CA2878135C - Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs - Google Patents
Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs Download PDFInfo
- Publication number
- CA2878135C CA2878135C CA2878135A CA2878135A CA2878135C CA 2878135 C CA2878135 C CA 2878135C CA 2878135 A CA2878135 A CA 2878135A CA 2878135 A CA2878135 A CA 2878135A CA 2878135 C CA2878135 C CA 2878135C
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- chemical substance
- treatment
- medicament
- cognitive impairment
- salt
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- 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
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- 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
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
- A61K9/2846—Poly(meth)acrylates
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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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- 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
-
- 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
-
- 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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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Nutrition Science (AREA)
- Dispersion Chemistry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Physiology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Toxicology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261676348P | 2012-07-27 | 2012-07-27 | |
| US61/676,348 | 2012-07-27 | ||
| EP12178187.6 | 2012-07-27 | ||
| EP12178187 | 2012-07-27 | ||
| PCT/EP2013/065880 WO2014016430A1 (en) | 2012-07-27 | 2013-07-29 | Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2878135A1 CA2878135A1 (en) | 2014-01-30 |
| CA2878135C true CA2878135C (en) | 2019-12-03 |
Family
ID=49996636
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2878135A Active CA2878135C (en) | 2012-07-27 | 2013-07-29 | Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20150190401A1 (enExample) |
| EP (2) | EP3417862B1 (enExample) |
| JP (2) | JP6272857B2 (enExample) |
| CN (2) | CN104507461A (enExample) |
| AU (1) | AU2013294917B2 (enExample) |
| CA (1) | CA2878135C (enExample) |
| DK (2) | DK3417862T3 (enExample) |
| ES (1) | ES2700473T3 (enExample) |
| HK (1) | HK1206242A1 (enExample) |
| IN (1) | IN2015DN00229A (enExample) |
| PL (2) | PL2877165T3 (enExample) |
| WO (1) | WO2014016430A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090253654A1 (en) | 2005-09-22 | 2009-10-08 | Galantos Pharma Gmbh | Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment |
| ES2880399T3 (es) * | 2012-07-27 | 2021-11-24 | Neurodyn Life Sciences Inc | Biodisponibilidad cerebral mejorada de galantamina mediante formulaciones seleccionadas y administración transmucosa de profármacos lipofílicos |
| AU2015258814B2 (en) | 2014-05-16 | 2018-04-05 | Synaptec Development Llc | Clearance of amyloid ss |
| JP2020033304A (ja) * | 2018-08-30 | 2020-03-05 | 医療法人ふじいやさか | 薬剤又はサプリメント、組成物、及び水素供給器の使用 |
| JP2022538608A (ja) * | 2019-06-28 | 2022-09-05 | ザ トラスティーズ オヴ ザ ユニヴァーシティー オヴ ペンシルバニア | アルツハイマー病の治療のための鼻腔内ダントロレン投与 |
| EP4029867A1 (en) | 2021-01-13 | 2022-07-20 | Alpha Cognition Inc. | Solid forms of galantamine benzoate gluconate |
| WO2022236396A1 (en) * | 2021-05-14 | 2022-11-17 | Alpha Cognition Inc. | Self-preserving compositions and multi-use dispensers for administering alpha-1062 |
| EP4186509A1 (en) | 2021-11-26 | 2023-05-31 | Alpha Cognition Inc. | Alpha-1062 for treating traumatic brain injury |
| US12589099B2 (en) | 2021-11-26 | 2026-03-31 | Alpha Cognition Inc. | Alpha-1062 for treating traumatic brain injury |
| CN121443298A (zh) * | 2023-05-25 | 2026-01-30 | 阿尔法认知公司 | 用于治疗持续性脑震荡后症状的苯加兰他敏 |
| US12208167B1 (en) * | 2024-02-06 | 2025-01-28 | Alpha Cognition Inc. | Coated tablets for pH-dependent release of benzgalantamine |
| US12551491B1 (en) * | 2025-07-23 | 2026-02-17 | Alpha Cognition Inc. | Dosage regimens for benzgalantamine |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1248059B (it) * | 1991-06-14 | 1995-01-05 | Miat Spa | Insufflatore multidose per farmaci in polvere |
| BR0213696A (pt) * | 2001-10-31 | 2004-10-26 | Pfizer Prod Inc | Agonistas do receptor de acetilcolina nicotìnicos no tratamento da sìndrome de pernas inquietas |
| US20040254146A1 (en) * | 2002-05-21 | 2004-12-16 | Nastech Pharmaceutical Company Inc. | Carboxylate salts of galantamine and their pharmaceutical use |
| DE10338544B4 (de) * | 2003-08-19 | 2017-08-31 | Janssen Pharmaceutica N.V. | Buccale Formulierungen des Galanthamins und deren Anwendungen |
| US20090253654A1 (en) * | 2005-09-22 | 2009-10-08 | Galantos Pharma Gmbh | Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment |
| ATE473219T1 (de) * | 2005-09-22 | 2010-07-15 | Galantos Pharma Gmbh | Cholinerge enhancer mit verbesserter durchgängigkeit durch die blut-hirn-schranke zur behandlung von krankheiten, die mit kognitiven störungen einhergehen |
| EP2152240A4 (en) * | 2007-06-08 | 2012-05-09 | Healthpartners Res Foundation | PHARMACEUTICAL COMPOSITIONS AND METHOD FOR REINFORCED TARGETING OF THERAPEUTIC COMPOUNDS TO THE CENTRAL NERVOUS SYSTEM |
| JP2009197874A (ja) * | 2008-02-20 | 2009-09-03 | Works Bell:Kk | 動力伝達装置 |
| EP2137192B8 (en) * | 2008-04-14 | 2014-06-11 | Neurodyn Life Sciences Inc. | Derivatives of galantamine as pro-drugs for the treatment of human brain diseases |
| US20130317117A1 (en) * | 2010-11-24 | 2013-11-28 | Pharmaceutics International, Inc. | Self micro-emulsifying drug delivery system with increased bioavailability |
-
2013
- 2013-07-29 ES ES13745810T patent/ES2700473T3/es active Active
- 2013-07-29 DK DK18186075.0T patent/DK3417862T3/da active
- 2013-07-29 CA CA2878135A patent/CA2878135C/en active Active
- 2013-07-29 EP EP18186075.0A patent/EP3417862B1/en active Active
- 2013-07-29 WO PCT/EP2013/065880 patent/WO2014016430A1/en not_active Ceased
- 2013-07-29 DK DK13745810.5T patent/DK2877165T3/da active
- 2013-07-29 JP JP2015523573A patent/JP6272857B2/ja not_active Expired - Fee Related
- 2013-07-29 CN CN201380039870.3A patent/CN104507461A/zh active Pending
- 2013-07-29 AU AU2013294917A patent/AU2013294917B2/en not_active Ceased
- 2013-07-29 PL PL13745810T patent/PL2877165T3/pl unknown
- 2013-07-29 US US14/417,502 patent/US20150190401A1/en not_active Abandoned
- 2013-07-29 PL PL18186075T patent/PL3417862T3/pl unknown
- 2013-07-29 CN CN201810140325.8A patent/CN108245522A/zh active Pending
- 2013-07-29 EP EP13745810.5A patent/EP2877165B1/en active Active
- 2013-07-29 HK HK15106777.9A patent/HK1206242A1/xx unknown
-
2015
- 2015-01-09 IN IN229DEN2015 patent/IN2015DN00229A/en unknown
-
2018
- 2018-01-04 JP JP2018000060A patent/JP6574002B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DK2877165T3 (da) | 2019-01-02 |
| EP3417862B1 (en) | 2021-05-05 |
| CA2878135A1 (en) | 2014-01-30 |
| JP2018100272A (ja) | 2018-06-28 |
| EP2877165A1 (en) | 2015-06-03 |
| IN2015DN00229A (enExample) | 2015-06-12 |
| JP2015524423A (ja) | 2015-08-24 |
| ES2700473T3 (es) | 2019-02-18 |
| PL2877165T3 (pl) | 2019-05-31 |
| JP6574002B2 (ja) | 2019-09-11 |
| US20150190401A1 (en) | 2015-07-09 |
| CN104507461A (zh) | 2015-04-08 |
| AU2013294917A1 (en) | 2015-01-22 |
| EP2877165B1 (en) | 2018-09-05 |
| PL3417862T3 (pl) | 2021-11-22 |
| AU2013294917B2 (en) | 2016-12-15 |
| HK1206242A1 (en) | 2016-01-08 |
| CN108245522A (zh) | 2018-07-06 |
| DK3417862T3 (da) | 2021-07-12 |
| EP3417862A1 (en) | 2018-12-26 |
| WO2014016430A1 (en) | 2014-01-30 |
| JP6272857B2 (ja) | 2018-01-31 |
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Free format text: ST27 STATUS EVENT CODE: N-6-6-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT Effective date: 20260713 |