KR102062936B1 - 불소 함유 아미노산의 프로드러그 - Google Patents

불소 함유 아미노산의 프로드러그 Download PDF

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KR102062936B1
KR102062936B1 KR1020147032686A KR20147032686A KR102062936B1 KR 102062936 B1 KR102062936 B1 KR 102062936B1 KR 1020147032686 A KR1020147032686 A KR 1020147032686A KR 20147032686 A KR20147032686 A KR 20147032686A KR 102062936 B1 KR102062936 B1 KR 102062936B1
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carbonyl
group
hexane
amino
oxy
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KR20150016248A (ko
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다까시 하시하야따
노리까즈 오따께
나오끼 미야꼬시
가즈나리 사까가미
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다이쇼 세이야꾸 가부시끼가이샤
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/265Esters, e.g. nitroglycerine, selenocyanates of carbonic, thiocarbonic, or thiocarboxylic acids, e.g. thioacetic acid, xanthogenic acid, trithiocarbonic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C229/50Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms being part of the same condensed ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D317/34Oxygen atoms
    • C07D317/40Vinylene carbonate; Substituted vinylene carbonates
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
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    • C07C2602/14All rings being cycloaliphatic
    • C07C2602/18All rings being cycloaliphatic the ring system containing six carbon atoms
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/56Ring systems containing bridged rings
    • C07C2603/58Ring systems containing bridged rings containing three rings
    • C07C2603/70Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74Adamantanes

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  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020147032686A 2012-06-01 2013-05-31 불소 함유 아미노산의 프로드러그 Active KR102062936B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2012126162 2012-06-01
JPJP-P-2012-126162 2012-06-01
JP2013052574 2013-03-15
JPJP-P-2013-052574 2013-03-15
PCT/JP2013/065202 WO2013180271A1 (ja) 2012-06-01 2013-05-31 含フッ素アミノ酸のプロドラッグ

Publications (2)

Publication Number Publication Date
KR20150016248A KR20150016248A (ko) 2015-02-11
KR102062936B1 true KR102062936B1 (ko) 2020-01-06

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US (1) US9428483B2 (enExample)
EP (1) EP2857385B1 (enExample)
JP (1) JP5979230B2 (enExample)
KR (1) KR102062936B1 (enExample)
CN (1) CN104334524B (enExample)
AU (1) AU2013268303B2 (enExample)
BR (1) BR112014029478B1 (enExample)
CA (1) CA2875080C (enExample)
CY (1) CY1119646T1 (enExample)
DK (1) DK2857385T3 (enExample)
ES (1) ES2637986T3 (enExample)
HR (1) HRP20171373T1 (enExample)
HU (1) HUE034513T2 (enExample)
IL (1) IL235897B (enExample)
IN (1) IN2014DN10538A (enExample)
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ME (1) ME02833B (enExample)
MX (1) MX355161B (enExample)
MY (1) MY169069A (enExample)
NO (1) NO2857385T3 (enExample)
NZ (1) NZ702237A (enExample)
PH (1) PH12014502670B1 (enExample)
PL (1) PL2857385T3 (enExample)
PT (1) PT2857385T (enExample)
RS (1) RS56328B1 (enExample)
RU (1) RU2639868C1 (enExample)
SG (1) SG11201407973SA (enExample)
SI (1) SI2857385T1 (enExample)
SM (1) SMT201700486T1 (enExample)
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EA201591931A1 (ru) 2013-04-09 2016-05-31 Ликсте Байотекнолоджи, Инк. Композиции оксабициклогептанов и оксабициклогептенов
JP5983713B2 (ja) * 2013-11-29 2016-09-06 大正製薬株式会社 含フッ素アミノ酸のプロドラッグを含有する医薬
JP5983714B2 (ja) * 2013-11-29 2016-09-06 大正製薬株式会社 含フッ素アミノ酸プロドラッグの結晶形とその製造方法
MX2016008110A (es) * 2013-12-20 2016-08-19 Hoffmann La Roche Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.
MX386975B (es) * 2015-05-15 2025-03-19 Lixte Biotechnology Inc Fármacos precursores de oxabicicloheptanos.
HRP20211277T1 (hr) * 2016-04-18 2021-11-12 Taisho Pharmaceutical Co., Ltd. Predlijek derivata aminokiseline
IL290857B2 (en) 2016-12-08 2023-03-01 Lixte Biotechnology Inc Oxabicycloheptanes for immune response modulation
JP7314494B2 (ja) * 2017-10-17 2023-07-26 大正製薬株式会社 アミノ酸誘導体のプロドラッグを含有する医薬
CN119059935A (zh) * 2024-11-07 2024-12-03 安徽金禾合成材料研究院有限公司 一种采用前馏分溶剂法合成2,2-二异丙基丙腈的方法

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CA2318800C (en) 1998-01-28 2005-12-20 Taisho Pharmaceutical Co., Ltd. Fluorine-containing amino acid derivatives
JP4171549B2 (ja) * 1998-01-28 2008-10-22 大正製薬株式会社 含フッ素アミノ酸誘導体
WO2000037410A1 (fr) 1998-12-18 2000-06-29 Taisho Pharmaceutical Co., Ltd. Intermediaires et procedes de production de compose aminoacide contenant du fluor utilisant ces intermediaires
JP4783967B2 (ja) * 1999-07-21 2011-09-28 大正製薬株式会社 含フッ素アミノ酸誘導体を有効成分とする医薬
MXPA04006322A (es) * 2001-12-27 2004-10-04 Taisho Pharmaceutical Co Ltd Derivados de 6-fluorobiciclo[3.1.0]hexano.
CN100482680C (zh) * 2002-06-11 2009-04-29 伊莱利利公司 兴奋性氨基酸前药
ATE421526T1 (de) * 2002-06-11 2009-02-15 Lilly Co Eli Prodrugs von exzitatorischen aminosäuren
JP5983713B2 (ja) * 2013-11-29 2016-09-06 大正製薬株式会社 含フッ素アミノ酸のプロドラッグを含有する医薬
JP5983714B2 (ja) * 2013-11-29 2016-09-06 大正製薬株式会社 含フッ素アミノ酸プロドラッグの結晶形とその製造方法

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SG11201407973SA (en) 2015-01-29
US9428483B2 (en) 2016-08-30
ES2637986T3 (es) 2017-10-18
CY1119646T1 (el) 2018-04-04
CN104334524B (zh) 2016-10-12
IL235897A0 (en) 2015-02-01
HK1202526A1 (en) 2015-10-02
BR112014029478B1 (pt) 2023-01-17
ME02833B (me) 2018-01-20
JPWO2013180271A1 (ja) 2016-01-21
NZ702237A (en) 2016-08-26
TWI602801B (zh) 2017-10-21
AU2013268303A1 (en) 2014-12-18
CA2875080C (en) 2020-03-24
HUE034513T2 (en) 2018-02-28
EP2857385A4 (en) 2015-11-11
US20150141669A1 (en) 2015-05-21
ZA201408857B (en) 2016-08-31
MX2014014642A (es) 2015-02-12
RS56328B1 (sr) 2017-12-29
CN104334524A (zh) 2015-02-04
LT2857385T (lt) 2017-10-25
SMT201700486T1 (it) 2017-11-15
DK2857385T3 (en) 2017-09-11
NO2857385T3 (enExample) 2017-12-30
CA2875080A1 (en) 2013-12-05
HRP20171373T1 (hr) 2017-11-03
TW201408627A (zh) 2014-03-01
AU2013268303B2 (en) 2017-01-05
WO2013180271A1 (ja) 2013-12-05
EP2857385A1 (en) 2015-04-08
PH12014502670A1 (en) 2015-02-02
BR112014029478A2 (pt) 2017-06-27
SI2857385T1 (sl) 2017-10-30
RU2639868C1 (ru) 2017-12-25
MY169069A (en) 2019-02-12
EP2857385B1 (en) 2017-08-02
JP5979230B2 (ja) 2016-08-24
BR112014029478A8 (pt) 2021-03-16
PT2857385T (pt) 2017-11-08
PL2857385T3 (pl) 2018-01-31
IL235897B (en) 2019-09-26
PH12014502670B1 (en) 2015-02-02
MX355161B (es) 2018-04-06
IN2014DN10538A (enExample) 2015-08-21
KR20150016248A (ko) 2015-02-11

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