AU2007226983A1 - Pharmaceutical compositions - Google Patents
Pharmaceutical compositions Download PDFInfo
- Publication number
- AU2007226983A1 AU2007226983A1 AU2007226983A AU2007226983A AU2007226983A1 AU 2007226983 A1 AU2007226983 A1 AU 2007226983A1 AU 2007226983 A AU2007226983 A AU 2007226983A AU 2007226983 A AU2007226983 A AU 2007226983A AU 2007226983 A1 AU2007226983 A1 AU 2007226983A1
- Authority
- AU
- Australia
- Prior art keywords
- solid dispersion
- polymers
- pharmaceutical composition
- polymer
- surfactant
- 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.)
- Abandoned
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 102
- 229920000642 polymer Polymers 0.000 claims description 393
- BBAWEDCPNXPBQM-GDEBMMAJSA-N telaprevir Chemical compound N([C@H](C(=O)N[C@H](C(=O)N1C[C@@H]2CCC[C@@H]2[C@H]1C(=O)N[C@@H](CCC)C(=O)C(=O)NC1CC1)C(C)(C)C)C1CCCCC1)C(=O)C1=CN=CC=N1 BBAWEDCPNXPBQM-GDEBMMAJSA-N 0.000 claims description 363
- 229960002935 telaprevir Drugs 0.000 claims description 362
- 239000007962 solid dispersion Substances 0.000 claims description 257
- 239000002904 solvent Substances 0.000 claims description 230
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 216
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 213
- 239000000203 mixture Substances 0.000 claims description 166
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 115
- 238000000034 method Methods 0.000 claims description 113
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 109
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 109
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 108
- 239000004094 surface-active agent Substances 0.000 claims description 104
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims description 95
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims description 85
- 239000006185 dispersion Substances 0.000 claims description 85
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 82
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 82
- 230000008569 process Effects 0.000 claims description 64
- 238000001694 spray drying Methods 0.000 claims description 55
- 239000003112 inhibitor Substances 0.000 claims description 44
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 42
- 239000003795 chemical substances by application Substances 0.000 claims description 42
- AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims description 41
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 39
- 239000000126 substance Substances 0.000 claims description 38
- 238000002425 crystallisation Methods 0.000 claims description 27
- 230000008025 crystallization Effects 0.000 claims description 27
- 229920002678 cellulose Polymers 0.000 claims description 23
- 239000001913 cellulose Substances 0.000 claims description 23
- 238000009472 formulation Methods 0.000 claims description 22
- 229920003169 water-soluble polymer Polymers 0.000 claims description 22
- 229930003427 Vitamin E Natural products 0.000 claims description 20
- 239000003443 antiviral agent Substances 0.000 claims description 20
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 20
- 239000011734 sodium Substances 0.000 claims description 20
- 229940046009 vitamin E Drugs 0.000 claims description 20
- 239000011709 vitamin E Substances 0.000 claims description 20
- 235000019165 vitamin E Nutrition 0.000 claims description 20
- 150000004347 all-trans-retinol derivatives Chemical class 0.000 claims description 18
- 229910052708 sodium Inorganic materials 0.000 claims description 17
- 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 claims description 16
- 238000004519 manufacturing process Methods 0.000 claims description 16
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 15
- 235000017858 Laurus nobilis Nutrition 0.000 claims description 14
- 235000005212 Terminalia tomentosa Nutrition 0.000 claims description 14
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- 208000015181 infectious disease Diseases 0.000 claims description 12
- 241000124008 Mammalia Species 0.000 claims description 9
- 208000003311 Cytochrome P-450 Enzyme Inhibitors Diseases 0.000 claims description 7
- 239000003937 drug carrier Substances 0.000 claims description 7
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- 239000004365 Protease Substances 0.000 claims description 6
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims description 5
- 101710200424 Inosine-5'-monophosphate dehydrogenase Proteins 0.000 claims description 4
- 230000002519 immonomodulatory effect Effects 0.000 claims description 4
- 229940122280 Cytochrome P450 inhibitor Drugs 0.000 claims description 3
- 244000125380 Terminalia tomentosa Species 0.000 claims 7
- 239000003814 drug Substances 0.000 description 88
- 229940079593 drug Drugs 0.000 description 83
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 64
- 239000000306 component Substances 0.000 description 50
- 239000007787 solid Substances 0.000 description 39
- -1 e.g. Substances 0.000 description 34
- 229960000583 acetic acid Drugs 0.000 description 32
- 239000012362 glacial acetic acid Substances 0.000 description 32
- 239000012530 fluid Substances 0.000 description 30
- 229910052799 carbon Inorganic materials 0.000 description 26
- 239000011877 solvent mixture Substances 0.000 description 25
- 239000007921 spray Substances 0.000 description 23
- 239000002552 dosage form Substances 0.000 description 22
- 238000001035 drying Methods 0.000 description 22
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 22
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 22
- 239000000243 solution Substances 0.000 description 22
- 150000001875 compounds Chemical class 0.000 description 20
- 239000002245 particle Substances 0.000 description 20
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- 238000002360 preparation method Methods 0.000 description 17
- 239000003826 tablet Substances 0.000 description 17
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- 235000010980 cellulose Nutrition 0.000 description 14
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 14
- 238000010922 spray-dried dispersion Methods 0.000 description 13
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 12
- 239000002270 dispersing agent Substances 0.000 description 12
- 238000004090 dissolution Methods 0.000 description 12
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- 229940124158 Protease/peptidase inhibitor Drugs 0.000 description 11
- 230000001965 increasing effect Effects 0.000 description 11
- 239000004615 ingredient Substances 0.000 description 11
- 229920001223 polyethylene glycol Polymers 0.000 description 11
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 11
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 10
- 230000002496 gastric effect Effects 0.000 description 10
- 239000000546 pharmaceutical excipient Substances 0.000 description 10
- 239000013557 residual solvent Substances 0.000 description 10
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 9
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 9
- 230000001419 dependent effect Effects 0.000 description 9
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 9
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 9
- 235000002639 sodium chloride Nutrition 0.000 description 9
- 238000003860 storage Methods 0.000 description 9
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical class CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 8
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 8
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 description 8
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 8
- 229920001903 high density polyethylene Polymers 0.000 description 8
- 239000004700 high-density polyethylene Substances 0.000 description 8
- 239000000463 material Substances 0.000 description 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 8
- 238000011282 treatment Methods 0.000 description 8
- 244000147568 Laurus nobilis Species 0.000 description 7
- 238000010521 absorption reaction Methods 0.000 description 7
- 238000000889 atomisation Methods 0.000 description 7
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- 150000003839 salts Chemical class 0.000 description 7
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 6
- GAMPNQJDUFQVQO-UHFFFAOYSA-N acetic acid;phthalic acid Chemical compound CC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O GAMPNQJDUFQVQO-UHFFFAOYSA-N 0.000 description 6
- 239000008186 active pharmaceutical agent Substances 0.000 description 6
- 229940035676 analgesics Drugs 0.000 description 6
- 239000000730 antalgic agent Substances 0.000 description 6
- 230000036765 blood level Effects 0.000 description 6
- 235000004626 essential fatty acids Nutrition 0.000 description 6
- 239000013022 formulation composition Substances 0.000 description 6
- 229940035363 muscle relaxants Drugs 0.000 description 6
- 239000003158 myorelaxant agent Substances 0.000 description 6
- 235000016709 nutrition Nutrition 0.000 description 6
- 229920000193 polymethacrylate Polymers 0.000 description 6
- 229920002451 polyvinyl alcohol Polymers 0.000 description 6
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- 239000000843 powder Substances 0.000 description 6
- 229960000329 ribavirin Drugs 0.000 description 6
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 description 6
- 230000000087 stabilizing effect Effects 0.000 description 6
- 238000001291 vacuum drying Methods 0.000 description 6
- 108010050904 Interferons Proteins 0.000 description 5
- 102000014150 Interferons Human genes 0.000 description 5
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- JBPUGFODGPKTDW-SFHVURJKSA-N [(3s)-oxolan-3-yl] n-[[3-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoylamino]phenyl]methyl]carbamate Chemical compound C=1C=C(C=2OC=NC=2)C(OC)=CC=1NC(=O)NC(C=1)=CC=CC=1CNC(=O)O[C@H]1CCOC1 JBPUGFODGPKTDW-SFHVURJKSA-N 0.000 description 5
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- 238000000634 powder X-ray diffraction Methods 0.000 description 5
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- 229940124597 therapeutic agent Drugs 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78442806P | 2006-03-20 | 2006-03-20 | |
| US60/784,428 | 2006-03-20 | ||
| PCT/US2007/064293 WO2007109604A2 (en) | 2006-03-20 | 2007-03-19 | Pharmaceutical compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2007226983A1 true AU2007226983A1 (en) | 2007-09-27 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2007226983A Abandoned AU2007226983A1 (en) | 2006-03-20 | 2007-03-19 | Pharmaceutical compositions |
Country Status (11)
| Country | Link |
|---|---|
| US (4) | US20070218138A1 (https=) |
| EP (1) | EP2001498A4 (https=) |
| JP (1) | JP2009530415A (https=) |
| CN (1) | CN101494979A (https=) |
| AR (1) | AR059978A1 (https=) |
| AU (1) | AU2007226983A1 (https=) |
| CA (1) | CA2645566A1 (https=) |
| PE (2) | PE20110286A1 (https=) |
| TW (1) | TW200812611A (https=) |
| UY (1) | UY30226A1 (https=) |
| WO (1) | WO2007109604A2 (https=) |
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| KR20210033067A (ko) | 2012-06-04 | 2021-03-25 | 파마싸이클릭스 엘엘씨 | 브루톤 타이로신 키나아제 저해제의 결정 형태 |
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| PT3038601T (pt) | 2013-08-27 | 2020-06-30 | Gilead Pharmasset Llc | Formulação combinada de dois compostos antivirais |
| EP3089736B1 (en) * | 2013-12-31 | 2025-07-23 | Ascendia Pharmaceuticals, LLC | Pharmaceutical compositions for poorly water-soluble compounds |
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| KR20170033358A (ko) * | 2014-08-07 | 2017-03-24 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나아제 저해제의 신규한 제제 |
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| CN106620711B (zh) * | 2015-11-03 | 2019-06-25 | 中国科学院大连化学物理研究所 | 一种含有白藜芦醇的组合物及其制备方法 |
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| ES2287971T3 (es) * | 1997-08-11 | 2007-12-16 | Pfizer Products Inc. | Dispersiones farmaceuticas solidas con biodisponibilidad incrementada. |
| US20010053791A1 (en) * | 2000-03-16 | 2001-12-20 | Babcock Walter C. | Glycogen phosphorylase inhibitor |
| GB0102342D0 (en) * | 2001-01-30 | 2001-03-14 | Smithkline Beecham Plc | Pharmaceutical formulation |
| AR038375A1 (es) * | 2002-02-01 | 2005-01-12 | Pfizer Prod Inc | Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo |
| JP2007509950A (ja) * | 2003-10-27 | 2007-04-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｈｃｖ処置の組合せ剤 |
| US8187874B2 (en) * | 2003-10-27 | 2012-05-29 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| AR049297A1 (es) * | 2004-06-08 | 2006-07-12 | Vertex Pharma | Una composicion farmaceutica y dispersiones solidas de vx-950 (inhibidor de la proteasa de hcv ns3/4a) y proceso de obtencion |
-
2007
- 2007-03-19 CA CA002645566A patent/CA2645566A1/en not_active Abandoned
- 2007-03-19 JP JP2009501678A patent/JP2009530415A/ja active Pending
- 2007-03-19 AU AU2007226983A patent/AU2007226983A1/en not_active Abandoned
- 2007-03-19 WO PCT/US2007/064293 patent/WO2007109604A2/en not_active Ceased
- 2007-03-19 CN CNA2007800171770A patent/CN101494979A/zh active Pending
- 2007-03-19 TW TW096109379A patent/TW200812611A/zh unknown
- 2007-03-19 US US11/687,716 patent/US20070218138A1/en not_active Abandoned
- 2007-03-19 EP EP07758805A patent/EP2001498A4/en not_active Withdrawn
- 2007-03-20 PE PE2011000165A patent/PE20110286A1/es not_active Application Discontinuation
- 2007-03-20 PE PE2007000305A patent/PE20080123A1/es not_active Application Discontinuation
- 2007-03-20 UY UY30226A patent/UY30226A1/es unknown
- 2007-03-20 AR ARP070101120A patent/AR059978A1/es not_active Application Discontinuation
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2010
- 2010-04-26 US US12/767,409 patent/US20100267744A1/en not_active Abandoned
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2011
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-
2012
- 2012-07-10 US US13/545,562 patent/US20130079289A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2645566A1 (en) | 2007-09-27 |
| EP2001498A2 (en) | 2008-12-17 |
| UY30226A1 (es) | 2007-10-31 |
| CN101494979A (zh) | 2009-07-29 |
| WO2007109604A2 (en) | 2007-09-27 |
| US20120083441A1 (en) | 2012-04-05 |
| US20070218138A1 (en) | 2007-09-20 |
| PE20080123A1 (es) | 2008-03-10 |
| AR059978A1 (es) | 2008-05-14 |
| US20100267744A1 (en) | 2010-10-21 |
| JP2009530415A (ja) | 2009-08-27 |
| TW200812611A (en) | 2008-03-16 |
| EP2001498A4 (en) | 2013-01-23 |
| US20130079289A1 (en) | 2013-03-28 |
| WO2007109604A3 (en) | 2009-04-09 |
| PE20110286A1 (es) | 2011-05-21 |
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Legal Events
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| MK4 | Application lapsed section 142(2)(d) - no continuation fee paid for the application |