ES2547117T3 - Utilización de ésteres de ácidos amidoxima-carboxílicos y de ésteres de ácidos N-hidroxiguanidino-carboxílicos para la preparación de profármacos - Google Patents
Utilización de ésteres de ácidos amidoxima-carboxílicos y de ésteres de ácidos N-hidroxiguanidino-carboxílicos para la preparación de profármacos Download PDFInfo
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- ES2547117T3 ES2547117T3 ES09705303.7T ES09705303T ES2547117T3 ES 2547117 T3 ES2547117 T3 ES 2547117T3 ES 09705303 T ES09705303 T ES 09705303T ES 2547117 T3 ES2547117 T3 ES 2547117T3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/62—Oximes having oxygen atoms of oxyimino groups esterified
- C07C251/64—Oximes having oxygen atoms of oxyimino groups esterified by carboxylic acids
- C07C251/66—Oximes having oxygen atoms of oxyimino groups esterified by carboxylic acids with the esterifying carboxyl groups bound to hydrogen atoms, to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
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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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
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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
- 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
- A61P25/28—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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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
- A61P9/12—Antihypertensives
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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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Biomedical Technology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- AIDS & HIV (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Utilización de un éster de ácido amidoxima-carboxílico de la fórmula (I) o de un éster de ácido N-hidroxiguanidinocarboxílico de la fórmula (II)**Fórmula** siendo n >= 0,..., 12, y escogiéndose R1 entre el conjunto que se compone de hidrógeno, un radical alquilo y un radical arilo y unas sales de éstos, como reemplazo de una o varias funciones de amidina, N-hidroxiamidina (amidoxima), guanidina o respectivamente N-hidroxiguanidina de una sustancia medicamentosa en unos medicamentos destinados al mejoramiento de la solubilidad y/o la biodisponibilidad de la sustancia medicamentosa, caracterizado por que la sustancia medicamentosa se escoge entre el conjunto que se compone de las sustancias inhibidoras de proteasas, siendo la sustancia inhibidora de una proteasa una sustancia inhibidora de la trombina, una sustancia inhibidora del factor Xa, del factor VII o de todas las proteasas de la cascada de coagulación, o una sustancia inhibidora de la matriptasa, los compuestos intercaladores de ADN y ARN, las sustancias inhibidoras de enzimas víricas y del agente antagonista del receptor de N-metil-D-aspartato.
Description
E09705303
11-09-2015
Rata 21 38,7
Tal como se puede deducir de la Tabla superior, la benzamidina posee, después de una administración por vía oral de la O-succinil-benzamidoxima, una biodisponibilidad de 32 %. Este hecho pone de manifiesto que el profármaco es resorbido después de una administración por vía oral y es reducido en la sangre para dar la forma activa.
Los resultados de los ensayos se han expuesto en los dibujos adjuntos, en los cuales:
Fig.1 las curvas del nivel en plasma de la benzamidina después de una aplicación por vía oral de la O-succinilbenzamidoxima
Fig. 2 el metabolismo del éster de ácido diminazen-succínico y
9
Claims (1)
-
imagen1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102008007381 | 2008-02-01 | ||
| DE102008007381A DE102008007381A1 (de) | 2008-02-01 | 2008-02-01 | Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten |
| PCT/EP2009/051132 WO2009095499A1 (de) | 2008-02-01 | 2009-02-02 | Verwendung von amidoximcarbonsäureesters und n-hydroxyguanidincarbonsäureesters zur herstellung von prodrugs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2547117T3 true ES2547117T3 (es) | 2015-10-01 |
Family
ID=40532565
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09705303.7T Active ES2547117T3 (es) | 2008-02-01 | 2009-02-02 | Utilización de ésteres de ácidos amidoxima-carboxílicos y de ésteres de ácidos N-hidroxiguanidino-carboxílicos para la preparación de profármacos |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US20110028756A1 (es) |
| EP (3) | EP2732816A1 (es) |
| JP (2) | JP2011510956A (es) |
| KR (1) | KR20100110875A (es) |
| CN (1) | CN101951897B (es) |
| AU (1) | AU2009209560B2 (es) |
| BR (1) | BRPI0906569A2 (es) |
| CA (1) | CA2713784C (es) |
| CY (1) | CY1116801T1 (es) |
| DE (1) | DE102008007381A1 (es) |
| DK (1) | DK2249821T3 (es) |
| ES (1) | ES2547117T3 (es) |
| HK (1) | HK1153144A1 (es) |
| HR (1) | HRP20150961T1 (es) |
| HU (1) | HUE026276T2 (es) |
| IL (1) | IL207286A0 (es) |
| PL (1) | PL2249821T3 (es) |
| PT (1) | PT2249821E (es) |
| SI (1) | SI2249821T1 (es) |
| WO (1) | WO2009095499A1 (es) |
| ZA (1) | ZA201004767B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9662308B2 (en) | 2008-02-01 | 2017-05-30 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co. Kg | Orally bioavailable pentamidine prodrugs for the treatment of diseases |
| DE102008007381A1 (de) | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten |
| DE102009004204A1 (de) * | 2009-01-09 | 2010-07-15 | Christian-Albrechts-Universität Zu Kiel | Verfahren zur verbesserten Bioaktivierung von Arzneistoffen |
| EP2550966B1 (de) * | 2011-07-25 | 2016-10-19 | Dritte Patentportfolio Beteiligungsgesellschaft mbH & Co. KG | Dabigatran-Amidoximsäureesters als Prodrugs und ihre Verwendung als Arzneimittel |
| LT2550963T (lt) | 2011-07-25 | 2017-02-27 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co. Kg | Pentamidino-amidoksimo karboksirūgšties esteriai, kaip provaistai, ir jų naudojimas kaip vaistų |
| ES2416004B1 (es) * | 2012-01-24 | 2014-01-28 | Investigaciones Farmaceuticas Y Veterinarias, S.L. | Composición farmacéutica que comprende cloruro de isometamidium en solución para el tratamiento de la tripanosomiasis en animales. |
| CN103420994B (zh) * | 2012-05-24 | 2016-04-06 | 天津药物研究院 | 作为前药的达比加群酯衍生物及其制备方法和用途 |
| US9375411B2 (en) * | 2012-12-21 | 2016-06-28 | Verlyx Pharma Inc. | Uses and methods for the treatment of liver diseases or conditions |
| CN106831611B (zh) * | 2017-01-23 | 2019-06-21 | 北京化工大学 | 一种偕胺肟类化合物及其在制备抑制癌细胞增殖药的应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4321444A1 (de) * | 1993-06-28 | 1995-01-05 | Bernd Prof Dr Clement | Pharmazeutische Zubereitung |
| JP2001031586A (ja) * | 1999-07-14 | 2001-02-06 | Sunstar Inc | 動脈硬化症及び動脈硬化症に起因する疾患の予防又は治療組成物 |
| EP1294405A2 (en) | 2000-06-14 | 2003-03-26 | Corixa Corporation | Prodrug compounds cleavable by thimet oligopeptidase |
| ES2364452T3 (es) * | 2001-06-11 | 2011-09-02 | Medarex, Inc. | Método para diseñar compuestos profármacos activados por cd10. |
| MXPA04003169A (es) * | 2001-10-03 | 2004-07-08 | Pharmacia Corp | Profarmacos de compuestos policiclicos sustituidos utiles para inhibicion selectiva de la cascada de coagulacion. |
| DE10323898A1 (de) * | 2003-05-26 | 2004-12-23 | Wilex Ag | Hydroxyamidin- und Hydroxyguanidin-Verbindungen als Urokinase-Hemmstoffe |
| JPWO2005049636A1 (ja) * | 2003-11-21 | 2007-06-07 | 日本電気株式会社 | タンパク質の分析方法 |
| CA2572161C (en) | 2004-06-30 | 2012-10-02 | Toyama Chemical Co., Ltd. | Novel arylamidine derivative, salt thereof, and antifungal containing these |
| DE102006034256A1 (de) * | 2006-07-21 | 2008-01-31 | Christian-Albrechts-Universität Zu Kiel | Verbesserung der Bioverfügbarkeit von Wirkstoffen mit Amidinfunktion in Arzneimitteln |
| DE102008007381A1 (de) | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten |
-
2008
- 2008-02-01 DE DE102008007381A patent/DE102008007381A1/de not_active Withdrawn
-
2009
- 2009-02-02 EP EP20140155230 patent/EP2732816A1/de not_active Ceased
- 2009-02-02 EP EP15178466.7A patent/EP2985021A1/de not_active Withdrawn
- 2009-02-02 JP JP2010544724A patent/JP2011510956A/ja not_active Withdrawn
- 2009-02-02 DK DK09705303.7T patent/DK2249821T3/en active
- 2009-02-02 EP EP09705303.7A patent/EP2249821B1/de active Active
- 2009-02-02 HU HUE09705303A patent/HUE026276T2/en unknown
- 2009-02-02 CN CN200980103401.7A patent/CN101951897B/zh not_active Expired - Fee Related
- 2009-02-02 ES ES09705303.7T patent/ES2547117T3/es active Active
- 2009-02-02 SI SI200931253T patent/SI2249821T1/sl unknown
- 2009-02-02 AU AU2009209560A patent/AU2009209560B2/en not_active Ceased
- 2009-02-02 WO PCT/EP2009/051132 patent/WO2009095499A1/de active Application Filing
- 2009-02-02 CA CA2713784A patent/CA2713784C/en active Active
- 2009-02-02 KR KR1020107018471A patent/KR20100110875A/ko not_active Application Discontinuation
- 2009-02-02 PT PT97053037T patent/PT2249821E/pt unknown
- 2009-02-02 PL PL09705303T patent/PL2249821T3/pl unknown
- 2009-02-02 BR BRPI0906569-5A patent/BRPI0906569A2/pt not_active IP Right Cessation
-
2010
- 2010-07-07 ZA ZA2010/04767A patent/ZA201004767B/en unknown
- 2010-07-29 IL IL207286A patent/IL207286A0/en unknown
- 2010-07-30 US US12/847,415 patent/US20110028756A1/en not_active Abandoned
-
2011
- 2011-07-15 HK HK11107361.3A patent/HK1153144A1/zh not_active IP Right Cessation
-
2014
- 2014-08-08 US US14/455,272 patent/US9353047B2/en active Active
-
2015
- 2015-09-11 HR HRP20150961TT patent/HRP20150961T1/hr unknown
- 2015-10-20 CY CY20151100936T patent/CY1116801T1/el unknown
-
2016
- 2016-06-14 JP JP2016117936A patent/JP2016193927A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA2713784A1 (en) | 2009-08-06 |
| PT2249821E (pt) | 2015-10-13 |
| BRPI0906569A2 (pt) | 2015-07-07 |
| KR20100110875A (ko) | 2010-10-13 |
| DE102008007381A1 (de) | 2009-08-13 |
| US9353047B2 (en) | 2016-05-31 |
| WO2009095499A1 (de) | 2009-08-06 |
| AU2009209560A1 (en) | 2009-08-06 |
| SI2249821T1 (sl) | 2015-12-31 |
| CN101951897B (zh) | 2016-01-20 |
| US20140350293A1 (en) | 2014-11-27 |
| EP2249821B1 (de) | 2015-07-29 |
| EP2249821A1 (de) | 2010-11-17 |
| ZA201004767B (en) | 2011-04-28 |
| AU2009209560B2 (en) | 2013-10-31 |
| HK1153144A1 (zh) | 2012-03-23 |
| EP2732816A1 (de) | 2014-05-21 |
| DK2249821T3 (en) | 2015-10-05 |
| EP2985021A1 (de) | 2016-02-17 |
| CN101951897A (zh) | 2011-01-19 |
| IL207286A0 (en) | 2010-12-30 |
| US20110028756A1 (en) | 2011-02-03 |
| HRP20150961T1 (hr) | 2015-11-06 |
| JP2011510956A (ja) | 2011-04-07 |
| JP2016193927A (ja) | 2016-11-17 |
| PL2249821T3 (pl) | 2015-12-31 |
| HUE026276T2 (en) | 2016-06-28 |
| CY1116801T1 (el) | 2017-03-15 |
| CA2713784C (en) | 2016-09-27 |
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