CA2806737A1 - Dispersions of rasagiline citrate - Google Patents
Dispersions of rasagiline citrate Download PDFInfo
- Publication number
- CA2806737A1 CA2806737A1 CA2806737A CA2806737A CA2806737A1 CA 2806737 A1 CA2806737 A1 CA 2806737A1 CA 2806737 A CA2806737 A CA 2806737A CA 2806737 A CA2806737 A CA 2806737A CA 2806737 A1 CA2806737 A1 CA 2806737A1
- Authority
- CA
- Canada
- Prior art keywords
- rasagiline
- solid dispersion
- solvent
- mixture
- citrate
- 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
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- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 229960004502 levodopa Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
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- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
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- 239000010452 phosphate Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
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- 238000000746 purification Methods 0.000 description 1
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- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
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- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
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- 239000006190 sub-lingual tablet Substances 0.000 description 1
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- 150000008163 sugars Chemical class 0.000 description 1
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- 239000000829 suppository Substances 0.000 description 1
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- 230000009747 swallowing Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
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- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
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- 125000002348 vinylic group Chemical group 0.000 description 1
- 238000011179 visual inspection Methods 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- 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
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- A—HUMAN NECESSITIES
- 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
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- 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
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- 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
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Inorganic Chemistry (AREA)
- Psychology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40036910P | 2010-07-27 | 2010-07-27 | |
| US61/400,369 | 2010-07-27 | ||
| PCT/US2011/045569 WO2012015946A1 (en) | 2010-07-27 | 2011-07-27 | Dispersion of rasagiline citrate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2806737A1 true CA2806737A1 (en) | 2012-02-02 |
Family
ID=45530490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2806737A Abandoned CA2806737A1 (en) | 2010-07-27 | 2011-07-27 | Dispersions of rasagiline citrate |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US8691872B2 (enExample) |
| EP (1) | EP2598136A4 (enExample) |
| JP (1) | JP2013537530A (enExample) |
| AU (1) | AU2011282716A1 (enExample) |
| CA (1) | CA2806737A1 (enExample) |
| RU (1) | RU2013108256A (enExample) |
| WO (1) | WO2012015946A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2643235C (en) * | 2006-02-21 | 2014-06-17 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of multiple system atrophy |
| MX2008012781A (es) * | 2006-04-03 | 2008-10-14 | Teva Pharma | Uso de rasagilina para el tratamiento de sindrome de piernas inquietas. |
| EA016820B1 (ru) * | 2006-12-14 | 2012-07-30 | Тева Фармасьютикал Индастриз, Лтд. | Кристаллическое твердое основание разагилина |
| EP1987816A1 (de) * | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| AU2009204454B2 (en) * | 2008-01-11 | 2015-02-05 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations, their preparation and use |
| JP2011524353A (ja) * | 2008-06-10 | 2011-09-01 | テバ ファーマシューティカル インダストリーズ リミティド | ラサギリン軟ゼラチンカプセル |
| CA2767592A1 (en) | 2009-07-09 | 2011-01-13 | Ratiopharm Gmbh | Salts of rasagiline and pharmaceutical preparations thereof |
| CA2777185A1 (en) * | 2009-10-09 | 2011-04-14 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of progressive supranuclear palsy |
| EP2515891A4 (en) * | 2009-12-22 | 2013-06-05 | Teva Pharma | 3-keto-N-propargyl-1-aminoindan |
| JP2013537530A (ja) | 2010-07-27 | 2013-10-03 | テバ ファーマシューティカル インダストリーズ リミティド | ラサギリンシトレートの分散物 |
| EP2603212A4 (en) | 2010-07-27 | 2014-01-08 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF SMOKING DISORDER |
| BR112014008552A2 (pt) | 2011-10-10 | 2017-04-18 | Teva Pharma | r(+)-n-metil-propargilaminoindano |
| AU2012323349A1 (en) | 2011-10-10 | 2014-05-22 | Teva Pharmaceutical Industries Ltd. | R(+)-N-formyl-propargyl-aminoindan |
| TW201412304A (zh) | 2012-08-17 | 2014-04-01 | Teva Pharma | 瑞沙吉林之非經腸調配物 |
| CN110840845B (zh) | 2018-11-16 | 2022-10-21 | 江苏恒瑞医药股份有限公司 | 一种包含parp抑制剂的药物组合物 |
| EP4035654A1 (en) | 2021-01-30 | 2022-08-03 | Intas Pharmaceuticals Limited | An orodispersible pharmaceutical solid dosage form of rasagiline |
| WO2022162612A1 (en) | 2021-01-30 | 2022-08-04 | Intas Pharmaceuticals Ltd. | An orodispersible pharmaceutical solid dosage form of rasagiline |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
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| IL92952A (en) | 1990-01-03 | 1994-06-24 | Teva Pharma | R-enantiomers of n-propargyl-1-aminoindan compounds, their preparation and pharmaceutical compositions containing them |
| US5744500A (en) | 1990-01-03 | 1998-04-28 | Teva Pharmaceutical Industries, Ltd. | Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof |
| IL112819A (en) | 1991-10-16 | 2001-11-25 | Teva Pharma | Fluorinated 1-aminoindan compounds and a process for their preparation |
| IL115357A (en) | 1995-09-20 | 2000-01-31 | Teva Pharma | Stable compositions containing N-propargyl-1-aminoindan and polyhydric alcohols |
| IL118836A (en) | 1996-07-11 | 2001-01-11 | Teva Pharma | Pharmaceutical compositions comprising s-(-)-n-propargyl-1-aminoindan |
| EP0966435B1 (en) | 1996-12-18 | 2005-04-06 | Teva Pharmaceutical Industries, Ltd. | Aminoindan derivatives |
| EP1567152B1 (en) | 2002-11-15 | 2013-08-14 | Teva Pharmaceutical Industries Limited | Use of rasagiline with riluzole to treat amyotrophic lateral sclerosis |
| EP1694305B1 (en) * | 2003-12-01 | 2019-10-16 | Recordati Ireland Limited | Pharmaceutical compositions comprising lercanidipine |
| AU2005269416B2 (en) | 2004-07-26 | 2011-07-28 | Teva Pharmaceutical Industries, Ltd. | Pharmaceutical dosage forms including rasagiline |
| ES2371883T3 (es) | 2004-11-24 | 2012-01-11 | Teva Pharmaceutical Industries Ltd. | Composiciones de rasagilina de disgregación oral. |
| KR20130129300A (ko) | 2005-02-23 | 2013-11-27 | 테바 파마슈티컬 인더스트리즈 리미티드 | 함량 균일성이 개선된 라사길린 제형 |
| CA2630037C (en) | 2005-11-17 | 2015-03-31 | Teva Pharmaceutical Industries Ltd. | Methods for isolating propargylated aminoindans |
| US7572834B1 (en) | 2005-12-06 | 2009-08-11 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations and processes for their preparation |
| CA2643235C (en) | 2006-02-21 | 2014-06-17 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of multiple system atrophy |
| CN101032474B (zh) | 2006-03-06 | 2011-02-16 | 重庆医药工业研究院有限责任公司 | 一种治疗或预防神经系统疾病的雷沙吉兰透皮贴片及其制备方法 |
| MX2008012781A (es) | 2006-04-03 | 2008-10-14 | Teva Pharma | Uso de rasagilina para el tratamiento de sindrome de piernas inquietas. |
| EP1892233A1 (de) | 2006-08-18 | 2008-02-27 | Ratiopharm GmbH | Neue Salze des Wirkstoffs Rasagilin |
| EA016820B1 (ru) | 2006-12-14 | 2012-07-30 | Тева Фармасьютикал Индастриз, Лтд. | Кристаллическое твердое основание разагилина |
| NZ577623A (en) | 2006-12-14 | 2011-05-27 | Teva Pharma | Tannate salt of rasagiline |
| EP1987816A1 (de) | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| AU2008296908B2 (en) | 2007-09-05 | 2014-01-09 | Teva Pharmaceutical Industries, Ltd. | Method of treating glaucoma using rasagiline |
| US8188149B2 (en) | 2007-09-17 | 2012-05-29 | Teva Pharmaceutical Industries, Ltd. | Use of R(+)-N-propargy1-1-aminoindan to treat or prevent hearing loss |
| AU2009204454B2 (en) | 2008-01-11 | 2015-02-05 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations, their preparation and use |
| JP2011524353A (ja) | 2008-06-10 | 2011-09-01 | テバ ファーマシューティカル インダストリーズ リミティド | ラサギリン軟ゼラチンカプセル |
| MX2010013766A (es) * | 2008-06-13 | 2011-03-15 | Teva Pharmaceutical Ind Ltd Star | Rasagilina para modificacion de enfermedad de parkinson. |
| AU2009260728B2 (en) | 2008-06-19 | 2015-01-29 | Teva Pharmaceutical Industries, Ltd. | Process for preparing and drying solid rasagiline base |
| US8334409B2 (en) | 2008-06-19 | 2012-12-18 | Teva Pharmaceutical Industries, Ltd. | Process for purifying rasagiline base |
| DE102008064061A1 (de) | 2008-12-19 | 2010-06-24 | Ratiopharm Gmbh | Feste Zusammensetzung mit dem Wirkstoff Rasagilin |
| EP2218444A3 (en) * | 2009-01-23 | 2010-08-25 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline formulation |
| US20100189788A1 (en) | 2009-01-23 | 2010-07-29 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline base formulation |
| CA2767592A1 (en) | 2009-07-09 | 2011-01-13 | Ratiopharm Gmbh | Salts of rasagiline and pharmaceutical preparations thereof |
| CA2777185A1 (en) | 2009-10-09 | 2011-04-14 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of progressive supranuclear palsy |
| EP2515891A4 (en) | 2009-12-22 | 2013-06-05 | Teva Pharma | 3-keto-N-propargyl-1-aminoindan |
| EP2603212A4 (en) | 2010-07-27 | 2014-01-08 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF SMOKING DISORDER |
| JP2013537530A (ja) | 2010-07-27 | 2013-10-03 | テバ ファーマシューティカル インダストリーズ リミティド | ラサギリンシトレートの分散物 |
| PH12013500821A1 (en) | 2010-10-26 | 2019-07-03 | Teva Pharma | Deuterium enriched rasagiline |
| BR112014008552A2 (pt) | 2011-10-10 | 2017-04-18 | Teva Pharma | r(+)-n-metil-propargilaminoindano |
| AU2012323349A1 (en) | 2011-10-10 | 2014-05-22 | Teva Pharmaceutical Industries Ltd. | R(+)-N-formyl-propargyl-aminoindan |
| EA201490756A1 (ru) | 2011-10-10 | 2014-09-30 | Тева Фармасьютикал Индастриз, Лтд. | Разагилина цитрамид |
-
2011
- 2011-07-27 JP JP2013521947A patent/JP2013537530A/ja not_active Withdrawn
- 2011-07-27 AU AU2011282716A patent/AU2011282716A1/en not_active Abandoned
- 2011-07-27 CA CA2806737A patent/CA2806737A1/en not_active Abandoned
- 2011-07-27 EP EP11813128.3A patent/EP2598136A4/en not_active Withdrawn
- 2011-07-27 RU RU2013108256/15A patent/RU2013108256A/ru not_active Application Discontinuation
- 2011-07-27 WO PCT/US2011/045569 patent/WO2012015946A1/en not_active Ceased
- 2011-07-27 US US13/192,082 patent/US8691872B2/en not_active Expired - Fee Related
-
2014
- 2014-03-10 US US14/203,209 patent/US20140194510A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012015946A8 (en) | 2013-01-31 |
| US20120059058A1 (en) | 2012-03-08 |
| US8691872B2 (en) | 2014-04-08 |
| AU2011282716A1 (en) | 2013-03-14 |
| WO2012015946A1 (en) | 2012-02-02 |
| EP2598136A4 (en) | 2015-03-25 |
| EP2598136A1 (en) | 2013-06-05 |
| RU2013108256A (ru) | 2014-09-10 |
| JP2013537530A (ja) | 2013-10-03 |
| US20140194510A1 (en) | 2014-07-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20160727 |