ES2621958T3 - Derivados de pirazina como agonistas receptores de CB2 - Google Patents

Derivados de pirazina como agonistas receptores de CB2 Download PDF

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Publication number
ES2621958T3
ES2621958T3 ES13799545.2T ES13799545T ES2621958T3 ES 2621958 T3 ES2621958 T3 ES 2621958T3 ES 13799545 T ES13799545 T ES 13799545T ES 2621958 T3 ES2621958 T3 ES 2621958T3
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Spain
Prior art keywords
pyrazin
cyclopropylmethoxy
difluoro
azetidin
carbonyl
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ES13799545.2T
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English (en)
Spanish (es)
Inventor
Baledi DHURWASULU
Uwe Grether
Matthias Nettekoven
Stephan Roever
Mark Rogers-Evans
Tanja Schulz-Gasch
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • 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
    • A61P1/02—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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • C07D417/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
ES13799545.2T 2012-12-07 2013-12-04 Derivados de pirazina como agonistas receptores de CB2 Active ES2621958T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12196024 2012-12-07
EP12196024 2012-12-07
PCT/EP2013/075444 WO2014086807A1 (en) 2012-12-07 2013-12-04 Novel pyrazine derivatives as cb2 receptor agonists

Publications (1)

Publication Number Publication Date
ES2621958T3 true ES2621958T3 (es) 2017-07-05

Family

ID=47290805

Family Applications (1)

Application Number Title Priority Date Filing Date
ES13799545.2T Active ES2621958T3 (es) 2012-12-07 2013-12-04 Derivados de pirazina como agonistas receptores de CB2

Country Status (32)

Country Link
US (1) US9512141B2 (enExample)
EP (1) EP2928882B1 (enExample)
JP (1) JP6322646B2 (enExample)
KR (1) KR20150092156A (enExample)
CN (1) CN104837830B (enExample)
AR (1) AR093804A1 (enExample)
AU (1) AU2013354115B2 (enExample)
BR (1) BR112015009603A2 (enExample)
CA (1) CA2885418A1 (enExample)
CL (1) CL2015001318A1 (enExample)
CR (1) CR20150210A (enExample)
CY (1) CY1118808T1 (enExample)
DK (1) DK2928882T3 (enExample)
EA (1) EA025840B1 (enExample)
ES (1) ES2621958T3 (enExample)
HR (1) HRP20170572T1 (enExample)
HU (1) HUE030836T2 (enExample)
IL (1) IL237982A (enExample)
IN (1) IN2015DN03145A (enExample)
LT (1) LT2928882T (enExample)
MA (1) MA38217B1 (enExample)
MX (1) MX2015006036A (enExample)
PE (1) PE20151060A1 (enExample)
PH (1) PH12015501072B1 (enExample)
PL (1) PL2928882T3 (enExample)
PT (1) PT2928882T (enExample)
RS (1) RS55951B1 (enExample)
SG (1) SG11201504011UA (enExample)
SI (1) SI2928882T1 (enExample)
TW (1) TW201427960A (enExample)
UA (1) UA116894C2 (enExample)
WO (1) WO2014086807A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2964646T3 (en) 2013-03-07 2017-07-10 Hoffmann La Roche UNKNOWN PYRAZOLD DERIVATIVES
DK2978755T3 (en) 2013-03-26 2018-03-05 Hoffmann La Roche Hitherto unknown pyridine derivatives
SI2991988T1 (sl) 2013-05-02 2017-09-29 F. Hoffmann-La Roche Ag Derivati pirolo(2,3-d)pirimidina kot agonisti receptorja CB2
KR20210145303A (ko) 2013-05-02 2021-12-01 에프. 호프만-라 로슈 아게 Cb2 수용체 작용제로서의 퓨린 유도체
UA116395C2 (uk) 2013-09-06 2018-03-12 Ф. Хоффманн-Ля Рош Аг ПОХІДНІ ТРИАЗОЛ[4,5-b]ПІРИМІДИНУ
SG10201809066TA (en) * 2014-04-04 2018-11-29 Hoffmann La Roche 5,6-Disubstituted Pyridine-2-Carboxamides and 5,6-Disubstituted Pyrazine-2-Carboxamides as Cannabinoid Receptor Agonists
BR112018011562B1 (pt) * 2015-12-09 2023-05-02 F. Hoffmann-La Roche Ag Novos derivados de fenil
CN110753690B (zh) 2017-06-20 2023-12-05 豪夫迈·罗氏有限公司 吡啶衍生物
CN116640118B (zh) 2018-06-27 2025-12-19 豪夫迈·罗氏有限公司 放射性标记的大麻素受体2配体
CN119161323A (zh) * 2018-06-27 2024-12-20 豪夫迈·罗氏有限公司 作为大麻素受体2的抑制剂的新型吡啶和吡嗪化合物
CN112074513B (zh) 2018-06-27 2024-06-14 豪夫迈·罗氏有限公司 作为优先大麻素2激动剂的吡啶和吡嗪衍生物
WO2020002280A1 (en) 2018-06-27 2020-01-02 F. Hoffmann-La Roche Ag Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
WO2022128050A1 (en) 2020-12-14 2022-06-23 Symrise Ag Medicament for fighting inflammation and pain

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7629346B2 (en) * 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
WO2008040649A2 (en) * 2006-10-04 2008-04-10 F. Hoffmann-La Roche Ag Pyrazine-2-carboxamide derivatives as cb2 receptor modulators
WO2012031817A1 (en) 2010-09-09 2012-03-15 F. Hoffmann-La Roche Ag Determination of abca1 protein levels in cells
US9321727B2 (en) 2011-06-10 2016-04-26 Hoffmann-La Roche Inc. Pyridine derivatives as agonists of the CB2 receptor
US9403808B2 (en) * 2011-10-28 2016-08-02 Hoffmann-La Roche Inc. Pyrazine derivatives

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Publication number Publication date
DK2928882T3 (en) 2017-02-20
CL2015001318A1 (es) 2015-10-02
US9512141B2 (en) 2016-12-06
EP2928882A1 (en) 2015-10-14
WO2014086807A1 (en) 2014-06-12
KR20150092156A (ko) 2015-08-12
CN104837830A (zh) 2015-08-12
PH12015501072A1 (en) 2015-08-03
EA025840B1 (ru) 2017-02-28
RS55951B1 (sr) 2017-09-29
CA2885418A1 (en) 2014-06-12
MX2015006036A (es) 2015-08-07
IL237982A (en) 2017-06-29
JP6322646B2 (ja) 2018-05-09
CR20150210A (es) 2015-05-29
SG11201504011UA (en) 2015-07-30
BR112015009603A2 (pt) 2017-07-04
CY1118808T1 (el) 2018-01-10
PL2928882T3 (pl) 2017-07-31
EP2928882B1 (en) 2017-01-18
CN104837830B (zh) 2018-07-20
UA116894C2 (uk) 2018-05-25
SI2928882T1 (sl) 2017-05-31
PT2928882T (pt) 2017-03-16
HRP20170572T1 (hr) 2017-06-16
PH12015501072B1 (en) 2015-08-03
MA38217A1 (fr) 2017-02-28
AU2013354115A1 (en) 2015-04-09
HUE030836T2 (en) 2017-06-28
HK1208030A1 (en) 2016-02-19
AU2013354115B2 (en) 2017-10-05
PE20151060A1 (es) 2015-07-25
LT2928882T (lt) 2017-03-27
EA201590827A1 (ru) 2015-09-30
AR093804A1 (es) 2015-06-24
TW201427960A (zh) 2014-07-16
JP2016505557A (ja) 2016-02-25
IN2015DN03145A (enExample) 2015-10-02
US20150299220A1 (en) 2015-10-22
MA38217B1 (fr) 2017-11-30

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