EA027174B1 - N-алкил 2-(дизамещенные)алкиниладенозин-5-уронамиды в качестве a-агонистов - Google Patents

N-алкил 2-(дизамещенные)алкиниладенозин-5-уронамиды в качестве a-агонистов Download PDF

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Publication number
EA027174B1
EA027174B1 EA201590205A EA201590205A EA027174B1 EA 027174 B1 EA027174 B1 EA 027174B1 EA 201590205 A EA201590205 A EA 201590205A EA 201590205 A EA201590205 A EA 201590205A EA 027174 B1 EA027174 B1 EA 027174B1
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EA
Eurasian Patent Office
Prior art keywords
pharmaceutically acceptable
adenosine
stereoisomer
independently selected
acceptable salt
Prior art date
Application number
EA201590205A
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English (en)
Russian (ru)
Other versions
EA201590205A1 (ru
Inventor
Роберт Томпсон
Энтони Биглхол
Гоцюань Ван
Original Assignee
Льюис Энд Кларк Фармасьютикалз, Инк.
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Application filed by Льюис Энд Кларк Фармасьютикалз, Инк. filed Critical Льюис Энд Кларк Фармасьютикалз, Инк.
Publication of EA201590205A1 publication Critical patent/EA201590205A1/ru
Publication of EA027174B1 publication Critical patent/EA027174B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • 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
    • A61P1/04—Drugs 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
    • 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
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/04—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
    • 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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • 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
    • A61P9/10—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)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Nutrition Science (AREA)
  • Transplantation (AREA)
EA201590205A 2012-08-01 2013-07-31 N-алкил 2-(дизамещенные)алкиниладенозин-5-уронамиды в качестве a-агонистов EA027174B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261678605P 2012-08-01 2012-08-01
US201361787188P 2013-03-15 2013-03-15
PCT/US2013/053053 WO2014022577A1 (en) 2012-08-01 2013-07-31 N-alkyl 2-(disubstituted)alkynyladenosine-5-uronamides as a2a agonists

Publications (2)

Publication Number Publication Date
EA201590205A1 EA201590205A1 (ru) 2015-06-30
EA027174B1 true EA027174B1 (ru) 2017-06-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590205A EA027174B1 (ru) 2012-08-01 2013-07-31 N-алкил 2-(дизамещенные)алкиниладенозин-5-уронамиды в качестве a-агонистов

Country Status (15)

Country Link
US (1) US9067963B2 (enExample)
EP (1) EP2879683B1 (enExample)
JP (1) JP6545618B2 (enExample)
KR (1) KR20150036767A (enExample)
CN (1) CN104582709A (enExample)
AU (1) AU2013296420B2 (enExample)
BR (1) BR112015002249A2 (enExample)
CA (1) CA2880040A1 (enExample)
EA (1) EA027174B1 (enExample)
IL (1) IL236986A (enExample)
IN (1) IN2015DN00538A (enExample)
MX (1) MX367879B (enExample)
NZ (1) NZ703992A (enExample)
WO (1) WO2014022577A1 (enExample)
ZA (1) ZA201501350B (enExample)

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AU2006249866B2 (en) 2005-05-26 2011-10-13 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
CA2782015C (en) 2009-12-11 2020-08-25 Neuron Systems, Inc. Topical ophthalmic compositions and methods for the treatment of macular degeneration
US9822141B2 (en) * 2012-08-01 2017-11-21 Lewis And Clark Pharmaceuticals, Inc. N-alkyl 2-(disubstituted)alkynyladenosine-5-uronamides as A2A agonists
CN111135171B (zh) 2013-01-23 2023-09-08 奥尔德拉医疗公司 与毒性醛相关的疾病和治疗
CN118724806A (zh) 2015-08-21 2024-10-01 奥尔德拉医疗公司 氘化化合物和其用途
CN109152774A (zh) 2016-05-09 2019-01-04 奥尔德拉医疗公司 眼部炎性病症和疾病的组合治疗
WO2018170476A1 (en) 2017-03-16 2018-09-20 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
CN111356451A (zh) 2017-10-10 2020-06-30 奥尔德拉医疗公司 炎性病症的治疗
CN112714762A (zh) 2018-08-06 2021-04-27 奥尔德拉医疗公司 多晶型化合物及其用途
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
CN113784954A (zh) 2019-05-02 2021-12-10 奥尔德拉医疗公司 多晶型化合物和其用途
US20220332750A1 (en) * 2019-06-21 2022-10-20 Academy Of Military Medical Sciences Adenosine compound, its pharmaceutically acceptable salt or its stereoisomer and use thereof
WO2021231792A1 (en) 2020-05-13 2021-11-18 Aldeyra Therapeutics, Inc. Pharmaceutical formulations and uses thereof
WO2024258897A1 (en) 2023-06-13 2024-12-19 Dem Biopharma, Inc. Alkoxypyridinyl and related compounds and their use in therapy
WO2025194015A1 (en) 2024-03-15 2025-09-18 Dem Biopharma, Inc. Heteroaryl modulators of gpr84 and uses thereof
WO2025194014A1 (en) 2024-03-15 2025-09-18 Dem Biopharma, Inc. Hetero aryl modulators of apmap and uses thereof
US20260183268A1 (en) 2024-12-27 2026-07-02 Alphina Therapeutics, Inc. Heteroaryl Compounds and Their Use in Treating Medical Conditions

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Publication number Priority date Publication date Assignee Title
US6322771B1 (en) * 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
US6387889B1 (en) * 1998-09-01 2002-05-14 Yamasa Corporation Medicinal compositions for treating eye diseases
US20080009460A1 (en) * 2006-02-10 2008-01-10 Linden Joel M Method to treat sickle cell disease
US20080312160A1 (en) * 2007-04-09 2008-12-18 Guerrant Richard L Method of treating enteritis, intestinal damage, and diarrhea from c. difficile with an a2a adenosine receptor agonist

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LU84979A1 (fr) 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
JPS6299395A (ja) 1985-10-25 1987-05-08 Yamasa Shoyu Co Ltd 2−アルキニルアデノシンおよび抗高血圧剤
US4820508A (en) 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US4992478A (en) 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US4938949A (en) 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
JPH02104783A (ja) * 1988-10-11 1990-04-17 Kanai Hiroyuki スチールコードおよびタイヤ
US5270304A (en) 1988-11-15 1993-12-14 Yamasa Shoyu Kabushiki Kaisha Therapeutic 2-alkynyl adenosine agent for ischemic diseases of the heart or brain
WO1990015812A1 (en) 1989-06-20 1990-12-27 Yamasa Shoyu Kabushiki Kaisha Intermediate for 2-alkynyladenosine synthesis, production of said intermediate, production of 2-alkynyladenosine from said intermediate, and stable 2-alkynyladenosine derivative
US5189027A (en) 1990-11-30 1993-02-23 Yamasa Shoyu Kabushiki Kaisha 2-substituted adenosine derivatives and pharmaceutical compositions for circulatory diseases
JP3025557B2 (ja) * 1991-06-28 2000-03-27 ヤマサ醤油株式会社 2‐アルキニルアデノシン誘導体
IT1254915B (it) 1992-04-24 1995-10-11 Gloria Cristalli Derivati di adenosina ad attivita' a2 agonista
PL208098B1 (pl) 2000-03-23 2011-03-31 Solvay Pharm Bv Pochodne 4,5-dihydro-1H-pirazolu, kompozycja farmaceutyczna, sposób wytwarzania związków oraz ich zastosowanie
AU2002362443B2 (en) 2001-10-01 2008-05-15 University Of Virginia Patent Foundation 2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
US6914053B2 (en) 2002-09-09 2005-07-05 Cv Therapeutics, Inc. Adenosine A3 receptor agonists
NZ585697A (en) 2004-08-02 2011-12-22 Univ Virginia Patent Found 2-propynyl adenosine analogs with modified 5'-ribose groups having A2A agonist activity
WO2006091896A2 (en) * 2005-02-25 2006-08-31 Adenosine Therapeutics, Llc Pyridyl substituted xanthines
US7906518B2 (en) * 2006-06-27 2011-03-15 Cbt Development Limited Therapeutic compounds
KR20140041965A (ko) 2007-05-17 2014-04-04 씨브이 쎄러퓨틱스, 인코포레이티드 A2a-아데노신 수용체 효능제 및 이의 다형체의 제조 방법
US8058259B2 (en) 2007-12-20 2011-11-15 University Of Virginia Patent Foundation Substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters as A2AR agonists
US8293720B2 (en) 2007-12-20 2012-10-23 Dogwood Pharmaceuticals, Inc. Substituted 4-{3-[6-amino-9-(3, 4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters as A2AR agonists
EP2448953A1 (en) * 2009-06-30 2012-05-09 Forest Laboratories Holdings Limited Alkoxy-carbonyl-amino-alkynyl-adenosine compounds and derivatives thatreof as a2ar agonists

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6387889B1 (en) * 1998-09-01 2002-05-14 Yamasa Corporation Medicinal compositions for treating eye diseases
US6322771B1 (en) * 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
US20080009460A1 (en) * 2006-02-10 2008-01-10 Linden Joel M Method to treat sickle cell disease
US20080312160A1 (en) * 2007-04-09 2008-12-18 Guerrant Richard L Method of treating enteritis, intestinal damage, and diarrhea from c. difficile with an a2a adenosine receptor agonist

Also Published As

Publication number Publication date
JP6545618B2 (ja) 2019-07-17
ZA201501350B (en) 2016-12-21
EA201590205A1 (ru) 2015-06-30
KR20150036767A (ko) 2015-04-07
NZ703992A (en) 2018-04-27
WO2014022577A1 (en) 2014-02-06
MX367879B (es) 2019-09-10
AU2013296420B2 (en) 2017-12-07
US20140037538A1 (en) 2014-02-06
CA2880040A1 (en) 2014-02-06
AU2013296420A1 (en) 2015-02-12
EP2879683A4 (en) 2016-04-20
MX2015001370A (es) 2016-04-26
IL236986A (en) 2017-06-29
JP2015524440A (ja) 2015-08-24
US9067963B2 (en) 2015-06-30
CN104582709A (zh) 2015-04-29
EP2879683A1 (en) 2015-06-10
BR112015002249A2 (pt) 2017-07-04
IN2015DN00538A (enExample) 2015-06-26
EP2879683B1 (en) 2020-01-22

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