PL2782915T3 - Pochodne [1,2,3]triazolo[4,5-d]pirymidyny jako agoniści agonistów receptora kanabinoidowego 2 - Google Patents

Pochodne [1,2,3]triazolo[4,5-d]pirymidyny jako agoniści agonistów receptora kanabinoidowego 2

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Publication number
PL2782915T3
PL2782915T3 PL12794684T PL12794684T PL2782915T3 PL 2782915 T3 PL2782915 T3 PL 2782915T3 PL 12794684 T PL12794684 T PL 12794684T PL 12794684 T PL12794684 T PL 12794684T PL 2782915 T3 PL2782915 T3 PL 2782915T3
Authority
PL
Poland
Prior art keywords
agonists
triazolo
pyrimidine derivatives
cannabinoid receptor
cannabinoid
Prior art date
Application number
PL12794684T
Other languages
English (en)
Inventor
Caterina Bissantz
Uwe Grether
Atsushi Kimbara
Matthias Nettekoven
Stephan Roever
Mark Rogers-Evans
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PL2782915T3 publication Critical patent/PL2782915T3/pl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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]
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
PL12794684T 2011-11-25 2012-11-22 Pochodne [1,2,3]triazolo[4,5-d]pirymidyny jako agoniści agonistów receptora kanabinoidowego 2 PL2782915T3 (pl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11190777 2011-11-25
EP12794684.6A EP2782915B1 (en) 2011-11-25 2012-11-22 [1,2,3]TRIAZOLO[4,5-d]PYRIMIDINE DERIVATIVES AS AGONISTS OF THE CANNABINOID RECEPTOR 2 AGONISTS
PCT/EP2012/073315 WO2013076182A1 (en) 2011-11-25 2012-11-22 [1, 2, 3]triazolo [4, 5 -d] pyrimidine derivatives as agonists of the cannabinoid receptor 2 agonists

Publications (1)

Publication Number Publication Date
PL2782915T3 true PL2782915T3 (pl) 2016-03-31

Family

ID=47278275

Family Applications (1)

Application Number Title Priority Date Filing Date
PL12794684T PL2782915T3 (pl) 2011-11-25 2012-11-22 Pochodne [1,2,3]triazolo[4,5-d]pirymidyny jako agoniści agonistów receptora kanabinoidowego 2

Country Status (32)

Country Link
US (1) US9067943B2 (pl)
EP (1) EP2782915B1 (pl)
JP (1) JP6077558B2 (pl)
KR (1) KR20140097201A (pl)
CN (1) CN104039791B (pl)
AR (1) AR088970A1 (pl)
AU (1) AU2012342471B2 (pl)
BR (1) BR112014012479A2 (pl)
CA (1) CA2850697A1 (pl)
CL (1) CL2014001309A1 (pl)
CO (1) CO6930360A2 (pl)
CR (1) CR20140222A (pl)
CY (1) CY1116984T1 (pl)
DK (1) DK2782915T3 (pl)
EA (1) EA024108B1 (pl)
ES (1) ES2550967T3 (pl)
HR (1) HRP20151423T1 (pl)
HU (1) HUE028020T2 (pl)
IL (1) IL232304A (pl)
MA (1) MA35663B1 (pl)
MX (1) MX346248B (pl)
PE (1) PE20141578A1 (pl)
PH (1) PH12014501026A1 (pl)
PL (1) PL2782915T3 (pl)
PT (1) PT2782915E (pl)
RS (1) RS54319B1 (pl)
SG (1) SG11201402198XA (pl)
SI (1) SI2782915T1 (pl)
TW (1) TWI598350B (pl)
UA (1) UA111643C2 (pl)
WO (1) WO2013076182A1 (pl)
ZA (1) ZA201403441B (pl)

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* Cited by examiner, † Cited by third party
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UA111640C2 (uk) * 2011-11-08 2016-05-25 Ф. Хоффманн-Ля Рош Аг ПОХІДНІ [1,2,3]ТРИАЗОЛО[4,5-d]ПІРИМІДИНУ ЯК АГОНІСТИ КАНАБІНОЇДНОГО РЕЦЕПТОРА 2
EP3943497A1 (en) * 2013-09-06 2022-01-26 F. Hoffmann-La Roche AG Triazolo[4,5-d]pyrimidine derivatives as cb2 receptor antagonists
CN107074864B (zh) 2014-11-07 2019-12-27 豪夫迈·罗氏有限公司 作为大麻素受体2的激动剂的三唑并[4，5-d]嘧啶类
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EP3475283B1 (en) * 2016-06-23 2021-08-11 F. Hoffmann-La Roche AG Novel[1,2,3]triazolo[4,5-d]pyrimidine derivatives
EP3475281A1 (en) 2016-06-23 2019-05-01 H. Hoffnabb-La Roche Ag Novel [1,2,31triazolo[4,5-d]pyrimidine derivatives
EP3475280B1 (en) * 2016-06-23 2020-04-08 H. Hoffnabb-La Roche Ag Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives
KR20230062680A (ko) * 2016-06-23 2023-05-09 에프. 호프만-라 로슈 아게 2형 칸나비노이드 수용체에 대한 친화성을 갖는 [1,2,3]트라이아졸로[4,5-d]피리미딘 유도체
MA52489A (fr) * 2018-05-04 2021-03-10 Inflazome Ltd Nouveaux composés
CN112007156A (zh) * 2019-05-30 2020-12-01 复旦大学 大麻素受体药物在制备治疗心肌细胞坏死性凋亡药剂中的应用
CN112755189A (zh) * 2019-11-02 2021-05-07 复旦大学 1型大麻素受体拮抗剂在制备治疗心肌细胞焦亡药剂中的应用
EP4423087A1 (en) * 2021-10-28 2024-09-04 F. Hoffmann-La Roche AG Synthesis of [1,2,3]triazolo[4,5-d]pyrimidines
CN115246832B (zh) * 2022-06-15 2024-05-24 深圳湾实验室 一类去泛素化酶usp25和usp28靶向抑制剂及制备和应用

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US2543333A (en) * 1950-02-02 1951-02-27 American Cyanamid Co Derivatives of upsilon-triazolo (d) pyrimidine and methods of preparing the same
US4157443A (en) * 1976-11-11 1979-06-05 Ciba-Geigy Corporation V-Triazolyl-[4,5-d]-pyrimidines
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
US7268133B2 (en) * 2003-04-23 2007-09-11 Pfizer, Inc. Patent Department Cannabinoid receptor ligands and uses thereof
US7141669B2 (en) 2003-04-23 2006-11-28 Pfizer Inc. Cannabiniod receptor ligands and uses thereof
WO2005061505A1 (en) 2003-12-16 2005-07-07 Pfizer Products Inc. Bicyclic imidazolyl pyrimidin-4-one cannabinoid receptor ligands and uses thereof
DE102004014534A1 (de) * 2004-03-23 2005-10-13 Basf Ag Triazolderivate und Verwendung von Triazolderivaten in organischen Leuchtdioden (OLEDs)
AR051596A1 (es) * 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
JP5159630B2 (ja) * 2006-09-13 2013-03-06 協和発酵キリン株式会社 縮環複素環誘導体
JP2010533658A (ja) * 2007-07-20 2010-10-28 メルク フロスト カナダ リミテツド ステアロイル補酵素ａデルタ−９デサチュラーゼ阻害剤としての二環性へテロ芳香族化合物
US7655685B2 (en) 2007-11-02 2010-02-02 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
UA104010C2 (en) * 2008-12-18 2013-12-25 Эли Лилли Энд Компани Purine compounds
CA2795006C (en) 2010-03-31 2014-05-13 Eli Lilly And Company Purine compounds used as cb2 agonists
AR080711A1 (es) * 2010-03-31 2012-05-02 Lilly Co Eli Compuesto de piperazin-purina composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento o prevencion del dolor
UA111640C2 (uk) * 2011-11-08 2016-05-25 Ф. Хоффманн-Ля Рош Аг ПОХІДНІ [1,2,3]ТРИАЗОЛО[4,5-d]ПІРИМІДИНУ ЯК АГОНІСТИ КАНАБІНОЇДНОГО РЕЦЕПТОРА 2

Also Published As

Publication number Publication date
DK2782915T3 (en) 2015-10-19
NZ622847A (en) 2015-05-29
CO6930360A2 (es) 2014-04-28
ES2550967T3 (es) 2015-11-13
EP2782915A1 (en) 2014-10-01
HRP20151423T1 (hr) 2016-01-29
CL2014001309A1 (es) 2014-10-17
CA2850697A1 (en) 2013-05-30
WO2013076182A1 (en) 2013-05-30
SI2782915T1 (sl) 2015-12-31
MX346248B (es) 2017-03-13
AR088970A1 (es) 2014-07-23
IL232304A0 (en) 2014-06-30
TW201329080A (zh) 2013-07-16
SG11201402198XA (en) 2014-09-26
EA201491002A1 (ru) 2014-09-30
ZA201403441B (en) 2015-08-26
CR20140222A (es) 2014-06-20
HUE028020T2 (en) 2016-11-28
AU2012342471B2 (en) 2017-06-08
US9067943B2 (en) 2015-06-30
BR112014012479A2 (pt) 2017-06-06
KR20140097201A (ko) 2014-08-06
AU2012342471A1 (en) 2014-04-10
UA111643C2 (uk) 2016-05-25
MX2014005692A (es) 2014-07-28
US20130137676A1 (en) 2013-05-30
CY1116984T1 (el) 2017-04-05
IL232304A (en) 2016-02-29
TWI598350B (zh) 2017-09-11
CN104039791B (zh) 2016-11-09
JP2014533711A (ja) 2014-12-15
EA024108B1 (ru) 2016-08-31
MA35663B1 (fr) 2014-11-01
EP2782915B1 (en) 2015-09-30
JP6077558B2 (ja) 2017-02-08
CN104039791A (zh) 2014-09-10
PE20141578A1 (es) 2014-10-25
PT2782915E (pt) 2015-11-19
RS54319B1 (sr) 2016-02-29
PH12014501026A1 (en) 2014-06-23

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