JP5969017B2 - Trpv4拮抗薬 - Google Patents

Trpv4拮抗薬 Download PDF

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Publication number
JP5969017B2
JP5969017B2 JP2014516020A JP2014516020A JP5969017B2 JP 5969017 B2 JP5969017 B2 JP 5969017B2 JP 2014516020 A JP2014516020 A JP 2014516020A JP 2014516020 A JP2014516020 A JP 2014516020A JP 5969017 B2 JP5969017 B2 JP 5969017B2
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Japan
Prior art keywords
methyl
azaspiro
oxa
carbonitrile
oxo
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Japanese (ja)
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JP2014518214A (ja
JP2014518214A5 (enExample
Inventor
カール、ブルックス
ムイ、チュン
ヒラリー、シェンク、アイダム
クリスタ、ビー.グッドマン
マーリス、ハモンド
マーク、エイ.ヒルフィカー
トレム、エイチ.ホアン
ジャクリン、アール.パターソン
パトリック、シュトイ
グォセン、イェ
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47558389&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5969017(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by GlaxoSmithKline Intellectual Property No 2 Ltd filed Critical GlaxoSmithKline Intellectual Property No 2 Ltd
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Publication of JP2014518214A5 publication Critical patent/JP2014518214A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D419/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2014516020A 2011-06-17 2012-06-15 Trpv4拮抗薬 Active JP5969017B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161498110P 2011-06-17 2011-06-17
US61/498,110 2011-06-17
PCT/US2012/042622 WO2013012500A1 (en) 2011-06-17 2012-06-15 Trpv4 antagonists

Publications (3)

Publication Number Publication Date
JP2014518214A JP2014518214A (ja) 2014-07-28
JP2014518214A5 JP2014518214A5 (enExample) 2015-07-16
JP5969017B2 true JP5969017B2 (ja) 2016-08-10

Family

ID=47558389

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014516020A Active JP5969017B2 (ja) 2011-06-17 2012-06-15 Trpv4拮抗薬

Country Status (38)

Country Link
US (1) US9187464B2 (enExample)
EP (2) EP3121177B1 (enExample)
JP (1) JP5969017B2 (enExample)
KR (1) KR101870003B1 (enExample)
CN (1) CN103732583B (enExample)
AR (1) AR086958A1 (enExample)
AU (1) AU2012284540B2 (enExample)
BR (1) BR112013032391B1 (enExample)
CA (1) CA2839743C (enExample)
CL (1) CL2013003602A1 (enExample)
CO (1) CO6821953A2 (enExample)
CR (1) CR20130671A (enExample)
CY (1) CY1117792T1 (enExample)
DK (1) DK2721016T3 (enExample)
DO (1) DOP2013000307A (enExample)
EA (1) EA023616B1 (enExample)
ES (2) ES2688733T3 (enExample)
HR (1) HRP20160539T1 (enExample)
HU (1) HUE029594T2 (enExample)
IL (1) IL229872A (enExample)
JO (1) JO3154B1 (enExample)
MA (1) MA35184B1 (enExample)
ME (1) ME02416B (enExample)
MX (1) MX337440B (enExample)
MY (1) MY173521A (enExample)
PE (1) PE20141943A1 (enExample)
PH (1) PH12013502463A1 (enExample)
PL (1) PL2721016T3 (enExample)
PT (1) PT2721016E (enExample)
RS (1) RS54858B1 (enExample)
SG (1) SG195106A1 (enExample)
SI (1) SI2721016T1 (enExample)
SM (1) SMT201600150B (enExample)
TW (1) TWI538912B (enExample)
UA (1) UA113963C2 (enExample)
UY (1) UY34138A (enExample)
WO (1) WO2013012500A1 (enExample)
ZA (1) ZA201308816B (enExample)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2595606T3 (es) 2011-06-17 2017-01-02 Glaxosmithkline Intellectual Property (No. 2) Limited Antagonistas TRPV4
ES2571409T3 (es) 2011-06-17 2016-05-25 Glaxosmithkline Intellectual Property (No 2) Ltd Antagonistas espiro-cíclicos de TRPV4
US9499533B2 (en) 2012-03-27 2016-11-22 Shionogi & Co., Ltd. Aromatic 5-membered heterocyclic derivative having TRPV4-Inhibiting activity
JPWO2015046193A1 (ja) 2013-09-25 2017-03-09 塩野義製薬株式会社 Trpv4阻害活性を有する芳香族複素環式アミン誘導体
US10968209B2 (en) 2016-05-19 2021-04-06 Glaxosmithkline Intellectual Property (No.2) Limited TRPV4 antagonist
EP3458451B1 (en) 2016-05-19 2020-06-03 Glaxosmithkline Intellectual Property (No. 2) Limited Trpv4 antagonist
JP7101171B2 (ja) 2016-10-03 2022-07-14 ヤンセン ファーマシューティカ エヌ.ベー. Prmt5阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体
WO2018185701A1 (en) 2017-04-06 2018-10-11 Glaxosmithkline Intellectual Property (No.2) Limited Trpv4 antagonists as antitussive agents
JP7228595B2 (ja) * 2017-11-01 2023-02-24 ブリストル-マイヤーズ スクイブ カンパニー ファルネソイドx受容体モジュレーターとしてのスピロ環化合物
WO2021170811A1 (en) 2020-02-27 2021-09-02 Glaxosmithkline Intellectual Property (No.2) Limited Method of treating eye disease using trpv4 antagonists
MX2022013607A (es) 2020-04-30 2022-11-16 Raqualia Pharma Inc Derivados de la pirimidina-4(3h)-ona como antagonistas de trpv4.
CN111704613B (zh) * 2020-06-23 2021-07-06 中国人民解放军军事科学院军事医学研究院 咪唑类衍生物及其作为trpv4抑制剂的用途
CN115776890A (zh) * 2020-07-16 2023-03-10 拉夸里亚创药株式会社 作为眼病治疗剂的trpv4抑制剂
AU2023303522A1 (en) 2022-07-08 2025-01-16 Actio Biosciences, Inc. Therapeutic compounds and methods
WO2024217452A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217439A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
CN120225516A (zh) * 2023-04-18 2025-06-27 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
CN120641413A (zh) * 2023-04-18 2025-09-12 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217429A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2025014818A1 (en) * 2023-07-07 2025-01-16 Actio Biosciences, Inc. Solid forms of gsk2798745, a trpv4 antagonist

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KR20080070749A (ko) * 2005-11-23 2008-07-30 페인셉터 파마 코포레이션 개폐 이온 통로를 조절하기 위한 조성물 및 방법
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TW200944520A (en) * 2008-01-29 2009-11-01 Glaxo Group Ltd Spiro compounds as NPY Y5 receptor antagonists
US8450484B2 (en) 2008-07-25 2013-05-28 GlaxoSmithKline, LLC TRPV4 antagonists
JP2012006837A (ja) * 2008-09-30 2012-01-12 Mochida Pharmaceut Co Ltd 2−インドールアクリルアミド類縁体
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ES2595606T3 (es) 2011-06-17 2017-01-02 Glaxosmithkline Intellectual Property (No. 2) Limited Antagonistas TRPV4
ES2571409T3 (es) * 2011-06-17 2016-05-25 Glaxosmithkline Intellectual Property (No 2) Ltd Antagonistas espiro-cíclicos de TRPV4

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Publication number Publication date
ZA201308816B (en) 2015-02-25
EP2721016A4 (en) 2014-10-08
AU2012284540A1 (en) 2013-04-04
HUE029594T2 (en) 2017-03-28
UA113963C2 (xx) 2017-04-10
EA201490037A1 (ru) 2015-12-30
US9187464B2 (en) 2015-11-17
NZ618221A (en) 2015-02-27
PL2721016T3 (pl) 2017-01-31
KR20140041733A (ko) 2014-04-04
SMT201600150B (it) 2016-07-01
HK1195068A1 (zh) 2014-10-31
CA2839743C (en) 2017-03-28
JO3154B1 (ar) 2017-09-20
EP2721016B1 (en) 2016-04-06
RS54858B1 (sr) 2016-10-31
ES2688733T3 (es) 2018-11-06
ES2569193T3 (es) 2016-05-09
KR101870003B1 (ko) 2018-06-22
SG195106A1 (en) 2013-12-30
MX2013014898A (es) 2014-03-21
CR20130671A (es) 2014-02-04
CA2839743A1 (en) 2013-01-24
CO6821953A2 (es) 2013-12-31
CL2013003602A1 (es) 2014-07-04
AU2012284540B2 (en) 2014-08-28
CN103732583B (zh) 2015-12-23
PH12013502463A1 (en) 2014-01-20
TWI538912B (zh) 2016-06-21
BR112013032391A2 (pt) 2016-08-16
WO2013012500A1 (en) 2013-01-24
SI2721016T1 (sl) 2016-06-30
DOP2013000307A (es) 2014-06-01
DK2721016T3 (en) 2016-06-06
EP3121177A1 (en) 2017-01-25
MX337440B (es) 2016-03-03
CY1117792T1 (el) 2017-05-17
PT2721016E (pt) 2016-06-06
EP3121177B1 (en) 2018-08-01
JP2014518214A (ja) 2014-07-28
IL229872A (en) 2017-03-30
BR112013032391B1 (pt) 2020-11-24
TW201313705A (zh) 2013-04-01
ME02416B (me) 2016-09-20
CN103732583A (zh) 2014-04-16
AR086958A1 (es) 2014-02-05
MY173521A (en) 2020-01-30
EA023616B1 (ru) 2016-06-30
EP2721016A1 (en) 2014-04-23
UY34138A (es) 2013-01-03
PE20141943A1 (es) 2014-12-28
MA35184B1 (fr) 2014-06-02
US20140121206A1 (en) 2014-05-01
HRP20160539T1 (hr) 2016-06-17

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