/sl unknown
- 2006-05-20 SG SG201003850-3A patent/SG162744A1/en unknown
- 2006-05-20 NZ NZ563871A patent/NZ563871A/en not_active IP Right Cessation
- 2006-05-20 ES ES06743005T patent/ES2373917T3/es active Active
- 2006-05-20 RS RS20120002A patent/RS52111B/en unknown
- 2006-05-31 AR ARP060102261A patent/AR057341A1/es unknown
- 2006-06-01 TW TW095119296A patent/TWI374740B/zh not_active IP Right Cessation
-
2007
- 2007-11-27 ZA ZA200710251A patent/ZA200710251B/xx unknown
- 2007-11-29 IL IL187772A patent/IL187772A/en not_active IP Right Cessation
- 2007-11-30 TN TNP2007000452A patent/TNSN07452A1/en unknown
- 2007-11-30 CR CR9556A patent/CR9556A/es not_active Application Discontinuation
- 2007-12-20 NO NO20076592A patent/NO20076592L/no not_active Application Discontinuation
- 2007-12-26 MA MA30515A patent/MA29604B1/fr unknown
-
2011
- 2011-12-30 CY CY20111101292T patent/CY1112185T1/el unknown
-
2012
- 2012-01-02 HR HR20120003T patent/HRP20120003T1/hr unknown
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