MA37944B2 - Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson - Google Patents

Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson

Info

Publication number
MA37944B2
MA37944B2 MA37944A MA37944A MA37944B2 MA 37944 B2 MA37944 B2 MA 37944B2 MA 37944 A MA37944 A MA 37944A MA 37944 A MA37944 A MA 37944A MA 37944 B2 MA37944 B2 MA 37944B2
Authority
MA
Morocco
Prior art keywords
lower alkyl
halogen
substituted
disorders
hydroxy
Prior art date
Application number
MA37944A
Other languages
English (en)
Other versions
MA37944A1 (fr
Inventor
Guido Galley
Roger Norcross
Philippe Pflieger
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 MA37944A1 publication Critical patent/MA37944A1/fr
Publication of MA37944B2 publication Critical patent/MA37944B2/fr

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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/06—Antimigraine 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Emergency Medicine (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)

Abstract

La présente invention concerne des composés de formule (i) dans laquelle r1 est phényle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alcoxy inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxy ; ou est pyridine-2, 3 ou 4-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxyle ; ou est pyrimidin-2, 4 ou 5-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par hydroxy ou alkyle inférieur substitué par halogène ; ou est pyrazin-2-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy ou cyano ; ou est 2,2-difluorobenzo[d][1,3]dioxol-5-yle, ou est thiazolyle, facultativement substitué par alkyle inférieur substitué par halogène ; r2 est hydrogène ou alkyle inférieur ; r3 est hydrogène, amino ou alkyle inférieur ; z est une liaison, -ch2- ou -o- ; ou un sel d'addition d’acide pharmaceutiquement adapté. Il a maintenant été découvert que les composés de formule i ont une bonne affinité pour les récepteurs associés aux amines traces (taar), notamment taar1. Les composés peuvent être utilisés pour le traitement de la dépression, des troubles anxieux, du trouble bipolaire, de l'hyperactivité avec déficit de l'attention (adhd), des troubles relatifs au stress, des troubles psychotiques tels que la schizophrénie, des maladies neurologiques telles que la maladie de parkinson, des maladies neurodégénératives telles que la maladie d'alzheimer, de l'épilepsie, de la migraine, de l'hypertension, de l'abus d'alcool ou d'autres drogues et de troubles métaboliques tels que les troubles de l'alimentation, le diabète, les complications diabétiques, l'obésité, la dyslipidémie, les troubles de la consommation d'énergie et de l'assimilation, les troubles et le mauvais fonctionnement de l'homéostasie de la température corporelle, les troubles du sommeil et du rythme circadien, et les troubles cardiovasculaires.
MA37944A 2012-09-14 2013-09-11 Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson MA37944B2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12184360 2012-09-14
PCT/EP2013/068769 WO2014041007A1 (fr) 2012-09-14 2013-09-11 Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson

Publications (2)

Publication Number Publication Date
MA37944A1 MA37944A1 (fr) 2016-04-29
MA37944B2 true MA37944B2 (fr) 2017-10-31

Family

ID=47044779

Family Applications (1)

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MA37944A MA37944B2 (fr) 2012-09-14 2013-09-11 Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson

Country Status (35)

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US (1) US9487501B2 (fr)
EP (1) EP2895477B1 (fr)
JP (2) JP2015531782A (fr)
KR (1) KR101706486B1 (fr)
CN (2) CN107903251A (fr)
AR (1) AR092537A1 (fr)
AU (1) AU2013314388B2 (fr)
BR (1) BR112015004511B1 (fr)
CA (1) CA2882821C (fr)
CL (1) CL2015000580A1 (fr)
CR (1) CR20150087A (fr)
DK (1) DK2895477T3 (fr)
EA (1) EA026062B1 (fr)
ES (1) ES2654653T3 (fr)
HK (2) HK1206720A1 (fr)
HR (1) HRP20171981T1 (fr)
HU (1) HUE037689T2 (fr)
IL (1) IL237332B (fr)
LT (1) LT2895477T (fr)
MA (1) MA37944B2 (fr)
MX (1) MX363362B (fr)
MY (1) MY178667A (fr)
NO (1) NO2895477T3 (fr)
NZ (1) NZ705154A (fr)
PE (1) PE20150735A1 (fr)
PH (1) PH12015500489B1 (fr)
PL (1) PL2895477T3 (fr)
PT (1) PT2895477T (fr)
RS (1) RS56747B1 (fr)
SG (1) SG11201501958QA (fr)
SI (1) SI2895477T1 (fr)
TW (1) TWI610926B (fr)
UA (1) UA113776C2 (fr)
WO (1) WO2014041007A1 (fr)
ZA (1) ZA201501126B (fr)

Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
TW201617309A (zh) * 2014-07-30 2016-05-16 赫孚孟拉羅股份公司 6-胺基-5,6,7,8-四氫萘-2-基或3-胺基唍-7-基衍生物
RS60825B1 (sr) 2016-03-17 2020-10-30 Hoffmann La Roche Aktivnost derivata 5-etiol-4-metil-pirazol-3-karboksamida kao agonista taar-a
CN110291084A (zh) 2016-12-15 2019-09-27 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
US20220340597A1 (en) 2019-04-09 2022-10-27 Hoffmann-La Roche Inc. Hexahydro-1h-pyrazino[1,2-a]pyrazine compounds for the treatment of autoimmune disease
CN117120427B (zh) * 2021-06-18 2026-07-21 上海拓界生物医药科技有限公司 一种malt1抑制剂及其制备方法和用途
CN118206543A (zh) * 2022-12-15 2024-06-18 江苏恒瑞医药股份有限公司 一种苯并[c][1,2,5]噁二唑化合物的结晶形式及其制备方法
CN118206538A (zh) * 2022-12-15 2024-06-18 江苏恒瑞医药股份有限公司 一种苯并[c][1,2,5]噁二唑化合物与酒石酸复合物及其晶型
CN116236478A (zh) * 2022-12-27 2023-06-09 浙江大学 芳香杂环甲酰胺类化合物的应用
JPWO2026048597A1 (fr) 2024-08-27 2026-03-05

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GB9425211D0 (en) 1994-12-14 1995-02-15 Ucb Sa Substituted 1H-imidazoles
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MX2009008465A (es) 2007-02-15 2009-08-20 Hoffmann La Roche Nuevas 2-aminooxazolinas como ligandos de taar1.
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
TW201236685A (en) * 2010-11-11 2012-09-16 Daiichi Sankyo Co Ltd New pyrazole amide derivatives
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US9029370B2 (en) * 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives

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JP2017122103A (ja) 2017-07-13
EP2895477A1 (fr) 2015-07-22
MX2015002900A (es) 2015-06-03
ES2654653T3 (es) 2018-02-14
SI2895477T1 (en) 2018-02-28
LT2895477T (lt) 2018-01-25
TW201425308A (zh) 2014-07-01
JP2015531782A (ja) 2015-11-05
MA37944A1 (fr) 2016-04-29
NZ705154A (en) 2018-03-23
AR092537A1 (es) 2015-04-22
BR112015004511B1 (pt) 2022-08-02
BR112015004511A8 (pt) 2021-11-03
JP6529998B2 (ja) 2019-06-12
EA201590454A1 (ru) 2015-09-30
HUE037689T2 (hu) 2018-09-28
HK1252981A1 (zh) 2019-06-06
MX363362B (es) 2019-03-21
ZA201501126B (en) 2016-01-27
IL237332A0 (en) 2015-04-30
DK2895477T3 (en) 2018-01-15
WO2014041007A1 (fr) 2014-03-20
KR101706486B1 (ko) 2017-02-13
RS56747B1 (sr) 2018-03-30
SG11201501958QA (en) 2015-04-29
KR20150054947A (ko) 2015-05-20
CN104619700A (zh) 2015-05-13
PT2895477T (pt) 2017-12-29
HK1206720A1 (en) 2016-01-15
CR20150087A (es) 2015-04-06
AU2013314388B2 (en) 2016-07-14
MY178667A (en) 2020-10-20
NO2895477T3 (fr) 2018-03-31
HRP20171981T1 (hr) 2018-02-09
PH12015500489A1 (en) 2015-04-20
IL237332B (en) 2018-07-31
BR112015004511A2 (pt) 2017-07-04
PH12015500489B1 (en) 2015-04-20
EP2895477B1 (fr) 2017-11-01
EA026062B1 (ru) 2017-02-28
US9487501B2 (en) 2016-11-08
US20150218131A1 (en) 2015-08-06
CA2882821C (fr) 2018-05-22
UA113776C2 (xx) 2017-03-10
TWI610926B (zh) 2018-01-11
AU2013314388A1 (en) 2015-03-05
CL2015000580A1 (es) 2015-07-10
CN107903251A (zh) 2018-04-13
PE20150735A1 (es) 2015-05-17
CA2882821A1 (fr) 2014-03-20
PL2895477T3 (pl) 2018-03-30

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