EA201100424A1 - Новые ингибиторы - Google Patents

Новые ингибиторы

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Publication number
EA201100424A1
EA201100424A1 EA201100424A EA201100424A EA201100424A1 EA 201100424 A1 EA201100424 A1 EA 201100424A1 EA 201100424 A EA201100424 A EA 201100424A EA 201100424 A EA201100424 A EA 201100424A EA 201100424 A1 EA201100424 A1 EA 201100424A1
Authority
EA
Eurasian Patent Office
Prior art keywords
new inhibitors
glutaminyl cyclase
inhibitors
modulating
context
Prior art date
Application number
EA201100424A
Other languages
English (en)
Other versions
EA021150B1 (ru
Inventor
Михаэль Альмштеттер
Ханс-Ульрих Демут
Антье Хаманн
Ульрих Хайзер
Торстен Хоффманн
Роберт Зоммер
Михаэль Торманн
Андреас Тремль
Ульф-Торстен Гэртнер
Original Assignee
Пробиодруг Аг
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Пробиодруг Аг filed Critical Пробиодруг Аг
Publication of EA201100424A1 publication Critical patent/EA201100424A1/ru
Publication of EA021150B1 publication Critical patent/EA021150B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Anesthesiology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pregnancy & Childbirth (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)

Abstract

В заявке описаны соединения общей формулы (I)где R, R, R, R, Х и Y определены в данном контексте, в качестве ингибиторов глутаминилциклазы и, следовательно, их применение для лечения состояний, которые можно лечить при модуляции активности глутаминилциклазы.
EA201100424A 2008-09-04 2009-09-04 Производные имидазолидина в качестве ингибиторов глутаминилциклазы EA021150B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9411808P 2008-09-04 2008-09-04
PCT/EP2009/061453 WO2010026212A1 (en) 2008-09-04 2009-09-04 Novel inhibitors

Publications (2)

Publication Number Publication Date
EA201100424A1 true EA201100424A1 (ru) 2011-10-31
EA021150B1 EA021150B1 (ru) 2015-04-30

Family

ID=41278686

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201100424A EA021150B1 (ru) 2008-09-04 2009-09-04 Производные имидазолидина в качестве ингибиторов глутаминилциклазы

Country Status (17)

Country Link
US (1) US8962860B2 (ru)
EP (1) EP2344157B1 (ru)
JP (1) JP5707327B2 (ru)
KR (1) KR101694556B1 (ru)
CN (1) CN102186475B (ru)
AU (1) AU2009289238B2 (ru)
BR (1) BRPI0918564B1 (ru)
CA (1) CA2735795C (ru)
DK (1) DK2344157T3 (ru)
EA (1) EA021150B1 (ru)
ES (1) ES2599621T3 (ru)
IL (1) IL211018A (ru)
MX (1) MX2011002106A (ru)
NZ (1) NZ591531A (ru)
SG (1) SG193828A1 (ru)
WO (1) WO2010026212A1 (ru)
ZA (1) ZA201100898B (ru)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5788320B2 (ja) * 2008-09-04 2015-09-30 プロビオドルグ エージー イソｑｃ阻害剤の使用
KR101755737B1 (ko) 2009-09-11 2017-07-07 프로비오드룩 아게 글루타미닐 사이클라제의 억제제로서 헤테로사이클릭 유도체
WO2011076854A1 (en) 2009-12-22 2011-06-30 Probiodrug Ag CLEAVAGE OF β-AMYLOID PRECURSOR PROTEIN
ES2570167T3 (es) * 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
JP2014515364A (ja) * 2011-05-27 2014-06-30 プロビオドルグ エージー 放射能標識グルタミニルシクラーゼ阻害剤
CN105263927B (zh) * 2013-03-15 2019-03-15 前体生物药物股份公司 谷氨酰胺酰环化酶抑制剂
WO2016097305A1 (en) 2014-12-19 2016-06-23 Probiodrug Ag Novel method for the detection of pglu-abeta peptides
CN108658869A (zh) * 2017-03-29 2018-10-16 复旦大学 具有抗肿瘤活性的化合物及其制备方法和在制药中的用途
RU2665633C1 (ru) * 2017-05-26 2018-09-03 Общество С Ограниченной Ответственностью "Фарминтерпрайсез" Новый ингибитор глутаминилциклаз и его применение
RU2662559C1 (ru) * 2017-10-27 2018-07-26 Общество С Ограниченной Ответственностью "Фарминтерпрайсез" Новый ингибитор глутаминилциклаз и его применение для лечения заболеваний легких и дыхательных путей
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
AU2019223215B2 (en) 2018-02-23 2022-09-15 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Novel inhibitors of bacterial glutaminyl cyclases for use in the treatment of periodontal and related diseases
TWI715156B (zh) 2018-08-31 2021-01-01 財團法人國家衛生研究院 苯并咪唑化合物及其用於治療阿茲海默症或亨丁頓氏症之用途
WO2020242933A1 (en) * 2019-05-24 2020-12-03 Emory University Asparagine endopeptidase (aep) inhibitors, compositions, and uses related thereto
EP4359405A1 (en) * 2021-06-24 2024-05-01 Insilico Medicine IP Limited Beta-lactam derivatives for the treatment of diseases

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD293584A5 (de) * 1990-03-23 1991-09-05 Adw,Zi Fuer Organische Chemie,De Verfahren zur herstellung von neuen 3,5,5-trisubstituierten 1-(benzimidazol-2-yl)-imidazolidin-2,4-dionen bzw. -4-on-2-thionen
DE4320432A1 (de) * 1993-06-21 1994-12-22 Bayer Ag Substituierte Mono- und Bipyridylmethylderivate
US20040006011A1 (en) * 1996-07-12 2004-01-08 Gour Barbara J. Peptidomimetic modulators of cell adhesion
WO1999006361A2 (en) 1997-07-31 1999-02-11 Abbott Laboratories N-hydroxyformamide derivatives as inhibitors of matrix metalloproteinases
US6235786B1 (en) 1997-08-06 2001-05-22 Abbott Laboratories Reverse hydroxamate inhibitors of matrix metalloproteinases
EP1620091B1 (en) * 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
JP4996926B2 (ja) * 2004-02-05 2012-08-08 プロビオドルグ エージー グルタミニルシクラーゼの新規の阻害剤
US7795287B2 (en) 2006-09-01 2010-09-14 Allergan, Inc. Therapeutic substituted hydantoins and related compounds
NZ590631A (en) * 2006-09-21 2011-12-22 Probiodrug Ag Novel genes related to glutaminyl cyclase
EP2091945B1 (en) * 2006-11-09 2014-01-15 Probiodrug AG Novel inhibitors of glutaminyl cyclase
TW200831080A (en) 2006-12-15 2008-08-01 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
CN101519376B (zh) * 2008-02-27 2012-10-10 上海药明康德新药开发有限公司 一种芳香环双酰胺螺环类药物模板的合成方法
JP5788320B2 (ja) * 2008-09-04 2015-09-30 プロビオドルグ エージー イソｑｃ阻害剤の使用

Also Published As

Publication number Publication date
EA021150B1 (ru) 2015-04-30
EP2344157A1 (en) 2011-07-20
JP5707327B2 (ja) 2015-04-30
AU2009289238B2 (en) 2014-09-04
US20100119475A1 (en) 2010-05-13
KR20110074975A (ko) 2011-07-05
NZ591531A (en) 2012-03-30
ZA201100898B (en) 2012-02-29
BRPI0918564B1 (pt) 2023-11-28
IL211018A (en) 2015-11-30
SG193828A1 (en) 2013-10-30
DK2344157T3 (en) 2016-09-05
CN102186475A (zh) 2011-09-14
US8962860B2 (en) 2015-02-24
AU2009289238A1 (en) 2010-03-11
CA2735795C (en) 2018-02-20
CN102186475B (zh) 2016-08-03
EP2344157B1 (en) 2016-05-25
JP2012502006A (ja) 2012-01-26
CA2735795A1 (en) 2010-03-11
WO2010026212A1 (en) 2010-03-11
BRPI0918564A2 (pt) 2015-12-01
ES2599621T3 (es) 2017-02-02
KR101694556B1 (ko) 2017-01-09
IL211018A0 (en) 2011-04-28
MX2011002106A (es) 2011-04-07

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